WO2019234635A1 - 包含金钗石斛的组合物及其使用方法 - Google Patents

包含金钗石斛的组合物及其使用方法 Download PDF

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Publication number
WO2019234635A1
WO2019234635A1 PCT/IB2019/054649 IB2019054649W WO2019234635A1 WO 2019234635 A1 WO2019234635 A1 WO 2019234635A1 IB 2019054649 W IB2019054649 W IB 2019054649W WO 2019234635 A1 WO2019234635 A1 WO 2019234635A1
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Prior art keywords
skin
air pollution
composition
induced
dendrobium
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PCT/IB2019/054649
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English (en)
French (fr)
Inventor
黄满莲
宋贤丽
黄娟
李波
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捷通国际有限公司
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Application filed by 捷通国际有限公司 filed Critical 捷通国际有限公司
Priority to JP2020567120A priority Critical patent/JP2021532064A/ja
Priority to EP19815641.6A priority patent/EP3804694A4/en
Priority to KR1020217000018A priority patent/KR20210018893A/ko
Priority to US17/056,957 priority patent/US20210212926A1/en
Publication of WO2019234635A1 publication Critical patent/WO2019234635A1/zh

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Classifications

    • 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)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/898Orchidaceae (Orchid family)
    • A61K36/8984Dendrobium
    • 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
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9794Liliopsida [monocotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/18Antioxidants, e.g. antiradicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/04Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
    • 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
    • A61Q19/004Aftersun preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/005Preparations for sensitive 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
    • A61Q19/08Anti-ageing preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair

Definitions

  • compositions and methods of using the same for preventing, treating and / or curing human skin from air pollution-induced damage.
  • Human skin is the outer covering of the body. In humans, it is the largest organ of the skin system. The skin has multiple layers of ectodermal tissue and protects the underlying muscles, bones, primordial bands, and internal organs.
  • the two main layers of skin include the stratum corneum (or epidermis) and the dermis.
  • the epidermal layer is the top or outer layer of the skin and its main function is to provide protective coverage and delay the internal water loss through evaporation.
  • the epidermal layer resists mechanical damage, ingress of foreign chemicals and contaminants, and microbial attack. It also provides the first protection against UV rays.
  • the dermis is below the epidermis and makes up 90% of the skin's thickness.
  • the dermis contains dense collagen and elastin networks, providing strength and elasticity to the skin.
  • Fibroblasts are the main cell types that make up the dermal layer and are responsible for the synthesis and secretion of dermal matrix components, including collagen, elastin, and glycosaminoglycans such as hyaluronic acid.
  • collagen provides strength to the skin
  • elastin provides elasticity
  • glycosaminoglycan is to keep the skin moist and plump.
  • the skin To stay healthy, the skin must be able to cope with changes in environmental conditions and air pollution, while repairing any damage to the skin.
  • Environmental factors and air pollution play important roles in aging, wrinkles, skin discoloration, and degenerative skin conditions and skin diseases such as skin cancer.
  • Air pollution occurs when harmful substances, including particles and biomolecules, are released into the Earth's atmosphere. It can cause illness, allergy, or death in humans; it can also cause harm to other organisms, such as animals and food crops, and it can damage natural or man-made environments. Both human activities and natural processes produce air pollution. Exposure to air pollution can adversely affect the skin, cause skin aging, wrinkles and inflammation, and may even cause skin cancer. Epidemiological studies have shown that repeated exposure of human skin to air pollution is one of the causes of external skin aging associated with stains and wrinkles (Vierkoetter et al., J Invest Dermatol, 130 (12): 2719-26 (2010)) . Exposure to sunlight and UV radiation are also major causes of skin damage, accounting for 90% of symptoms of premature aging.
  • Free radicals can cause wrinkles by activating metalloproteinases (such as gelatinase) responsible for breaking skin connective tissue (collagen and elastin). The result is premature aging. Free radical damage can also cause thinning of the dermal layer. This can cause skin sagging. Skin sagging is the first and most commonly seen phenomenon of aging, causing wrinkles and lines.
  • metalloproteinases such as gelatinase
  • compositions and methods that can not only improve the appearance and condition of the skin, but also combat the adverse consequences of air pollutants on human skin and protect skin cells from air pollution-induced skin damage, method.
  • these compositions and methods optionally also combat the adverse consequences of skin exposure to sunlight and UV radiation and / or other environmental conditions.
  • the application provides combinations for preventing, treating, and / or curing human skin and / or hair from air pollution-induced and / or air pollution-induced skin and / or hair damage, optionally with additional skin benefits. Things and methods. Summary of the invention
  • One embodiment relates to a cosmetic composition
  • a cosmetic composition comprising an effective amount of an isolated ingredient or extract of Dendrobium nobile and a cosmetically acceptable carrier or excipient sufficient to achieve at least one of the following: reducing or preventing air Pollution-induced or air pollution-induced skin and / or hair damage; Reduce or prevent air pollution-induced oxidative stress; Reduce or prevent air pollution-induced cell viability; Reduce or prevent air pollution-induced increase in IL-6; Or reduce or prevent air pollution-induced cell damage.
  • the skin damage is skin aging, lines, fine lines, wrinkles Wrinkles, crow's feet, dark circles, scars, age spots, dark spots, iridescent lines, skin cancer, skin inflammation, skin discoloration, skin pigmentation, or a combination thereof.
  • the composition may be a personal care composition, a skin care composition, a hair care composition, an anti-aging care composition, a sun care composition, or a combination thereof.
  • the composition can be in the form of: aerosol, cream, emulsion, solid, liquid, dispersant, foam, gel, toner, mousse, ointment, powder, patch, balm, solution, pump Spray, stick, oil, wipes, or a combination thereof.
  • the ingredients or extracts of Dendrobium candidum can be present in an amount of about 0.0001% to about 5% of the total weight of the composition.
  • the ingredients or extracts of Dendrobium candidum can be present in an amount of about 0.01% to about 0.1% of the total weight of the composition.
  • the cosmetically acceptable carrier or excipient may be selected from the group consisting of water, glycerol, C1-C4S, fatty alcohols, fatty ethers, fatty esters, polyols, glycols, vegetable oils, mineral oils, liposomes, Layer of lipid material, silicone oil, or a combination thereof.
  • Another embodiment relates to a medicament comprising a component or extract of Dendrobium nobile and a pharmaceutically acceptable carrier or excipient, wherein the medicament is for preventing, treating and / or curing human skin and / or hair At least one of the following: air pollution-induced or air pollution-induced skin and / or hair damage; air pollution-induced oxidative stress; air pollution-induced cell viability reduction; air pollution-induced IL-6 increase; or air Contamination-induced cell damage.
  • the skin damage may be skin aging, lines, fine lines, wrinkles, crow's feet, dark circles, scars, age spots, dark spots, nimbus lines, skin cancer, skin inflammation, skin discoloration, skin pigmentation, skin barrier function damage , Or a combination of them.
  • the ingredients or extracts of Dendrobium candidum can be present in an amount of about 0.0001% to about 5% of the total weight of the composition.
  • the ingredients or extracts of Dendrobium candidum can be present in an amount of about 0.01% to about 0.1% of the total weight of the composition.
  • Yet another embodiment relates to a packaging system comprising one or more containers and instructions for administering the composition from the one or more containers, the containers collectively containing the composition.
  • the packaging system may include at least one of: (a) one or more containers collectively containing a composition described herein; or (b) for applying the composition from the one or more containers Manual.
  • Another embodiment relates to a method of protecting human skin and / or hair against air pollution-induced damage, comprising topically applying the composition to the skin and / or hair.
  • An ingredient or extract of Dendrobium nobile is applied to human skin and / or hair in an effective amount of about 0.01 to about 5 mg / cm 2 .
  • the component or extract of Dendrobium nobile is applied to human skin and / or hair in an effective amount of about 0.05 to about 5 mg / cm 2 .
  • Yet another embodiment relates to the use of a component or extract of Dendrobium nobile as an antifouling agent for protecting human skin and / or hair.
  • the anti-contamination involves protecting and reducing the barrier and dysfunction of human skin and hair.
  • the bar graph shown in Figure 1 shows PM2.5 toxicity testing.
  • the bar graph shown in Figure 2 is the toxicity test of D. officinale extract at 4 hours and 24 hours after treatment.
  • the bar graph shown in Figure 3 demonstrates that Dendrobium nobile extract is effective against PM2.5 without increasing oxidative stress in Hacat cells due to increased reactive oxygen species (ROS) levels.
  • ROS reactive oxygen species
  • the bar graph depicted in Figure 4 shows the results of the mitochondrial membrane potential (MMP) test; PM2.5 significantly reduces MMP levels, while Dendrobium nobile extract protects cell viability.
  • MMP mitochondrial membrane potential
  • Figure 5 depicts a bar graph showing IL-6 levels induced by various test samples; PM2.5 significantly increased IL-6 levels, and compared with the PM2.5 treated group, Dendrobium nobile extract significantly reduced IL- 6 levels (down 41.3%).
  • the present invention is based on the unexpected discovery that plant components and / or plant extracts of Dendrobium candidum reduce and / or prevent air pollution-induced or air pollution-induced skin and / or hair damage, and reduce and / or prevent air pollution induction Oxidative stress reduces and / or prevents air pollution-induced cell viability, reduces and / or prevents air pollution-induced increase in IL-6, and / or reduces or prevents air pollution-induced cell damage.
  • the component or extract may be derived from any species member of the genus Dendrobium; preferably, the component or extract may be a component or extract of Dendrobium nobile.
  • compositions comprising isolated plant components and / or plant extracts of Dendrobium plants (eg Dendrobium nobile) and uses of these compositions in an amount sufficient to prevent, treat and / or Heal human skin and / or hair from at least one of the following: air pollution-induced or air pollution-induced skin and / or hair damage, air pollution-induced oxidative stress, air pollution-induced reduction of cell viability, air Increased pollution-induced IL-6; and / or air pollution-induced cell damage.
  • Dendrobium plants eg Dendrobium nobile
  • composition means a treatable,? Products that are gentle, promote, increase, manage, control, maintain, optimize, modify, reduce, inhibit or prevent specific conditions associated with natural states, biological processes or diseases or disorders.
  • the compositions described herein can improve at least one of the following conditions in a subject: pollution-induced or air pollution-induced skin and / or hair damage, air pollution-induced oxidative stress, air pollution-induced Cell viability decreases, air pollution-induced IL-6 increases; and / or air pollution-induced cell damage.
  • composition includes, but is not limited to, a pharmaceutical product (ie, a drug), an over-the-counter drug (OTC), a cosmetic, a food, a food ingredient, or a dietary supplement composition comprising an effective amount of an extract, at least one component thereof, or a mixture thereof.
  • a pharmaceutical product ie, a drug
  • OTC over-the-counter drug
  • compositions described herein include aerosols, creams, emulsions, solids, liquids, dispersants, foams, foam coatings, gels, toners, mousses, ointments, kits or powders, emulsions , Patches, balms, solutions, pump sprays, sticks, oils, wipes, tablets, plasters, granules, and / or combinations thereof.
  • air pollution refers to any natural or man-made source caused by smog and / or harmful gases (such as traffic emissions and industrial exhaust gases), mainly carbon, sulfur and nitrogen oxides, any released particles or droplets Air pollution.
  • gases such as traffic emissions and industrial exhaust gases
  • any particles released from the wear of rubber tires can be considered air pollutants.
  • These air pollutants can bind PAHs, but they also include other chemicals.
  • the carbon black particles released by the printer can be considered as air pollutants in the indoor environment. Indoor cooking, such as with coal or firewood, can also produce air pollutants.
  • Air pollutants are substances in the air that can adversely affect humans and ecosystems, and contribute to air pollution.
  • the substance can be a solid particle, a droplet, or a gas.
  • Contaminants can be of natural origin or man-made.
  • Pollutants are classified as primary or secondary pollutants.
  • the primary pollutant is usually produced by a process, such as the ash from a volcanic eruption. Other examples include carbon monoxide gas in automobile exhaust or sulfur dioxide released from factories.
  • Secondary pollutants are not directly discharged. Instead, they are formed in the air when the primary pollutants react or interact.
  • Ground-level ozone is a prominent example of secondary pollutants.
  • Some pollutants may be both primary and secondary pollutants: they are both directly emitted and formed by other primary pollutants.
  • Exemplary primary air pollutants comprising: carbon dioxide (C0 2) (e.g. by burning of fossil fuel emissions); volcanic and various industrial processes (e.g., coal and oil, generally contain sulfur compounds, they are burned to produce sulfur dioxide) generated by sulfur oxides ( SOx), such as sulfur dioxide (S0 2 ); nitrogen oxides (NO x ) emitted by high temperature combustion, such as nitrogen dioxide (N0 2 ); — carbon oxide (CO) is a colorless, odorless, toxic but non-irritating
  • SOx sulfur oxides
  • NO x nitrogen oxide
  • CO carbon oxide
  • the gas is a combustion product of fuels such as natural gas, coal, or wood, and is produced by automobile exhaust
  • Volatile Organic Compounds (VOC) a well-known outdoor air pollutant, such as pinane (CH 4 ) or non-pinane ( NMVOC) (aromatic NMVOC, including benzene, toluene, and dibenzobenzene are suspected carcinogens; 1,3-but
  • Exemplary secondary air pollutants include particulate matter resulting from gaseous primary pollutants and compounds in photochemical smog.
  • Haze is a type of air pollution.
  • Traditional smog originates from the burning of large amounts of charcoal in an area and is caused by a mixture of smog and sulfur dioxide.
  • Modern haze usually does not come from coal, but from vehicle and industrial emissions. These emissions form secondary pollutants in the atmosphere under the action of ultraviolet light from the sun.
  • the secondary pollutants combine with the main emissions to form a photochemical haze.
  • Ground-level ozone (0 3 ) is formed from NO x and VOC.
  • Ozone (0 3 ) is an important component of the troposphere. It is also an important component of some areas of the stratosphere, often called the ozone layer.
  • air pollution-induced skin and / or hair damage refers to any skin and / or hair damage, disease, and / or condition caused by short-term and / or long-term exposure to air pollution.
  • Air pollution-induced skin and / or hair damage can manifest, for example, as skin aging; formation of wrinkles and inflammation; formation of lines (such as fine lines), wrinkles, crow's feet; formation of dark circles; formation of Scars, acne, senile plaques, dark spots, rengio lines; cancer formation (including skin cancer); skin discoloration, skin pigmentation, or a combination thereof.
  • air pollution-induced skin and / or hair damage can manifest as psoriasis, eczema, seborrhea, dermatitis, sunburn, estrogen imbalance, yellowing, freckles, skin atrophy, skin rash, skin fragility, dryness, and touch Roughness, cleft palate, sagging, thinning, hyperplasia, fibrosis, enlarged pores, cellulite formation, dementia, apoptosis, cell differentiation, cell dedifferentiation, virus infection, fungal infection, bacterial infection, spider vein (capillary expansion ), Hirsutism, rosacea, pruritus, old stems, fatigue, corns, or combinations thereof.
  • air pollution-induced skin and / or hair damage refers to any skin and / or hair damage, disease, and / or condition that can form in response to the presence of air pollutants.
  • extract or "plant extract” as used herein means a solid, viscous, or liquid substance or article containing an isolated active ingredient of a plant material, such as Dendrobium (eg, Dendrobium nobile) .
  • the ingredients or extracts may be from members of any species of Dendrobium.
  • extract includes not only derived from Dendrobium (eg Dendrobium nobile) and by using a lower alcohol selected from water, 1-4 carbon atoms (such as acetol, ethanol, butanol, etc.), Otome, acetone, hexane Alkane, diethyl ether, chloroform, ethyl acetate, butyl acetate, dichloromethane, N, N-dimethylfluorenamide (DMF), dimethylsulfoxide (DMSO), 1,3-butanediol, propylene glycol And a combination thereof, and also includes a part of the crude extract in the solvent. Any extraction method can be used as long as the method guarantees the extraction and preservation of the active ingredient.
  • An example of a plant extract includes an extract from a Dendrobium plant.
  • the "foot t '", “effective amount” or “therapeutically effective amount” means that the amount of the pure compound, composition, extract, plant extract, extract mixture, plant extract mixture,
  • a subject eg, a mammal such as a human
  • Induced or air pollution can induce skin and / or hair damage, air pollution induced oxidative stress, air pollution induced cell viability decrease, air pollution induced IL-6 increase; and / or air pollution induced cell damage, etc.
  • compositions, extract, extract, plant extract, extract mixture, plant extract mixture, extract component and / or active agent or ingredient that constitutes an "effective amount” or “therapeutically effective amount” will be based on the active agent or Compounds, the condition to be treated, its severity, the The method of medication, duration of treatment, or age of the subject to be treated varies, but can be routinely determined by one of ordinary skill in the art based on their own knowledge and the content disclosed in this application.
  • the term "protect, treat and / or cure human skin and hair growth against air pollution-induced damage” refers to preventing, preventing, reversing, improving, reducing and / or reducing air pollution-induced damage, particularly to human skin and / Or hair damage.
  • Representative signs of air pollution-induced damage include, but are not limited to, skin aging, lines, fine lines, wrinkles, crow's feet, dark circles, scars, age spots, dark spots, irritated lines, cancer (including skin cancer), skin inflammation, Skin discoloration, skin pigmentation, or a combination thereof.
  • Other signs of air pollution-induced damage to skin and hair include psoriasis, eczema, seborrhea, dermatitis, sunburn, estrogen imbalance, yellowing, freckles, skin atrophy, skin hair treatment, skin fragility, dryness, and rough touch , Cleft palate, relaxation, thinning, hyperplasia, fibrosis, enlarged pores, cellulite formation, dementia, acne formation, apoptosis, cell differentiation, cell dedifferentiation, prevention of tumor induction or tumor progression, viral infection, fungal infection, bacteria Infection, spider veins (capillary dilation), hirsutism, rosacea, pruritus, calluses, fatigue, corns, or a combination thereof.
