CN104546523A - Compositions comprising extract of paulownia tomentosa wood and uses thereof - Google Patents

Compositions comprising extract of paulownia tomentosa wood and uses thereof Download PDF

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CN104546523A
CN104546523A CN201410545360.XA CN201410545360A CN104546523A CN 104546523 A CN104546523 A CN 104546523A CN 201410545360 A CN201410545360 A CN 201410545360A CN 104546523 A CN104546523 A CN 104546523A
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skin
extract
panlownin
compositions
paulownia
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S·考尔
K·马哈茂德
C·萨利欧
M·索撒尔
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Johnson and Johnson Consumer Inc
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Johnson and Johnson Consumer Companies LLC
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Priority claimed from US14/056,521 external-priority patent/US9962326B2/en
Application filed by Johnson and Johnson Consumer Companies LLC filed Critical Johnson and Johnson Consumer Companies LLC
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/80Scrophulariaceae (Figwort family)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/28Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4973Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/06Preparations for care of the skin for countering cellulitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/08Anti-ageing preparations

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Abstract

Provided are compositions comprising paulownin or an extract of paulownia tomentosa wood and using methods thereof.

Description

Comprise the composition and use thereof of paulownia wood extract
The cross reference of related application
Present patent application is the part continuation application of the U.S. Patent application 13/211,626 that on August 17th, 2011 submits to, and described U.S. Patent application 13/211,626 is the part continuation applications of the U.S. Patent application 12/859,323 that on August 19th, 2010 submits to.
Technical field
The present invention relates to the compositions comprising panlownin for using on skin.The invention still further relates to the compositions comprising the plant extract from Paulownia (Paulownia) for using on skin.More specifically, it relates to the multi-purpose compositions comprising Paulownia (Paulownia tomentosa) wood extractive on skin.
Background technology
Paulownia is that the plant that Asia originates in belongs to, and it is transmitted to Europe and the U.S. gradually.Species from Paulownia regard as ornamental trees usually, and its timber has technique and Ecological Information widely.Such as, in Japan, China and Korea S, the timber of this type of tree is commonly used to the soundboard making stringed musical instrument.It is also generally commercial in making furniture by wood.Paulownia trees have ecological purposes and are regarded as phytoremediation body (phyto-remediator), that is, they by its vascular system process industrial pollutants with help cleaning and land reclamation.
In Japan, Paulownia is referred to as Japanese Paulownia (kiri), and it refers in particular to species, Paulownia, also known as work " princess sets (Princess Tree) ".Other conventional title has " queen sets (empress tree) ", " digitalis tree (Foxglove Tree) ", " imperial Paulownia (Royal Paulownia) ", " Paulownia (Pao tong) " (in China) and " Odong-Namoo " (in Korea S).Formal name used at school is " Paulownia ", there are the multiple synonyms be reported in various document, i.e. " rust royal paulownia (Paulownia imperialis) ", " Xing Shantong (Paulownia recurva) " and " royal paulownia (Bignonia tomentosa) ".Paulownia belongs to " Paulowniaceae " or be sometimes referred to as " Scrophulariaceae ".With unique symbol " PATO2 ", United States Department of Agriculture (USDA) (plants.USDA.gov) plant database identifies that princess sets, wherein Paulownia and rust royal paulownia synonymously title.
The caul-fat of Paulownia is subject to well research and it is found that its richer fragrance compared with other species.Many biological activitys are associated with the extract of the multiple part of Paulownia, such as, from the anticancer component of flower extract, the anthelmintic activity from nonspecific extract, the antibacterial activity from fruit and flower extract, the antioxidant activity from flower extract and the ntiviral characteristic from peel of stem.The hair growth and the hair that describe the leaf extract of Paulownia promote characteristic.
Panlownin, also referred to as isopaulownin or new panlownin, is be separated the lignan from various plants aerial parts.This chemical constitution can provide as follows:
The present invention relates to the following discovery of applicant: the extract of paulownia wood is useful for the use of compositions on skin.Such as, applicant has found that such composition is tending towards demonstrating significantly and the unexpected characteristic for skin comprises lighten skin, improves aging sign and reduce inflammation.The invention still further relates to the following discovery of applicant: described compound panlownin shows remarkable and unexpected skin lightening, defying age beneficial effect and other characteristic.
Summary of the invention
In one aspect, the present invention relates to the compositions comprising panlownin and carrier.
On the other hand, the present invention relates to the method for the aging sign improved in skin, described method comprises the step to needing the dermal administration improving aging sign to comprise the compositions of panlownin and carrier.
On the other hand, the present invention relates to the compositions comprising paulownia wood extract and carrier.
On the other hand, the present invention relates to the method for lighten skin, described method comprises the step of the dermal administration paulownia wood extract to the bright skin process of needs.
On the other hand, the present invention relates to the method improving signs of skin aging, described method comprises the step to the dermal administration paulownia wood extract needing to improve aging sign.
On the other hand, the present invention relates to the method reducing scytitis, described method comprises the step to needing the dermal administration paulownia wood extract reducing scytitis.
Detailed description of the invention
As noted above, applicant finds unexpectedly, and panlownin and/or paulownia wood extract can be used in the preferred skin care compositions of compositions, and for including but not limited to the using method improving aging sign, skin lightening and reduction inflammation.
As used herein, term " lighten skin " instigates the colour of skin usually, skin color and/or skin colourity thin out, brighten, to bleach and/or evenly, and/or refer to Huang of dispelling, and/or refer to that pigment spot and/or disease damage (include but not limited to pigment spot, melanocyte speckle, senile plaque, day sunburn, lentigo senilis, freckle (freckles), lentigo, pigmentosa actinic keratosis, seborrheic keratosis, melasma, acne speckle trace, hyperpigmentation after inflammation, lentigo, freckle (ephelides), two or more combination etc. in them) desalination and/or fade.In certain embodiments, " lighten skin " skin brightness, glossiness, translucence and/or luminous and/or obtain brighter, gloss, translucent or luminous colour of skin outward appearance or lower yellow or the chlorotic color colour of skin of also referring to increase.In some preferred embodiment, " lighten skin " instigates colour of skin blast with even, increases skin brightness and/or desalination senile plaque.
As used herein, term " needs the skin of bright skin process " and generally refers to the skin showing one or more performances, described performance is selected from: individual type angle (ITA) value with measurement lower than 41 skin, as being incorporated herein by reference, and what hereafter further describe, COLIPA GUIDELINE:GUIDELINE FOR THE COLORIMETRIC DETERMINATION OF SKIN COLOUR TYPING AND PREDICTION OF THE MINIMAL ERYTHEMAL DOSE (MED) the WITHOUT UV EXPOSURE announced according to 2007, COLIPA is determined, the skin of obfuscation and/or lark, comprise the skin of ultraviolet darkening, there is the skin of uneven skin color, or there is the Pigmented spot in a place or many places and/or disease damage (includes but not limited to pigment spot, melanocyte speckle, senile plaque, day sunburn, senile lentigo, passeris montani saturati speckle, lentigo, pigmentosa actinic keratosis, seborrheic keratosis, melasma, acne speckle trace, hyperpigmentation after inflammation, lentigo, passeris montani saturati speckle, two or more combination etc. in them) skin.In COLIPA guide, skin color is defined as along with ITA value: very light skin >55; Light skin 41-55; Medium 28-41, and sepia skin <28.In some preferred embodiment, " needing the skin of blast " refers to that the ITA value of skin is lower than 41, such as about 40 or lower, about 35 or lower, about 30 or lower, or more preferably from about 28 or lower individuality.In some other preferred embodiment, the present invention relates to for be selected from sallow and/or darkening skin need carry out the compositions on the skin of bright skin process and method.In some other preferred embodiment, the present invention relates to compositions and the method for spot for staying after needing to carry out being selected from senile plaque, freckle, acne and the bright skin process of the combination of two or more in them.
As used herein, " needing the skin improving aging sign " refer to its be but be not limited to sagging, lax, loose, coarse, have wrinkle, the skin that thinning, the colour of skin is uneven.Improve aging sign and refer to the external aggression improving skin tightness, improve texture, improve the appearance of wrinkle on skin, improve skin color or treat in skin.
As used herein, " improving the degree of compacting of skin " means to strengthen the degree of compacting of skin or elasticity, the degree of compacting of prevention skin or elastic loss or prevention or process sagging, loose and lax skin.The degree of packing of skin or elasticity are measured by using skin elasticity tester (cutometer).See Handbook of Non-Invasive Methods and the Skin, J.Serup, G.Jemec and G.Grove edit, the 66.1st chapter (2006).The loss of skin elasticity or degree of compacting may be that many factors causes, and includes but not limited to aging, environmental nuisance or the result to dermal administration cosmetics.
As used herein, " improving the skin texture of skin " means to make skin surface smoothly to remove bump on skin surface or crack.
As used herein, " improving the appearance of wrinkle in skin " means to prevent, delay, stop or process that on reversing skin, wrinkle and microgroove are formed.
As used herein, " external aggression in treatment skin " means to reduce or prevent skin peripheral to encroach on the infringement brought.The example of external aggression includes but not limited to use cleaning agent (topical cleansers such as containing surfactant), cosmetics, shave and environmental nuisance as brought the infringement to skin from ultraviolet illumination (such as from the sun damage of daylight or from the infringement of non-natural origin as Burdick lamp and solar simulator), ozone, waste gas, pollution, chlorine and chlorine-containing compound and smoking.The impact of external aggression on skin includes but not limited to the oxidation of lipid, carbohydrate, peptide, protein, nucleic acid and vitamin and/or nitrosation damage and the modification to these materials.External aggression also includes but not limited to the change of the loss of cell viability, the loss of cell function or change and gene and/or protein expression to the impact of skin.
As used herein, " improving the colour of skin " refers to lighten skin outward appearance (e.g., blast pigment spot or disease damage, alleviate the color of skin sallow and/or homogenize skin).
As used herein, " needing the skin alleviating scytitis " refers to and shows rubescent or erythema, edema or have reactive or hypersensitive skin to external factor.External factor includes but not limited to compound, smoke from cigarette, low temperature, the heat of sunray (ultraviolet, visible ray, IR), microorganism, atmosphere pollution (such as ozone), exhaust emission, chlorine and generation chlorine.Include but not limited to as follows by the inflammatory diseases that uses compositions of the present invention to treat or prevent and associated conditions: arthritis, bronchitis, contact dermatitis, atopic dermatitis, psoriasis, seborrheic dermatitis, eczema, allergic dermatitis, polymorphous light eruption, inflammatory dermatosis, folliculitis, alopecia, the erythra that contact poison paint causes, insect bite, acne inflammation, the stimulation that extrinsic factor causes, include but not limited to chemicals, wound, pollutant (such as smoke from cigarette) and sunshine, the secondary disease caused by inflammation includes but not limited to axersis, hyperkeratosis, pruritus, hyperpigmentation after inflammation, cicatrix etc.Preferably, method of the present invention can be used to treat or the inflammatory diseases of prevention and associated conditions be arthritis, inflammatory dermatosis, contact dermatitis, allergic dermatitis, atopic dermatitis, polymorphous light eruption, stimulation (comprising the erythema that extrinsic factor causes), acne inflammation, psoriasis, seborrheic dermatitis, eczema, contact poison paint cause erythra, insect bite, folliculitis, alopecia and secondary condtions etc.
As used herein, except as otherwise noted, otherwise percentage compositions all in compositions is the percentage by weight (total weight by compositions) of activity/solid constituent.
As used herein, the compositions of " being substantially free of " a certain composition refers to the compositions (total weight by said composition) containing have an appointment 2 % by weight or this less composition.Preferably, be substantially free of the compositions of a certain composition containing having an appointment 1 % by weight or less, more preferably from about 0.5 % by weight or less, more preferably from about 0.1 % by weight or less, more preferably from about 0.05 % by weight or less, more preferably from about 0.01 % by weight or this less composition (total weight by said composition).In some preferred embodiment, the compositions being substantially free of a certain composition, not containing this composition, does not namely contain this composition in compositions completely.
As used herein, the composition that " cosmetically/dermatological is acceptable " means this term description is suitable for contacting with tissue (as skin or hair) and uses and can not cause unsuitable toxicity, incompatibility, unstability, excitatory, atopic reaction etc.
The extract comprising panlownin can be via one or more fraction derived from the material of paulownia wood of any one in extracting method as described herein, or is made up of it.In certain embodiments, this extract comprises the combination of a kind of fraction derived from paulownia wood or two or more fraction.
Any suitable extract of paulownia wood can use according to the present invention.Generally speaking, the timber of paulownia comprises the timber from bar, branch or both combinations.The suitable extract of paulownia wood can derived from wood flour, wood powder and/or little chip etc.
The suitable extract of paulownia wood can use conventional method to obtain, described conventional method include but not limited to by following from timber extracting directly material: grind, flood, extrude, squeeze, smash to pieces, centrifugal, and/or such as cold percolation, stirring/distillation, microwave auxiliary extraction, supersound process, containing or not containing the supercritical/subcritical CO of polarity modifier 2the pressurized hot water extraction that Compressed Gas extraction, pressurized liquid extraction, accelerated solvent extractor, pressurization or atmospheric hot-water extract, surfactant is auxiliary, oil extraction, film extraction, surname extraction, golden finger distillation/extract and/or such as awarding to Integrated Botanical Technologies, the process of process etc. disclosed in the U.S. Patent number 7442391,7473435 and 7537791 (being incorporated to by reference herein) of LLC, or pass through other method of such as solvent extraction etc.Comprise polar solvent, non-polar solven or in them any one being combined in interior multi-solvents of two or more can be used for comprising in solvent-extracted method.Suitable polar solvent comprises: polar inorganic is as water etc., and polar organic solvent such as monohydric alcohol and corresponding organic acid (such as comprise the C of methanol, ethanol, propanol, butanols etc. 1-C 8alcohol and comprise the organic acid of acetic acid, formic acid, propanoic acid etc.), polyhydric alcohol and glycol (comprise C 1-C 8polyhydric alcohol/glycol etc.) and they two or more combination.Suitable non-polar solven comprises non-polar organic solvent such as alkane and (comprises C 1-C 8alkane), cycloalkane (comprises C 1-C 8alkane), alkyl ether (comprises C 1-C 8alkyl ether), petroleum ether, ketone (comprises C 1-C 8ketone), dichloromethane, ethyl acetate, dimethylbenzene, toluene, chloroform, vegetable oil, mineral oil etc.In another embodiment, by above-mentioned non-polar solven or containing or not containing polarity modifier (such as C 1-C 8alcohol, water, C 1-C 8polyhydric alcohol/glycol or C 1-C 8organic acid) supercritical extraction and obtain extract.In some preferred embodiment, extract of the present invention is by being pulverized by timber and using the polar solvent of dielectric constant values between 1 to 100 at 20 DEG C to extract, preferably extract with the polar solvent of dielectric constant values at 20 DEG C between 4 to 60, more preferably extract with the polar solvent of dielectric constant values at 20 DEG C between 4 and 50, also more preferably extract and the polar extract of preparation with the polar solvent of dielectric constant at 20 DEG C between 4 to 40.The example of preferred polar solvent comprises and to have at 20 DEG C 1 to 100, preferably 4 to 60 and the C of dielectric constant values more preferably between 5 to 40 1-C 8alcohol, C 1-C 8polyhydric alcohol/glycol, C 1-C 8organic acid, water and two or more combination in them, include but not limited to as " Dielectric Constants of Some Organic Solvent-Water Mixtures at Various Temperatures (some organic solvent-aqueous mixtures dielectric constant at different temperatures) ", Akerlof, Gosta; JACS " JACS ", the 54th volume, No.11 (in November, 1932), has those solvents of required dielectric constant values and the combination of solvent described in 4125-4139 page (be incorporated to by reference herein).In some preferred embodiment, use one or more C 1-C 8monohydric alcohol, C 1-C 8polyhydric alcohol, C 1-C 8glycol and in them two or more combination extract polar extract.In some preferred embodiment, use one or more C 1-C 4monohydric alcohol, C 1-C 4polyhydric alcohol and/or C 1-C 4two alcohol extraction extracts.In some preferred embodiment, when presence or absence water with comprising methanol, the solvent of ethanol or their combination prepares extract.In a more preferred embodiment, with absolute alcohol or SILVER REAGENT denatured alcohol and drying Japan paulownia wood powder, at room temperature stir and prepare extract over 3 days.In some preferred embodiment, by Linesless charcoal (also referred to as active carbon) refining extract further.