  • cosmetically acceptable and “pharmaceutically acceptable” mean those drugs, medicines, ointments, extracts or inert ingredients suitable for use in contact with human and lower animal tissues, without excessive toxicity, without Compatibility, instability, stimulus, etc., are commensurate with a reasonable benefit / risk ratio.
  • administering and “administering” are used interchangeably and are defined to provide a composition to a subject by means known in the art, including but not limited to topical, oral, intravenous, intraarterial, parenteral, containing Administration route of administration, transdermal, rectal, intramuscular, subcutaneous, intraosseous, transmucosal or intraperitoneal.
  • the composition is suitable for topical administration (i.e., “topical application").
  • module refers to a pure compound, composition, extract, extract mixture, extract component, and / or active agent or ingredient of Dendrobium, or a combination thereof that increases, stimulates, or enhances, or decreases, The ability to prevent or inhibit the expression or activity of specific molecules, thereby reducing or preventing air pollution-induced or air pollution-induced skin and / or hair damage.
  • modulation can refer to the ability of Dendrobium to reduce air pollution-induced oxidative stress, reduce air pollution-induced cell viability, reduce air pollution-induced increase in IL-6, and / or reduce air pollution-induced cell damage.
  • the term also refers to the anti-irritant or anti-inflammatory properties of Dendrobium, which is used to combat the potential irritation of the skin caused by air pollution.
  • reduced refers to protein activity and / or expression in the absence of plant components or plant extracts of Dendrobium (Dendrobium nobile) (eg, in a control sample) In comparison, in the presence of Dendrobium In the case of Dendrobium) plant components or plant extracts, the protein activity and / or expression and / or its downstream effects are reduced or reduced.
  • Dendrobium Dendrobium nobile
  • the degree of reduction or inhibition of protein activity and / or expression and / or its downstream effects will vary with the nature and amount of the plant component or plant extract of Dendrobium present, but it is obvious that it is detectable, for example Reduction in protein activity and / or expression; ideally, the degree of reduction is greater than 10%, 25%, 50%, 75%, compared to protein activity and / or expression in the absence of plant components or plant extracts of Dendrobium 90%, 95%, or 99%.
  • prevention when used to prevent air pollution-induced skin and / or hair damage, air pollution-induced oxidative stress, air pollution-induced decrease in cell activity, air pollution-induced increase in IL-6 in a subject; and In the case of air pollution-induced cell damage, etc., it is meant to maintain these effects not to occur or absent.
  • the terms “increase”, “energize P”, “stimulate” or “stimulate” refer to proteins that are associated with plant components or plant extracts where Dendrobium is absent (eg, in a control sample). Compared to activity and / or expression, protein activity and / or expression and / or its downstream effects are increased in the presence of plant components or plant extracts of Dendrobium.
  • the degree of increase in protein activity and / or expression and / or its downstream effects will vary with the nature and amount of the plant component or plant extract of Dendrobium present, but it is obvious that it is a detectable protein activity And / or an increase in expression; ideally, the degree of increase is greater than 10%, 25%, 50%, 75%, 90%, compared to protein activity and / or expression in the absence of plant components or plant extracts of Dendrobium 95% or 99%.
  • the term "subject” or “individual” includes mammals to which a composition can be administered or applied.
  • mammals include humans, non-human primates, rodents (including transgenic and non-transgenic mice), and the like.
  • the subject is a mammal, and in some embodiments, the subject is a human.
  • One embodiment relates to a cosmetic composition
  • a cosmetic composition comprising an isolated component or extract of Dendrobium (eg, Dendrobium nobile) and at least one pharmaceutically or cosmetically acceptable vehicle, wherein the amount of the isolated component or extract is sufficient to reduce or Prevent air pollution-induced or air pollution-induced skin and / or hair damage (eg, skin cancer, skin inflammation and / or pigmentation), reduce or prevent air pollution-induced oxidative stress, reduce or prevent air pollution-induced Reduced cell viability, reduced or prevented air pollution-induced increase in IL-6 and / or reduced or prevented air pollution-induced cell damage.
  • Dendrobium is a large genus of Orchidaceae and currently contains about 1,200 species.
  • Dendrobium species can be epiphytic or occasionally rock surface plants. They have adapted to a variety of habitats, from the high altitudes of the Himalayas to low-lying tropical forests and even the dry climate of the Australian desert.
  • Exemplary species of the litholytic genus include Dendrobium anosmum, Dendrobium aphyllum, Dendrobium begaudii, Dendrobium bilobum, Dendrobium brevicaudum, Dendrobium bukidnonensis, Dendrobium bullenianum, Dendrobium bullenianum Dendrobium cariniferum), Dendrobium ceraula, Dendrobium chameleon, Dendrobium chrysanthum, Dendrobium conanthum, Dendrobium crispilinguum, Dendrobium crumenatum, Dendrobium cuthbertendiumiumiium, , Dendrobium epidendropsis, Dendrobium euryanthum, Dendrobium fairchildae, Dendrobium falcorostrum, Dendrobium forbesii, Dendrobium formosum, Dendrobium gerlandianum, Dendrobium gibsonii, Dendrobium gnommium
  • an isolated component or extract of Dendrobium nobile is used to produce the composition described herein.
  • Dendrobium nobile is a very precious and famous Chinese herbal plant with beautiful flowers. Its name comes from its shape; Dendrobium nobile looks like an ancient Chinese pin.
  • Extracts from Dendrobium candidum stems can be obtained from 17 phenanthrenes, including 3, 4, 8-trimethoxyphenanthrene-2, 5-diol, 2,8-dihydroxy- 3 -Hydroxy-2,4,7-trisanthol t-9,10-dihydrophenanthrene, 2, 8-dihydroxy-3,4,7-trisoxol-9, 10 -dihydrophenanthrene, 2- Hydroxy-4, 7-dioxo-9, 10-dihydrophenanthrene, 2,2'-dihydroxy-3,3 ', 4,4', 7,7'-hexaoxo-9,9 ', 10, 10'-tetrahydro-1, 1'-biphenanthrene and 2, 3, 5-triyl-4, 9-diphenanthrene (Hwang, Ji Sang, et al., "Phenanthrenes from
  • the extract of Dendrobium candidum can be standardized to about 0.01-80% polysaccharide. In some alternative embodiments, the extract of Dendrobium candidum can be standardized to about 0.1-0.2% (w / w) polysaccharide.
  • plant extracts used in the unique compositions described herein can be obtained using deionized water extraction techniques.
  • polysaccharide extraction can be performed by extracting the stem of Dendrobium nobile with deionized water at a temperature (10-100 ° C), centrifuging, and filtering. Next, the extract was concentrated in vacuo at low temperature. The polysaccharide was purified and concentrated by adding ethanol to obtain a sediment-dispersed solvent. Next, the sediment was centrifuged and collected, and dissolved in water. It is subsequently sterilized and the extract is packaged.
  • water extraction and alcohol precipitation methods (0-30% ethanol-7jc (v / v)) can be used to obtain plant extracts that can be used in the unique compositions described herein.
  • the plant extracts produced in this process can contain a variety of phytochemicals, the continuous use of alcohol precipitation can achieve purification and concentration of polysaccharides.
  • a membrane filtration method can be used to obtain a plant extract that can be used in the unique composition described herein.
  • the plant extract produced by the extraction process will contain various phytochemicals present in the extract.
  • any suitable plant component and plant extract of Dendrobium candidum can be obtained using any of the extraction and purification techniques discussed more fully below or known in the art.
  • Topical composition described herein can reduce or prevent air pollution-induced or air pollution-induced skin and / or hair damage, reduce or prevent air pollution-induced oxidative stress, and reduce or prevent air pollution-induced cell viability Reduce, reduce or prevent air pollution-induced increase in IL-6 and / or reduce or prevent air pollution-induced cell damage.
  • the administration of a topical composition described herein can result in a reduction in ROS levels of at least about 5%, at least about 10%, at least about 15%, at least about 20%, at least about 21%, at least about 21.5 %; At least about 22%, at least about 22.5%; at least about 23%, at least about 23.5%; at least about 24%; at least about 24.5%, at least about 25%, at least about 25.5%, at least about 26%, at least about 26.5 %, At least about 27%, at least about 27.5%, at least about 28%, at least about 28.5, at least about 29%, at least about 29.5%, or at least about 30% (the percentages between the exemplary percentages provided in this application should also be consider). Higher percentage reductions can also be considered.
  • the application of the topical composition described herein can result in a reduction in ROS levels of about 27.78%.
  • the administration of the topical composition described herein can result in a reduction in the rate of cellular damage by about 5%, at least about 10%, at least about 15%, at least about 20%, at least about 21%, at least about 21.5 %; At least about 22%, at least about 22.5%; at least about 23%, at least about 23.5%; at least about 24%; at least about 24.5%, at least about 25%, at least about 25.5%, at least about 26%, at least about 26.5 %, At least about 27%, at least about 27.5%, at least about 28%, at least about 28.5, at least about 29%, at least about 29.5%, at least about 30%, at least about 30.5%, at least about 31%, at least about 31.5% , At least about 32%, at least about 32.5%, at least about 33%, at least about 33.5%, at least about 34%, at least about 34.5%, or at least about 35% (percentages between the exemplary percentages provided herein should also be considered ).
  • the administration of the topical composition described herein can result in a reduction in IL-6 7jc level of about 5%, at least about 10%, at least about 15%, at least about 20%, at least about 21%, at least About 21.5%; at least about 22%, to Less than about 22.5%; at least about 23%, at least about 23.5%; at least about 24%; at least about 24.5%, at least about 25%, at least about 25.5%, at least about 26%, at least about 26.5%, at least about 27%, At least about 27.5%, at least about 28%, at least about 28.5, at least about 29%, at least about 29.5%, at least about 30%, at least about 30.5%, at least about 31%, at least about 31.5%, at least about 32%, at least About 32.5%, at least about 33%, at least about 33.5%, at least about 34%, at least about 34.5%, at least about 35%, at least about 35.5%, at least about 36%, at least about 36.5%
  • the composition can also provide a variety of anti-aging and texture benefits. It is believed that the composition comprising Dendrobium nobile provides significant anti-pollution effects and has significant anti-aging and texture benefits over other commercially available topical skin health products.
  • the anti-pollution benefits of a composition comprising Dendrobium nobile are manifested as anti-aging and improving cosmetic appearance. Accordingly, some embodiments relate to topical compositions and their use to treat the skin to prevent, prevent, reverse, improve, reduce, reduce or improve the signs of aging (including air pollution-induced or air pollution-induced skin and / or hair damage Or signs related to it).
  • Signs of aging include but are not limited to fragile skin; loss of collagen and / or elastin; estrogen imbalance in the skin; skin atrophy; appearance and / or deepening of lines and / or wrinkles (including fine lines); skin discoloration including dark circles Crow's feet; sagging skin; skin tiredness and / or tension such as skin rash; dry skin, fine lines due to dry skin, rough skin; exfoliated skin; cell aging; loss of skin tone, elasticity, transparency, brightness and / Or gloss; loss of skin firmness; poor skin texture; loss of skin elasticity and / or resilience; skin thinning and inflammation.
  • the benefits and improvements to the cosmetic appearance of the skin can manifest as any of the following: reduced pore size, fine lines, wrinkles, rough touch, and inflammation; improved skin tone, light, transparency, and / or tightness; promoted resistance Oxidative activity; Improve skin firmness, fullness, softness and / or softness; Improve collagen production and / or collagen production; Improve skin texture and / or promote re-kinetics; Skin barrier repair and / or function Improved; Improved appearance of skin contours; Restored skin gloss, transparency, and whiteness; Basic nutrients and ingredients in skin caused by aging and / or menopause Reduced supplementation; improved skin cell connections; increased cell proliferation and / or proliferation; decreased skin cell metabolism due to aging and / or menopause; improved skin moisturization; promoted and / or accelerated cell renewal; skin thickness Increased skin elasticity and / or resilience; and increased exfoliation with or without the use of a or P light acids, keto acids, or other exfoliants.
  • Other benefits may include increased skin smoothness and / or softness, increased feeling of skin condition, increased skin moisture, reduced skin pressure and fine lines, increased brightness and / or whiteness, improved skin texture, and improved skin firmness.
  • the topical composition comprises an isolated component or extract of Dendrobium (e.g. Dendrobium nobile) in an amount sufficient to at least reduce and / or prevent air pollution-induced or air pollution-induced skin and / or Hair damage, reduce or prevent air pollution-induced oxidative stress, reduce and / or prevent air pollution-induced cell viability, reduce or prevent air pollution-induced increase in IL-6, and / or reduce or prevent air pollution-induced cell damage .
  • Dendrobium e.g. Dendrobium nobile
  • Dendrobium candidum can be present in an amount ranging from about 0.0001% to 5% of the total weight of the composition; desirably, from about 0.001% to about 2.5% of the total weight of the composition; more desirably, from about 0.001% to about 0.001% of the total weight of the composition About 0.5%; even more desirably, from about 0.01% to about 0.1% of the total weight of the composition.
  • the composition may be a personal care composition, a skin care composition, a hair care composition, an anti-aging care composition, or a sun care composition.
  • the composition may have a pH of about 6.0 to about 8.0, or the composition may have a substantially neutral pH. In some embodiments, the composition in which the plant extract is used has a substantially neutral pH.
  • Some further embodiments relate to a topical composition
  • a topical composition comprising Dendrobium in an amount sufficient to provide an anti-irritant or anti-inflammatory benefit to the skin, thereby resisting potential skin irritation caused by air pollution.
  • Other components comprising Dendrobium in an amount sufficient to provide an anti-irritant or anti-inflammatory benefit to the skin, thereby resisting potential skin irritation caused by air pollution.
  • compositions described herein may further include a DNA repair enzyme.
  • DNA repair enzyme is intended to include the aforementioned enzymes and other enzymes currently known or subsequently discovered or developed, including glycosylases, purine-free / pyrimidine-free endonucleases Or other enzymes that have the ability to repair damaged DNA.
  • DNA repair enzymes can include enzymes involved in base excision repair (BER), nucleotide excision repair (NER) pathways, or other excision repair pathways, as described in US Patent 6,368,594. These pathways are mediated by histones capable of DNA excision, damage removal, gap filling, and conjugation reactions.
  • the NER pathway constitutes a widely distributed non-specific repair pathway for damage, which coordinates the removal of DNA damage through a double nick response upstream and downstream of the damage site, resulting in the release of the oligonucleotide containing the damage. After removing the damaged DNA, fill the resulting gap and join the DNA ends together.
  • the BER pathway is the primary defense against all major forms of DNA base damage. This approach is responsible for the detection and removal of specific single-base lesions from large amounts of undamaged DNA.
  • the BER pathway usually involves the activity of N-glycosylase / AP lyase specific for CPD.
  • the N-glycosylase / AP lyase first cleaves the N-glycosidic bond of CPD5 'pyrimidine, and then cleaves the diester backbone at the abasic site through the P-lyase mechanism.
  • DNA repair enzymes suitable for use in combination with the ingredients and / or extracts of Dendrobium have N-glycosylase / AP lyase that recognizes, excises and repairs damaged DNA (such as CPD and (6-4) photo products) active.
  • the activity of these enzymes can be light-dependent (eg, photolytic enzymes) or light-independent.
  • Exemplary DNA repair enzymes in this group include, but are not limited to, phage T4 pyrimidine dimer-specific endonuclease (denV endonuclease), Micrococcus luteus N-glycosylase / AP lyase, Saccharomyces cerevisiae N-glycosylase / purine-free-pyrimidine lyase, Schizosaccharomyces pombe UV damage endonuclease (UVDE), chlorella virus isolate PBCV- 1 Pyrimidine dimer-specific glycosylases, Aspergillus nidulans photolyases, and their modified non-natural (eg, recombinant) enzyme products.
  • phage T4 pyrimidine dimer-specific endonuclease denV endonuclease
  • Micrococcus luteus N-glycosylase / AP lyase Saccharomyces cerevisiae N-glycosy
  • DNA repair enzymes can also include other members from BER, NER or other pathways. These enzymes may include 0 6 -guanosylguanine-DNA glutamyltransferases, uracil and hypoxanthine-DNA glycosylases, DNA exonucleases, damaged base glycosylases (eg, 3- ⁇ Adenine-DNA glycosylase), endonucleases alone or in complexes (such as E. coli uvrA / uvrB / uvrC endonuclease complexes) and other enzymes and enzymes whose activity is currently only partially understood Complexes, such as the human ERCC gene product and yeast's RAD gene.
  • Exemplary DNA repair enzymes include, but are not limited to, uracil DNA glycosylase, 3-methyladenine DNA glycosylase, endonuclease III / thymine glycol DNA glycosylase, endonuclease VIII, fapy / 8-oxoguanine DNA glycosylase, AG-mismatched DNA glycosylase, GT mismatched DNA glycosylase, galacyluracil DNA glycosylase, hydroxymethyluracil DNA glycosylase, XPC-hHR23B, XPA, RPA , XPB, TFIIH, XPG, XPF-ERCC1, Rad-4-Rad23, Radl4, Rfa, Rad25 / Ssl2, Rad3, Rad2, Radi -Rad 10 ⁇ various DNA polymerization Enzymes, DNA ligases, etc.
  • Exemplary sources of these enzymes may include bacterial or mammalian cell sources, including but not limited to E. coli, Saccharomyces cerevisiae, Schizosaccharomyces pombe, humans, monkeys, mice, rats, hamsters, and the like.
  • DNA repair enzymes can be derived or extracted from suitable sources, such as E. coli, micrococcus, and the like. DNA repair enzymes can be encapsulated in liposomes, as described in US Patent 5,296,231, the entire contents of which are incorporated herein by reference.