In certain embodiments, Paulownia extract can be prepared as and be substantially free of some material.In one embodiment, extract be substantially free of maloic acid, cupreol or both.
In certain embodiments, said composition can comprise the extract of the other parts (such as bark, leaf, root, fruit, seed or one or more in spending) from Paulownia in addition.In other embodiments, said composition is substantially free of the extract of other non-woody parts from Paulownia.
The present invention also comprises the skin care compositions and methods containing panlownin and the method by treating skin to the compositions needing the dermal administration improving aging sign to comprise panlownin, such as process one or more signs of skin aging, lighten skin, treatment inflammation and/or similar method, the compound of described panlownin and following formula:
Panlownin for this paper purposes can derive via the arbitrary source in multiple natural origin, such as extract from plant, maybe can use known synthetic method carry out synthesizing (see such as, Stereoselective Synthesis of 3-Alkyl-2-aryltetrahydrofuran-4-ols:Total Synthesis of (±)-Paulownin.Angle, Steven R.; Choi, Inchang; Tham, Fook S.Department of Chemistry.Wright State University, Dayton, OH, USA.Journal of Organic Chemistry (2008), 73 (16), 6268-6278; With Total synthesis of (+)-Paulownin.Okazaki,Momotoshi;Ishibashi,Fumito;Shuto,Yoshihiro;Taniguchi,Eiji.Faculty Agric.,Ehime Univ.,Matsuyama,Japan.Bioscience,Biotechnology,and Biochemistry(1997),61(4),743-745)。In some preferred embodiment, panlownin extracts from plant.The example of Suitable botanical comprises the plant of Paulownia, such as Paulownia, fortune paulownia (Paulownia fortunei), Paulownia elongata (Paulownia elongata), Formosan paulownia (Cortex seu Radix Paulowniae kawakamii) (Paulownia kawakamii), and other plant, such as Amanoa oblongifolia, Dolichandrone crispa, Firmiana platanifolia (Linn. f.) Marsili (Firmiana platanifolia), koombar (Gmelina arborea), Asia Ramulus et Folium Gmelinae (Gmelina asiatica), Gmelina vitiensis, Rabdosia parvifolia (Isodon parvifolius), hang melon tree (Kigelia pinnata), Markhamia platycalyx, Markhamia stipulate, crow chimney flower (Millingtonia hortensis), plant species Olea (Olea), Fei Laer wood (Phyllarthron comorense), Ying Kana violet (Tabebuia incana), Fructus Viticis (Vitex trifolia), Prasium majus, two or more combination etc. in them.In some preferred embodiment, panlownin extracts from paulownia wood.
In certain embodiments, panlownin obtains by the cell culture (comprising the cell culture of Paulownia plant such as Paulownia) extracting various plants.Carrying out extracting the cell culture obtained for extract/panlownin of the present invention can be any form, comprises suspended cell culture etc.
In the panlownin of any appropriate amount or paulownia wood extract compositions all used in the present invention.Preferably, said composition comprises panlownin or the paulownia wood extract of safe and effective amount.As used herein, " safe and effective amount " refers to that as many as is enough to produce Expected Results but lacks to being enough to avoid the extract of serious side effects (comprising cytotoxicity etc.) or the amount of compositions.For comprise described compositions bright skin purposes embodiment for, " bright skin effective dose " refers to the amount of extract of Δ L-value effectively reached in the epiderm skin equivalent model as bright skin test (Δ L) higher than zero, as mentioned below.In some preferred embodiment, bright skin effective dose is the amount of the Δ L-value effectively reaching about 1 or higher.
Use compositions to for the embodiment improving signs of skin aging for relating in the present invention, " improve aging sign effective dose " and refer to the amount to the suppression percentage ratio that MMP-1 or MMP-9 generates provided higher than zero, described suppression percentage ratio is that the method program of the suppression of inducing according to the MMP of Examples below 11 pairs of ultraviolet inductions records.In some preferred embodiment, improve the amount to suppression percentage ratio that MMP-1 or MMP-9 generate of aging sign effective dose for providing about 10% or higher, described suppression percentage ratio records according to the method program of the suppression in the MMP induction of Examples below 11 pairs of ultraviolet inductions.In some preferred embodiment, improving aging sign effective dose refers in the reconstruct epidermis and HEP's method provided respectively in Examples below 8 and 9, measure according to reactive oxygen species formation suppression, reactive oxygen species (ROS) is provided to suppress the amount of percentage ratio, described suppression percentage ratio is about 10% or larger, and preferably 20% or larger.
Use for the embodiment that reduces inflammation of compositions for relating in the present invention, " for alleviating the effective dose of speech " refers to the amount providing the scytitis (IL-8) higher than zero to suppress percentage ratio, and described scytitis (IL-8) suppresses percentage ratio to be record according to the method program for IL-8 of pro-inflammatory mediator release to the antiphlogistic effects rebuilding epidermis of Examples below 7 pairs of ultraviolet inductions.In some preferred embodiment, improve the amount of effective dose for providing the scytitis of about 10% or higher (IL-8) to suppress percentage ratio of aging sign, described scytitis (IL-8) suppresses percentage ratio to be record according to the method program for IL-8 of release to the antiphlogistic effects rebuilding epidermis of the pro-inflammatory mediator of Examples below 7 pairs of ultraviolet inductions.
In some preferred embodiment, said composition comprises the panlownin or paulownia wood extract that are greater than zero to about 20%.In some other preferred embodiment, said composition comprises about 0.0001 to about 20%, about 0.001 to about 10%, about 0.01 to about 5%, about 0.1 to about 5% or the panlownin of about 0.2 to about 2% or paulownia wood extract.In some other preferred embodiment, said composition comprises and is greater than zero to about 1%, about 0.0001 to about 1%, about 0.001 to about 1% or the panlownin of about 0.01 to about 1% or paulownia wood extract.In some other preferred embodiment, said composition comprises about 1 to about 5%, the preferably panlownin of about 2 to about 5% or paulownia wood extract.
Any suitable carrier compositions all used in the present invention.Preferably, for skin care compositions, this carrier is cosmetically acceptable carrier.The carrier without character such as unsuitable toxicity, incompatibility, unstability, zest, atopic reactions with skin whitening is suitable for health especially contact skin as it will be appreciated by those skilled in the art that cosmetically acceptable carrier comprises.The carrier of safe and effective amount accounts for about 50% to about 99.999%, preferably about 80% of compositions to about 99.9%, more preferably from about 99.9% to about 95%, most preferably from about 99.8% to about 98%.Described carrier can take various forms.Such as, include but not limited to that the emulsion carrier of oil-in-water, Water-In-Oil, W/O/W and water-in-silicone bag oil emulsion all can be used for herein.These emulsion can contain a series of viscosity, and such as about 100 centipoises are to about 200,000 centipoise.The example of suitable cosmetically acceptable carrier comprises cosmetically acceptable for following solvent and material: cosmetic solution, suspension, lotion, cream, essence, essence, gel, toner, stick, spray, ointment, washing liquid and soap slab, shampoo, hair conditioner, paste, foam, mousse, powder, shaving cream, cleaning piece, paster, band, powerful paster, microneedle patch, binder, hydrogel, film-forming products, facial film and skin sticking membrane, foundation cream, drop etc.These product types can comprise multiple cosmetically acceptable carrier, include but not limited to that solution, suspension, emulsion are as microemulsion and nano-emulsion, gel, solid, liposome, other wrapper technology etc.It is below the non-limitative example of examples of such carriers.Other carrier can be prepared by those of ordinary skill in the art.
In one embodiment, carrier comprises water.In another embodiment, described carrier also can comprise one or more aqueous solvents or organic solvent.The example of organic solvent includes but not limited to: Isosorbide dimethyl ether; Isopropyl myristate; The surfactant of cation, anion and nonionic character; Vegetable oil; Mineral oil; Wax; Natural gum; Synthesis and natural gelling agents; Alkanol; Glycol; And polyhydric alcohol.The example of dihydroxylic alcohols includes but not limited to glycerol, propylene glycol, butanediol, pentanediol, hexanediol, Polyethylene Glycol, polypropylene glycol, diethylene glycol, 2,2'-ethylenedioxybis(ethanol)., ethohexadiol, glycerol, butanediol and hexanetriol and their copolymer or mixture.The example of alkanol includes but not limited to that those have the alkanol of about 2 carbon atoms to about 12 carbon atoms (such as, about 2 carbon atoms are to about 4 carbon atoms), as isopropyl alcohol and ethanol.The example of polyhydric alcohol includes but not limited to have the polyhydric alcohol of about 2 carbon atoms to about 15 carbon atoms (such as, about 2 carbon atoms are to about 10 carbon atoms), as those of propylene glycol.Based on the total weight of carrier, organic solvent can the amount of about 1% to about 99.99% (such as, about 20% to about 50%) be present in described carrier.Based on the total weight of carrier, water can the amount of about 5% to about 95% (such as, about 50% to about 90%) be present in described carrier (before use).Solution can comprise the solvent of any appropriate amount, comprises about 40 to about 99.99%.Some preferred solution accounts for about 50% to about 99.9%, about 60% to about 99%, about 70% to about 99%, about 80% to about 99% or about 90% to 99%.
Lotion can be made up of this class solution.Except solvent, emulsion is usually containing at least one emollient.Emulsion can comprise the water of one or more emollient and about 50% to about 90% (such as, about 60% to about 80%) of about 1% to about 20% (such as, about 5% to about 10%).
Can be cream by the another kind of product of solution preparation.Cream comprises the moisture of one or more emollient and about 45% to about 85% (such as, about 50% to about 75%) of about 5% to about 50% (such as, about 10% to about 20%) usually.
Can be also ointment by the another kind of product of solution preparation.Ointment can contain the simple base material of animal oil, vegetable oil or artificial oil or semisolid hydrocarbon.Unguentum can comprise one or more emollient of about 2% to about 10% and one or more thickening agents of about 0.1% to about 2%.
Compositions used in the present invention can also be mixed with emulsion.If carrier is emulsion, then the carrier of about 1% to about 10% (such as, about 2% to about 5%) contains emulsifying agent.Emulsifying agent can be nonionic, anionic or cationic.
Lotion and ointment can be mixed with emulsion.This type of lotion comprises the emulsifying agent of 0.5% to about 5% usually, and this type of cream will comprise the emollient of about 1% to about 20% (such as, about 5% to about 10%) usually; The water of about 20% to about 80% (as 30 to about 70%); One or more emulsifying agents of about 1% to about 10% (according to appointment 2% to about 5%).
Oil-in-water type and water-in-oil type single-phase emulsion skin care formulation (such as emulsion and cream) are known in the art, and can be used for the invention of this theme.Heterogeneous emulsion composition (such as water-in-oil-in water or Water-In-Oil oil-in) also can be used for the invention of this theme.Usually, this type of single-phase emulsion or heterogeneous emulsion contain moisture, emollient and emulsifying agent as basis.
Compositions of the present invention also can be mixed with gel (aqueous alcohol, alcohol/water or the oleogel that such as, use one or more suitable gellant to make).Suitable gellant for aqueous gel and/or alcohol gellike includes but not limited to natural gum, acrylic acid and acrylate polymer and copolymer and cellulose derivative (such as hydroxy methocel and hydroxypropyl cellulose).Suitable gellant for oil (such as mineral oil) includes but not limited to hydrogenation butylene/ethylene/styrene copolymer and hydrogenation of ethylene/propylene/styrene copolymer.This gellike comprises this type of gellant between about 0.1 % by weight and 5 % by weight usually.
Compositions of the present invention also can be mixed with solid preparation (e.g., cerul stick, bar composition, powder or cleaning piece).Compositions of the present invention also can combine with solid, semisolid or soluble base material (such as, cleaning piece, facial film, pad, glove or band).
Compositions of the present invention also can be mixed with the preparation for oral cavity, such as toothpaste, gutta-percha, rinsing solution, solution, patch etc.Described tumor also can be passed through preparation for eye, such as solution, emulsion, suspension etc. that eye drop or collyrium use, or through preparation for vaginal mucosa, such as by uses such as gel, lotion, lubricants.
Compositions of the present invention also can comprise any one of multiple additional cosmetic activity agent.The example of suitable additional active agents comprises: additional skin lightening agent, dark agent, additional age resister, tropoelastin promoter, collagen promoter, anti-acne agents, control glossy dose, antimicrobial is as against yeasts agent, antifungal and antibacterial, antiinflammatory, antiparasitic, external-use analgesic, sunscreen, illumination protective agent, antioxidant, keratolytic agent, detergent/surfactant, wetting agent, nutrient substance, vitamin, energy booster, antiperspirant, astringent, deodorizer, depilatory, hair growth promoter, hair growth delayer, firming agent, moisturizing agent, synergist, anti-scleroma agent, skin conditioning agent, the scorching agent of anti-cellulite, fluoride, teeth whitening, antiplaque agent and dental plaque cosolvent, odor control agent (such as odor masking agent) or pH adjusting agent etc.The example of various suitable additional cosmetically acceptable active substance comprises hydroxy acid, benzoyl peroxide, D-panthenol, ultraviolet filtering agent is (such as but not limited to avobenzone (Parsol 1789), phenyl dibenzimidazole tetrasulfonic acid ester disodium (Neo Heliopan AP), the own ester of diethylamino hydroxybenzoyl benzoylbenzoic acid (Uvinul A Plus), ecamsule (Mexoryl SX), artificial neroli oil, PABA (PABA), cinoxate, Uvinul T 150 (Uvinul T 150), homosalate, 4 methyl benzylidene camphor (Parsol 5000), octyl methoxycinnamate (Octinoxate), ethylhexyl salicylate (Octisalate), padimate O (Escalol 507), Phenylbenzimidazolesulfonic acid (Ensulizole), Dimethicodiethylbenzalmalonate (Parsol SLX), trolamine salicylate, Tinosorb S (Tinosorb S), benzophenone 1 – 12, dioxybenzone, Ethylhexysalicylate (Mexoryl XL), Diethylhexyl Butamido Triazon (Uvasorb HEB), octocrylene, Neo-Heliopan BB (Eusolex 4360), sulisobenzone, methylene dibenzo triazole 4-tert-octyl phenol (Tinosorb M), titanium dioxide, zinc oxide), carotenoid, free radical scavenger, spin traps, retinoid and retinoid precursor are (as retinol, tretinoin and retinyl palmitate), ceramide, polyunsaturated fatty acid, essential fatty acid, enzyme, enzyme inhibitor, mineral, hormone (as estrogen), steroid is (as hydrocortisone, 2-dimethyl aminoethanol), mantoquita (as Cu-lyt .), peptide (as Cu:Gly-His-Lys) containing copper, coenzyme Q10, aminoacid (as proline), vitamin, lactobionic acid, S-acetyl-coenzyme-A, nicotinic acid, riboflavin, thiamine, ribose, electron transit mediator (as NADH and FADH2) and other plant extract are (as Herba bromi japonici, Aloe, chryanthemum parthenium, Semen sojae atricolor, Lentinus Edodes extract) and their derivant and mixture.
In some preferred embodiment, compositions of the present invention is the skin care compositions comprising the bright skin activating agent that panlownin and/or paulownia wood extract and at least one add.The example of suitable additional bright skin activating agent includes but not limited to tyrosinase inhibitor, melanocyte degradation agent, melanosome transfer inhibitor (comprising PAR-2 antagonist), cracking-off agent, sunscreen, retinoid, antioxidant, tranexamic acid, hydrochloric acid tranexamic acid hexadecyl ester, Porcelana Skin Bleaching Agent Porcelana, linoleic acid, adenosine monophosphate disodium salt, Flos Chrysanthemi extract, allantoin, opacifier, Talcum and silicon dioxide, zinc salt etc., and other reagent as described in people Int J Mol Sci 11 (2566-2575) such as people Pigment Cell Res.19 (550-571) and Ando such as Solano.
The example of suitable tyrosinase inhibitor includes but not limited to vitamin C and derivant thereof, vitamin E and derivant thereof, kojic acid, arbutin, resorcinol, hydroquinone, flavone is (as Radix Glycyrrhizae total flavones, licorice root extract, Mulberry Roots extract, Dioscorea camposita root extract, Herba Saxifragae extract etc.), ellagic acid, Salicylate and derivant, glycosamine and derivant, fullerene, chamenol, fat hydroxy acid (Dioic acid), acetylglucosamine, 5, 5 '-dipropyl-biphenyl-2, 2 '-glycol (magnolignan), 4-(4-hydroxy phenyl)-2-butanols (4-HPB), and two or more combination etc. in them.The example of vitamin C derivatives includes but not limited to ascorbic acid and salt, ascorbic acid-2-glucoside, sodium ascorbyl phosphate, Magnesium L-Asacorbic Acid 2-O-Phosphate, and is rich in ascorbic natural extract.The example of vitamin e derivative includes but not limited to the natural extract of alpha-tocopherol, betatocopherol, Gamma-Tocopherol, Delta-Tocopherol, alpha-tocotrienol, β-tocotrienol, γ-tocotrienol, δ-tocotrienol and their mixture, tocopherol acetas, tocopherol phosphate and rich in vitamin E derivant.The example of resorcinol derivatives includes but not limited to that resorcinol that resorcinol, 4-replace is as 4-alkyl-resorcin such as 4-butyl resorcinol (rucinol), 4-hexyl resorcin ((Synovea HR, Sytheon)), Symwhite-337 (Symwhite, Symrise), 1-(2,4-dihydroxy phenyl)-3-(2,4-dimethoxy-3-aminomethyl phenyl)-propane (nivitol, etc., and be rich in the natural extract of resorcinol Unigen).The example of Salicylate includes but not limited to 4-methoxysalicylic acid potassium, salicylic acid, aspirin, 4-methoxysalicylic acid and their salt.In some preferred embodiment, tyrosinase inhibitor comprises resorcinol, vitamin C derivatives or the vitamin e derivative that 4-replaces.In a more preferred embodiment, tyrosinase inhibitor comprises Symwhite-337,4-hexyl resorcin or ascorbic acid-2-glucoside.
The example of suitable melanin degradation agent includes but not limited to peroxide and enzyme, as peroxidase and ligninase.In some preferred embodiment, melanin inhibitors comprises peroxide or ligninase.
The example of suitable melanosome transfer inhibitor comprises PAR-2 antagonist if soybean trypsin inhibitor or BBI, vitamin B3 and derivant are as nicotiamide, Semen sojae atricolor elite, full Semen sojae atricolor, soybean extract.In some preferred embodiment, melanosome transfer inhibitor comprises soybean extract or nicotiamide.
The example peeling off element includes but not limited to a-hydroxy acid (combination in any as lactic acid, glycolic, malic acid, tartaric acid, citric acid or above-mentioned substance), beta-hydroxy acid (as salicylic acid), polyhydroxy acid (as lactobionic acid and gluconic acid), and mechanical stripping (as crystallite changes skin art).In some preferred embodiment, peel off element and comprise glycolic or salicylic acid.
The example of sunscreen includes but not limited to avobenzone (Parsol 1789), phenyl dibenzimidazole tetrasulfonic acid ester disodium (Neo Heliopan AP), diethylamino-hydroxybenzoyl-hexyl-benzoate (Uvinul A Plus), Ecamsule (Mexoryl SX), artificial neroli oil, PABA (PABA), cinoxate, Uvinul T 150 (Uvinul T 150), homosalate, 4 methyl benzylidene camphor (Parsol 5000), octyl methoxycinnamate (Octinoxate), ethylhexyl salicylate (Octisalate), padimate O (Escalol 507), Phenylbenzimidazolesulfonic acid (Ensulizole), Dimethicodiethylbenzalmalonate (Parsol SLX), trolamine salicylate, two ethyl hexyl oxy phenol anisyl triazine (Tinosorb S), benzophenone 1 – 12, dioxybenzone, drometrizole three alcoxyl alkane (Mexoryl XL), Diethylhexyl Butamido Triazon (Uvasorb HEB), octocrilene, oxybenzone (Eusolex 4360), sulisobenzone, methylene dibenzo triazole tetramethyl fourth phenol (Tinosorb M), titanium dioxide, zinc oxide etc.
The example of retinoid includes but not limited to retinol (retinol), retinal (axerophthal), retinyl acetate, retinyl propionate, retinol linoleate, tretinoin, retinyl palmitate, Accutane, tazarotene, Bexarotene, adapalene, two or more combination etc. in them.In some preferred embodiment, described retinoid is selected from retinol, retinal, retinyl acetate, retinyl propionate, retinol linoleate and two or more combination in them.In some preferred embodiment, described retinoid is retinol.
The example of antioxidant includes but not limited to that water soluble antioxidant is if sulfhydryl compound and derivant (such as sodium pyrosulfite and NAC, glutathion), thioctic acid and dihydrolipoic acid, stilbenes compound are as the chelating agen of resveratrol and derivant, lactoferrin, ferrum and copper and ascorbic acid and ascorbic acid derivates (such as ascorbic acid-2-glucoside, ascorbyl palmitate and ascorbyl polypeptide).The oil-soluble inhibitor be applicable in compositions of the present invention include but not limited to Yoshinox BHT, retinoid (as, retinol and retinyl palmitate), tocopherols (such as, tocopherol acetas), tocotrienol and ubiquinone.The natural extract comprising the antioxidant be applicable in compositions of the present invention includes but not limited to: comprise the extract of flavonoid and osajin and their derivant (e.g., genistein and bigeminy zein), comprise the extract etc. of resveratrol.The example of this type of natural extract comprises Semen Vitis viniferae, green tea, black tea, Ramulus et Folium Mussaendae Pubescentis, pine bark, chryanthemum parthenium, does not belong to extract, soybean extract, Fructus Citri grandis extract, malt extract extract, hesperetin, Fructus Vitis viniferae extract, Portulaca extract, licochalcone, chalcone derivative, 2,2'-dihydroxy chalcone derivative, Flos Primulae Vittatae extract, propolis etc. containing the chryanthemum parthenium of parthenolide, oat extract, blackberry extract, Ramulus et Folium Cotini Coggygiae.
Additional cosmetic activity agent can any suitable amount, such as by the weighing scale about 0.0001% of compositions to about 20%, the amount of such as about 0.001% to about 10% (according to appointment 0.01% to about 5%) is present in compositions.In some preferred embodiment, described amount is 0.1% to 0.5%, and in other preferred embodiment, described amount is 1% to 2%.
In some preferred embodiment, compositions of the present invention is the skin care compositions comprising the antiinflammatory that panlownin and/or paulownia wood extract and at least one add.Suitable additional agent having ahtiphlogistic activity includes but not limited to the compound for the interleukin-2 in the antiinflammatory algoscopy hereafter illustrated with the IC50 (compound on inflammation produces 50% concentration suppressed) less than or equal to 100 μ g/ml.In a preferred embodiment, the IC50 of the second anti-inflammatory compound lower than about 70 μ g/ml, more preferably lower than about 50 μ g/ml, more preferably lower than about 40 μ g/ml, more preferably lower than about 30 μ g/ml.
Described antiinflammatory algoscopy has been estimated described medicament and has been reduced the ability being subject to the human lymphocyte generation cytokine that φt cell receptor (TCR) activator phytohaemagglutinin (PHA) stimulates, and described algoscopy is carried out as follows.Human lymphocyte is gathered from NAM by leukapheresis (leukopheresis), and at serum-free lymphocyte growth culture medium (ExVivo-15, Biowhittaker, Walkersville, Md.) in be adjusted to 1 × 10 6the density of cell/mL.According to disclosed method people such as (, Exp Dermatol 2:231-235,1993) Hamamoto Y., 10 μ g/mL PHA are used to stimulate PBL when presence or absence test sample.The CO of 5% is used at 37 DEG C 2supernatant, after 48 hours, is removed by incubation, and uses commercially available multiplexed cytokines measurement external member assessment cytokine concentrations.
The example of suitable antiinflammatory comprises the resorcinol of replacement, (E)-3-(4-Methyl benzenesulfonyl base)-2-acrylonitrile (as " Bay 11-7082 "; can from Sigma-Aldrich (St.Louis; Missouri) commercially available), tetrahydrocurcumin is (as tetrahydrocurcumin CG; Sabinsa Corporation (Piscataway, NJ) can be derived from) and be derived from extract and the material of following material:
The outer peel extract (PCE) of Cortex Phellodendri
Non-degeneration Semen sojae atricolor (Semen Glycines)
Flos Chrysanthemi (chryanthemum parthenium)
Rhizoma Zingiberis Recens
Semen Ginkgo (Ginkgo)
Asiaticoside (Herba Centellae extract composition)
Ramulus et Folium Cotini Coggygiae (Ramulus et Folium Cotini Coggygiae genus)
Petasites japonicus extract (Petasites japonicus)
Fructus Lycii (Fructus Lycii)
Herba Silybi mariani extract (Herba Silybi mariani (Silybum marianum))
Flos Lonicerae (Flos Lonicerae (Lonicera japonica))
Myroxylon pereirae(Royle) Klotzsch (myroxylon pereirae)
Salvia japonica Thunb. (Sage)
Pericarpium Citri tangerinae extract (genus vaccinium)
Amaranthus mangostanus L. oil (numerous fringe Herba Amaranthi tricoloris)
Punica granatum L. (Punicaceae)
Paraguay tea (paraguay tea leaf extract)
Flos Lilii viriduli extract (Bulbus Lilii)
Olive leaf P.E (Fructus Canarii albi)
Phloretin (Fructus Mali pumilae extract)
Oatmeal (Herba bromi japonici)
Lifenol (hops: Flos lupuli (Flos Humuli Lupuli) (Humulus lupulus)) extract
Radix Ononis hircinae P (ononis spinosa)
Licochalcone (Radix Glycyrrhizae: Glycyrrhiza inflata Bat. (Glycyrrhiza inflate) extract component)
Fragrant quick easypro (bisabolol and Rhizoma Zingiberis Recens extract)
Two or more combination etc. in them.
Resorcinol is the dihydric phenol compound (i.e. 1,3 dihydroxy benzenes) with following structure:
As used herein, " resorcinol of replacement " means in 2,4,5 or 6, have at least one substituent group resorcinol.Thus, the resorcinol of replacement can have few to one and the substituent group of as many as four.The position 1 and 3 Ju You – OH hydroxyl of the resorcinol replaced, as implied above.
The resorcinol of replacement is used in the embodiment of antiinflammatory wherein, it is highly preferred that all substituent groups of the resorcinol of replacement are not all containing phenyl (– C 6h 5aromatics) part.In certain embodiments, all substituent groups are not all containing (have or do not have heteroatomic) aromatic fractions.In some this type of embodiment, all substituent groups of the resorcinol preferably replaced all not ketone containings (with the carbonyl of two other carbon atom bonding).At some in other this type of embodiment, all substituent groups of the resorcinol of replacement are neither containing phenyl functional group also not ketone containing.At some in other this type of embodiment, the resorcinol of replacement comprises the substituent group that at least one has 5 to 11 carbon atoms, preferably 5 to 10 carbon atoms, more preferably 5 to 9 carbon atoms, most preferably 5 to 8 carbon atoms.At some in other this type of embodiment, at least one substituent group comprises alkyl, such as, have above-mentioned carbon number object alkyl.This alkyl is preferably undersaturated.