  • a DNA repair enzyme derived from Micrococcus luteus cell lysate is provided to a liposome preparation containing ovalbumin and water, and it can be used as ULTRASOMESä (from Applied Genetics, Inc. Dermatics, Freeport, NY) or ULTRAS OMES-Vä (Barnet Products Corporation, Englewood Cliffs, NJ).
  • Liposomes containing Anacystis nidulans lysate which contains Anacystis nidulans photolyase, can be obtained as PHOTOSOMESä or PHOTOSOMES-Vä from Applied Genetics, Inc. Dermatics, (Freeport, NY).
  • Liposomes may include conventional grease, oleic acid, and / or cholesterol hemi-succinate from plant sources, such as soybeans, or they may be prepared from other suitable sources generally known to those skilled in the art.
  • Exemplary implementations can be added to ULTRASOMESä, ULTRAS OMES-Vä,
  • PHOTOSOMESä or PHOTOSOMES-Vä the amount of which ranges from about 0.01% to 20% of the total weight of the composition, desirably about 0.1% to about 10%, and more desirably about 0.5% to about 3%.
  • Liposomes can be used as delivery agents to promote the transfer of cosmetic actives to the dermis of the skin, such as the plants or plant components and DNA repair enzymes of the invention.
  • Other delivery agents can be used for skin delivery instead of liposomes, including but not limited to skin delivery vehicles known to those skilled in the art, including emulsions, microemulsions, nanoemulsions, nanoparticles, microspheres, alcohol bodies, delivery Body and lipid vesicles.
  • the cosmetic composition described in the present application may further include additional cosmetic ingredients, including but not limited to the following ingredients: licorice, licorice extract, licorice derivative (such as glycyrrhizinate); lemon Extracts; Cucumber Extracts; Sunflower Seed Extracts; Castor Seed Oil; Oat Protein, Oat Extracts, Hydrolyzed Oats; Silk Proteins (eg Sericin); Hyaluronic Acid and its Derivatives (eg Sodium Hyaluronate) Vitamins; minerals; antioxidants; fats, sphingolipids, cholesterol; and / or have anti-aging, antioxidant, anti-inflammatory, anti-irritant, anti-cancer or other skin protective properties, aesthetic appearance enhancement properties, and / or increase Other ingredients or combinations of dermal delivery properties.
  • additional cosmetic ingredients including but not limited to the following ingredients: licorice, licorice extract, licorice derivative (such as glycyrrhizinate); lemon Extracts; Cucumber Extracts; Sunflower Seed Extract
  • Cosmetically useful vitamins, minerals and / or antioxidants for topical application in the present invention include plant ingredients and extracts with antioxidant properties (eg rosemary extract, Asiaticoside, etc.); Vitamin A and its precursors or derivatives (such as P-carotene, retinyl palmitate); Vitamin B3 and its precursors or derivatives (such as nicotinamide); Vitamin B5 and its precursors or derivatives (such as pan Alcohol); Vitamin C and its precursors or derivatives (such as tetrahexyldecyl ascorbate, ascorbyl palmitate); Vitamin E and its precursors or derivatives (such as da-tocopherol, acetate tocopherol) Test); vitamin K and its precursors or derivatives; glutamate and its derivatives (such as L- sulfamidine); and a-lipoic acid (ALA).
  • antioxidant properties eg rosemary extract, Asiaticoside, etc.
  • Vitamin A and its precursors or derivatives such as P-carotene, retinyl palm
  • ALA is an effective natural antioxidant and is sometimes referred to as a "universal antioxidant" because it is active and soluble in both water and lipids. ALA can penetrate into skin cells, prevent the activation of the pro-inflammatory NF-KB pathway responsible for the breakdown of collagen and elastin, and enhance the protective effect of vitamins E and C, thereby enhancing the natural antioxidants in the cells.
  • tetrahexyldecyl ascorbate can be added to the compositions described herein.
  • Ascorbic acid Tetrahexyldecyl ester is a stable fat-soluble ester derivative of vitamin C. According to reports, vitamin C promotes collagen synthesis, inhibits lipid breakdown, regenerates vitamin E, reduces fine lines and wrinkles, and cures sunburn. It is an effective free radical scavenger-type antioxidant with significant anti-inflammatory properties. Hinders, for example, arachidonic acid production.
  • panthenol or its equivalent in a composition is contemplated.
  • Ubiquinol is an effective film-forming wetting agent with anti-inflammatory properties.
  • Panthenol equivalents can include alcohol derivatives of pantothenic acid, such as those described in the CTFA Cosmetic Ingredient Handbook, The Cosmetic, Toiletry and Fragrance Association. Inc., pp. 272-273, 1992.
  • the amount of ubiquinol should be selected so that the composition can dry out reasonably quickly. The more ubiquinol in the composition, the longer it takes to dry the composition after it is applied to the skin or other surface.
  • Vitamins, minerals and / or antioxidants may be present in an amount ranging from about 0.01% to 20% of the total weight of the composition, desirably from about 0.1% to about 10%, more preferably from about 0.5% to about 3% of the total The amount range exists.
  • composition of the present invention may further include one or more anesthetics, antiallergic agents, anti-irritants, antifungals, antimicrobials, anti-inflammatory agents, antibacterial agents, chelating agents, colorants, decolorants, Demulcents, emulsifiers, film formers, fragrances, humectants, insect repellents, lubricants, humectants, pharmaceuticals, light stabilizers, preservatives, skin protectants, skin penetration enhancers, sunscreens, stabilizers, surfaces An active agent, a thickener, a viscosity modifier, or any combination thereof.
  • anti-irritants include, but are not limited to: aloe, a-bisabolol, caffeine or other gutton, chamomile, cola nitada extract, dipotassium glycyrrhizinate, glycyrrhizic acid and its derivatives, Green tea extract, oval or hydrogenated ovalbumin, licorice extract, tea tree oil, steroidal or non-steroidal anti-inflammatory agents, including but not limited to cyclooxygenase inhibitors (e.g.
  • Desirable anti-irritants may include dipotassium glycyrrhizinate, egg crust fat, and hydrogenated egg scale fat.
  • the anti-irritant or anti-inflammatory agent may be present alone or collectively in an amount ranging from about 0.01% to 10% of the total weight of the composition, desirably from about 0.05% to about 5%, and more desirably from about 0.2% to about 1.5%.
  • Botanical ingredients, plant extracts, oils, vitamins, minerals, antioxidants, anti-irritants or other active agents may be contained individually or collectively in a pharmaceutically or cosmetically acceptable vehicle.
  • pharmaceutically or cosmetically acceptable carriers suitable for use in embodiments of the present invention include, but are not limited to, water, C1-C4 Sf, fatty alcohols, fatty ethers, fatty esters, glycerol, ethylene glycol, vegetable oils, mineral oils, egg clams Lipids, hydrogenated egg crust lipids, liposomes, layered lipid substances, lipids, polyglycols, polyols, propanols, silicone oils, vegetable oils, or any combination thereof.
  • the pharmaceutically or cosmetically acceptable carriers used with the compositions described herein can be in the form of a homogeneous formulation or an emulsion or microemulsion, including, but not limited to, oil-in-water emulsions, water-in-oil emulsions, and multiphase (Including three phases) emulsion.
  • the consistency of these emulsions can vary over a wide range, including thin toners (which are also suitable for spray or aerosol delivery), milky toners, light emulsions, and heavy emulsions.
  • topical carriers include anhydrous liquid solvents such as oils and alcohols; 7JC-based single-phase liquid solvents (eg, water-alcohol solvent systems); anhydrous solids and semi-solids (such as gels and sticks); and water-based Gel and mousse system.
  • anhydrous liquid solvents such as oils and alcohols
  • 7JC-based single-phase liquid solvents eg, water-alcohol solvent systems
  • anhydrous solids and semi-solids such as gels and sticks
  • water-based Gel and mousse system water-based Gel and mousse system.
  • Pharmaceutically or cosmetically acceptable vehicles typically comprise from about 5% to about 99.9% by weight of the composition, desirably from about 25% to about 80%, more desirably from about 50% to about 70%, and in the absence of other In the case of a cosmetic adjuvant, the balance of the composition can be formed. Any percentage between 5% and 99% of the total weight of the composition is also contemplated.
  • Emollients are humectants that maintain or rehydrate the skin by providing a protective emollient coating.
  • Emollients can be classified into conventional chemical categories such as esters, fatty acids and alcohols, polyols and hydrocarbons.
  • the ester may be a monoester or a diester.
  • Representative examples of fatty diesters include, but are not limited to, dipotassium glycyrrhizinate, dibutyl adipate, diethyl sebacate, diisopropyl dimer, and dioctyl succinate.
  • Acceptable branched chain fatty esters include, but are not limited to, 2-ethylhexyl myristate, isopropyl stearate, and isostearyl palmitate.
  • Acceptable tribasic acid esters include, but are not limited to, triisopropyl trilinoleate and trilauryl citrate.
  • Acceptable linear fatty esters include, but are not limited to, lauryl palmitate, myristyl lactate, and stearyl oleate.
  • Suitable fatty alcohols and acids may include, but are not limited to, alcohols or acids having about 10 to 20 carbon atoms.
  • alcohols such as cetyl alcohol, myristyl alcohol, palmityl and stearyl alcohol and the corresponding acids can be used.
  • Polyols can be used as emollients, including but not limited to linear and branched chain alkyl polyols. Representative polyols include, but are not limited to, butanediol, propylene glycol, sorbitol, glycerol, polymeric polyols such as polypropylene glycol and polyethylene glycol, and the like.
  • Hydrocarbons can be used as emollients and can include hydrocarbon chains having about 12 to 30 carbon atoms, including, but not limited to, mineral oils, petrolatum oils, carrageenans, and isochain dazzles.
  • Exemplary emollients include, but are not limited to, butan, caprylic / capric triglyceride, castor oil, cetylstearyl alcohol polyether-20, synthetic stearyl alcohol poly-30, synthetic stearyl alcohol, synthetic ⁇ Stearyl alcohol 20, cetostearyl alcohol, cetyl stearyl alcohol, cetyl stearyl alcohol, cholesterol, cocoa butter, diisopropyl adipate, glycerol, single oil Glyceride, glyceryl monostearate, glyceryl stearate, isochain dazzle, isopropyl myristate, isopropyl palmitate, lanolin, lanolin alcohol, hydrogenated lanolin, isochain dazzle Hydrocarbon, liquid paraffin, linoleic acid, mineral oil, oleic acid, petroleum jelly, petrolatum, polyethylene glycol, polyethylene glycol-7 glyceryl cocoate, polyethylene glycol-18 methyl ester dioxin , Poly
  • the amount of the emollient ranges from about 0.005% to 20% of the total weight of the composition, desirably about 0.1% to about 10%, and more desirably about 1.0% to about 5.0%.
  • wetting agents are humectants that bind water and retain it on the skin surface.
  • Exemplary wetting agents include, but are not limited to, acetylglucosamine, disaccharide gum, butanediol, ethoxydiol, ethylene glycol polypropylene, glucose, glycerin polyether-26, glycerol, glycerol, ethylene glycol Alcohol, lactitol, maltitol, propylene glycol, sericin, sodium hyaluronate, sorbitol, xylitol, sodium citrate, glucose, etc.
  • Co-existing amounts of wetting agents range from about 0.1% to 40% of the total weight of the composition, desirably from about 2.5% to about 25%, and more desirably from about 5% to about 15%.
  • the present composition may contain one or more preservatives.
  • Suitable preservatives include EDTA dinaphthol, phenethyl alcohol, ethyl p-hydroxybenzoate, phenoxyethanol, propyl p-hydroxybenzoate, ethyl p-hydroxybenzoate, butyl p-hydroxybenzoate, and Isobutyl p-phenylbenzoate.
  • a thickener is a cross-linked polypropionate material. You can use gums such as: xanthan gum, carrageenan, gelatin, sycamore gum, pectin and prickly pear Locust Bean Gum.
  • the thickening function can be achieved by substances that are also used as silicones or emollients. For example, silicone rubbers and esters such as glyceryl stearate that have more than 10 centiseconds have a dual function.
  • a skin whitening agent may be included in the composition.
  • Skin whitening agents include, but are not limited to, tyrosinase inhibitors, free radical scavengers, and mixtures thereof.
  • Powder can be added to the cosmetic composition.
  • These powders include chalk, talc, kaolin, starch, montmorillonite clay, chemically modified magnesium silicate, organically modified montmorillonite, Synthetic acid inscription, fumed silicon dioxide, starch xinfuji horn acid inscription and mixtures thereof.
  • auxiliary minor components may also be added to the cosmetic composition. These ingredients can include colorants, sunscreens, and perfumes. The amount of these other auxiliary minor components may range from 0.001% to up to 20% of the composition.
  • composition of the invention can be formulated in any convenient form suitable for topical application to the skin.
  • product forms include, but are not limited to, aerosol sprays, creams, dispersants, emulsions, foams, gels, liquids, toners, mousses, ointments, patches, balms, kits or powders, Pump sprays, solids, solutions, sticks and wipes.
  • Desirable cosmetic forms are creams in the form of oil-in-water emulsions, including also water-in-oil and water-in-one emulsions.
  • various known conventional cosmetic ingredients can be added.
  • it may contain cosmetic ingredients such as alcohols, fats and oils, surfactants, fatty acids, silicone oils, wetting agents, humectants, viscosity modifiers, emulsifiers, stabilizers, colorants, and fragrances.
  • composition may be administered as needed, once a day, several times a day, or on any suitable schedule to achieve the desired result.
  • composition can be administered continuously or intermittently.
  • Some embodiments relate to a cosmetic treatment system comprising a patch impregnated with the topical composition of the present invention.
  • the patch used in the present invention may be in any shape suitable for processing a specific target area.
  • the patch may contain a small area for a specific area, or it may cover a large area, such as covering the face in the form of a mask.
  • the overall size and geometry of patches currently used to administer drugs around the eyes makes it difficult to apply eye treatment products close to the eyes.
  • the patch may be made of any removal material suitable for absorbing, containing and releasing the composition of the invention.
  • the patch may be made of a nonwoven material.
  • the non-woven material may include cotton, cotton / polyester blends or other suitable combinations of natural or synthetic materials.
  • the patch may be further adapted to provide an occlusive, semi-occlusive or non-occlusive barrier.
  • the patch may be adhesive or non-adhesive.
  • the patch may include a single layer of material, or it may include multiple layers of the same and / or different materials to provide additional structural integrity and / or Flexibility. Suitable patches or patch materials are disclosed in, for example, U.S. Patents 6,096,334; 6, 120,792; 6,495, 158; 6,623,751; 8,697,099; U.S. Patent Application 2002/0086043; U.S. Patent Application 2003/0152610; US 2003/0175328; and their references The contents of these references are incorporated herein by reference.
  • the cosmetic treatment system of the present invention may include a packaging system for holding various components of the cosmetic treatment system.
  • a cosmetic treatment system comprises a patch; at least one container; and a topical composition formulated for treating at least a portion of a face
  • One or more containers may be used to contain one or more components of the cosmetic treatment system.
  • any container suitable for containing components of a cosmetic treatment system may be used.
  • the patch may be packaged in a container in the form of a recessed tray, which is covered by a sealably removable covering, thereby holding the patch firmly in the recessed tray before use.
  • the container can be prepared by thermoforming of a suitable material, such as polypropylene, or by thin-wall injection molding.
  • a suitable material such as polypropylene
  • the design of the container can be modified and adapted to the shape of a particular patch. Suitable containers are disclosed in U.S. Patent 6,623,751, the contents of which are incorporated herein by reference.
  • a cosmetic treatment system that includes a packaging system that contains a suitable amount of a cosmetic composition for a desired period of time (eg, fourteen days).
  • the cosmetic treatment system comprises a packaging system comprising a plurality of containers, each container having a cosmetic composition according to the invention suitable for a single use.
  • the container may be in the form of a vial or other suitable holding device.
  • the cosmetic treatment system includes a packaging system having a plurality of vials, each vial containing a sufficient amount of a cosmetic composition suitable for a single application of the cosmetic composition to the skin.
  • the packaging system can be formulated to provide a number of vials that match the number of days the cosmetic composition is applied to the skin. Alternatively, the packaging system is formulated for administration more than once a day.
  • the packaging system may contain 14 vials for daily treatment of the skin over 14 days.
  • the packaging system may further include one or more applicators for applying the composition, and may also include a set of instructions for using the packaging system provided with the cosmetic treatment system.
  • the present invention also includes a method for treating the skin by topically applying the cosmetic composition of the present invention.
  • a small amount of the composition such as 0.1 to 100 mL, can be applied to an exposed area of the skin from a suitable container or applicator, and if necessary, then apply it using hands or fingers or a suitable device and / Or apply to the skin.
  • the The composition may be applied to the skin in the form of a patch that has been impregnated with the composition.
  • the patch may be made of a non-woven material, and may further contain an adhesive to adhere the patch to the skin.
  • Some additional embodiments relate to a medicament comprising an isolated component or extract of Dendrobium (eg Dendrobium nobile) for preventing, treating and / or curing human skin and / or hair from at least one of the following: air pollution induction Or air pollution can induce skin and / or hair damage, air pollution-induced oxidative stress, air pollution-induced decrease in cell viability, air pollution-induced increase in IL-6, and / or air pollution-induced cell damage.
  • Dendrobium eg Dendrobium nobile
  • the components or extracts of Dendrobium candidum can be present in an amount ranging from about 0.0001% to 5% of the total weight of the drug; desirably, from about 0.001% to about 2.5% of the total weight of the drug; more desirably, from the total weight of the drug From about 0.001% to about 0.5%; even more desirably, from about 0.01% to about 0.1% of the total weight of the drug.
  • the medicaments described herein may also include any of the other ingredients listed above for the topical compositions of the present application.