In certain embodiments, 4 of resorcinol are substituted, and in certain embodiments, only 4 are substituted.In another embodiment, 4 are replaced by alkyl.In some preferred embodiment, the resorcinol of replacement comprises single 4 bit substituents, and this substituent group comprises alkyl.In some other preferred embodiment, the resorcinol of replacement comprises single 4 bit substituents, and this substituent group is made up of the alkyl with phenyl ring Direct Bonding.
Resorcinol for the specially suitable replacement of antiinflammatory comprises 4-Crystoids and 4-octyl resorcinol, especially 4-Crystoids.4-hexyl resorcin and 4-octyl resorcinol illustrate below:
4-hexyl resorcin can " SYNOVEA HR " commercially available from Sytheon (Lincoln Park, NJ).4-octyl resorcinol can be commercially available from City Chemical LLC (West Haven, Connecticut).
In certain embodiments, the resorcinol of replacement has at least two substituent groups at 2,4,5 or 6.This substituent group optionally can connect and form ring, such as, optionally comprise the cyclic aliphatic hydrocarbon of hetero atom such as sulfur or oxygen.The substituent group such as connected can comprise 5 to 10 carbon atoms, such as 8 to 10 carbon atoms, and optionally comprises 1 to 3 hetero atom.The example comprising the resorcinol of the substituent suitable replacement of cyclic aliphatic of connection 2 and 3 comprises zearelone and β-ZER:
Zearelone and β-ZER can be commercially available from Sigma Chemicals (St.Louis, Missouri).
In some other embodiment, the resorcinol of replacement has Halogen and/or contains nitroso substituent group.Suitable example contains and phenyl ring Direct Bonding – Cl Huo – N=O.These substituent groups can be present on (such as) 2 and 4,2 and 6 or 4 and 6.The example of the resorcinol that dihalo-replaces is 2,6-bis-chloro resorcinol.The example of the resorcinol that dinitroso replaces is A2,4-dinitroso-resorcin:
2,6-bis-chloro resorcinol and 2,4-dinitroso-resorcin can derive from City Chemical LLC (West Haven, Connecticut).
The resorcinol replaced is prepared by methods known in the art, such as, use United States Patent (USP) 4,337, and the technology preparation described in 370, is incorporated to by reference by the content of this patent herein.
The resorcinol replaced can have any suitable molecular weight.In certain embodiments, the molecular weight of the resorcinol of replacement is in about 175 and scope about between 300.
" Feverfew P.E " refers to the extract that such as can be called plant " chryanthemum parthenium " prepared by the details arranged in the U.S. Patent Application Publication 2007/0196523 of " PARTHENOLIDE FREE BIOACTIVE INGREDIENTS FROM FEVERFEW (TANACETUM PARTHENIUM) AND PROCESSES FOR THEIR PRODUCTION " (not bioactive ingredients containing parthenolide deriving from chryanthemum parthenium (Flos Chrysanthemi) and preparation method thereof) according to name.A kind of especially suitable Feverfew P.E can about 20% active chryanthemum parthenium commercially available from Integrated Botanical Technologies (Ossining, NY).
Compositions of the present invention can comprise one or more additional anti-inflammatory compounds of beauty treatment effective dose.Said composition preferably comprises based on active substances about 0.1% to the additional anti-inflammatory compound of about 10%, more preferably from about 0.5% to about 5%.
In the compositions of the present invention, panlownin and/or paulownia wood extract can change with the concentration rate of additional anti-inflammatory compound.Such as, described extract and described anti-inflammatory compound can about 0.001 to about 100, preferably about 0.01 to about 10, and more preferably from about the weight concentration ratio (weight concentration percentage ratio is by measuring by the weight concentration of the described dry extract weight concentration divided by described additional anti-inflammatory compound) of 0.25 to about 2 exists.
In some preferred embodiment, compositions of the present invention is the skin care compositions of the reagent comprising the improvement aging sign that panlownin and/or paulownia wood extract and at least one add.The suitable additional example improving the medicament of aging sign includes but not limited to tropoelastin promoter, collagen promoter, retinoid, hyaluronic acid, dimethyl aminoethanol, N, N, N', N'-tetra-(2-hydroxypropyl) ethylenediamine, 'alpha '-hydroxy acids, polyhydroxy acid, and two or more combination in them.
As used herein, " tropoelastin promoter " refers to a bioactive compounds with the generation strengthening tropoelastin.According to the present invention, tropoelastin promoter comprise all can strengthen the natural of the generation of tropoelastin in human body or synthesis compound.
Suitable tropoelastin promoter can (such as) be determined by " tropoelastin promoter algoscopy " hereafter." tropoelastin promoter algoscopy " carries out as follows.Use rat heart muscle blast cell H9C2 (it can such as be buied from ATCC (Manassas, VA)).Culture is maintained and is supplemented with 10% hyclone, 2mm glutamine, 100 units/ml penicillin and 50ug/ml streptomycin (Invitrogen LifeTechnologies, Carlsbad, CA) Da Erbai kirschner MEM (DMEM, Invitrogen Life Technologies, Carlsbad, Calif.) in.With elastin laminin promoter-luciferase reporter gene construct (Elp2.2,2.2kb elastin laminin promoter fragment from nt-2267 to nt+2, drive fluorescence luciferase gene, it can obtain from Promega (Madison Wis.)) transient transfection cell culture.DNA is prepared by Qiagen Maxi post (Qiagen Valencia, CA).In all transfections, include there is thymidine kinase promoter and Renilla luciferase reporter gene construct (pRL-TK, Promega, Madison Wis.) as internal contrast.Usually, Lipofectamine 2000 (Invitrogen Life Technologies, Carlsbad, CA) is used, by 0.45ug STb gene/hole transfection cultured cells in 48 orifice plates.Transfection one day after, with reagent with about 24 hours of the concentration process cell of specifying, then making its cracking for using the dual-luciferase reporter system purchased from Promega (Madison, Wis.), carrying out luciferase assay according to the code of manufacturer.Use purchased from Molecular Devices (Sunnyvale, CA) luminometer LMAX, first measure LUC Photinus pyralis LUC Photinus pyralis FL activity (representing elastin laminin promoter active), then measure renilla luciferase activity (internal contrast).The ratio of these two kinds of uciferase activities (RLU) is used for evaluate " tropoelastin promoter is active ".With at least one concentration in 0.5 mcg/ml to 2.5 mg/ml (with active substances) scope, and preferably with at least one concentration in 1.0 mcg/ml to 2.5 mg/ml (with active substances) scopes, tropoelastin promoter preferably has at least 1.1, preferred at least 1.25, more preferably at least 1.3, and most preferably the tropoelastin promoter of at least 1.5 is active.
The example of suitable tropoelastin promoter includes but not limited to blackberry extract, common smoketree extract, Feverfew P.E, Herba Scopariae (Phyllanthus niruri) extract and has the bimetal complex of copper and/or zinc component.The bimetal complex with copper and/or zinc component can be such as copper citrate-zinc, cupric oxalate-zinc, cupric tartrate-zinc, malic acid copper-zinc, succinic acid copper-zinc, malonic acid copper-zinc, maleic acid copper-zinc, aspartic acid copper-zinc, cupric glutamate-zinc, 1,3-propanedicarboxylic acid copper-zinc, fumaric acid copper-zinc, glucosaccharic acid copper-zinc, polyacrylic acid copper-zinc, adipic acid copper-zinc, 1,5-pentanedicarboxylic acid. copper-zinc, suberic acid copper-zinc, Azelaic Acid copper-zinc, decanedioic acid copper-zinc, dodecoic acid copper-zinc or their combination.In a preferred embodiment, tropoelastin promoter is selected from blackberry extract, common smoketree extract, Feverfew P.E and their combination.In a particularly preferred embodiment, tropoelastin promoter is selected from blackberry extract, Feverfew P.E and their combination.
So-called " common smoketree extract " refers to the extract of " Ramulus et Folium Cotini Coggygiae (Cotinus coggygria) " leaf, and such as its water extract, can derive from Bilkokoop (Sofia, Bulgaria).So-called " blackberry extract " refers to from Fructus Rubi corchorifolii Immaturus (Rubus) platymiscium, the blend of the compound that preferred blackberry (Rubus fruticosus) is separated.In one embodiment, described compound separation is from the flower of described plant.In another embodiment, described extract is separated the dried floral from described plant.The separable one or more parts from plant of this compounds (flower of such as whole strain plant, plant, seed, root, root stock, stem, fruit and/or leaf).In a preferred embodiment, blackberry extract is blackberry leaf extract.
Extraction process can comprise physics and shifts out one piece of this kind of plant and such as grind it.Also available extracting method well known in the art is (such as the further extraction of suitable combination thing, with an organic solvent as rudimentary C1-C8 alcohol, C1-C8 alkyl polyols, C1-C8 alkyl ketone, C1-C8 alkyl ether, acetic acid C1-C8 Arrcostab and chloroform, and/or inorganic solvent as water, mineral acid example hydrochloric acid with inorganic base as sodium hydroxide) from as described in plant be separated.
Such as, by extracting with water, alcohol such as ethanol or their combination and prepare blackberry leaf extract.But it is preferred for preparing extract with the solvent comprising both second alcohol and waters.Before extraction, preferably drying is carried out to blackberry leaf.Also preferably only the leaf of blackberry plant is used for extracting, and does not also use other plant part such as fruit (berry) or its branch and the root of blackberry.In one embodiment, the extraction process for the preparation of blackberry leaf extract comprises the steps: a) to add the solvent of alcohol containing being selected from methanol, ethanol, normal propyl alcohol, isopropyl alcohol to blackberry leaf, b) reaches 72 hours with this solvent extraction blackberry leaf.
Method detailed for the preparation of blackberry leaf extract is open in U.S. Patent Application Publication 2008/0095719, the disclosure of the document is incorporated in full herein.A kind of specially suitable blackberry extract is by extracting blackberry leaf with the mixture of water and ethanol, by maltodextrin substrate (commercially available and sell with title " SymMatrix " from Symrise Inc. (Teterboro, NJ)) the compounding activity into about 5% to about 10% and preparing.
The extract of " Herba Scopariae " can be gathered and use with whole plant, or the optional one or more parts (leaf as flower, seed, root, root stock, stem, fruit and/or plant) using plant.Can by Herba Scopariae plant or its part segmentation (such as by grinding or milling) powdered.The suitable form of milling of Herba Scopariae can be commercially available from Raintree Nutrition, Inc. (Carson City, Nevada).Preferably, use the low molecular weight fraction of Herba Scopariae, the essentially no molecular weight of such as Herba Scopariae is greater than about 100, the fraction of 000 daltonian molecular species.Preferably, this low molecular weight fraction can be extracted from Herba Scopariae plant.
Compositions of the present invention can comprise one or more tropoelastin promoter of beauty treatment effective dose, tropoelastin promoter such as mentioned above.With active substances, described compositions preferably comprises the tropoelastin promoter of tropoelastin promoter, most preferably from about 0.5% to about 2% of tropoelastin promoter, more preferably from about 0.5% to about 5% of about 0.1% to about 10%.
As used herein, " collagen promoter " refers to the bioactive compound having and strengthen collagen and produce.According to the present invention, " non-retinoid collagen promoter " comprises not retinoid or from visual pigment, and all natural or synthesis compound that the collagen that can strengthen in human body produces.
Suitable collagen promoter can such as use " collagen promoter algoscopy " to measure." collagen promoter algoscopy " carries out as follows.Use rat heart muscle blast cell H9C2 (it can be buied from ATCC (Manassas, VA)).Culture is maintained and is supplemented with 10% hyclone, 2mM glutamine, 100 units/mL penicillin and 50ug/mL streptomycin (Invitrogen life technologies, Carlsbad, CA) Da Erbai kirschner MEM (DMEM, Invitrogen Life Technologies, Carlsbad, CA) in.With driving the Collagen1A promoter-luciferase reporter gene construct of firefly luciferase gene, (it such as can derive from PREMAS Biotech Pvt.Ltd (Haryana, India) transient transfection cell culture.In all transfections, include there is thymidine kinase promoter and Renilla luciferase reporter gene construct (pRL-TK, Promega, Madison, Wisconsin) as internal contrast.Use Lipofectamine 2000 (Invitrogen life technologies, Carlsbad, CA), the cell grown in 48 orifice plates with 0.45ug STb gene/hole transfection.Transfection one day after, with reagent with about 24 hours of the concentration process cell of specifying, then make its cracking for the dual-luciferase reporter system used purchased from Promega (Madison, WI), carry out luciferase assay according to the code of manufacturer.Use purchased from Molecular Devices (Sunnyvale, CA) luminometer LMAX, first measure firefly luciferase activity (representing collagen promoter activity), then measure renilla luciferase activity (internal contrast).By the ratio of these two kinds of uciferase activities (RLU) for evaluating the activity of often kind of promoter.
At least one concentration in 0.5 mcg/ml to 2.5 mg/ml (with active substances) scope, under at least one concentration preferably in 1.0 mcg/ml to 2.5 mg/ml (with active substances) scopes, suitable collagen promoter preferably has at least 1.2, preferred at least 1.25, more preferably the collagen promoter of at least 1.3 is active.The example of suitable non-retinoid collagen promoter includes but not limited to following material: chryanthemum parthenium (chryanthemum parthenium (Tanacetum parthenium) extract, Herba Centellae (Centella asiatica) extract, Swine Siegesbeckiae (Siegesbeckia orientalis) extract; Soybean extract; Collagen promotes peptide; Maloic acid; And asiaticoside.
Herba Centellae is (also referred to as Violette marronne on Reunion (Reunion Island), Gotu Kola or Indian pennywort is called in India, Centella repanda is called in North America, and be called Talapetraka in Madagascar) be polymorphic draft (polymorphous herb), belong to Umbelliferae (Umbelliferae, Apiaceae), Herba Hydrocotyles (Hydrocotyle) subfamily is specifically belonged to.It is in whole tropical grows wild, the moist dark area of hobby height above sea level about 600 to 1200 meters.Herba Centellae has three kinds of kinds: typical case (Typica) Herba Centellae, Abyssinia's type (Abyssinica) Herba Centellae and Florida type (Floridana) Herba Centellae.This draft is known and is used because of its healing, calmness, pain relieving, antidepressant, antiviral and anti-microbial properties.The biological activity of this draft looks like owing to there is triterpene molecule in this draft.Herba Centellae can trade name TECA purchased from Bayer Consumer HealthCare (Basel, Switzerland).
The extract of Suo Wei “ Herba Siegesbeckiae " mean in the multiple extract of Zhi Wu Herba Siegesbeckiae any one, comprise and can derive from Sederma (Croda International Group, Edison, NJ) darutoside (Darutoside).
Suitable collagen promotes that peptide comprises following material: (1) matrikine peptide (i.e. extracellular matrix protein-collagen, elastin laminin or Proteoglycan Degradation and derivative peptide), comprise Matrixyl, particularly derive from Sederma (Croda International Group with trade name MATRIXYL, (Edison, NJ)) Pal-Lys-Thr-Thr-Lys-Ser-OH; (2) GHK copper peptide, can derive from Photomedex (Montgomeryville, PA) by trade name PROCYTE; (3) palmityl GHK peptide, can derive from Sederma (Croda International Group, (Edison, NJ)) by trade name Biopoeptide CL; (4) open in Peptides EP1775306B1 and that describe in formula I, II and III below peptide VFTRN, TRNDKL or their cosmetically acceptable salt:
R1-A1-A2-A3-A4-A5-A6-A7-A8-A9-R3 (I)
/
R2
Its Chinese style I contains at least six amino acid residues; And:
A1 is Val, Ala, Leu, Met or does not exist;
A2 is Arg, Lys or does not exist;
A3 is Phe, Tyr or does not exist;
A4 is Thr, Ser, Ala or Lys;
A5 is Arg or Lys;
A6 is Asn, Asp, Gly or Gln;
A7 is Asp, Asn, Glu or does not exist;
A8 is Lys, Arg or does not exist; And
A9 is Leu, Met, Val, Ile, Phe or does not exist;
Precondition is that only in the non-existent situation of A2, A3 can not exist, and only in the non-existent situation of A1, A2 can not exist, and only in the non-existent situation of A8, A7 can not exist, and only in the non-existent situation of A8, A9 can not exist; R1 and R2 is H, C1-12 alkyl, C7-10 phenylalkyl or C (=O) E1 independently of one another, and wherein E 1 is C1-12 alkyl, C3-14 thiazolinyl, C3-14 alkynyl, phenyl, 3,4-dihydroxy phenyl alkyl, naphthyl or C 7-10 phenylalkyl; Precondition is that another one is necessary for H when R1 or R2 is C (=O) E1; And R3 is OH, NH2, C1-12 alkoxyl, C7-10 phenyl alkoxyl, C11-14 naphthyl alkoxyl, C1-12 alkylamino, C7-10 octadecyloxy phenyl amino or C11-14 naphthyl alkylamino; Or their cosmetically acceptable salt.
R1-A'1-A'2-A'3-A'4-A'5-A'6-A'7-A'8-A'9-A'10-A'11-R3 (II)
/
R2
Its Chinese style II contains six amino acid residues; And:
A'1 is Val, Ala, Leu or Met;
A'2 is Arg or Lys;
A'3 is Phe or Tyr;
A'4 is Leu, Met, Val, Ile or Phe;
A'5 is His, Tyr or Phe;
A'6 is Ser, Thr, Ala or Lys;
A'7 is Tyr or Phe;
A'8 is Asp, Asn or Glu;
A'9 is Leu, Met, Val, Ile or Phe;
A'10 is Lys or Arg;
A'11 is Asn, Asp, Gly or Gln; And
R1, R2 and R3 with define in formula I identical.
R1-A"1-A"2-A"3-A"4-A"5-A"6-A"7-A"8-A"9-A"10-R3 (III)
/
R2
Wherein formula III contains at least six amino acid residues; And:
" 1 is Cys or Ser to A;
" 2 is His, Tyr or Phe to A;
" 3 is Lys or Arg to A;
" 4 is Leu, Met, Val, Ile or Phe to A;
" 5 is Leu, Met, Val, Ile or Phe to A;
" 6 is His, Tyr or Phe to A;
" 7 is Asn, Asp, Gly or Gln to A;
" 8 is Val, Ala, Leu or Met to A;
" 9 is Asn, Asp, Gly or Gln to A;
" 10 is Lys or Arg to A; And
R1, R2 and R3 with define in formula I identical.
(5) bionical tetrapeptide, such as can trade name Chronoline Tri peptide purchased from those of Qu é bec, the Unipex of Canada; And
(6) palmityl tripeptides, can trade name Syn-Coll purchased from DSM (Basel, Switzerland).Maloic acid is also known as Pentacyclic triterpenic acid, ursolic acid (Prunol), ursolic acid (Malol), ursolic acid (Urson), β-maloic acid and 3-beta-hydroxy-Urs-12-En-28-Oic Acid, it such as can be commercially available by the Sigma-Aldrich of St.Louis, MO.
Asiaticoside, also chemically be called: [6-[[3, 4-dihydroxy-6-(methylol)-5-(3, 4, 5-trihydroxy-6-methyl Pentamethylene oxide .-2-base) oxygen base Pentamethylene oxide .-2-base] oxygen ylmethyl]-3, 4, 5-trihydroxy Pentamethylene oxide .-2-base] 10, 11-dihydroxy-9-(methylol)-1, 2, 6a, 6b, 9, 12a-hexamethyl-2, 3, 4, 5, 6, 6a, 7, 8, 8a, 10, 11, 12, 13, 14b-ten tetrahydrochysene-1H-Pi-4a-carboxylate), can such as from Bayer Sant é Familiale Division Serdex, 69, Boulevard Victor Hugo 93400SAINT-OUEN France is commercially available.
Compositions of the present invention can comprise one or more collagen promoters of beauty treatment effective dose.With active substances, described compositions preferably comprises the collagen promoter of about 0.1% to about 10%, more preferably from about the collagen promoter of 0.5% to about 5%, most preferably from about the collagen promoter of 0.5% to about 2%.
Other materials many also can be present in compositions of the present invention.In some preferred embodiment, said composition comprises the skin care compositions being selected from one or more materials, and described material is selected from: surfactant, chelating agen, emollient, wetting agent, conditioner, antiseptic, opacifier, spice etc.
Emollient refers to and contributes to maintaining the softness of skin, the compound (such as, by retaining in the effect playing lubricant in skin surface or horny layer) of smooth and pliable appearance.The example of suitable emollient is included in Handbook of Cosmetic Science and Technology " cosmetic science and technical manual " (by A.Barel, M.Paye and H.Maibach edits, calendar year 2001 is by Marcel moral Kerr Corp (the Marcel Dekker of New York, NY, Inc New York, NY) publish) in the 35th chapter, the emollient found in 399-415 page (the Skin Feel Agent (dermal sensation agent) by G Zocchi), and include but not limited to vaseline, hexyldecanol stearate and plant, nut and vegetable oil, such as macadimia nut oil, Testa oryzae oil, Oleum Vitis viniferae, Petiolus Trachycarpi oil, Radix Oenotherae erythrosepalae oil, hydrogenated groundnut and American Avocado Tree oil.
Wetting agent refers to the compound (such as, the compound of moisture absorption) being intended to improve skin surface water content.The example of suitable wetting agent is included in Handbook of Cosmetic Science and Technology, and (A.Barel, M.Paye and H.Maibach edit, calendar year 2001 is by Marcel Dekker, Inc New York, NY publish) the 35th chapter 399-415 page (Skin Feel Agents, G Zocchi writes) seen in wetting agent, and it includes but not limited to glycerol, sorbitol or trehalose (such as, α, α-trehalose, β, β-trehalose, α, β-trehalose) or their salt or ester (such as, trehalose 6-phosphoric acid).
Surfactant means for cleaning or the surfactant of emulsifying.The example of suitable surfactant is included in Handbook of Cosmetic Science and Technology " cosmetic science and technical manual " (by A.Barel, M.Paye and H.Maibach edits, calendar year 2001 is published by the Marcel moral Kerr Corp of New York, NY) in the 37th chapter, the surfactant found in 431-450 page (the Classification of surfactants (surfactant classification) by L.Oldenhove de Guertechin), and include but not limited to anion surfactant (such as sulfuric ester), cationic surfactant (such as betanin), amphoteric surfactant (such as sodium cocoyl glycinate), non-ionic surface active agent (such as Alkylpolyglucoside).
The example of suitable chelating agen comprises those that can protect and preserve the present composition.Preferably, described chelating agen is ethylenediaminetetraacetic acid (" EDTA "), and more preferably tetrasodium ethylenediamine tetraacetate, it can trade name " Versene 100XL " be purchased from Dow Chemical Company (Midland, Michigan).
The antiseptic be applicable to comprises such as p-Hydroxybenzoate, quaternary amines material, phenyl phenol, benzoate, DMDM Hydantoin, organic acid, and based on the total weight of compositions, be present in compositions with the amount of about 0% to about 1% or about 0.05% to about 0.5%.
Any one (such as volatile siloxane) of giving in the multiple conditioner of other characteristic of hair (such as gloss) is all applicable to the present invention.Example includes but not limited to that atmospheric boil is lower than the volatile siloxane conditioner of about 220 DEG C.The example of suitable volatile siloxane not exclusively comprises polydimethylsiloxane, ring poly dimethyl oxosilane, hexamethyl disiloxane, Cyclomethicone (cyclomethicone) liquid, such as ring poly dimethyl oxosilane (can trade name " DC-345 " be purchased from Dow Corning Corporation of Midland, Michigan), and their mixture, and it preferably includes Cyclomethicone liquid.Other suitable conditioner comprises cationic polymer (comprising polyquaternary ammonium salt, cationic guar gum etc.).
Any one in the pearling agent of multiple commercially available acquisition or opacifier is all applicable to the present invention.The pearling agent be suitable for or the example of opacifier include but not limited to that (a) has the fatty acid of about 16 to about 22 carbon atoms and the monoesters of (b) ethylene or propylene glycol or diester; The monoesters of the poly alkylene glycol that a fatty acid (b) that () has about 16 to about 22 carbon atoms is expressed from the next or diester; HO-(JO) a-H, wherein J is the alkylidene group with about 2 to about 3 carbon atoms; And a is 2 or 3; Fatty alcohol comprises about 16 to about 22 carbon atoms; The fatty ester be expressed from the next: KCOOCH 2l, wherein K and L comprises about 15 to about 21 carbon atoms independently; Be insoluble to inoganic solids and their mixture of shampoo Compositions.
Be adapted on skin use and any aromatic desirable for skin care compositions all can be used for the present invention.
In some preferred embodiment, form of the present invention is the base material comprising the present composition.Any suitable base material all can be used for the present invention.In the U.S. Patent application 2005/0226834 and 2009/0241242 announced, such as disclose the example of suitable base material and base material material, this full patent texts is incorporated herein by reference.
In some preferred embodiment, base material is cleaning piece, glove or facial film.Preferably, this type of embodiment comprises water-insoluble base material, this type of base material as in above-cited document define.For some embodiment, water-insoluble base material can have certain size and dimension, can cover the face of individual user, thus is conducive to water-insoluble base material to be placed on user on the face as face mask substrate material.Such as, water-insoluble face mask substrate material can have the opening for the configuration of the mouth of user, nose and/or eye.Alternatively, water-insoluble base material can not have this type of opening.This astomous structure embodiments more used in the present invention, wherein the water-insoluble base material large stretch of skin or water-insoluble base material be intended to for covering non-face is intended to be used as cleaning piece.Water-insoluble base material can have various shape, if any angular shape (as rectangle) or arc, such as circular or oval.For some embodiment, described base material is glove, is such as described in the glove that the U.S. openly applies in 2006/0141014, and it is incorporated herein by reference in full.
In one embodiment of the invention, product comprises and multiplely has difform water-insoluble base material.In one embodiment of the invention, product comprises the first water-insoluble base material and the second water-insoluble base material.The first water-insoluble base material is shaped as and is applied on forehead, and the second water-insoluble base material is then shaped as and is applied near mouth, as upper area and/or lower zone, chin and/or the buccal of lip.In one embodiment of the invention, the first water-insoluble base material also can be applied to the nasal region of face.The surface area of the first water-insoluble base material can be about 100cm 2to about 200cm 2, 120cm according to appointment 2to about 160cm 2, and the surface area of the second water-insoluble base material is about 100cm 2to about 300cm 2, 150cm according to appointment 2to about 250cm 2.In one embodiment of the invention, the hardness of water-insoluble base material is lower, makes it possible to the face or other body part that such as cover or be obedient to user easily.
In certain embodiments, method of the present invention comprises to needs process (such as, need to improve one or more aging signs etc.) dermal administration comprise at least about the panlownin of 20 % by weight or the compositions of plant extract, wherein said extract comprises the panlownin of at least by weight about 20%.In some preferred embodiment, the method comprise use comprise by weight at least about 40% panlownin compositions or comprise by weight at least about 40% the plant extract of panlownin, such as at least about 50 % by weight, by weight at least about 60%, by weight at least about 70% or by weight at least about 80% panlownin.
In certain embodiments, method of the present invention comprises the compositions that the dermal administration for the treatment of to needs comprises panlownin, and described panlownin reaches at least 90% through separation and/or purification.In some preferred embodiment, said composition has been mixed wherein or has been added panlownin material, and it is the pure panlownin more than 90%.
In certain embodiments, the panlownin of described separation and/or the compositions that comprises described panlownin can be passed through preparation and are substantially free of Cucumber.In one embodiment, described panlownin material, comprise the compositions of described panlownin material or both be substantially free of maloic acid, cupreol or both all do not comprise.
Preferably, method of the present invention comprises the panlownin to dermal administration effective dose (preferred security and effective dose).In some preferred embodiment, the method comprises the panlownin being greater than zero to about 20% to dermal administration in need.In some other preferred embodiment, described method comprises the panlownin to dermal administration in need about 0.0001 to about 20%, about 0.001 to about 10%, about 0.01 to about 5%, about 0.1 to about 5% or about 0.2 to about 2%.In some other preferred embodiment, the method comprises and is greater than zero to about 1%, about 0.0001 to about 1%, about 0.001 to about 1% or the panlownin of about 0.01 to about 1% to dermal administration.In some other preferred embodiment, the method comprises the panlownin to dermal administration about 1 to about 5%, preferably about 2 to about 5%.
The present invention also comprises the method by carrying out lighten skin to the dermal administration panlownin of the bright skin process of needs or paulownia wood extract, and this type of extract and embodiment are as described above.In certain embodiments, the method dermal administration comprised to the bright skin process of needs comprises the present composition of panlownin or paulownia wood extract, and such composition is as above as described in multiple embodiment.
The present invention can comprise and to take up an official post dermal administration to be processed of what is the need for health.Such as, can use on any one or many places skin of face, lip, cervical region, chest, back, arm, armpit, hand, foot and/or leg.