  • the drugs described in this application can reduce or prevent air pollution-induced or air pollution-induced skin and / or hair damage, reduce or prevent air pollution-induced oxidative stress, reduce or prevent air pollution-induced cell viability, Reduce or prevent air pollution-induced increase in IL-6 and / or reduce or prevent air pollution-induced cell damage.
  • the drugs described herein can also provide a variety of anti-aging and texture benefits. It is believed that the composition containing Dendrobium nobile provides significant anti-pollution effects, and the present application has significant anti-aging and texture benefits relative to other commercially available skin health topical products. Exemplary benefits of the drugs described herein include those described above for topical compositions.
  • Some further embodiments relate to protecting human skin and / or hair against air pollution-induced damage, including applying a composition or medicament comprising an isolated component or extract of Dendrobium (eg, Dendrobium nobile), wherein the composition or drug
  • the amount used is sufficient to achieve at least one of the following: reduce and / or prevent air pollution-induced or air pollution-induced skin and / or hair damage, reduce and / or prevent air pollution-induced oxidative stress, and reduce and / or prevent air Pollution-induced cell viability is reduced, air pollution-induced IL-6 is reduced and / or prevented, and / or air pollution-induced cell damage is reduced and / or prevented.
  • Ingredients or extracts of Dendrobium candidum can be present in an amount ranging from about 0.0001% to 5% of the total weight of the drug; desirably, from about 0.001% to about 2.5% of the total weight of the drug; more desirably about 0.001% to about 0.5%; even more desirably about 0.01% to about 0.1% of the total weight of the drug.
  • Some further embodiments involve using isolated components or extracts of Dendrobium (eg Dendrobium nobile) as an antifouling agent (respective antifouling mixture) for protecting human skin and / or hair.
  • Anti-pollution specifically relates to protecting and / or inhibiting and / or reducing human skin and hair disorders and dysfunctions which are associated with the induction of oxidative stress, decreased cell viability, and / or increased expression of the IL-6 gene, respectively.
  • Some other embodiments are directed to methods for improving the cosmetic appearance of skin and / or hair damaged by air pollution, wherein the composition or medicament described herein is applied topically to the skin in a cosmetically or pharmaceutically effective amount, respectively, sufficient to improve the skin Beauty look.
  • the improvement involves skin aging, wrinkles, fine lines, wrinkles, crow's feet, dark circles, scars, age spots, dark spots, iris lines, cancer (including skin cancer), skin inflammation, skin discoloration, skin pigmentation, skin thickness Elasticity, resilience, moisturizing, hue, texture, light, gloss, brightness, brightness, transparency, outline appearance, firmness, tightness, softness, softness, sensitivity, pore size, skin barrier Features, or a combination of them.
  • the improvement further relates to adverse skin conditions caused or brought about by air pollution, including psoriasis, eczema, seborrhea, dermatitis, sunburn, estrogen imbalance, pigmentation, hypopigmentation, discoloration, yellowing, freckles, skin Atrophy, skin rash, skin fragility, dryness, chapped, sagging, thinning, hyperplasia, fibrosis, enlarged pores, formation of cellulite, dementia, acne formation, apoptosis, cell differentiation, cell dedifferentiation, prevention of tumor induction or Tumor progression, viral infection, fungal infection, bacterial infection, spider vein (capillary dilation), hirsutism, rosacea, pruritus, calluses, warts, corns, or combinations thereof.
  • air pollution including psoriasis, eczema, seborrhea, dermatitis, sunburn, estrogen imbalance, pigmentation, hypopigmentation, discoloration, yellowing, freckles
  • the topical compositions or medicaments described herein can be applied topically to enhance the overall health, vitality, and appearance of the skin.
  • the composition of the present invention can be applied to the skin to improve microcirculation, communication between skin cells, supplement essential nutrients or skin components, or improve metabolism, proliferation, reproduction, conversion and / or exfoliation of skin cells.
  • Some other embodiments relate to a cosmetic treatment system comprising a topical composition comprising a plant component, a plant extract, or a natural complex of Dendrobium such as Dendrobium nobile or an extract thereof, as well as pharmaceutically or cosmetically Acceptable vehicle.
  • a cosmetic treatment system comprising a topical composition comprising a plant component, a plant extract, or a natural complex of Dendrobium such as Dendrobium nobile or an extract thereof, as well as pharmaceutically or cosmetically Acceptable vehicle.
  • a cosmetic treatment system comprising a topical composition comprising a plant component, a plant extract, or a natural complex of Dendrobium such as Dendrobium nobile or an extract thereof, as well as pharmaceutically or cosmetically Acceptable vehicle.
  • the following are non-limiting examples of the invention. Unless otherwise stated, all ratios and percentages are by weight. Examples The following are examples of formulations and methods of the invention.
  • Example 1 Preparation of Dendrobium nobile extract
  • Plant extracts of Dendrobium nobile were obtained using deionized water extraction technology.
  • polysaccharide extraction was performed by extracting a stem of Dendrobium nobile with deionized water at a low temperature (about 80 ° C.), followed by centrifugation and filtration through a 10 nm membrane. Next, the polysaccharide extract was also concentrated in vacuo at low temperature (about 60 ° C). The polysaccharide extract was purified and concentrated by adding some ethanol to a concentration of about 80% (v / v) to obtain a sediment-dispersed solvent. Next, the sediment was centrifuged and collected, and dissolved in water. It is subsequently sterilized and the extract is packaged.
  • the Cell Counting Kit-8 (CCK-8) provides tools for studying the induction and inhibition of cell proliferation in any in vitro model.
  • CCK-8 can be easily measured by using a highly water-soluble tetrazolium salt.
  • WST-8 [2- (2-Methoxy-4-nitrophenyl) -3- (4-nitrophenyl) -5- (2,4-disulfophenyl) -2H-tetrazole Gun sodium salt] produces water-soluble formazan dyes after reduction in the presence of an electron mediator.
  • the CCK-8 colorimetric assay was performed using Cell Counting Kit-8 (Dojindo Laboratories, Kumamoto, Japan) purchased from Dojindo Laboratories according to the manufacturer's instructions, so that after treatment with Dendrobium nobile extract was performed in Cell viability was measured in a cytotoxicity assay (compared to treatment with PM2.5 particles).
  • PM2.5 particles are air pollutants collected from the air with a diameter of about 2.5 microns or less.
  • Concentrations that reduced cell viability by 10% compared to controls were defined as cytotoxicity criteria. As shown in Figure 1, the concentration used for the PM2.5 particle group was selected so that the cell viability of the PM2.5-treated group was higher than 80% of the control at 4 hours. As shown in Figure 2, the concentration of the Dendrobium nobile extract treatment group was selected so that the cell survival rate of the Dendrobium nobile extract treatment group was higher than 80% of the control at 24 hours, and had no toxic effect at 4 hours.
  • Table 1 Dose for further testing;
  • the concentrations of Dendrobium nobile extract treatment group and PM2.5 particle treatment group were selected for the following tests.
  • Example 3 In vitro potency test
  • ROS reactive oxygen species
  • ROS is the result of reduced oxygen during aerobic respiration and is produced by a variety of enzyme systems within the cell. At the physiological level, ROS contributes to cell signaling and host defense. Increased ROS production exceeds the detoxification capacity of biological systems, resulting in oxidative stress and cellular damage. The main damage to cells is the alteration of macromolecules (such as polyunsaturated fatty acids, essential proteins and DNA in membrane lipids) induced by ROS.