Preferably, method of the present invention comprises to the bright skin effective dose of dermal administration, preferred security and the panlownin of effective dose or paulownia wood extract.In some preferred embodiment, the method comprises the panlownin from zero to about 20% to dermal administration in need or the paulownia wood extract that are greater than.In some other preferred embodiment, the method comprises to dermal administration in need about 0.0001 to about 20%, about 0.001 to about 10%, about 0.01 to about 5%, about 0.1 to about 5% or the panlownin of about 0.2 to about 2% or paulownia wood extract.In some other preferred embodiment, the method comprises and is greater than zero to about 1%, about 0.0001 to about 1%, about 0.001 to about 1% or the panlownin of about 0.01 to about 1% or paulownia wood extract to dermal administration.In some other preferred embodiment, the method comprises to dermal administration about 1 to about 5%, the preferably panlownin of about 2 to about 5% or paulownia wood extract.
Used according to the inventionly anyly can be suitable for method extract being applied to skin in need.Such as, can extract be directly applied on skin in need from packaging, be applied on skin in need with hands, or shift by base material (as cleaning piece or facial film), or two or more combination in them.In other embodiments, use extract by dropper, pipe, roller, spray, paster, or extract added in bathtub or otherwise add to be administered in the water of skin etc.
In certain embodiments, method of the present invention also comprises the step making panlownin or paulownia wood extract and contact skin a period of time.Such as, in some preferred embodiment, after using, extract and about 15 minutes of contact skin or longer time can be made.In some preferred embodiment, make extract and contact skin about 20 minutes or longer time, more preferably from about 1 hour or longer time.
In certain embodiments, method of the present invention comprises such scheme, and the program is included in the selected time period repeatedly to dermal administration panlownin or paulownia wood extract.Such as, in certain embodiments, the invention provides the method for skin lightening, the method comprises once a day or twice to the compositions needing the dermal administration of skin lightening to comprise panlownin or paulownia wood extract, altogether at least 12 weeks, preferably at least 8 weeks and more preferably at least 2 weeks.
In some preferred embodiment, method of the present invention comprises to the different compositions comprising panlownin or paulownia wood extract of dermal administration at least two kinds or product.Such as, the method can comprise to needing the dermal administration of skin lightening that the first comprises the compositions of panlownin or paulownia wood extract, uses the second subsequently and comprises panlownin or paulownia wood extract but the compositions being different from the first compositions.In some preferred embodiment, the first and the second compositions can independently selected from emulsions, cleaning agent, facial film, cleaning piece, cream, essence, gel etc.In some preferred embodiment, the first is cleaning agent, emulsion, cream, essence or essence with at least one in the second compositions, and another kind is facial film or cleaning piece.In some other preferred embodiment, the first is cleaning agent with at least one in the second compositions, and another kind is emulsion or cream.
In some other preferred embodiment, the method comprises the product to needing the dermal administration at least three kinds of skin lightening to comprise panlownin or paulownia wood extract.Preferably, these three kinds of products are selected from cleaning agent, emulsion, cream, essence and facial film.
The present invention also comprises the method improving signs of skin aging, described method comprises the step to the dermal administration panlownin or paulownia wood extract (this type of extract and compositions thereof are as described above) needing to improve aging sign, and reducing the method for scytitis, described method comprises to needing to reduce the dermal administration panlownin of scytitis or the step of paulownia wood extract (this type of extract and compositions thereof are as described above).
The present invention can comprise and to take up an official post dermal administration to be processed of what is the need for health.Such as, can use on any one or many places skin of face, lip, cervical region, chest, back, arm, armpit, hand, foot and/or leg.
Preferably, method of the present invention comprise to the bright skin effective dose of dermal administration, preferred security and the panlownin of effective dose or paulownia wood extract.In some preferred embodiment, the method comprises the panlownin from zero to about 20% to dermal administration in need or the paulownia wood extract that are greater than.In some other preferred embodiment, the method comprises to dermal administration in need about 0.0001 to about 20%, about 0.001 to about 10%, about 0.01 to about 5%, about 0.1 to about 5% or the panlownin of about 0.2 to about 2% or paulownia wood extract.In some other preferred embodiment, the method comprises and is greater than zero to about 1%, about 0.0001 to about 1%, about 0.001 to about 1% or the panlownin of about 0.01 to about 1% or paulownia wood extract to dermal administration.In some other preferred embodiment, the method comprises to dermal administration about 1 to about 5, the preferably panlownin of about 2 to about 5% or paulownia wood extract.
Can any appropriate method to dermal administration extract in need used according to the invention.Such as, can extract be directly applied on skin in need from packaging, be applied on skin in need with hands, or shift by base material (as cleaning piece or facial film), or two or more combination in them.In other embodiments, use extract by dropper, pipe, roller, spray, paster, or extract added in bathtub or to be in other words added to the water to be applied on skin etc.
In certain embodiments, method of the present invention also comprises the step making panlownin or paulownia wood extract and contact skin a period of time.Such as, in some preferred embodiment, after using, extract and about 15 minutes of contact skin or longer time can be made.In some preferred embodiment, make extract and contact skin about 20 minutes or longer time, more preferably from about 1 hour or longer time.
In certain embodiments, method of the present invention comprises such scheme, and the program is included in the selected time period repeatedly to dermal administration panlownin or paulownia wood extract.Such as, in certain embodiments, the invention provides such method, the method comprises once a day or twice to comprise panlownin or compositions from paulownia wood extract to dermal administration in need, altogether at least 12 weeks, preferably at least 8 weeks and more preferably at least 2 weeks.
In some preferred embodiment, method of the present invention comprises to the different compositions comprising panlownin or paulownia wood extract of dermal administration at least two kinds or product.Such as, the method can comprise to dermal administration in need that the first comprises the compositions of panlownin or paulownia wood extract, uses the second subsequently and comprises panlownin or paulownia wood extract but the compositions being different from the first compositions.In some preferred embodiment, the first and the second compositions can independently selected from emulsions, cleaning agent, facial film, cleaning piece, cream, essence, gel etc.In some preferred embodiment, the first is cleaning agent, lotion, cream, essence or essence with at least one in the second compositions, and another kind is facial film or cleaning piece.In some other preferred embodiment, the first is cleaning agent with at least one in the second compositions, and another kind is lotion or cream.
In some other preferred embodiment, the method comprises the product to needing the dermal administration at least three kinds improving aging sign or other process to comprise panlownin.Preferably, these three kinds of products are selected from cleaning agent, emulsion, cream, essence and facial film.
Compositions of the present invention can be suitable for other purposes multiple.Such as, compositions of the present invention can be used for clean and/or moistening skin, treatment aging sign and/or treatment inflammation (after comprising inflammation hyperpigmentation), for reduced bore, acne treatment, generate for reducing sebum, for cicatrix abatement and reduce striae atrophicae outward appearance, for reducing outward appearance or the Pericarpium Citri tangerinae shape of liparitosis.In some other embodiment, compositions of the present invention and machinery or physics exfoliation process (such as crystallite grinds skin process) can be used simultaneously or used within a few hours of this process, or use with Chemical peeling agent or keratolytic agent such as salicylic acid simultaneously.In some other embodiment, compositions of the present invention can be applied to mucosa or other organizes such as vagina tissue, oral cavity tissue or ocular tissue.In some other embodiment, compositions of the present invention can be applied to slight wound or post-surgical sites with Promotive union, be applied to sting place, be applied to malicious rattan skin disorder or similar skin, or be generally used for alleviating pruritus.In some other embodiment, compositions of the present invention is for reducing skin irritation.This stimulation can have the outside origin caused by the composition in following skin protection and cosmetics: such as retinoid and derivant thereof, benzoyl peroxide, 'alpha '-hydroxy acids and derivant, salicylic acid, surfactant, natural plant extracts, sunscreen actives agent, urea and antiseptic etc.This stimulation can have other outside origin, the such as sun, wind or shave hair.This stimulation also can be caused by congenital disorders condition, such as acne, acne erythematosa, atopic dermatitis and Other diseases state.In other embodiments, to can be used for alleviating gingiva rubescent for compositions of the present invention.Described extract is also applicable to the outward appearance reducing telangiectasis or spider-like vein, the outward appearance reducing rosacea, skin splash and skin speckle.In certain embodiments, compositions of the present invention is applied to hair, scalp or both are to improve hair health, quality and intensity, promotes hair growth or delay alopecia, preventing or treatment of dandruff, seborrhea, seborrhea capitis prevented or treated, and scalp health and humidity improved.In other embodiments, compositions of the present invention thing in mouth is applied to gingiva to prevent or to treat gingiva rubescent or stimulate, alleviates periodontitis, treat or prevent gingivitis, the treatment symptom of xerostomia or sensation.In further embodiments, compositions of the present invention is applicable to eye with treatment, the outward appearance preventing or alleviate blood-shot eye illness or Ocular irritation, prevents or treat conjunctivitis, improving eye humidity, alleviating the sensation that eye is dry.In other embodiments, compositions of the present invention is applied to vaginal mucosa with prevent or treat stimulate or dry sign, degree of compacting forfeiture.
Compositions of the present invention can comprise any suitable optional cosmetic composition as above and can be any suitable cosmetic forms (such as solution, suspension, stick, abluent, lotion, ointment, essence, facial film etc.) as above.In addition, compositions of the present invention can comprise one or more additional skin lightening agents as above, antiinflammatory, collagen promoter and/or tropoelastin promoter.In some preferred embodiment, described compositions comprises one or more additional skin lightening agents.In some preferred embodiment, described compositions comprises one or more additional antiinflammatories.In some preferred embodiment, described compositions comprises one or more additional collagen promoters.In some preferred embodiment, described compositions comprises one or more additional tropoelastin promoter.
example
Following method of testing is have employed in example:
b16 cell suppresses test
The control sample of preparation B16 (F10) Mus melanoma cell as follows is also gathered in the crops, but does not add any test sample, is not also exposed to UVB (untreated contrast).Other control sample of preparation as follows is also gathered in the crops, and does not wherein add test sample, but is as described belowly exposed to UVB (contrast of process).Prepare one or more B16 (F10) cell sample, all use test sample (as E1) to carry out pretreatment, be then as described belowly exposed to UVB.After process, UVB have stimulated melanogen in cell and generates, and then evaluates this test compounds according to the ability of test compounds suppression or reduction melanogen generating rate.Cell lysis, to carry out protein measurement at 595nm place, carries out melanin content measurement at 470nm place.Compared with contrasting of process by the suppression percentage ratio that test compounds is obtained, to determine the effect of test compounds.
test program:
First day, is inoculated in 60mm flat board by Mus melanoma b16 (F10) cell, and density is every block flat board about 100 ten thousand cells, and at 37 DEG C, 5%CO 2lower incubation 48 hours.2nd day, utilize the test compounds process of predetermined concentration (as 25 μ g/mL) to converge cell two hours (only for test compounds sample) that rate is 90-100%, was then exposed to 200mJ/cm 2uVB in (for testing the contrast of sample and process).At the 3rd day (carrying out latter 24 hours of UVB irradiation to the contrast of test sample and process) harvesting, and at protein lysis buffer (50mM Tris, pH8,2mM EDTA, 150mM NaCl and 1%Triton X 100-is purchased from the non-ionic surface active agent of BioRad catalog number (Cat.No.) 161-0407) middle cracking, and centrifugal.Gained supernatant is fully mixed with protein dyestuff quantitative analysis reagent (Bio-rad protein assay reagent), then uses spectrophotometer (Molecular Devices VERSAmax) in the optical density (protein quantification OD value) of 595nm place working sample.Remaining cell precipitation after removing supernatant is dissolved in alkaline DMSO buffer, then the solution of gained is used for the melanocyte absorbance measurement at 470nm place, thus determines melanocyte quantitative analysis OD.
Three samples respectively prepared by untreated control, process contrast and test sample, then measure melanocyte and the albumen OD value of each sample.By each untreated control of following formulae discovery (3 samples), process contrast (3 samples) and the normalization melanocyte testing sample (often kind of test compounds 3 samples):
Normalization melanocyte=melanocyte quantitative analysis OD/ protein quantification OD.
Calculate the average normalized melanocyte (three value of calculation sums are divided by 3) of untreated control, then with the average normalized melanocyte of same method computing contrast.
The induction value contrasted by following formulae discovery:
The average normalized melanocyte of the average normalized Hei Su – untreated control of the induction value=process contrast of contrast.
Then by the induction value of each test sample of following formulae discovery:
The induction of test sample is worth=tests the average normalized melanocyte of the black plain – untreated control of normalization of sample.
Then by the suppression percentage ratio of each test sample of following formulae discovery:
100 × [the induction value of (the induction value – of contrast tests the induction value of sample)/contrast].According to suppress percentages for three groups of each test sample gained and calculate mean percent inhibition divided by three.
Explained the computation sequence suppressing percentage ratio by theoretical example, see table.
as the epiderm skin equivalent model of bright skin test (Δ L)
Epiderm skin equivalence tissue can from the MelanoDerm of MatTek tMsystem is commercially available and for following test.The MelanoDerm of MatTek tMsystem is made up of normal humanized's epidermal keratinocyte (NHEK) and melanocyte (NHM), and these cells define multilamellar, well differentiated people's epidermis model through cultivation.Specifically, in following test, have employed MEL-300-B tissue, each diameter is 9mm.
These are adopted suitable carrier and are locally applied on skin model with test material prepared by test concentrations by every day, Therapy lasted 8 days.Measured at the 9th day.
By taking pictures with digital camera, measuring both macro and micro visual organization and to darken terminal.Spectrophotometer (Konica Minolta CM-2600d) is used to measure the lightness (L-value) of each tissue.Δ L (lightness compared to contrast) according to each test sample of following formulae discovery:
The L-value of the L Zhi – control sample of Δ L=processing sample.
cell viability is tested
Use MTT algoscopy as described below to assess the cell viability of experimental session tissue.It is a kind of colorimetric determination system that MTT organizational vitality measures, and it measures the ability that yellow Thiazolyl blue (MTT) is reduced to purple insoluble product by living cells mitochondrion.
By be used for before the epiderm skin tissue of the lightness measuring each test material and untreated tissue be used for determination experiment at the end of the percentage ratio of remaining living cells.By epiderm skin tissue and the common incubation 3h of MTT reagent after blast Tachistoscope.After incubation terminates, add Extraction buffer with cell lysis and place spend the night.Utilize microplate reader to read sample at the wavelength place of 570nm, then compare with untreated contrast, to represent relative to the cell survival percentage ratio of contrast.Relative to contrast, cell survival rate reduces >=30%, be then considered as test material and cause obvious cytotoxicity.The amount of the purple produced is directly proportional to viable count.
Following instance shows preparation and effect of paulownia wood extract.
example 1
Four kinds of Paulownia extracts of each at least 20mg derive from the plant extract storehouse in Korea S's bioscience and life technology institute (Korea Research Institute of Biosciences & Biotechnologies), the described combination of four kinds of Paulownia extract On behalf of plant parts or the various piece of plant.They derive from: the combination (E1) of bar/bark/branch, leaf (C1), bark (C2) and bar (E2).Whole described extract all uses methanol to prepare with ultrasonic method at 50 c.
example 2
Following instance some embodiment according to the present invention shows the preparation of paulownia wood extract (E3).
Paulownia wood powder available from Kurosawa Kiri Wood Supply Shop, Kitakata-city, Japan.Ten grams of (10g) dry wood powders to be suspended in the reagent straight alcohol of 250mL and at room temperature to stir 72h.
Filtration is carried out to produced suspension and under low pressure uses rotary evaporator with 30 degrees Celsius of these filtered solutions of drying.Productive rate with 3.5% obtains dry crude extract (350mg).By described crude extract with 1% concentration be dissolved in methanol, and at room temperature use active carbon (700mg) to process 5 minutes.By the filter paper filtering suspension of 0.45 micron.This filtered solution dry is to obtain the obviously more shallow material E3 of color, 210mg (productive rate is 60% of crude extract).
example 3
Following instance shows the preparation of the paulownia wood extract (E4) being substantially free of cupreol and maloic acid.
The water (2.4mL) of deionization rank is added Paulownia trunk/bark/branch extract (E1,24mg) from example 1 above and at room temperature supersound process 5 minutes.Filtered the suspension of gained by the filter cylinder of 0.45 μ, and make this filtered solution carry out drying by lyophilization, the yield with 43% obtains water-soluble component (E4; 10.3mg).HPLC analyzes the described compositions of display and is substantially free of cupreol and maloic acid.Not existing in E4 can any one compound of detection limit.The detectability (lod value) of cupreol is 9ppm (w/v), and the detection of maloic acid is limited to 0.5ppm (w/v).
example 4
Following instance shows bright skin characteristic and the comparative example C1-C2 of Paulownia extract E1-E5.
Whole seven groups of extracts are tested as mentioned above by testing (Δ L) using epiderm skin equivalent model as bright skin under the different concentration (as listed in table 1) being up to 2%.
Utilize MTT algoscopy to measure the cytotoxic potentials of all extracts, account form is the cell viability decline percentage ratio relative to contrast, and wherein the cell viability decline of >30% shows to there is obvious cytotoxicity problem.Result is shown in following table 1.
Also at room temperature implement the simple onestep extraction (E5) that only using water as solvent, described wood powder carried out and this is extracted in described bright skin test and does not produce activity.It is believed that more violent extraction (additional heating, stirring etc.) can produce activity.
table 1
from the bright skin of extract in 3D skin model of the part of Paulownia
* significant cytotoxicity problem is represented.
example 5
Following instance shows the melanin genesis rejection characteristic being associated with paulownia wood extract.
Suppress test to come to suppress test trunk/bark/branch extract (E1) and wood powder extract (E3) for melanin genesis according to above-described melanin genesis, and also suppress to test for tryrosinase.The bright skin effect of the measurement display E1 & E3 of gained generates with melanin at least in part and to suppress instead of tryrosinase suppresses to be associated.Extract E1 and E3 is 30 and 40 μ g/mL for the IC50 value that melanin genesis suppresses, and each extract all suppresses without tryrosinase.
example 6
nF-κ B suppresses algoscopy
NF-κ B promoter algoscopy is carried out as follows: buy rat heart muscle sarcoplast H9c2 cell from ATCC (Manassas, VA.).Culture is maintained and is supplemented with 10% hyclone, 100 units/ml penicillin and 50ug/ml streptomycin (Invitrogen life technologies, Carlsbad, CA.) Da Erbai kirschner MEM (DMEM, Invitrogen Life Technologies, Carlsbad, CA.) in.Usually, Lipofectamine 2000 (Invitrogen life technologies, Carlsbad, Calif.) is used, grow in 96 orifice plates with 0.45 μ g STb gene/hole transient transfection 1 × 10 4cell.In all transfections, further comprises except luciferase promoter there is thymidine kinase promoter and Renilla luciferase reporter gene construct (pRL-TK, Promega, Madison Wis.) as internal contrast.Transfection one day after, with described extract with the concentration process cell of specifying and with the tumor necrosis factor-alpha of 100ng/mL (TNF α, Sigma-Aldrich, St Louis, MO) about 24 hours of irritation cell, then makes its cracking for luciferase assay, uses from Promega (Madison, Wis.) dual-luciferase reporter system, follows the scheme of manufacturer.In brief, use from Molecular Devices (Sunnyvale, Calif.) luminometer LMAX, first measures LUC Photinus pyralis LUC Photinus pyralis FL activity (representing NF-κ B promoter activity), then measures renilla luciferase (internal contrast).By the ratio of these two kinds of uciferase activities (RLU) for evaluating the activity of often kind of promoter.
NF-κ B suppression=[1-(RLU sample/ RLU contrast)] × 100
Wherein RLU sampleand RLU contrastthe normalized uciferase activity ratio of described sample and contrast respectively.
Above-mentioned NF-κ B is implemented to not commensurability extract E3 and E5 and suppresses algoscopy.Report described through normalized NF-κ 1 B gene reporter gene activity and NF-κ B suppression percentage ratio in table 2a and 2b.
table 2a
table 2b
example 7
the pro-inflammatory mediator release of ultraviolet induction is to the antiphlogistic effects rebuilding epidermis
For the effect of local anti-inflammatory activity assessment Paulownia extract (E3) on people's epidermis equivalent.Epidermis equivalent (EPI 200HCF), comprises the multilamellar differentiation epidermis of Normal human epidermal's horn cell purchased from MatTek (Ashland, MA).After receiving, epidermis equivalent in without the maintain base of hydrocortisone at 37 DEG C incubation 24 hours.Be exposed to solar ultraviolet (the 1000W-Oriel solar simulator of outfit 1-mm Schott WG320 wave filter; The ultraviolet dosage used: as the 70kJ/m measured at 360nm place 2) before, equivalent is used in the Paulownia extract Local treatment (2mg/cm in 70% ethanol/30% propylene glycol vehicle 2) 2 hours.Equivalent is used maintain base incubation 24 hours at 37 DEG C, then uses commercially available external member (Millipore Corp. (Billerica, MA)) to analyze IL-8 and IL-1 α release of cytokines to supernatant.
table 3
table 4
According to above-mentioned example, the local application of described Paulownia extract can reduce the inflammatory mediator release of ultraviolet induction significantly.Therefore, Paulownia extract is expected to when being applied to skin obtain effective antiphlogistic effects.
example 8
reactive oxygen species is formed in the suppression of rebuilding in epidermisuse and the hydrogen peroxide formation measuring ultraviolet induction in epidermis and HEP system KB is being rebuild to improving one's methods of method in people Arch Dermatol Res. " research of skin disorder associated profiles " (2008) 300:69-80 such as Martin.Epidermis equivalent (EPI 200HCF), comprises the multilamellar differentiation epidermis of Normal human epidermal's horn cell purchased from MatTek (Ashland, MA).After receiving, epidermis equivalent in without the maintain base of hydrocortisone at 37 DEG C incubation 24 hours.After 24 hours; by hydrogen peroxide responsive type fluorescent probe 5-(with-6)-chloromethyl-2' of tissue with 5 μMs; 7'-dichloro-dihydro-fluorescein diethylester, acetyl group ester (CM-H2DCFDA) (Invitrogen Corp. (Carlsbad, CA)) incubation 30 minutes.After incubation, described plate is cleaned to remove excessive probe and to use Paulownia extract (E3) Local treatment equivalent (2mg/cm in 70% ethanol/30% propylene glycol vehicle 2).Described plate is read immediately to detect the formation of basic peroxide on the fluorescence plate reader being set to 485nm excitation wavelength/530nm emission wavelength.Then make described plate be exposed to ultraviolet and (be equipped with the 1000W-Oriel solar simulator of 1-mm Schott WG 320 wave filter; 4.2KJ/m is used as what measure at 360nm place 2ultraviolet dosage).Within 60 minutes after uv light exposure, read described plate.
table 5
Process (dosage, in %w/v) Mean fluorecence unit The suppression percentage ratio that ROS generates
Ultraviolet+vehicle (70:30 ethanol: propylene glycol) 761.5 0%
Ultraviolet+Paulownia 0.1% 361.4 52.5%
Ultraviolet+Paulownia 1.0% 243.4 68.0
Ultraviolet+Paulownia 5.0% 261.9 65.6
Based on this example, the local application of Paulownia extract can reduce the ROS rebuilding the induction of epidermis middle-ultraviolet lamp significantly and produce.Therefore, Paulownia extract is expected to when being applied to skin provide protection in case sun exposure induction ROS.
example 9
reactive oxygen species is formed in the suppression in HEP
ATCC (ATCC#CCL-17 will be derived from, Manassas, VA) KB cell is paved plate with the density of 5000 cells/well and be supplemented with 10% hyclone (Invitrogen Corp. in the tissue culture treated plate in 96-hole, San Diego, CA) DMEM (DMEM) in.After 48 hours; by hydrogen peroxide responsive type fluorescent probe 5-(with-6)-chloromethyl-2' of cell and 5 μMs; 7'-dichloro-dihydro-fluorescein diethylester, acetyl group ester (CM-H2DCFDA) (Invitrogen Corp. (Carlsbad, CA)) incubation 30 minutes.After incubation, clean described plate to remove excessive probe and Paulownia extract (E3) under adding prescribed concentration.Described plate is read immediately to detect the formation of basic peroxide on the fluorescence plate reader being set to 485nm excitation wavelength/530nm emission wavelength.Then make described plate be exposed to ultraviolet and (be equipped with the 1000W-Oriel solar simulator of 1-mm Schott WG 320 wave filter; 4.2kJ/m is used as what measure at 360nm place 2ultraviolet dosage).Within 60 minutes after ultraviolet radiation, read described plate.
table 6
Based on this example, use Paulownia extract to carry out processing the ROS that can reduce the induction of HEP's middle-ultraviolet lamp significantly and produce.Therefore, Paulownia extract is expected to when being applied to skin provide protection in case sun exposure induction ROS.
example 10
for the protection of elastase degradation
Human leukocyte elastase (HLE) is purchased from Sigma (St.Louis, Mo.), and at phosphate buffer (PBS, the Invitrogen life Technologies of 1 unit/ml, Carlsbad, Calif.) in copy.With the solubility cattle paxwax elastin laminin of BODIPY FL dye marker purchased from Molecular Probes, Inc. (Eugene, Or), make fluorescence quencher in described conjugate, and can be postactivated in elastin laminin enzymic digestion.Human leukocyte elastase (0.0625U/ml), elastin laminin substrate (25 μ g/ml) and increase the test material of concentration incubation two hours under 37C.Use from Molecular Devices (Sunnyvale, CA) fluorescence microplate reader Gemini with the emission measurement fluorescence with 520nm that excites of 490nm.The background fluorescence of substrate self deducts from each measured value.In DMSO, prepare Paulownia extract (E3) with the stock concentrations of 10mg/ml and serial dilution is carried out to it.As shown in table 7, Paulownia extract suppresses HLE active in dose-dependent mode.
table 7
Paulownia extract (dosage, %w/v) Elastase Inhibitory (%)
0 0.0
0.00001% 23.1%
0.001% 30.2%
0.005% 66.6%
0.01% 75.5%
0.02% 99.4%
This example shows, and Paulownia extract can protect elastin fiber to avoid damage and degraded.
example 11
the suppression of the MMP induction of ultraviolet induction
The ability that Paulownia extract (E3) suppresses the matrix metallopeptidase 1 and 9 (MMP-1 and-9) of ultraviolet induction is have evaluated in the epidermis equivalent deriving from Normal human epidermal's horn cell.MMP is the enzyme family playing Main Function in the physiological reconstruct and pathological destruction of extracellular matrix.The secretion of ultraviolet illumination induction MMP in application on human skin of well-known SED (suberythemal dose), it then degrades extracellular matrix and plays a significant role in the formation of photoaging wrinkle and degree of compacting and elastic forfeiture.See people such as G.J.Fisher, J Investig Dermatol.Symposium Proceedings.14 (1): 20 – 24 (2009).
For assessment Paulownia extract suppresses the ability of ultraviolet induction MMP, epidermis equivalent (EPI 200HCF) is purchased from MatTek (Ashland, MA), and it is the epidermis of multilamellar and the differentiation be made up of Normal human epidermal's horn cell.After receiving, epidermis equivalent in without the maintain base of hydrocortisone at 37 DEG C incubation 24 hours.Be exposed to solar ultraviolet (the 1000W-Oriel solar simulator of outfit 1-mm Schott WG 320 wave filter; The ultraviolet dosage used: the 70kJ/m2 as measured at 360nm place) before, equivalent is used in Paulownia extract Local treatment (2mg/cm2) in 70% ethanol/30% propylene glycol vehicle 2 hours.Equivalent uses maintain base incubation 48 hours at 37 DEG C, then uses commercially available external member (R & D Systems, Minneapolis, MN) to analyze supernatant for MMP-1 and-9.Data in table 8 are meansigma methodss of 2 groups of independent experiments, and each group experiment uses the tissue repeated to carry out.
table 8
table 9
Based on this example, the local application of Paulownia extract can reduce the release of the MMP-1 and-9 that ultraviolet stimulates significantly.Therefore, when being applied to skin, the expection of Paulownia extract provides the protection of the MMP-1 and-9 for sun exposure induction.
example 12
to the suppression that TNF-α induces MMP to generate
In order to assess the ability of the MMP that Paulownia extract (E3) suppresses TNF-α to induce, epidermis equivalent (EPI 200HCF) (multilamellar be made up of Normal human epidermal's horn cell and differentiation epidermis) is purchased from MatTek (Ashland, MA).After receiving, epidermis equivalent in without the maintain base of hydrocortisone at 37 DEG C incubation 24 hours.Before use TNF-α (100ng/mL) process, equivalent is used in Paulownia extract (E3) Local treatment (2mg/cm in 70% ethanol/30% propylene glycol 2) 2 hours.Equivalent uses maintain base incubation 48 hours at 37 DEG C, then uses commercially available external member (R & D Systems, Minneapolis, MN) to analyze supernatant for MMP-1 and-9.
table 10
Process (dosage, in %w/v) Average MMP-1 release (ng/ml) The suppression percentage ratio that MMP-1 generates
Untreated 4848.4 -
TNF-α induces 7867.2 0%
TNF-α+Paulownia 1% 7225.2 0.8%
TNF-α+Paulownia 5% 5370.6 31.7%
table 11
Process (dosage, in %w/v) Average MMP-9 release (ng/ml) The suppression percentage ratio that MMP-9 generates
Untreated 13217.6 -
TNF-α induces 42958.6 0%
TNF-α+Paulownia 1% 35145.3 18.2%
TNF-α+Paulownia 5% 16101.1 62.5%
Based on this example, the local application of Paulownia extract can reduce the release of the MMP-1 and-9 that TNF-α stimulates significantly.Therefore, when being applied to skin, Paulownia extract expects the protection of the induction provided for MMP-1 and-9.
example 13
Chryanthemum parthenium (not containing the Feverfew P.E of parthenolide, it is from Integrated Botanical Technologies of Ossining, NY) is used to implement tropoelastin promoter algoscopy.