  • this kit provides a sensitive assay for the detection of intracellular ROS (especially superoxide and hydroxyl radicals) in living cells within 1 hour of incubation.
  • ROS react with cell-permeable sensors, resulting in fluorescent products that are proportional to the amount of ROS present.
  • FIG. 3 shows that PM2.5 can significantly increase ROS levels in Hacat cells. In other words, PM2.5 can increase oxidative stress in Hacat cells.
  • Figure 3 also shows that the extract of Dendrobium candidum can effectively resist the increased ROS level of PM2.5, and the extract of Dendrobium candidum itself does not cause oxidative stress in Hacat cells.
  • Example 4 Mitochondrial membrane potential (MMPV test
  • FIG. 4 shows the results of the mitochondrial membrane potential (MMP) test.
  • a mitochondrial membrane potential kit Mitsubishi Membrane Potential Kit, JC-10 assay for microplate reader, catalog number MAK159, Sigma-Aldrich, St. Louis, MO
  • This kit uses JC-10 to determine MMP loss in cells.
  • the kit can be used to monitor apoptosis and screen for apoptosis inhibitors and activators.
  • PM2.5 significantly reduced MMP 7jc levels and caused a decrease in cell viability.
  • the Dendrobium nobile extract itself does not reduce the cell MMP 7jC level.
  • the Dendrobium nobile extract significantly protects cell viability.
  • Example 5 IL-6
  • Figure 5 shows that multiple samples (control, PM2.5, Dendrobium nobile extract (50ug / ml) and Dendrobium nobile extract (50ug / ml) + PM2.5) can induce IL-6 levels.
  • PM2.5 significantly increased IL-6 7jc level.
  • D. officinale extract can also increase IL-6 levels at certain concentrations, it has been shown that the D. officinale extract significantly reduces IL-6 7JC levels and decreases by 41.3% compared with the PM2.5 treatment group.
  • Example 6 Lactate dehydrogenase (LDH or LD)
  • Lactate dehydrogenase (LDH or LD) is an enzyme found in almost all living cells (animals, plants and prokaryotes). LDH catalyzes the conversion of lactic acid to pyruvate and pyruvate to lactic acid because it converts NAD + to NADH and back. LDH is widely expressed in a variety of body tissues, such as blood cells and myocardium. Because it is released during cell damage, it acts as a marker of cell damage. Specifically, the higher the level of LDH 7JC in the tissue, the greater the cell damage observed.
  • a lactate dehydrogenase activity assay kit (Sigma Aldrich, catalog number MAK0660) purchased from Sigma-Aldrich was used to study cell damage after treatment with PM2.5 and Dendrobium nobile extract.
  • An exemplary cosmetic formulation can look like this: Based on Examples 1-5, it can be clearly seen that the extract of Dendrobium nobile has very good anti-pollution properties. In addition, it is water-soluble and can be widely used in beauty products.

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Abstract

本申请描述了用于预防、治疗和/或治愈人类皮肤免受空气污染诱导的损伤的组合物和使用所述组合物的方法。一个实施方案涉及美容组合物,其包含有效量的足以实现以下至少一种的金钗石斛(Dendrobium nobile)的分离成份或提取物:减少或预防空气污染诱导的或空气污染可诱导的皮肤和/或头发损伤;减少或预防空气污染诱导的氧化应激;减少或预防空气污染诱导的细胞活力降低;减少或预防空气污染诱导的IL-6增加;或减少或预防空气污染诱导的细胞损伤。还涉及美容学上可接受的载体或赋形剂。

Description

包含金钗石斛的组合物及其使用方法 技术领域
本申请描述了用于预防、 治疗和 /或治愈人类皮肤免受空气污染诱导的损伤的组合物 和使用所述组合物的方法。 背景技术
人类皮肤是身体的外层覆盖物。 在人类中, 其是皮肤系统的最大器官。 皮肤具有多层 外胚层组织并且保护下面的肌肉、 骨骼、 初带和内脏器官。
皮肤的两个主要层包括角质层(或称表皮层)和真皮层。 表皮层是皮肤的顶层或外层并 且其主要功能是提供保护性覆盖以及延缓内部的水经蒸发而流失。 表皮层可对抗机械损害、 外来化学物质和污染物进入以及微生物侵袭。 其也提供对抗紫外线的第一道防护。 真皮层 在表皮层之下, 构成皮肤厚度的 90%。 真皮层含有密集的胶原蛋白以及弹性蛋白网络, 为皮肤提供强度和弹性。 成纤维母细胞是构成真皮层的主要细胞类型, 并且负责合成以及 分泌真皮基质组份, 包括胶原蛋白、 弹性蛋白以及糖胺聚糖(诸如透明质酸)。 其中, 胶原 蛋白为皮肤提供强度, 弹性蛋白为其提供弹性, 而糖胺聚醣的作用是保持皮肤湿润以及丰 满。
为保持健康, 皮肤必须能应付环境条件的变化和空气污染, 同时修复对皮肤造成的任 何损伤。 环境因子和空气污染在老化、 皱纹、 皮肤变色以及退行性皮肤病症和皮肤疾病 (例如皮肤癌)方面发挥重要作用。
当有害物质(包括颗粒和生物分子)被释放到地球大气中时发生空气污染。 它可能导致 人类生病、 过敏或死亡; 它也可能对其他生物(如动物和粮食作物)造成伤害, 并可能破坏 自然或人造环境。 人类活动和自然过程都会产生空气污染。 暴露于空气污染会对皮肤造成 不良影响, 导致皮肤老化、 形成皱纹和炎症, 甚至可能导致皮肤癌。 流行病学研究显示, 人类皮肤反复暴露于空气污染是与色斑和皱纹相关的外在皮肤老化的原因之一(Vierkoetter 等人, J Invest Dermatol, 130(12):2719-26(2010))。 暴露于太阳光以及 UV辐射也是导致皮肤损伤的主要因素, 占过早老化的症状的 90%。 很重要地, 暴露于氧气、 太阳光以及其他环境或生活形态应激会诱导自由基形成。 自由基 可通过活化负责断裂皮肤结缔组织(胶原蛋白以及弹性蛋白)的金属蛋白酶(例如胶白蛋白酶) 而导致皱纹产生。 结果是过早老化。 自由基损伤也可引起真皮层的厚度变薄。 此可引起皮 肤松弛。 皮肤松弛是老化的第一个以及最常可看到的现象, 会引起皱纹以及纹路(line)。
鉴于众多会影响皮肤的有害作用, 需要有一种不仅可改善皮肤外观以及状况还可同时 对抗空气污染物给人类皮肤带来的不利后果并且保护皮肤细胞免受空气污染诱导的皮肤损 伤的组合物以及方法。 有利地, 这些组合物和方法任选地也会对抗由于皮肤暴露于太阳光 和 UV福射和 /或其他环境条件而带来的不利后果。
仍需要使用天然成份作为活性组份、 可向皮肤、 头发和 /或指(趾)曱提供抗污染益处的 有效的局部施用美容组成物。 非天然、 化学合成产品感觉上对环境或个人并不安全。 相反 的, 天然产品被视为纯净、 温和以及优于化学合成产品。 一般认为, 从植物或草药提取而 得到的天然产物含有可中和自由基损害作用的抗氧化物 /自由基清除剂。 此外, 天然产物 可含有这样的物质, 其会刺激真皮层中受损的结缔组织结构的合成以及修复以及刺激表皮 层中的屏障功能。
然而, 从’’天然’’来源诸如植物或草药开发出美容益处并不简单。 从这样的来源获得真 正的益处需要鉴识特定的植物 /草药提取物或成份、 它们的最小活性浓度以及它们与其他 提供抗污染和 /或皮肤改善益处的成份组合的叠加或协同活性。
本申请提供用于预防、 治疗和 /或治愈人类皮肤和 /或头发免受空气污染诱导的和 /或空 气污染可诱导的皮肤和 /或头发损伤(任选地具有额外的皮肤益处)的组合物和方法。 发明内容
一个实施方案涉及美容组合物, 其包含有效量的足以实现以下至少一种的金钗石斛 (Dendrobium nobile)的分离成份或提取物和美容学上可接受的载体或赋形剂: 减少或预防 空气污染诱导的或空气污染可诱导的皮肤和 /或头发损伤; 减少或预防空气污染诱导的氧 化应激; 减少或预防空气污染诱导的细胞活力降低; 减少或预防空气污染诱导的 IL-6增 加; 或减少或预防空气污染诱导的细胞损伤。 所述皮肤损伤为皮肤老化、 纹路、 细纹、 皱 纹、 鱼尾纹、 黑眼圈、 瘢点、 老年斑、 暗斑、 任娘纹、 皮肤癌、 皮肤炎症、 皮肤变色、 皮 肤色素沉着或它们的组合。 所述组合物可为个人护理组合物、 皮肤护理组合物、 头发护理 组合物、 抗老化护理组合物、 防晒护理组合物, 或它们的组合。 所述组合物可为以下形式: 气雾剂、 霜剂、 乳剂、 固体、 液体、 分散剂、 泡沫剂、 凝胶、 爽肤水、 摩丝、 软膏、 粉剂、 贴片、 香膏剂、 溶液、 泵式喷雾剂、 棒剂、 油剂、 湿巾, 或它们的组合。 所述金钗石斛的 成份或提取物的存在量可为组合物总重量的约 0.0001%至约 5%。 所述金钗石斛的成份或 提取物的存在量可为组合物总重量的约 0.01%至约 0.1%。 美容学上可接受的载体或赋形 剂可选自水、 甘油、 C1-C4 S事、 脂肪醇、 脂肪醚、 脂肪酯、 多元醇、 乙二醇、 植物油、 矿 物油、 脂质体、 分层脂质物质、 硅油, 或它们的组合。
另一个实施方案涉及药物, 其包含金钗石斛的成份或提取物和药学上可接受的载体或 赋形剂, 其中所述药物用于预防、 治疗和 /或治愈人类皮肤和 /或头发免受至少一种以下情 况: 空气污染诱导的或空气污染可诱导的皮肤和 /或头发损伤; 空气污染诱导的氧化应激; 空气污染诱导的细胞活力降低; 空气污染诱导的 IL-6增加; 或空气污染诱导的细胞损伤。 所述皮肤损伤可为皮肤老化、 纹路、 细纹、 皱纹、 鱼尾纹、 黑眼圈、 瘢点、 老年斑、 暗斑、 任娘纹、 皮肤癌、 皮肤炎症、 皮肤变色、 皮肤色素沉着、 皮肤屏障功能损伤, 或它们的组 合。 所述金钗石斛的成份或提取物的存在量可为组合物总重量的约 0.0001%至约 5%。 可 选择地, 所述金钗石斛的成份或提取物的存在量可为组合物总重量的约 0.01%至约 0.1%。
又一实施方案涉及一种包装系统, 其包括一个或多个容器和用于从所述一个或多个容 器施用所述组合物的说明书, 所述容器共同包含所述组合物。 所述包装系统可包括以下中 的至少一种: (a)共同包含本申请所述组合物的一个或多个容器; 或 (b)用于从所述一个或 多个容器施用所述组合物的说明书。
另一个实施方案涉及保护人类皮肤和 /或头发对抗空气污染诱导的损伤的方法, 包括 向皮肤和 /或头发局部施用所述组合物。 将金钗石斛的成份或提取物以约 0.01 至约 5 mg/cm2的有效量施用至人类皮肤和 /或头发。 可选择地, 将金钗石斛的成份或提取物以约 0.05至约 5 mg/cm2的有效量施用至人类皮肤和 /或头发。 又一个实施方案涉及金钗石斛的成份或提取物作为抗污染剂用于保护人类皮肤和 /或 头发的用途。 所述抗污染涉及保护和成抑制和成减少人类皮肤和成头发的障碍和功能失 调。 附图说明
图 1所示的条形图展示 PM2.5毒性测试。
图 2所示的条形图为金钗石斛提取物在处理后 4小时和 24小时的毒性测试。
图 3 所示的条形图证明, 金钗石斛提取物可有效对抗因 PM2.5增加的反应性活性氧 (ROS)水平而没有造成 Hacat细胞的氧化应激。
图 4描绘的条形图显示线粒体膜电位 (MMP)测试结果; PM2.5显著降低 MMP水平, 而金钗石斛提取物保护细胞活力。
图 5描绘的条开 j图显示由各种测试样品诱导的 IL-6水平; PM2.5显著增加 IL-6水平, 而与 PM2.5处理组相比, 金钗石斛提取物显著降低 IL-6水平 (降低了 41.3%)。
图 6描绘的条形图证明, PM2.5可以增加细胞损伤率, 而金钗石斛提取物不损伤细胞。 相反, 它可以防止细胞受到 PM2.5处理造成的损害。 发明详述
应该理解的是, 本发明不限于在此描述的具体组合物、 方法或方案。 此外, 除非另外 定义, 否则本文使用的所有技术和科学术语具有与本发明所属领域的普通技术人员通常理 解的相同的含义。 还应该理解的是, 这里使用的术语仅用于描述特定实施例的目的, 而不 意图限制本发明的范围, 本发明的范围仅由权利要求限制。
本发明是基于出人意料的发现, 即金钗石斛的植物成份和 /或植物提取物减少和 /或防 止空气污染诱导的或空气污染可诱导的皮肤和 /或头发损伤, 减少和 /或防止空气污染诱导 的氧化应激, 减少和 /或防止空气污染诱导的细胞活力降低, 减少和 /或防止空气污染诱导 的 IL-6增加, 和 /或减少或防止空气污染诱导的细胞损伤。 所述成份或提取物可以来自石 斛属的任何物种成员; 优选地, 所述成份或提取物可以是金钗石斛的成份或提取物。 鉴于此, 本申请描述了包含石斛植物(例如金钗石斛)的分离的植物成份和 /或植物提取 物的组合物和这些组合物的用途, 所述组合物的量足以预防、 治疗和 /或治愈人类皮肤和 / 或头发免受以下中的至少一种: 空气污染诱导的或空气污染可诱导的皮肤和 /或头发损伤, 空气污染诱导的氧化应激, 空气污染诱导的细胞活力降低, 空气污染诱导的 IL-6增加; 和 /或空气污染诱导的细胞损伤。
术语“组合物”意指一种可治疗、 ?文善、 促进、 增加、 管理、 控制、 维持、 优化、 修饰、 降低、 抑制或防止与天然状态、 生物过程或疾病或障碍相关的具体状况的产品。 例如, 本 申请所述的组合物可改善受试者中的至少一种以下情况: 污染诱导的或空气污染可诱导的 皮肤和 /或头发损伤, 空气污染诱导的氧化应激, 空气污染诱导的细胞活力降低, 空气污 染诱导的 IL-6增加; 和 /或空气污染诱导的细胞损伤等。 术语组合物包括但不限于, 药品 (即, 药物)、 非处方药(OTC)、 化妆品、 食品、 食物成份或膳食补充组合物, 其包含有效 量的提取物、 其至少一种组份或其混合物。
本申请所述组合物的例示性形式包括气雾剂、 霜剂、 乳剂、 固体、 液体、 分散剂、 泡 沫剂、 泡沫涂剂、 凝胶、 爽肤水、 摩丝、 软膏、 药包或粉剂、 乳液、 贴片、 香膏剂、 溶液、 泵式喷雾剂、 棒剂、 油剂、 湿巾、 片剂、 膏药、 颗粒剂, 和 /或它们的组合。
术语“空气污染”是指由烟雾和 /或有害气体(例如交通排放物和工业废气), 主要是碳、 硫和氮的氧化物、 任何释放的颗粒或液滴带来的任何天然来源或人为的空气污染。 例如, 橡胶轮胎磨损释放的任何颗粒都可以被认为是空气污染物。 这些空气污染物可结合多环芳 炫(PAH), 但也包括其他化学物质。 此外, 打印机释放的炭黑颗粒可被认为是室内环境中 的空气污染物。 室内烹任, 例如用煤或柴火也可能产生空气污染物。
“空气污染物”是空气中的一种物质, 可对人类和生态系统产生不利影响, 并助长空气 污染。 该物质可以是固体颗粒、 液滴或气体。 污染物可以是天然来源或人为的。 污染物被 分类为首要污染物或二次污染物。 首要污染物通常是由一个过程产生的, 例如火山爆发的 灰烬。 其他例子包括汽车尾气中的一氧化碳气体, 或工厂释放的二氧化硫。 二次污染物不 会直接被排放。 相反, 它们是当首要污染物发生反应或相互作用时在空气中形成的。 地面 臭氧是二次污染物的突出例子。 有些污染物可能既是首要污染物也是二次污染物: 它们既 是被直接排放的, 也是由其他首要污染物形成的。 示例性首要空气污染物包括: 二氧化碳 (C02) (例如通过燃烧化石燃料排放); 由火山 和各种工业过程 (例如煤和石油通常含有硫化合物, 它们燃烧产生二氧化硫)产生的硫氧化 物 (SOx), 例如二氧化硫 (S02); 由高温燃烧排放的氮氧化物 (NOx)例如二氧化氮 (N02); — 氧化碳 (CO)是一种无色, 无味, 有毒但无刺激性的气体, 是燃料诸如天然气、 煤炭或木 材等的燃烧产物和由汽车尾气产生; 挥发性有机化合物 (VOC), 一种众所周知的户外空气 污染物, 例如曱烷 (CH4)或非曱烷 (NMVOC)(芳香族 NMVOC, 包括苯、 曱苯和二曱苯是 疑似致癌物; 1,3 -丁二婦是经常与工业用途相关的另一种危险化合物); 颗粒 (或者被称为 颗粒物质 (PM), 大气颗粒物质或细颗粒是悬浮在气体中的微小的固体或液体颗粒; 气溶 胶 (“组合的颗粒和气体”) -一些颗粒是自然产生的, 来源于火山、 沙尘暴、 森林和草原火灾, 生物植被和海水喷雾, 有些来自人类活动, 如车辆中燃烧的化石燃料、 发电厂和各种工业 过程也会产生大量的气溶胶; 有毒金属, 如鉛和汞, 尤其是它们的化合物; 从产品排放的 氯氟烃 (CFC)目前被禁止使用, 这些是从空调、 冰箱、 气溶胶喷雾器等释放出来的气体 - 一旦释放到空气中, CFC上升到平流层, 在这里它们接触其他气体并破坏臭氧层, 并允 许有害的紫外线到达地球表面, 导致例如皮肤癌或眼部疾病; 和从农业过程中释放的氨气 (NH3), 其通常会形成可以与氮和硫的氧化物反应形成二次粒子的气体。