Chryanthemum parthenium be diluted in (DMEM culture medium, Invitrogen, San Diego CA) in cell culture medium and Paulownia be diluted in DMSO until " activity " concentration of hereafter indicating in table 12.These compounds are added into the H9C2 cell of transfection, and incubation 24 hours.Test sample is compared with respective contrasting.Result is shown in following table 12.
table 12
As can be seen from the result shown in table 12, Paulownia and chryanthemum parthenium demonstrate the change percentage ratio exceeding contrast 32% and 2% separately respectively in tropoelastin facilitation.By contrast, Paulownia and chryanthemum parthenium be combined in improvement tropoelastin facilitation demonstrating and exceeds vehicle control 55%.This performance of effect than only a kind of additive is much better.
When the concentration of chryanthemum parthenium is increased to 0.005% from 0.002%, observe similar collaborative reinforced effects.The chryanthemum parthenium of higher concentration demonstrates the change percentage ratio exceeding vehicle control 2% in tropoelastin facilitation, and Paulownia and chryanthemum parthenium be combined in change percentage ratio tropoelastin facilitation achieving and exceedes vehicle control 62%.
The tropoelastin that is combined in of these data display Paulownia and tropoelastin promoter (chryanthemum parthenium) promotes activity creates wonderful synergitic raising.
example 14: the separation andpreconcentration of panlownin
Use the combination of classification and preparation HPLC step, complete and be separated main component (panlownin) from Paulownia.Obtain the 170mg sample with the retention time identical with the main signal of extract and ultraviolet line spectrum.Spectral investigation is confirmed that it is panlownin.The purity testing of the panlownin be separated is 98%.
example 15
The suppression that the antioxidant activity of panlownin forms algoscopy via above-described reactive oxygen species is determined.In this study, primary human keratinocytes replaces people's epithelium (KB) cell.Horn cell is paved plate with the density of 5000 cells/well in the tissue culture treated plate in 96-hole, is supplemented with 10% hyclone (Invitrogen Corp., San Diego, CA) DMEM (DMEM) in.After 48 hours; by hydrogen peroxide responsive type fluorescent probe 5-(with-6)-chloromethyl-2' of cell and 5 μMs; 7'-dichloro-dihydro-fluorescein diethylester, acetyl group ester (CM-H2DCFDA) (Invitrogen Corp. (Carlsbad, CA)) incubation 30 minutes.After incubation, clean described plate to remove excessive probe and to add to indicate the panlownin of concentration.Described plate is read immediately to detect the formation of basic peroxide on the fluorescence plate reader being set to 485nm excitation wavelength/530nm emission wavelength.Then make described plate be exposed to ultraviolet and (be equipped with the 1000W-Oriel solar simulator of 1-mm Schott WG 320 wave filter; 4.2kJ/m is used as what measure at 360nm place 2ultraviolet dosage).Plate reads 60 minutes after uv light exposure, and data are as mean fluorecence unit (MFU) report.The results are shown in following table 13.
table 13
The Si Shi T that * instruction uses significance level to be set to P<0.05 checks with the significant difference through UV treatment based on this example, and the ROS that significantly can reduce the induction of HEP's middle-ultraviolet lamp with panlownin process produces.Therefore; when applied to the skin; panlownin expection provides for the protection from the ROS induction shined upon; and expection provides and reduces the primary activity of aging sign like this, such as, external aggression in the appearance of the wrinkle on skin that improves skin tightness, improves texture, improves and treatment skin.
example 16
Composition shown in following skin care compositions use table 14 is prepared according to the present invention.
table 14
Above compositions is prepared as follows: at the temperature of 20-40 DEG C, purified water is added in main tank with steadily stirring.Subsequently Versene NA (disodiumedetate) is added this main tank.Stop the stirring of main tank and Ultrez 10 (carbomer) is added by the mode on aqueous mixtures top described in uniform fold.Described mixture carries out soaking and stirring and starts heating.Heat described mixture and be maintained at 55-60 DEG C, and mixing 15 minutes or until even further.
Finsolv TN (C12-15 benzoic acid Arrcostab) is added and heating reaches 55-60 DEG C and prepare oil phase by stirring in clean suitable compatible device.After reaching this temperature, add Brij 72 & 721 (being respectively steareth-2 ,-21), Miglyol (caprylic/capric triglyceride), Emery 917 (glycerol) and Penreco snow-white (vaseline) and at 55-60 DEG C mixing until add when becoming owner of in tank.
Described oil phase is added in this main tank, add strong mixing simultaneously and stop heating.The mixture 10-20 minute produced with mixed at high speed.Polydimethylsiloxane (Dow Corning siloxanes fluids) is added under 50 DEG C or lower temperature.Subsequently described batch be cooled to 40 DEG C and add Phenonip XB (preservative blends).The described mixture of further mixing 10 minutes or until even.Add sodium hydroxide (target pH=5.4) fast and stir 10 minutes further or until reach homogeneous pH.
Independently beaker mixing is added until evenly prepare active matter premixed liquid by ethylene glycol monomethyl ether CG, butanediol, citric acid and princess being set extract.
By described active matter premixed liquid is added the principal phase of described main tank and the mixing carrying out other 10-20 minute to dissolve completely or until evenly, thus prepare final preparation.Obtain final volume with water, mix described preparation 10 minutes and record pH.
The sample of compositions is placed 2 weeks in the baking oven of 50 DEG C, and it shows basic good stability.
example 17
Composition shown in following skin care compositions use table 15 is prepared according to the present invention.
table 15
Serial number CTFA/INCI title Percentage ratio (w/w) in formula
1 Purified water 75.55
2 Disodiumedetate 0.15
3 AVC 0.30
4 Adermykon C 0.20
5 Butanediol 6.00
6 Olive oil spermaceti alcohol ester/olive oil sorbitol ester 0.50
7 Stearic acid 0.50
8 Sensiva SC50 1.00
9 Cyclopentasiloxane & cyclohexasiloxane 5.00
10 Cyclopentasiloxane gathers dimethicone cross linked polymer 3.00
11 Dimethiconol & polydimethylsiloxane 2.00
12 Sodium hydroxide 2.40
13 Polyacrylate 13& polyisobutylene TWEEN-20 1.00
14 Methylisothiazolinone 0.15
15 Aromatic 0.01
16 FD&C is red 0.12
17 D&C is yellow 0.12
18 Rust royal paulownia (princess tree) extract 2.00
Amount to 100.00
Above compositions is prepared as follows: purified water added in main tank, adds disodiumedetate subsequently and mixes until ethylenediaminetetraacetic acid dissolves.Spray into ammonium acryloyldime-thyltaurate/VP homopolymer and the mixture of gained is heated to 70-75 DEG C.After reaching the temperature of setting, add olive oil spermaceti alcohol ester/olive oil spermaceti sorbitan ester and stearic acid, at the temperature of setting, stir described mixture 5 minutes simultaneously.
Be dissolved in butanediol at 40-50 DEG C prepare active matter premixed liquid by princess being set extract in independently container.Polyacrylate 13 and polyisobutylene and TWEEN-20 are added this princess to set in mixture and mixing subsequently until evenly.Reduce temperature to 35-40 DEG C and aside to place until be ready to add described main tank.
By Chlorophehesin being added butanediol in autonomous container and being heated to 35 DEG C, add Methylisothiazolinone subsequently, thus preparation Chlorophehesin premixed liquid.The mixture of gained is heated to 50-55 DEG C and maintains this temperature until be ready to be mixed into main tank.
By cyclopentasiloxane and Dimethicone Crosspolymer being added cyclopentasiloxane and cyclohexasiloxane in independently container, carrying out mixing simultaneously and being heated to 55-60 DEG C until evenly, thus preparing oil phase.Add Sensiva SC50 subsequently and mix until evenly, add stearic acid subsequently, simultaneous temperature maintains 55-60 DEG C.
Subsequently described oil phase is slowly added this main tank, stir tempestuously at 70-75 DEG C simultaneously.Dimethiconol and polydimethylsiloxane are added described main batch thing, and stir gained mixture 20 minutes or until evenly, after this stop heating.Use sodium hydroxide by main pH regulator to 5.0-5.5.Described Chlorophenesin phase is slowly added, simultaneously Keep agitation at 50-55 DEG C.This mixture be cooled to 35-40 DEG C and add that aromatic, FD & C are red and D & C yellow, and mixing, maintaining this temperature simultaneously.
Add this main tank by described active pre-composition is stirred lentamente and prepare final preparation.10-20 minute is remixed to described mixture until evenly.Obtain final volume with water, mix described preparation 10 minutes and record pH.
The sample of compositions is placed 2 weeks in the baking oven of 50 DEG C, and it shows basic good stability.

Claims (20)

1. one kind is improved the method for signs of skin aging, the described signs of skin aging that improves is selected from: the external aggression in the appearance of the wrinkle on skin that improves skin tightness, improves texture, improves, treatment skin and two or more combination in them, and described method comprises effectively improving skin tightness, improves texture, improves the appearance of wrinkle on skin, external aggression in treatment skin or improve the panlownin of amount to application on human skin administering therapeutic effective dose of the combination of two or more in them.
2. method according to claim 1, wherein said step of applying comprises the described panlownin to needing the dermal administration improving aging sign to be greater than zero to about 20%.
3. method according to claim 1, wherein said step of applying comprise to the dermal administration needing to improve aging sign at least about 20 % by weight described panlownin.
4. method according to claim 1, wherein said step of applying comprise to the dermal administration needing to improve aging sign at least about 50 % by weight described panlownin.
5. method according to claim 1, wherein said step of applying comprise to the dermal administration needing to improve aging sign at least about 90 % by weight described panlownin.
6. method according to claim 1, wherein said step of applying comprises the described panlownin to the dermal administration about 0.01 to about 1% needing to improve aging sign.
7. method according to claim 1, wherein said step of applying comprises the described panlownin to the dermal administration about 0.1 to about 5% needing to improve aging sign.
8. method according to claim 1, wherein said step of applying comprises the compositions to needing the dermal administration improving aging sign to comprise panlownin and carrier, and wherein said compositions is following form: solution, suspension, lotion, cream, essence, gel, stick, spray, ointment, washing liquid, soap slab, shampoo, hair conditioner, paste, foam, powder, mousse, shaving cream, hydrogel or film-forming products.
9. method according to claim 8, wherein said compositions also comprises tropoelastin promoter.
10. method according to claim 9, wherein said tropoelastin promoter is selected from blackberry extract, common smoketree extract, Feverfew P.E, Herba Scopariae extract and two or more combination in them.
11. methods according to claim 8, wherein said compositions also comprises collagen promoter.
12. methods according to claim 11, wherein said collagen promoter is non-retinoid collagen promoter.
13. methods according to claim 12, wherein said non-retinoid collagen promoter is selected from Feverfew P.E, Herba Centellae extract, Herba Siegesbeckiae extract, soybean extract and two or more combination in them.
14. methods according to claim 11, wherein said collagen promoter is retinoid.
15. methods according to claim 14, wherein said retinoid is selected from retinol, retinal, retinyl acetate, retinyl propionate, retinol linoleate, retinyl palmitate and two or more combination in them.
16. methods according to claim 1, wherein improve aging sign and comprise and improve skin tightness, and described step of applying comprise the panlownin to needing the application on human skin improving skin tightness to use effective dose.
17. methods according to claim 16, wherein said need the application on human skin improving skin tightness comprise for sagging, lax, loose, coarse, have wrinkle, thinning, the colour of skin is uneven or the skin of the combination of two or more in them.
18. methods according to claim 1, wherein improve aging sign and comprise the appearance improving wrinkle on skin, and the described step of applying application on human skin comprised to the appearance needing to improve wrinkle on skin uses the panlownin of effective dose.
19. methods according to claim 18, the wherein said application on human skin needing to improve the appearance of wrinkle on skin comprises the skin with wrinkle, microgroove or their combination.
20. methods according to claim 8, wherein said compositions also comprises sunscreen.
CN201410545360.XA 2013-10-17 2014-10-15 Compositions comprising extract of paulownia tomentosa wood and uses thereof Pending CN104546523A (en)

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CN105031239A (en) * 2015-07-10 2015-11-11 北京国济众芳中医药研究所 External-use traditional Chinese medicine composition with efficacies of moisturizing and firming hair, preparation, and preparation method of preparation
CN112107639A (en) * 2020-11-13 2020-12-22 青州尧王制药有限公司 Application of fructus viticis extract in preparation of antidepressant drugs
CN113230175A (en) * 2021-05-28 2021-08-10 潍坊职业学院 A cosmetic containing Sterculia procumbens extract and its extraction method
CN113652396A (en) * 2021-08-24 2021-11-16 河南省鸣利隆医药科技有限公司 Adipose-derived mesenchymal stem cell osteogenesis inducing composition and osteogenesis inducing method

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CN103180016A (en) * 2010-08-19 2013-06-26 强生消费者公司 Compositions comprising paulownin and/or paulownia extracts and uses thereof
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Publication number Priority date Publication date Assignee Title
CN105031239A (en) * 2015-07-10 2015-11-11 北京国济众芳中医药研究所 External-use traditional Chinese medicine composition with efficacies of moisturizing and firming hair, preparation, and preparation method of preparation
CN105031239B (en) * 2015-07-10 2018-06-22 北京国济众芳中医药研究所 There is external medicine composition, preparation of scalp moisturization strengthen the hair and preparation method thereof
CN112107639A (en) * 2020-11-13 2020-12-22 青州尧王制药有限公司 Application of fructus viticis extract in preparation of antidepressant drugs
CN113230175A (en) * 2021-05-28 2021-08-10 潍坊职业学院 A cosmetic containing Sterculia procumbens extract and its extraction method
CN113652396A (en) * 2021-08-24 2021-11-16 河南省鸣利隆医药科技有限公司 Adipose-derived mesenchymal stem cell osteogenesis inducing composition and osteogenesis inducing method
CN113652396B (en) * 2021-08-24 2023-08-29 赛尔医学科技(山东)有限公司 Adipose-derived mesenchymal stem cell osteogenesis inducing composition and osteogenesis inducing method

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CA2867544A1 (en) 2015-04-17

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