示例性二次空气污染物包括由光化学雾霾中的气态首要污染物和化合物产生的颗粒物。 雾霾是一种空气污染。 传统雾霾源自一个区域中大量炭燃烧, 由烟雾和二氧化硫混合物引 起的。 现代雾霾通常不是来自煤炭, 而是来自车辆和工业排放, 这些排放在大气中在来自 太阳的紫外光的作用下形成二次污染物, 该二次污染物与主要排放物结合形成光化学雾霾。 地面臭氧 (03)形成自 NOx和 VOC。 臭氧 (03)是对流层的重要组成部分。 它也是平流层的一 些区域 (通常称为臭氧层)的重要组成部分。 其中牵涉的光化学和化学反应驱使昼夜发生在 大气中的许多化学过程。 在由于人类活动 (主要是化石燃料的燃烧)导致异常高浓度时, 它 就构成了一种污染物, 也是雾霾的组成部分。 类似地形成自 NOx VOC的过氧乙酰基硝 酸酯 (C2H3N05)是二次空气污染物的另一个实例。
术语“空气污染诱导的皮肤和 /或头发损伤”是指由短期和 /或长期暴露于空气污染引起 的任何皮肤和 /或头发损伤、 疾病和 /或病症。 空气污染诱导的皮肤和 /或头发损伤可表现为 例如皮肤老化; 形成皱纹和炎症; 形成纹路 (如细纹)、 皱纹、 鱼尾纹; 形成黑眼圈; 形成 瘢点、 痤疮、 老年斑、 暗斑、 任娘纹; 形成癌症(包括皮肤癌); 皮肤变色、 皮肤色素沉着, 或它们的组合。 此外, 空气污染诱导的皮肤和 /或头发损伤可表现为牛皮癖、 湿疹、 皮脂 溢出、 皮炎、 晒伤、 雌激素失衡、 变黄、 雀斑、 皮肤萎缩、 皮肤发疹、 皮肤脆弱、 干燥、 触感粗糙、 皲裂、 下垂、 变薄、 增生、 纤维化、 毛孔粗大、 形成脂肪团、 痴伤、 凋亡、 细 胞分化、 细胞去分化、 病毒感染、 真菌感染、 细菌感染、 物蛛样静脉(毛细管扩张)、 多毛 症、 酒渣鼻、 瘙痒症、 老莖、 疲、 鸡眼, 或它们的组合。
术语“空气污染可诱导的皮肤和 /或头发损伤”是指可在响应于空气污染物的存在时而 形成的任何皮肤和 /或头发损伤、 疾病和 /或病症。
本申请使用的术语“提取物”或“植物提取物”意指包含植物物质的分离的活性成份的固 态、 黏质或液态物质或制品, 所述植物物质为例如石斛(例如, 金钗石斛)。 所述成份或提 取物可以来自石斛属的任意物种成员。 术语“提取物”不仅包括产生自石斛(例如金钗石斛) 并且通过使用选自水、 1-4个碳原子的低级醇(如曱醇、 乙醇、 丁醇等)、 乙婦、 丙酮、 己 烷、 乙醚、 氯仿、 乙酸乙酯、 乙酸丁酯、 二氯曱烷、 N,N-二曱基曱酰胺(DMF)、 二曱基亚 砜(DMSO)、 1,3 -丁二醇、 丙二醇及它们的组合得到的粗提取物, 而且还包括在所述溶剂 中的粗提取物的一部分。 可以采用任何提取方法, 只要该方法保证了活性成份的提取和保 存。 植物提取物的一个实例包括来自金钗石斛植物的提取物。
本申请使用的术语“足量”、 “有效量”或“治疗有效量”的纯化合物、 组合物、 提取物、 提取混合物、 提取物的组份和 /或活性剂或成份, 或它们的组合意指以一定剂量在历经一 段时间后足以达到所期望的结果的有效量。 例如, 所述“足 t’、 “有效量”或“治疗有效量” 意指当将该量的本发明的纯化合物、 组合物、 提取物、 植物提取物、 提取混合物、 植物提 取混合物、 该提取物的组份和 /或活性剂或成份, 或它们的组合给予受试者(例如, 哺乳动 物如人类)时, 足以在受试者中达到预防、 治疗和 /或治愈例如以下方面: 污染诱导的或空 气污染可诱导的皮肤和 /或头发损伤、 空气污染诱导的氧化应激、 空气污染诱导的细胞活 力降低、 空气污染诱导的 IL-6增加; 和 /或空气污染诱导的细胞损伤等。 构成“有效量”或 “治疗有效量”的组合物、 提取物、 植物提取物、 提取物混合物、 植物提取物混合物、 提取 物组份和 /或活性剂或成份的量将根据活性剂或化合物、 待治疗的病症及其严重程度、 给 药方式、 治疗持续时间或待治疗受试者的年龄而变化, 但可由本领域普通技术人员根据自 己的知识和本申请披露的内容常规确定。
术语“保护, 治疗和 /或治愈人类皮肤和成头发对抗空气污染诱导的损伤”指的是预防、 阻止、 逆转、 改善、 减少和 /或降低空气污染诱导的损伤, 特别是对人类皮肤和 /或头发的 损伤。 空气污染诱导的损伤的代表性迹象包括但不限于皮肤老化、 纹路、 细纹、 皱纹、 鱼 尾纹、 黑眼圈、 瘢点、 老年斑、 暗斑、 任娘纹、 癌症(包括皮肤癌)、 皮肤炎症、 皮肤变色、 皮肤色素沉着, 或它们的组合。 空气污染诱导的对皮肤和头发的损伤的其他迹象包括牛皮 癖、 湿疹、 皮脂溢出、 皮炎、 晒伤、 雌激素失衡、 变黄、 雀斑、 皮肤萎缩、 皮肤发療、 皮 肤脆弱、 干燥、 触感粗糙、 皲裂、 松弛、 变薄、 增生、 纤维化、 毛孔粗大、 形成脂肪团、 痴伤、 形成痤疮、 凋亡、 细胞分化、 细胞去分化、 预防肿瘤诱导或肿瘤进展、 病毒感染、 真菌感染、 细菌感染、 物蛛样静脉(毛细管扩张)、 多毛症、 酒渣鼻、 瘙痒症、 老茧、 疲、 鸡眼, 或它们的组合。
术语“美容学上可接受的”和“药学上可接受的”意指适合用于与人类以及低等动物的组 织接触的那些药物、 药品、 软膏、 提取物或惰性成份, 无过度毒性、 不相容性、 不稳定、 刺激等情况, 与合理的利益 /风险比例相称。
术语“给药”和“施用”可以互换使用, 并且定义为通过本领域已知的途径向受试者提供 组合物, 包括但不限于局部、 口服、 静脉内、 动脉内、 肠胃外、 含服、 透皮、 直肠、 肌内、 皮下、 骨内、 透粘膜或腹膜内给药途径。 在优选的实施方案中、 局部途径给药(即“局部施 用”)组合物是合适的。
术语“调节”或“调整”是指石斛的纯化合物、 组合物、 提取物、 提取物混合物、 提取物 组份和 /或活性剂或成份, 或它们的组合增加、 刺激或增强、 或者减少、 预防或抑制特定 分子的表达或活性的能力, 从而减少或预防空气污染诱导的或空气污染可诱导的皮肤和 / 或头发损伤。 例如, 术语“调节”可以指石斛减少空气污染诱导的氧化应激、 减少空气污染 诱导的细胞活力降低、 减少空气污染诱导的 IL-6增加和 /或减少空气污染诱导的细胞损伤 的能力。 该术语还指石斛的抗刺激或抗炎特性, 用于抵抗空气污染对皮肤的潜在刺激。
术语“减少”, “降低”, “抑制”或“遏制”是指与在不存在石斛(金钗石斛)的植物成份或 植物提取物时(例如在对照样品中)的蛋白质活性和 /或表达相比较, 在存在石斛(例如金钗 石斛)的植物成份或植物提取物的情况下蛋白质活性和 /或表达和 /或其下游效应的减少或降 低。 蛋白质活性和 /或表达和 /或其下游效应的降低或抑制程度将随着存在的石斛的植物成 份或植物提取物的性质和量而变化, 但是是明显的, 例如, 其为可检测到的蛋白质活性和 /或表达的降低; 理想地, 与不存在石斛的的植物成份或植物提取物时的蛋白质活性和 /或 表达相比, 降低程度大于 10%、 25%、 50%、 75%、 90%、 95%或 99%。
术语“预防”当用于在受试者中防止空气污染诱导的皮肤和 /或头发损伤、 空气污染诱 导的氧化应激、 空气污染诱导的细胞活性降低、 空气污染诱导的 IL-6增加; 和 /或空气污 染诱导的细胞损伤等情况时是指维持这些效果不发生或不存在。
术语“增加”、 “使 ...增力 P”、 “刺激”或“对 ...进行刺激”是指当与不存在石斛的植物成份 或植物提取物(例如在对照样品中)的蛋白质活性和 /或表达相比, 在存在石斛的植物成份或 植物提取物的情况下使蛋白质活性和 /或表达和 /或其下游效应增加。 蛋白质活性和 /或表达 和 /或其下游效应的增加程度将随着存在的石斛的植物成份或植物提取物的性质和量而变 化, 但是是明显的, 例如, 其为可检测到的蛋白质活性和 /或表达的增加; 理想地, 与不 存在石斛的植物成份或植物提取物时的蛋白质活性和 /或表达相比, 增加程度大于 10%、 25%、 50%、 75%、 90%、 95%或 99%。
如本申请所用, 术语“受试者”或“个体”包括可以向其施用或应用组合物的哺乳动物。 哺乳动物的非限制性实例包括人类、 非人灵长类动物、 啮齿动物(包括转基因和非转基因 小鼠)等。 在一些实施方案中, 所述受试者是哺乳动物, 并且在一些实施方案中, 所述受 试者是人。 组合物
一个实施方案涉及美容组合物, 其包含石斛(例如金钗石斛)的分离成份或提取物和至 少一种药学上或美容学上可接受的媒介物, 其中分离成份或提取物的量足以减少或预防空 气污染诱导的或空气污染可诱导的皮肤和 /或头发损伤(例如, 皮肤癌、 皮肤炎症和 /或色素 沉着)、 减少或预防空气污染诱导的氧化应激、 减少或预防空气污染诱导的细胞活力降低、 减少或预防空气污染诱导的 IL-6增加和 /或减少或预防空气污染诱导的细胞损伤。 石斛是兰科的一个大属, 目前含有约 1,200个种。 该属出现在亚洲南部, 东部和东南 部的多个不同生长环境中, 包括中国、 日本、 印度、 菲律宾、 印度尼西亚、 澳大利亚、 新 几内亚、 越南和太平洋的许多岛码。 这个名字来自希腊语的 dendron (“树”)和 bios (“生 命”)。 石斛种既可以是附生植物, 也可以偶尔是岩表植物。 他们已经适应了各种各样的栖 息地, 从喜马拉雅山脉的高海拔地区到低洼热带森林, 甚至是澳大利亚沙漠的干燥气候。 石解属的示例性种包括卓花石解 (Dendrobium anosmum), 兜唇石解 (Dendrobium aphyllum), Dendrobium begaudii, Dendrobium bilobum, Dendrobium brevicaudum, Dendrobium bukidnonensis, 黄玉石解 (Dendrobium bullenianum), 翅萼石解 (Dendrobium cariniferum), Dendrobium ceraula,长爪石解 (Dendrobium chameleon),束花石解 (Dendrobium chrysanthum), Dendrobium conanthum, Dendrobium crispilinguum,木石解 (Dendrobium crumenatum), 雪山 石解 (Dendrobium cuthbertsonii), Dendrobium dearei, Dendrobium erosum, Dendrobium epidendropsis, Dendrobium euryanthum, Dendrobium fairchildae, 嫌萼石解 (Dendrobium falcorostrum), Dendrobium forbesii, Dendrobium formosum, Dendrobium gerlandianum, 曲轴 石解 (Dendrobium gibsonii), Dendrobium gnomus, 红花石解 (Dendrobium goldschmidtianum), Dendrobium guamense, Dendrobium guerreroi, Dendrobium hellwigianum, 重唇石 解 (Dendrobium hercoglossum), 尖 刀 唇 石 斛 (Dendrobium heterocarpum), Dendrobium hymenophyllum, Dendrobium ionopus, 约翰逊石解 (Dendrobium johnsoniae), Dendrobium junceum,澳洲石解 (Dendrobium kingianum), Dendrobium lydiae,聚石解 (Dendrobium lindleyi), Dendrobium lineale,嗦1 j 9石斛 (Dendrobium lituiflorum),美花石斛 (Dendrobium loddigesii),大 叶 石 解 (Dendrobium macrophyllum), Dendrobium macropus, Dendrobium milaniae, Dendrobium mindanaense, Dendrobium miyasakii, 细茎石解 (Dendrobium moniliforme),金权 石解, Dendrobium papilio, Dendrobium parthenium, 肿节石解 (Dendrobium pendulum), Dendrobium pentapterum, 蝴虫茱石解 (Dendrobium Phalaenopsis), Dendrobium philippinense, Dendrobium phillippsii, Dendrobium platycaulon, Dendrobium polysema, 贝 壳 石 解 (Dendrobium profusum), Dendrobium ramosii, Dendrobium sanderae, Dendrobium sanguinolentum, 舒氏石解 (Dendrobium schuetzei), Dendrobium secundum, Dendrobium seratilabium, 华石解 (Dendrobium sinense), 大明石 jl^KDendrobium speciosum), Dendrobium taurinum, 球花石解 (Dendrobium thyrsiflorum), Dendrobium thy s anophorum, Dendrobium uniflorum, Dendrobium velutinalabrum, Dendrobium victoriae-reginae, 金 沙 江 石 解 (Dendrobium wangliangii), Dendrobium wenzellii和 Dendrobium yeageri。
在一些实施方案中, 使用金钗石斛的分离成份或提取物来生产本申请所述的组合物。 金钗石斛是一种非常珍贵和著名的中草药植物, 花朵美丽。 它的名字来源于它的形状; 金 钗石斛看起来像一个古老的中国别针。
金钗石斛茎的提取物可得到 17 种菲, 包括 3, 4, 8 -三曱氧基菲 -2, 5 -二醇、 2,8-二羟基-
Figure imgf000012_0001
3 -羟基 -2, 4, 7 -三曱 t-9, 10 -二氢菲、 2, 8 -二羟基 -3, 4, 7 -三曱氧基 -9, 10 -二 氢菲、 2 -羟基 -4, 7 -二曱氧基 -9, 10 -二氢菲、 2,2’-二羟基-3,3’,4,4’,7,7’-六曱氧基-9,9’, 10, 10’-四 氢 - 1 , 1’-联菲和 2, 3, 5 -三 基 -4, 9 -二曱氧基菲 (Hwang, Ji Sang, 等人, “Phenanthrenes from
Dendrobium nobile and their inhibition of the LPS-induced production of nitric oxide in macrophage RAW 264.7 cells,” Bioorganic & Medicinal Chemistry Letters, 20 (12):3785 (2010); 和 Yang, H, 等人, "Antifibrotic Phenanthrenes of Dendrobium nobile stems,” Journal of Natural Products, 70 ( 12): 1925-9 (2007))。
在一些实施方案中, 金钗石斛茎的提取物可以标准化为约 0.01-80%的多糖。 在一些 替代实施方案中, 金钗石斛茎的提取物可以标准化为约 0.1-0.2% (w/w)的多糖。
在一个实例中, 用于本申请所述的独特组合物的植物提取物可以使用去离子水提取技 术来获得。
例如, 多糖提取可以通过在温度 (10-100°C)用去离子水提取金钗石斛的茎、 离心并过 滤来进行。 接下来, 将提取物在低温在真空中浓缩。 通过加入乙醇将多糖纯化并浓缩以获 得沉积物分散的溶剂。 接下来, 将沉积物离心并收集, 溶解于水中。 随后进行消毒, 然后 将提取物包装。
在另一个实例中, 可使用水提取和醇沉淀法 (0-30%乙醇 -7jc(v/v)), 从而获得可用于本 申请所述的独特组合物的植物提取物。 虽然在这个过程中产生的植物提取物可以含有多种 植物化学物质, 但连续使用醇沉法可以实现多糖的纯化和浓缩。
在又一个实例中, 可使用膜过滤方法获得可用于本申请所述的独特组合物的植物提取 物。 由所述提取过程产生的植物提取物将含有多种植物化学物质存在于提取物中。
另外, 可以使用任何下文更充分讨论的或本领域已知的提取和纯化技术来获得金钗石 斛的合适的植物成份和植物提取物。
本领域技术人员将会理解, 存在许多其他的提取方法, 这些提取方法都是本领域已知 的并且在用于获得提取物的各种专利和出版物中进行了描述, 它们可用于实施本发明。
应用本申请所述的局部组合物可减少或防止空气污染诱导的或空气污染可诱导的皮肤 和 /或头发损伤, 减少或防止空气污染诱导的氧化应激, 减少或防止空气污染诱导的细胞 活力降低, 减少或防止空气污染诱导的 IL-6增加和 /或减少或防止空气污染诱导的细胞损 伤。
在一些实施方案中, 本申请所述的局部用组合物的施用可导致 ROS 水平降低至少约 5%、 至少约 10%、 至少约 15%、 至少约 20%、 至少约 21%、 至少约 21.5% ; 至少约 22%、 至少约 22.5% ; 至少约 23%、 至少约 23.5% ; 至少约 24% ; 至少约 24.5%、 至少约 25%、 至少约 25.5%、 至少约 26%、 至少约 26.5%、 至少约 27%、 至少约 27.5%、 至少约 28%、 至少约 28.5、 至少约 29%、 至少约 29.5%或至少约 30%(本申请提供的示例性百分比之间 的百分比也应被考虑)。 还可以考虑更高的降低百分比。 在一些实施方案中, 本申请所述 的局部组合物的应用可导致 ROS水平降低约 27.78%。
在一些实施方案中, 本申请所述的局部用组合物的施用可导致细胞损伤率降低约 5%、 至少约 10%、 至少约 15%、 至少约 20%、 至少约 21 %、 至少约 21.5% ; 至少约 22%、 至 少约 22.5% ; 至少约 23%、 至少约 23.5% ; 至少约 24% ; 至少约 24.5%、 至少约 25%、 至 少约 25.5%、 至少约 26%、 至少约 26.5%、 至少约 27%、 至少约 27.5%、 至少约 28%、 至 少约 28.5、 至少约 29%、 至少约 29.5%、 至少约 30%、 至少约 30.5%、 至少约 31 %、 至少 约 31.5%、 至少约 32%、 至少约 32.5%、 至少约 33%、 至少约 33.5%、 至少约 34%、 至少 约 34.5%或至少约 35%(本文提供的示例性百分比之间的百分比也应被考虑)。 还可以考虑 更高的降低百分比。 在一些实施方案中, 本申请所述的局部组合物的应用可导致细胞损伤 率降低约 30.99%。
在一些实施方案中, 本申请所述的局部用组合物的施用可导致 IL-6 7jc平降低约 5%、 至少约 10%、 至少约 15%、 至少约 20%、 至少约 21 %、 至少约 21.5% ; 至少约 22%、 至 少约 22.5%; 至少约 23%、 至少约 23.5%; 至少约 24%; 至少约 24.5%、 至少约 25%、 至 少约 25.5%、 至少约 26%、 至少约 26.5%、 至少约 27%、 至少约 27.5%、 至少约 28%、 至 少约 28.5、 至少约 29%、 至少约 29.5%、 至少约 30%、 至少约 30.5%、 至少约 31%、 至少 约 31.5%、 至少约 32%、 至少约 32.5%、 至少约 33%、 至少约 33.5%、 至少约 34%、 至少 约 34.5%、 至少约 35%、 至少约 35.5%、 至少约 36%、 至少约 36.5%、 至少约 37%、 至少 约 37.5%、 至少约 38%、 至少约 38.5%、 至少约 39%、 至少约 40%、 至少约 40.5%、 至少 约 41%、 至少约 41.5%、 至少约 42%、 至少约 42.5%、 至少约 43%、 至少约 43.5%、 至少 约 44%、 至少约 44.5%、 至少约 45%(本文提供的示例性百分比之间的百分比也应被考虑)。 还可以考虑更高的降低百分比。 在一些实施方案中, 本申请所述的局部组合物的应用可导 致 IL-6水平降低约 41.3%。
由于本申请所述的组合物的抗污染作用, 该组合物还可以提供多种抗衰老和肌理益处。 据信, 包含金钗石斛的组合物提供显著的抗污染效果, 相对于其他市售局部用皮肤健康产 品, 其具有显著的抗衰老和肌理益处。
在一些实施方案中, 包含金钗石斛的组合物的抗污染益处表现为抗衰老和改善美容外 观。 因此, 一些实施方案涉及局部组合物及其用于处理皮肤以防止、 阻止、 逆转、 改善、 减小、 减少或改进衰老迹象(包括空气污染诱导的或空气污染可诱导的皮肤和 /或头发损伤 或与之相关的迹象)的方法。 衰老迹象包括但不限于皮肤脆弱; 胶原蛋白和 /或弹性蛋白流 失; 皮肤中的雌激素失衡; 皮肤萎缩; 纹路和 /或皱纹(包括细纹)的出现和 /或加深; 皮肤 变色包括黑眼圈; 鱼尾纹; 皮肤下垂; 皮肤疲倦和 /或紧张例如皮肤发疹; 皮肤干燥、 由 于皮肤干燥导致的细纹、 皮肤粗糙; 皮肤片状剥落; 细胞老化; 丧失皮肤色调、 弹性、 透 明度、 亮度和 /或光泽度; 丧失皮肤紧实度; 皮肤肌理变差; 丧失皮肤弹性和 /或回弹性; 皮肤变薄以及发炎。
对皮肤美容外观的益处以及改善可表现为如下列中的任一种: 毛孔大小、 细纹、 皱纹、 粗糙触感以及发炎减少; 皮肤色调、 光感、 透明度和 /或绷紧度改善; 促进抗氧化活性; 皮肤紧实度、 丰满度、 柔软度和 /或柔和度改善; 促胶原蛋白和 /或胶原蛋白的产生改善; 皮肤肌理改善和 /或促进再肌理化; 皮肤屏障修复和 /或功能改善; 皮肤轮廓外观改善; 皮 肤光泽、 透明度和成亮白度恢复; 因衰老和 /或停经导致的皮肤中基本营养素和成要素的 减少得到补充; 皮肤细胞间的联系改善; 细胞增生和 /或增殖增加; 因衰老和 /或停经引起 的皮肤细胞代谢的减少得以增加; 皮肤保湿性改善; 促进和 /或加速细胞更新; 皮肤厚度 增加; 皮肤弹性和 /或回弹性增加; 以及在有或无使用 a或 P轻酸、 酮酸或其他去角质剂 的情况下的表皮剥落提高。
其他益处可包括皮肤平滑度和 /或柔和度增加、 皮肤状况的感觉增加、 皮肤水份增加、 皮肤压力以及细纹减少、 亮度和 /或亮白度增加、 皮肤肌理以及皮肤紧实度改善。
在本发明的一个实施方案中, 局部组合物包含石斛 (例如金钗石斛)的分离成份或提取 物, 其量足以至少减少和 /或预防空气污染诱导的或空气污染可诱导的皮肤和 /或头发损伤, 减少或预防空气污染诱导的氧化应激, 减少和 /或预防空气污染诱导的细胞活力降低, 减 少或预防空气污染诱导的 IL-6增加和 /或减少或预防空气污染诱导的细胞损伤。 金钗石斛 的存在量范围可为组合物总重量的约 0.0001%至 5% ; 期望地, 组合物总重量的约 0.001% 至约 2.5%; 更期望地, 组合物总重量的约 0.001%至约 0.5% ; 甚至更期望地, 组合物总重 量的约 0.01%至约 0.1%。 所述组合物可以是个人护理组合物, 皮肤护理组合物, 头发护 理组合物, 抗衰老护理组合物或防晒护理组合物。 该组合物可具有约 6.0至约 8.0的 pH, 或者该组合物可具有大体中性的 pH。 在一些实施方案中, 其中使用植物提取物的组合物 具有大体中性的 pH。
一些进一步的实施方案涉及一种局哪用组合物, 其包含足以向皮肤提供抗刺激或抗炎 益处的量的石斛, 从而抵抗空气污染对皮肤造成的潜在刺激。 其他组份
在一些其他实施方案中, 本发明所述的组合物可另外包括 DNA修复酶。 如本申请中 所使用, 术语“DNA修复酶”意在包括前述酶和目前已知或随后发现或开发的其他酶, 包 括糖基化酶、 无嘌呤碱基 /无嘧啶碱基核酸内切酶或具有能够修复受损 DNA活性的其他酶。 DNA修复酶可包括涉及碱基切除修复 (BER)、 核苷酸切除修复 (NER)途径或其他切除修复 途径的酶, 如美国专利 6,368,594 中所述。 这些途径由能够进行 DNA切除、 损害移除、 缺口填补以及接合反应的各组蛋白介导。 NER途径构成广泛分布的损伤非特异性修复途径, 其通过损伤部位上游和下游的双 切口反应协调 DNA损伤移除, 导致释放含有损伤的寡核苷酸。 除去受损的 DNA后, 填 补所得的缺口并将 DNA末端接合在一起。
BER途径是针对所有主要形式的 DNA碱基损伤的主要防御。 该途径负责从大量未损 伤的 DNA中检测和去除特定的单个碱基病变。 BER途径通常涉及对 CPD特异性的 N-糖 基化酶 / AP裂解酶的活性。 N-糖基化酶 / AP裂解酶首先切割 CPD5’嘧啶的 N-糖苷键, 然 后通过 P-裂解酶机制在无碱基位点切割嶙酸二酯骨架。
适用于与石斛的成份和 /或提取物组合使用的 DNA修复酶具有能够识别, 切除和修复 受损 DNA(例如 CPD和(6-4)光产物)的 N-糖基化酶 /AP裂解酶活性。 这些酶的活性可以是 光依赖性的(例如光解酶)或不依赖光的。 该组中的示例性 DNA修复酶包括但不限于噬菌 体 T4嘧啶二聚体特异性内切核酸酶(denV核酸内切酶)、 藤黄微球菌 N-糖基化酶 / AP裂解 酶、 酿酒酵母 N-糖基化酶 /无嘌呤碱基 -无嘧咬碱基裂解酶、 粟酒裂殖酵母紫外线损伤核 酸内切酶(Schizosaccharomyces pombe UV damage endonuclease)(UVDE)、 小球藻病毒分离 物 PBCV-1 嘧啶二聚体特异性糖基化酶、 构巢曲霉光裂解酶, 以及它们经修饰的非天然 (例如重组)酶产物。
DNA修复酶也可包括来自 BER, NER或其他途径的其他成员。 这些酶可以包括 06- 曱基鸟嘌呤 -DNA曱基转移酶、 尿嘧啶和次黄嘌呤 -DNA糖基化酶、 DNA外切核酸酶、 受 损碱基糖基化酶(例如 3 -曱基腺嘌呤 -DNA糖基化酶)、 单独或在复合物中的内切核酸酶(例 如大肠杆菌 uvrA/uvrB/uvrC核酸内切酶复合物)以及其他目前仅部分理解其活性的酶和酶 复合物, 例如人类的 ERCC基因产物和酵母的 RAD基因。 示例性的 DNA修复酶包括但 不限于尿嘧啶 DNA糖基化酶、 3 -曱基腺嘌呤 DNA糖基化酶、 内切核酸酶 III /胸腺嘧啶二 醇 DNA糖基化酶、 内切核酸酶 VIII、 fapy/8 -氧鸟嘌呤 DNA糖基化酶、 A-G-错配 DNA糖 基化酶、 G-T错配 DNA糖基化酶、 曱酰基尿嘧啶 DNA糖基化酶、 羟曱基尿嘧啶 DNA糖 基化酶、 XPC-hHR23B、 XPA、 RPA、 XPB、 TFIIH、 XPG、 XPF-ERCC1、 Rad-4-Rad23、 Radl4、 Rfa、 Rad25/Ssl2、 Rad3、 Rad2、 Radi -Rad 10 < 各种 DNA聚合酶、 DNA连接酶 等。 这些酶的示例性来源可以包括细菌或哺乳动物细胞来源, 包括但不限于大肠杆菌、 酿 酒酵母、 粟酒裂殖酵母、 人、 猴、 小鼠、 大鼠、 仓鼠等。 DNA修复酶可以从合适的来源衍生或提取, 如大肠杆菌、 微球菌等。 DNA修复酶可 以被包封在脂质体中, 如美国专利 5,296,231 中所述, 将该专利的全部内容通过引用并入 本文。 例如, 向含有卵嶙脂和水的脂质体制剂中提供源自藤黄微球菌细胞裂解物的 DNA 修复酶, 并且其可以作为 ULTRASOMESä (来自 Applied Genetics , Inc. Dermatics , Freeport , N.Y.)或 ULTRAS OMES-Vä( Barnet Products Corporation, Englewood Cliffs, N.J.)。 包含 Anacystis nidulans 裂解物(其含有 Anacystis nidulans 光裂解酶)的脂质体可以作为 PHOTOSOMESä或 PHOTOSOMES-Vä从 Applied Genetics, Inc. Dermatics, (Freeport, N.Y.)获得。 脂质体可以包括来自植物来源(例如大豆)的常规嶙脂、 油酸和 /或胆固醇半琥 珀酸酯, 或者它们可以由本领域技术人员通常已知的其他合适来源制备。
示 例 性 的 实 施 方 案 可 加 入 ULTRASOMESä 、 ULTRAS OMES -Vä 、
PHOTOSOMESä或 PHOTOSOMES-Vä , 其量的范围为组合物总重量的约 0.01 %至 20% , 期望地为约 0.1 %至约 10% , 更期望地为约 0.5%至约 3%。
脂质体可用作递送剂以促进美容活性剂向皮肤真皮转移, 例如本发明的植物或植物成 份和 DNA修复酶。 其他递送剂可以用于代替脂质体进行皮肤递送, 包括但不限于本领域 技术人员已知的皮肤递送媒介物, 包括乳液、 微乳液、 纳米乳液、 纳米颗粒、 微球体、 醇 质体、 传递体和类脂嚢泡。
在一些实施方案中, 本申请所述的美容组合物中还可以包含额外的美容成份, 包括但 不限于以下成份: 甘草、 甘草提取物、 甘草衍生物(例如甘草酸盐)中的成份; 柠檬提取物; 黄瓜提取物; 葵花籽提取物; 蓖麻籽油; 燕麦蛋白, 燕麦提取物, 水解燕麦; 丝蛋白(例 如丝胶蛋白); 透明质酸及其衍生物(例如透明质酸納); 维生素; 矿物质; 抗氧化剂; 嶙脂, 鞘脂, 胆固醇; 和 /或具有抗衰老, 抗氧化, 抗炎, 抗刺激, 抗癌或其他皮肤保护性质、 美学外观增强性能、 和 /或增加皮肤递送性质的其他成份或它们的组合。
用于在本发明中进行局部施用的美容上有用的维生素, 矿物质和 /或抗氧化物包括具 有抗氧化特性的植物成份和提取物(例如迷迭香提取物, 积雪草苷等); 维生素 A及其前体 或衍生物(例如 P-胡萝卜素, 棕榈酸视黄酯); 维生素 B3及其前体或衍生物(例如烟酰胺); 维生素 B5及其前体或衍生物(例如泛醇); 维生素 C及其前体或衍生物(例如抗坏血酸四己 基癸酯, 棕榈酸抗坏血酸酯); 维生素 E及其前体或衍生物(例如 d-a-生育酚, 醋酸生育 驗); 维生素 K及其前体或衍生物; 砸及其衍生物(例如 L-砸代曱硫氨酸); 和 a-硫辛酸 (ALA)。
ALA是一种有效的天然抗氧化剂, 有时被称为“通用抗氧化剂”, 因为它在水和脂质 中都具有活性和溶解性。 ALA 能够渗入皮肤细胞, 能够阻止负责胶原蛋白和弹性蛋白分 解的促炎性 NF-KB通路的活化, 并且能够增强维生素 E和 C的保护作用, 从而增强细胞 内的天然抗氧化剂。
在一个实施方案中, 抗坏血酸四己基癸酯可以加入到本文所述的组合物中。 抗坏血酸 四己基癸基酯是维生素 C的稳定的脂溶性酯衍生物。 据报道, 维生素 C促进胶原蛋白合 成, 抑制脂质分解, 使维生素 E再生, 减少细纹和皱纹, 治愈晒伤, 是一种有效的自由 基清除剂式抗氧化剂, 具有显著的抗炎特性, 阻碍例如花生四婦酸的产生。
在另一个实施方案中, 考虑将泛醇或其等同物用于组合物。 泛醇是具有抗炎特性的有 效的成膜湿润剂。 泛醇等同物可以包括泛酸的醇衍生物, 例如在 CTFA Cosmetic Ingredient Handbook, The Cosmetic, Toiletry and Fragrance Association. Inc., pp.272 - 273, 1992中所述的那些。 为了达到最佳使用效果, 应该选择泛醇的量以使组合物能快速合 理地变干。 组合物中泛醇越多, 将组合物施用于皮肤或其他表面后使其变干所需的时间越 长。
维生素, 矿物质和 /或抗氧化剂共同的存在量范围可以为组合物总重量的约 0.01%至 20% , 期望地以约 0.1%至约 10% , 更优选约 0.5%至约 3%的总量范围存在。
任选地, 本发明组合物可另外包含一种或多种麻醉剂、 抗过敏剂、 抗刺激剂、 抗真菌 剂、 抗微生物剂、 抗炎剂、 抗菌剂、 螯合剂、 着色剂、 脱色剂、 缓和剂、 乳化剂、 成膜剂、 香料、 保湿剂、 驱虫剂、 润滑剂、 湿润剂、 药剂、 光稳定剂、 防腐剂、 皮肤保护剂、 皮肤 渗透促进剂、 防晒剂、 稳定剂、 表面活性剂、 增稠剂、 粘度调节剂, 或它们的任意组合。
虽然一些实施方案不使用剥脱剂, 但是可以包括这些药剂, 条件是包括足够的抗刺激 剂 /抗炎剂以缓解剥脱剂的刺激作用。 示例性抗刺激剂包括但不限于: 芦荟, a-没药醇, 咖啡因或其他咕吨, 洋甘菊, 光亮可乐果(cola nitada)提取物, 甘草酸二钾, 甘草酸及其 衍生物, 绿茶提取物, 卵嶙脂或氢化卵嶙脂, 甘草提取物, 茶树油, 甾族或非甾族抗炎剂, 包括但不限于环氧合酶抑制剂(例如水杨酸, 乙酰水杨酸), NF-KB抑制剂, 醋酸锶, 氯化 锶, 硝酸链, 脲, 或它们的组合。 理想的抗刺激剂可以包括甘草酸二钾、 卵嶙脂和氢化卵 鱗脂。
抗刺激剂或抗炎剂单独或共同的存在量范围为组合物总重量的约 0.01%至 10% , 期望 地为约 0.05%至约 5% , 更期望地为约 0.2%至约 1.5%。
植物成份、 植物提取物、 油、 维生素、 矿物质、 抗氧化剂、 抗刺激剂或其他活性剂可 以单独地或共同地包含在药学或美容学可接受的媒介物中。 适用于本发明实施方案的药学 或美容学可接受的载体的实例包括但不限于水、 C1-C4 Sf , 脂肪醇、 脂肪醚、 脂肪酯、 甘 油、 乙二醇、 植物油、 矿物油、 卵嶙脂、 氢化卵嶙脂、 脂质体、 分层脂质物质、 嶙脂、 聚 二醇、 多元醇、 丙醇、 娃油、 植物油, 或它们的任意组合。
与本申请所述的组合物一起使用的药学上或美容学上可接受的载体可以是均相制剂形 式或乳液或微乳液形式, 包括但不限于水包油乳液、 油包水乳液和多相(包括三相)乳化液。 这些乳液的浓稠度可以在很宽范围内变化, 包括稀的爽肤水(其也适合用于喷雾或气雾递 送)、 乳状爽肤水、 淡乳液以及重乳液。 其他适合的局部载体包括无水液体溶剂, 诸如油 与醇; 7JC基单相液体溶剂(如, 水-醇溶剂系统); 无水固体以及半固体(诸如凝胶以及棒剂); 以及水基凝胶与摩丝系统。
药学上或美容学上可接受的媒介物通常占组合物重量的约 5%至约 99.9% , 期望地约 25%至约 80% , 更期望地约 50%至约 70% , 并且在没有其他美容辅助剂的情况下可以形 成组合物的余量。 也考虑到组合物总重量的 5%至 99%之间的任何百分比。
润肤剂是通过提供保护性润肤涂层来保持水合或使皮肤再水合的保湿剂。 润肤剂可以 归类为诸如酯、 脂肪酸和醇、 多元醇和烃等的常规化学类别。 酯可以是单酯或二酯。 脂肪 二酯的代表性实例包括但不限于甘草酸二钾、 己二酸二丁酯、 癸二酸二乙酯、 二聚酸二异 丙酯和琥珀酸二辛酯。 可接受的支链脂肪酯包括但不限于肉豆蔻酸 2 -乙基己酯、 硬脂酸 异丙酯和棕榈酸异硬脂酯。 可接受的三元酸酯包括但不限于三亚油酸三异丙酯和挖檬酸三 月桂酯。 可接受的直链脂肪酯包括但不限于棕榈酸月桂酯、 乳酸肉豆蔻酯和油酸硬脂醇酯。
合适的脂肪醇和酸可以包括但不限于具有约 10至 20个碳原子的醇或酸。 例如, 可以 使用醇如鲸蜡醇、 肉豆蔻醇、 棕榈醇和硬脂醇和相应酸。 多元醇可以用作润肤剂, 包括但不限于直链和支链烷基多羟基化合物。 代表性的多元 醇包括但不限于丁二醇、 丙二醇、 山梨醇、 甘油、 聚合多元醇如聚丙二醇和聚乙二醇等。
烃可以用作润肤剂并且可以包括具有约 12至 30个碳原子的烃链, 包括但不限于矿物 油、 凡士林油、 角莖婦和异链炫炫。
示例性润肤剂包括但不限于丁婦、 辛酸 /癸酸甘油三酯、 蓖麻油、 鲸蜡硬脂醇聚醚 -20、 综婿硬脂醇聚酸 -30、 综婿硬脂醇、 综婿硬脂醇聚酸 20、 综婿硬脂醇 (cetostearyl alcohol)、 鲸婿醇、 十六十八醇 (cetyl stearyl alcohol)、 胆固醇、 可可脂、 己二酸二异丙酯、 甘油、 单 油酸甘油酯、 单硬脂酸甘油酯、 硬脂酸甘油酯、 异链炫炫、 肉豆蔻酸异丙酯、 棕榈酸异丙 酉旨、 羊毛脂、 羊毛脂醇、 氢化羊毛脂、 异链炫烃、 液体石蜡、 亚油酸、 矿物油、 油酸、 凡 士林、 嶙脂、 聚乙二醇、 聚乙二醇 -7甘油椰油酸酯、 聚乙二醇 -18 曱酯二曱基娃炫、 聚氧 乙婦二醇脂肪醇醚、 聚氧丙婦 15 -硬脂醚、 聚丙二醇二醇丙二醇、 丙二醇硬脂酸酯、 山梨 糖醇、 鞘脂、 角鲨婦、 硬脂醇聚醚 -2或 -100、 硬脂酸、 硬脂醇、 脲、 白凡士林等。
润肤剂单独或共同存在的量的范围为组合物总重量的约 0.005%至 20% , 理想地约 0.1% 至约 10% , 更理想地约 1.0%至约 5.0%。
润湿剂是结合水并将其保留在皮肤表面的保湿剂。 示例性润湿剂包括但不限于乙酰葡 糖胺、 双糖胶、 丁二醇、 乙氧基二醇、 乙二醇聚丙婦、 葡萄糖、 甘油聚醚 -26、 甘油、 丙 三醇、 乙二醇、 乳糖醇、 麦芽糖醇、 丙二醇、 丝胶蛋白、 透明质酸納、 山梨糖醇、 木糖醇、 柠檬酸钠、 葡萄糖等。
润湿剂的共同存在量范围为组合物总重量的约 0.1%至 40% , 期望地为约 2.5%至约 25% , 更期望地为约 5%至约 15%。
本组合物可以包含一种或多种防腐剂。 合适的防腐剂包括 EDTA二納、 苯曱醇、 对 羟基苯曱酸曱酯、 苯氧基乙醇、 对羟基苯曱酸丙酯、 对羟基苯曱酸乙酯、 对羟基苯曱酸丁 酯和对轻基苯曱酸异丁酯。
组合物中的另一类功能性成份是增稠剂。 增稠剂的共同存在量范围通常为组合物重量 的约 0.01至 10% , 期望地为约 0.05至 5% , 期望地为约 0.1 %至 1%。 示例性增稠剂是交联 的聚丙婦酸酯物质。 可以使用诸如以下胶: 黄原胶、 角叉菜胶、 明胶、 梧桐胶、 果胶和刺 槐豆胶。 在一些情况下, 增稠功能可以通过也用作硅酮或润肤剂的物质来实现。 例如, 超 过 10厘斯的硅酮橡胶和酯如甘油硬脂酸酯具有双重功能。
在一些实施方案中, 皮肤增白剂可以包含在所述组合物中。 皮肤增白剂包括但不限于 酪氨酸酶抑制剂, 自由基清除剂及它们的混合物。
粉末可以加入到美容组合物中。 这些粉末包括白垩, 滑石, 高岭土, 淀粉, 蒙脱石粘 土, 化学改性的娃酸镁铭, 有机改性的蒙脱土,
Figure imgf000021_0001
合娃酸铭, 气相二氧化娃, 淀粉辛婦基 號轴酸铭及它们的混合物。
其他辅助次要组份也可以加入到所述美容组合物中。 这些成份可以包括着色剂, 遮光 剂和香料。 这些其他辅助次要组份的量范围可以为所述组合物的 0.001%至高达 20%。
本发明的组合物可以配制成适用于局部应用于皮肤的任何便利形式。 这样的产品形式 包括但不限于气溶胶喷雾剂、 乳霜剂、 分散剂、 乳剂、 泡沫剂、 凝胶剂、 液体、 爽肤水、 摩丝、 软膏剂、 贴剂、 香膏、 药包或粉剂、 泵式喷雾剂、 固体、 溶液剂、 棒剂和湿巾。
期望的化妆品形式是为水包油乳液形式的霜剂, 也包括油包水和娃酮包水乳液。 在每 种制剂中, 可以加入各种已知的常规化妆品成份。 例如, 可以包含化妆品成份如醇、 脂肪 和油、 表面活性剂、 脂肪酸、 硅油、 润湿剂、 保湿剂、 粘度调节剂、 乳化剂、 稳定剂、 着 色剂和香料。
组合物可以根据需要, 每天一次、 每天数次或以任何合适的方案施用, 从而达到期望 的结果。
可以连续或间歇施用所述组合物。
一些实施方案涉及包括用本发明的局部用组合物浸渍的贴剂的美容处理系统。 用于本 发明的贴片可以呈适于处理特定目标区域的任何形状。 贴片可以包含针对特定区域的小区 域, 或者其可以覆盖大面积, 例如以面罩形式覆盖面部。 目前用于在眼睛周围施用药物的 贴片的整体尺寸和几何形状使得难以将眼睛处理产品贴近眼睛施用。 贴剂可以由适合吸收, 包含和释放本发明组合物的任何去除材料制成。 例如, 贴片可以由无纺材料制成。 所述无 纺材料可以包括棉, 棉 /聚酯混合物或其他天然或合成材料的合适组合。 贴片可以进一步 适用于提供闭塞, 半闭塞或非闭塞屏障。 贴剂可以是粘合性的或非粘合性的。 贴片可以包 括单层材料, 或者其可以包括相同和 /或不同材料的多个层以提供额外的结构完整性和 /或 灵活性。 合适的贴片或贴片材料披露在例如美国专利 6,096,334; 6, 120,792; 6,495, 158; 6,623,751 ; 8,697,099 ; 美国专利申请 2002/0086043 ; 美国专利申请 2003/0152610 ; U.S. 2003/0175328; 和它们引用的参考文献中, 将这些文献披露的内容并入本申请作为参考。
在一些实施方案中, 本发明的美容处理系统可以包括用于保持美容处理系统的各个部 件的包装系统。 在优选实施方案中, 美容处理系统包括贴片; 至少一个容器; 和经配制用 于处理面部的至少一部分的局部组合物
一个或多个容器可以用于容纳美容处理系统的一个或多个部件。 根据本领域技术人员 已知的常规实践, 可以使用适于容纳美容处理系统的部件的任何容器。 或者, 可以将贴剂 包装在凹陷盘形式的容器中, 该容器被可密封移除的覆盖物覆盖的, 从而在使用前将贴片 牢固地保持在凹陷盘中。
容器可以通过合适材料(例如聚丙婦)的热成形或通过薄壁注塑来制备。 可以对容器的 设计进行修改并适应特定贴片的形状。 合适的容器公开于美国专利 6,623,751 中, 其内容 通过引用并入本文。
一些进一步的实施方案涉及一种美容处理系统, 其包括包装系统, 该包装系统含有适 合期望时间段(例如十四天)的适当量的美容组合物。 根据该实施方案, 美容处理系统包括 包含多个容器的包装系统, 每个容器具有适合于单次使用量的根据本发明的美容组合物。 容器可以是小瓶形式或其他合适的保持装置。
在一个实施方案中, 美容处理系统包括具有多个小瓶的包装系统, 每个小瓶含有足够 量的适用于将美容组合物单次施用于皮肤的美容组合物。 可以配制包装系统以提供与美容 组合物施用于皮肤的天数相匹配的一定数目小瓶。 或者, 所述包装系统经配制用于每天多 于一次施用。 在一个实施例中, 包装系统可以包含用于在 14天内对皮肤进行每日处理的 14个小瓶。 包装系统可以进一步包含一个或多个用于施加组合物的施用器, 并且还可以 包括用于使用所述美容处理系统随附的包装系统的一套说明。
本发明还包括通过局部施用本发明的美容组合物来处理皮肤的方法。 在使用中, 少量 的组合物, 例如 0.1至 100mL, 可以从合适的容器或涂药器施加到皮肤的暴露区域, 并且 如果必要的话, 然后使用手或手指或合适的装置将其涂布和 /或涂抹到皮肤中。 或者, 该 组合物可以以已用组合物浸渍的贴剂形式施用于皮肤。 贴剂可以由无纺材料制成, 并且可 以进一步含有粘合剂以将贴剂粘附到皮肤上。
一些额外的实施方案涉及药物, 其包含石斛(例如金钗石斛)的分离成份或提取物, 用 于预防、 治疗和 /或治愈人类皮肤和 /或头发免受以下的至少一种: 空气污染诱导的或空气 污染可诱导的皮肤和 /或头发损伤, 空气污染诱导的氧化应激, 空气污染诱导的细胞活力 降低, 空气污染诱导的 IL-6增加和 /或空气污染诱导的细胞损伤。 金钗石斛的成份或提取 物的存在量范围可为药物总重量的约 0.0001%至 5% ; 期望地, 为药物总重量的约 0.001% 至约 2.5%; 更期望地, 为药物总重量的约 0.001%至约 0.5% ; 甚至更期望地, 为药物总重 量的约 0.01%至约 0.1%。 本申请所述的药物还可以包括上文针对本申请的局部组合物所 列出的任何其他组份。
应用本申请所述的药物可以减少或预防空气污染诱导的或空气污染可诱导的皮肤和 / 或头发损伤, 减少或预防空气污染诱导的氧化应激, 减少或预防空气污染诱导的细胞活力 降低, 减少或预防空气污染诱导的 IL-6增加和 /或减少或预防空气污染诱导的细胞损伤。 由于组合物的抗污染作用, 本文所述的药物还可以提供多种抗衰老和肌理益处。 据信, 包 含金钗石斛的组合物提供显著的抗污染作用, 相对于其他市售皮肤健康局部用产品, 本申 请组合物具有显著的抗衰老和肌理益处。 本文描述的药物的示例性益处包括上面针对局部 组合物描述的那些。 方法
些进一步的实施方案涉及保护人类皮肤和 /或头发对抗空气污染诱导的损伤, 包括 应用包含石斛(例如金仅石斛)的分离成份或提取物的组合物或药物, 其中所述组合物或药 物的使用量足以实现至少一个以下方面: 减少和 /或预防空气污染诱导的或空气污染可诱 导的皮肤和 /或头发损伤, 减少和 /或预防空气污染诱导的氧化应激, 减少和 /或预防空气污 染诱导的细胞活力降低, 减少和 /或预防空气污染诱导的 IL-6增加和 /或减少或预防空气污 染诱导的细胞损伤。 金钗石斛的成份或提取物的存在量范围可为药物总重量的约 0.0001% 至 5%; 期望地, 为药物总重量的约 0.001%至约 2.5% ; 更期望地为药物总重量的约 0.001% 至约 0.5%; 甚至更期望地为药物总重量的约 0.01%至约 0.1%。 一些进一步的实施方案涉及使用石斛(例如金钗石斛)的分离成份或提取物作为抗污染 剂(各自的抗污染混合物)用于保护人类皮肤和 /或头发。 抗污染特别涉及保护和 /或抑制和 / 或减少人皮肤和毛发的障碍和功能失调, 所述障碍和功能失调分别与诱导氧化应激, 细胞 活力降低和 /或增加 IL-6基因表达相关。
一些其他实施方案涉及用于改善受空气污染损害的皮肤和 /或毛发的美容外观的方法, 其中本申请所述的组合物或药物分别以美容学或药学有效量局部应用于皮肤, 足以改善皮 肤的美容外观。 所述改善涉及皮肤老化、 纹路、 细纹、 皱纹、 鱼尾纹、 黑眼圈、 瘢点、 老 年斑、 暗斑、 任娘纹、 癌症(包括皮肤癌)、 皮肤炎症、 皮肤变色、 皮肤色素沉着、 皮肤厚 度; 弹性、 回弹性、 保湿、 色调、 肌理、 光感、 光泽、 亮度、 亮白度、 透明度、 轮廓外观、 紧实度、 绷紧度、 柔软度、 柔和度、 敏感度、 毛孔大小、 皮肤屏障功能, 或它们的组合。
所述改善进一步涉及由空气污染导致或带来的不利皮肤病症、 其包括牛皮癖、 湿疹、 皮脂溢出、 皮炎、 晒伤、 雌激素失衡、 色素沉着、 色素减退、 变色、 变黄、 雀斑、 皮肤萎 缩、 皮肤发疹、 皮肤脆弱、 干燥、 皲裂、 下垂、 变薄、 增生、 纤维化、 毛孔粗大、 形成脂 肪团、 痴伤、 形成痤疮、 凋亡、 细胞分化、 细胞去分化、 预防肿瘤诱导或肿瘤进展、 病毒 感染、 真菌感染、 细菌感染、 物蛛样静脉(毛细管扩张)、 多毛症、 酒渣鼻、 瘙痒症、 老茧、 疣、 鸡眼或它们的组合。
除了对皮肤和 /或头发具有抗污染作用之外, 本申请所述的局部组合物或药物可局部 应用以增强皮肤的总体健康、 活力和外观。 例如, 本发明组合物可用于皮肤以改善微循环, ?文善皮肤细胞之间的通讯, 补充必需营养素或皮肤成份, 或改善皮肤细胞的代谢、 增殖、 繁殖、 转换和 /或剥脱。
一些其他实施方案涉及包含局部用组合物的美容治疗系统, 所述局部用组合物包含植 物成份、 植物提取物或石斛例如金钗石斛的天然复合物或其提取物, 以及药学上或美容学 上可接受的媒介物。 以下是本发明的非限制性实例。 除非另有说明, 否则所有比例和百分比均以重量计。 实施例 下面为本发明制剂和方法的实施例。 实施例 1: 制备金钗石斛提取物
使用去离子水提取技术获得金钗石斛的植物提取物。
具体地, 通过在低温(约 80 °C)用去离子水提取金钗石斛的茎, 随后离心和用 10nm膜 过滤来进行多糖提取。 接下来, 也在低温(约 60 °C)在真空中浓缩多糖提取物。 通过添加一 些乙醇至约 80%(v/v)的浓度来将多糖提取物纯化并浓缩, 以获得沉积物分散的溶剂。 接 下来, 将沉积物离心并收集, 溶解于水中。 随后进行消毒, 然后将提取物包装。
将金钗石斛的茎的提取物标准化为约 0.1-0.2%(w/w)的多糖。 实施例 2: 金钗石斛提取物的细胞毒性
细胞计数试剂盒 -8(CCK-8)为在任何体外模型中研究诱导和抑制细胞增殖提供了工具。 CCK-8通过利用高度水溶性四唑盐, 可以非常方便地进行测定。 WST-8 [2-(2 -曱氧基 -4 -硝 基苯基)-3-(4 -硝基苯基)-5-(2,4 -二磺基苯基)-2H-四唑鎗一钠盐]在电子介体存在下还原后产 生水溶性曱腊(formazan)染料。
根据制造商的说明书使用购自 Dojindo Laboratories 的细胞计数试剂盒 -8 (Cell Counting Kit- 8 , Dojindo Laboratories , Kumamoto , Japan)进行 CCK-8 比色测定, 从而在 用金钗石斛提取物处理后在细胞毒性测定中测定细胞活力(与用 PM2.5颗粒处理相比较)。 PM2.5颗粒是从空气中收集的直径为约 2.5微米或更小的空气污染物。
将使细胞活力相比于对照降低 10%的浓度定义为细胞毒性标准。 如图 1 所示, 选择 用于 PM2.5颗粒组的浓度, 使得 PM2.5处理组的细胞活力在 4小时时高于对照的 80%。 如图 2所示, 选择金钗石斛提取物处理组的浓度, 使得金钗石斛提取物处理组的细胞存活 率在 24小时时高于对照的 80% , 而在 4小时时没有毒性作用。
表 1 :用于进一步测试的剂量; |ig/mL.
Figure imgf000025_0001
如表 1中所示, 根据 CCK-8测定筛选, 选择金钗石斛提取物处理组和 PM2.5颗粒处 理组的浓度以用于下列测试。
基于针对细胞毒性测试所选的浓度(实施例 2)对金钗石斛提取物进行数次体外效力测 试(与抗 -PM2.5相比较)。 实施例 3: 体外效力测试
为了确定金钗石斛提取物对 Hacat细胞中活性氧(ROS)水平的影响, 使用购自 Sigma- Aldrich的焚:光细胞内 ROS试剂盒(Fluorometric Intracellular ROS Kit, Orange Fluorescence, 目录号 MAK144)。
ROS是有氧呼吸期间的氧气减少的结果并由细胞内多种酶系统产生。 在生理水平, ROS有助于细胞信号传导和宿主防御。 ROS生成增加超过生物系统的解毒能力时导致氧 化应激和细胞损伤。 对细胞的主要损害是由 ROS诱导的大分子(如膜脂中的多不饱和脂肪 酸、 必需蛋白质和 DNA)改变。
如制造商所述, 该试剂盒提供了一种灵敏的测定法, 用于在 1小时孵育内检测活细胞 中的细胞内 ROS(特别是超氧化物和羟基自由基)。 ROS与可透过细胞的传感器反应, 导 致与 ROS存在量成比例的荧光产物。
图 3显示 PM2.5可显著增强 Hacat细胞中的 ROS水平。 换句话说, PM2.5可以提高 Hacat细胞的氧化应激。 图 3还表明, 金钗石斛提取物能有效抵抗 PM2.5增加的 ROS水 平, 而且金钗石斛提取物本身不会引起 Hacat细胞的氧化应激。 实施例 4:线粒体膜电位(MMPV测试
图 4显示线粒体膜电位(MMP)测试结果。 使用购自 Sigma- Aldrich的线粒体膜电位试 剂盒(Mitochondria Membrane Potential Kit , 用于微板读数器的 JC-10 测定, 目录号 MAK159 , Sigma- Aldrich, St. Louis, MO), 按照制造商的说明书进行 MMP测试。 该试 剂盒利用 JC-10测定细胞中 MMP的损失。 该试剂盒可用于监测细胞凋亡和筛选细胞凋亡 抑制剂和激活剂。 如图 4所示, PM2.5显著降低 MMP 7jc平并引起细胞活力降低。 而金钗石斛提取物本 身不降低细胞 MMP 7jC平, 如图所示, 金钗石斛提取物明显保护了细胞活力。 实施例 5: IL-6
设计本研究旨在确定金钗石斛提取物对 IL-6 7jc平的影响(与对照样品相比)。 根据制造 商的说明使用购自 Sigma- Aldrich的 ELISA试剂盒。
图 5显示了多种样品(对照, PM2.5 , 金钗石斛提取物(50ug/ml)和金钗石斛提取物 (50ug/ml) + PM2.5)可诱导 IL-6水平。 当将金钗石斛提取物样品和 PM2.5对照样品相比较 时, PM2.5显著增加 IL-6 7jc平。 虽然金钗石斛提取物在某些浓度也可以增加 IL-6水平, 但经证明, 金钗石斛提取物相比于 PM2.5处理组显著降低 IL-6 7JC平, 降低了 41.3%。 实施例 6: 乳酸脱氢酶(LDH或 LD)
乳酸脱氢酶(LDH或 LD)是在几乎所有活细胞(动物, 植物和原核生物)中发现的一种 酶。 LDH催化乳酸向丙酮酸的转化以及丙酮酸向乳酸的转化, 因为它将 NAD+转化为 NADH并反向转化。 LDH在多种身体组织中广泛表达, 如血细胞和心肌。 因为它在细胞 损伤过程中被释放, 所以它起到了细胞损伤标记物的作用。 具体而言, 组织中 LDH 7JC平 越高, 观察到的细胞损伤越大。
用购自 Sigma- Aldrich 的乳酸脱氢酶活性测定试剂盒(Sigma Aldrich , 目录号 MAK0660)来研究用 PM2.5和金钗石斛提取物处理后的细胞损伤。
如图 6所示, PM2.5增加细胞损伤率, 而用金钗石斛提取物处理不损伤细胞。 相反, 用金钗石斛提取物处理可以出人意料地防止 PM2.5 引起的细胞损伤, 如深绿色柱中所示。 实施例 7: 制剂
示例性美容制剂可如下所示:
Figure imgf000028_0001
基于实施例 1-5可以清楚地看出, 金钗石斛提取物具有非常好的抗污染性质。 此外, 它是水溶性的, 可以广泛用于美容产品中。
因此, 预期的是, 前述详细描述应被认为是说明性的而不是限制性的, 并且应当理解 的是, 旨在限定本发明的精神和范围的是随附权利要求, 包括所有等同方案。

Claims

权利要求书
1.美容组合物, 其包含:
金钗石斛的分离成份或提取物, 其量足以实现以下至少一种:
(A)减少或预防空气污染诱导的或空气污染可诱导的皮肤和 /或头发损伤;
(B)减少或预防空气污染诱导的氧化应激;
(C)减少或预防空气污染诱导的细胞活力降低;
(D)减少或预防空气污染诱导的 IL-6增加; 或者
(E)减少或预防空气污染诱导的细胞损伤;
和美容学上可接受的载体或赋形剂。
2.权利要求 1的组合物, 其中所述皮肤损伤为皮肤老化、 纹路、 细纹、 皱纹、 鱼尾纹、 黑眼圈、 瘢点、 老年斑、 暗斑、 任娘纹、 皮肤癌、 皮肤炎症、 皮肤变色、 皮肤色素沉着、 皮肤屏障功能损伤, 或它们的组合。
3.权利要求 1或 2中任一项的组合物, 其中所述组合物为个人护理组合物、 皮肤护理 组合物、 头发护理组合物、 抗衰老护理组合物、 防晒护理组合物, 或它们的组合。
4.权利要求 1-3中任一项的组合物, 其中所述组合物为以下形式: 气雾剂、 霜剂、 乳 剂、 固体、 液体、 分散剂、 泡沫剂、 凝胶、 爽肤水、 摩丝、 软膏、 粉剂、 贴片、 香膏剂、 溶液、 泵式喷雾剂、 棒剂、 油剂、 湿巾, 或它们的组合。
5.权利要求 1-4中任一项的组合物, 其中所述金钗石斛的成份或提取物的存在量为组 合物总重量的约 0.0001 %至约 5%。
6.权利要求 1-4中任一项的组合物, 其中所述金钗石斛的成份或提取物的存在量为组 合物总重量的约 0.01%至约 0.1%。
7.权利要求 1-6中任一项的组合物, 其中所述美容学上可接受的载体或赋形剂选自水、 甘油、 C1-C4 S事、 脂肪醇、 脂肪醚、 脂肪酯、 多元醇、 乙二醇、 植物油、 矿物油、 脂质体、 分层脂质物质、 硅油, 或它们的组合。
8.药物, 其包含金钗石斛的成份或提取物和药学上可接受的载体或赋形剂, 其中所述 药物用于预防、 治疗和 /或治愈人类皮肤和 /或头发免受以下的至少一种:
(A)空气污染诱导的或空气污染可诱导的皮肤和 /或头发损伤; (B)空气污染诱导的氧化应激;
(C)空气污染诱导的细胞活力降低;
(D)空气污染诱导的 IL-6增加; 或者
(E)空气污染诱导的细胞损伤。
9.权利要求 8的药物, 其中所述皮肤损伤为皮肤老化、 纹路、 细纹、 皱纹、 鱼尾纹、 黑眼圈、 瘢点、 老年斑、 暗斑、 任娘纹、 皮肤癌、 皮肤炎症、 皮肤变色、 皮肤色素沉着、 皮肤屏障功能损伤, 或它们的组合。
10.权利要求 8或 9中任一项的药物, 其中所述金钗石斛的成份或提取物的存在量为 组合物总重量的约 0.0001%至约 5%。
11.权利要求 8或 9中任一项的药物, 其中所述金钗石斛的成份或提取物的存在量为 组合物总重量的约 0.01 %至约 0.1%。
12.包装系统, 其包含以下的至少一种:
(A) 一个或多个容器, 它们共同含有权利要求 1-7中任一项的组合物或权利要求
8-11中任一项的药物; 或者
(B) 从所述一个或多个容器应用所述组合物的说明书。
13. 一种保护人类皮肤和 /或头发对抗空气污染诱导的损伤的方法, 包括将权利要求 1- 7中任一项的组合物或权利要求 8-11中任一项的药物局部应用至所述皮肤和 /或头发。
14.权利要求 13的方法, 其中将金钗石斛的成份或提取物以约 0.01至约 5 MG/CM2 的有效量应用于人类皮肤和 /或头发。
15.金钗石斛的成份或提取物作为抗污染剂保护人类皮肤和 /或头发的用途。
16.权利要求 15的用途, 其中所述抗污染涉及保护和 /或抑制和 /或减少人类皮肤和 /或 头发的障碍和功能失调。
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