CN106691880A - Composition for improving skin - Google Patents

Composition for improving skin Download PDF

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Publication number
CN106691880A
CN106691880A CN201510424067.2A CN201510424067A CN106691880A CN 106691880 A CN106691880 A CN 106691880A CN 201510424067 A CN201510424067 A CN 201510424067A CN 106691880 A CN106691880 A CN 106691880A
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China
Prior art keywords
skin
composition
chemical formula
compound
weight
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Chinese (zh)
Inventor
金孝珍
金度亨
李相和
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LG H&H Co Ltd
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LG Household and Health Care Ltd
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Priority to CN201510424067.2A priority Critical patent/CN106691880A/en
Publication of CN106691880A publication Critical patent/CN106691880A/en
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Abstract

The invention relates to a composition for improving skin. Rutin shows a skin texture improved effect brought by improved skin tone, so the rutin can be used in pharmaceutical compositions, skin topical agents, cosmetic compositions, or health-care foods. In addition, the rutin shows the effects of promoting skin stem cell proliferation and dry maintenance, so the rutin can be used as a composition for promoting the activity of the stem cells and cosmetics comprising the composition.

Description

Composition for improving skin
Technical field
The present invention relates to improve dermatoglyph etc. for improving the composition of skin.
Background technology
It is characterised by as the dermatoglyph of skin surface form, with the three-dimensional produced by fine line Micro-structural, and it is dramatically different according to different ages/position.Depth area of the dermatoglyph according to grain It is divided into 1 (about 20-100 μm) line, 2 (about 5-40 μm) lines, 3 (about 0.5 μm) lines, Good skin, understands the webbed network structure of shape between each grain, and with intersecting between line The polygon of formation and star (star formation) more clearly feature [non-patent literature 1].
However, it is known that with age or due to skin injury, the fine and close micro-texture line of script Network structure is destroyed, and fine line (2 times, 3 inferior) disappears, and 1 time line is then deepened all the more and produced Wrinkle [non-patent literature 2].That is, the wrinkle of the representative disease for being shown with skin aging, is long The accumulation of phase fine change.
All constituents of the known application on human skin in embryology come from ectoderm or mesoderm.Epidermis, Hair follicle, sebaceous glands and sweat gland etc. originate from ectoderm, and melanocyte, neural and special sense Receiver comes from neuroderm.According to embryonic stage, embryonic stem cell repeats differentiation and turns into and meet each From function of organization characteristic cell, that is, become also leave in the tissue after adult it is a number of dry thin Born of the same parents, and stem cell is primarily present at two in skin.Firstly there are in hair follicle (hair follicle). Know it is herein the cell for not causing cell differentiation, the regeneration to epidermis is played an important role, for hair Regeneration with growth also function to important effect.Next to that being present in basalis (the basal layer of epidermis of epidermis).It has been found out that, not only arranging epidermis positioned at stem cell herein also dominates skin corium Fibroblast, plays the important effect of the Maintenance Of Skin Health.Stem cell herein has stem cell amount The relatively many, advantage that can be readily available and be widely used in the research of skin progenitor cell.Skin can continue Regeneration (renew), is present in the epithelial stem cell (epidermal of stem cell in the epithelium of skin, i.e. skin Stem cells) after wound, participate in the recovery [non-patent literature 3] of epithelium.The epithelium of above-mentioned skin is dry thin Born of the same parents are also referred to as skin progenitor cell (skin stem cells), when above-mentioned skin progenitor cell is activated, The skin traumas such as wound can be treated or promote trauma care, can also expect to alleviate wrinkle of skin.According to Report, integrin β_1 (integrin β 1) and integrin α6 (integrin are used as the index of skin progenitor cell α 6), skin progenitor cell needed for the formation of Epithelial morphology and differentiation is maintained by p63 protein Regulation.
Skin progenitor cell plays weight for the shape constancy in the health and physiology and biochemistry that maintain skin The effect wanted.The stem cell for being present in skin is also subject to aging influence and exception functionally occurs, by The shape constancy of this skin is broken, and produces various problems.Therefore, can by the activity of such stem cell To improve the various phenomenons [non-patent literature 4] of skin aging.
In addition, highly desirable develop for organism safely, effectively stable components, most importantly Effect is more excellent than the existing material with dermatoglyph improvement, improve work with dermatoglyph The composition of property.
Prior art literature
Non-patent literature
(non-patent literature 1) Journal of the European Academy of Dermatology and Venereology.12:103-114,1999
(non-patent literature 2) The British journal of dermatology.110:129-138,1984, Skin research and technology.5:189-194,1999
(non-patent literature 3) Epidermal Stem Cells of the Skin, Cedric Blanpain, Elaine Fuchs,Annual Review of Cell and Developmental Biology,November 2006, Vol.22,Pages 339-373
(non-patent literature 4) Human skin stem cells and the ageing process, Cather in Niemann,Stem Cell Aging and Regenerative Medicine,November 2008,Pages 986-997
The content of the invention
The invention problem to be solved
In this regard, the present inventor etc. are by confirming the skin that the improvement skin color of rutin (Rutin) is brought Skin texture improvement and confirm that stem cells hyperplasia facilitation effect and dryness maintain effect, so as to complete The present invention.
Therefore, it is an object of the present invention to provide a kind of composition for improving dermatoglyph, its work For active ingredient includes the compound represented by following chemical formula 1.
Chemical formula 1:
In addition, another object of the present invention is to, there is provided a kind of composition for promoting Stem Cell Activity And the cosmetic composition comprising said composition, the composition conduct for promoting Stem Cell Activity Active ingredient includes the compound represented by following chemical formula 1.
Chemical formula 1:
Solve the method used by problem
Method as above-mentioned problem is solved, the present invention is provided outside a kind of skin for improving dermatoglyph With agent, it includes the compound represented by following chemical formula 1 as active ingredient.
Chemical formula 1:
Used as the other method for solving above-mentioned problem, the present invention provides a kind of change for improving dermatoglyph Cosmetic compositions, it includes the compound represented by following chemical formula 1 as active ingredient.
Chemical formula 1:
Used as the other method for solving above-mentioned problem, the present invention provides a kind of for promoting stem cell to live The composition and the cosmetic composition comprising said composition of property, it is described for promoting Stem Cell Activity Composition includes the compound represented by following chemical formula 1 as active ingredient.
Chemical formula 1:
Invention effect
Rutin (Rutin) of the invention shown because improving the dermatoglyph improvement brought of skin color, Therefore can be used in medicine, cosmetics or health food.Promote skin progenitor cell in addition, also showing Propagation and maintain dryness effect, therefore can as promote Stem Cell Activity composition and comprising The cosmetics of said composition are used.
Specific embodiment
Below, composition of the invention is specifically described.
In order that the composition for improving dermatoglyph plays excellent effect when skin is applied to, it is desirable to It has following functions:The activity of improvement dermatoglyph high is shown at low concentrations;Through skin quilt The ability of absorption is excellent;The low improvement institute for showing dermatoglyph enough so as to stop of volatility The time for needing;The maintenance that active component can be stablized in composition or skin;It is easy to formulation to turn to Medicine or cosmetics;And to skin safe.But, can all meet above-mentioned in known composition The composition of characteristic is simultaneously few.Although for example, some compositions for improving dermatoglyph are low when in vitro testing Dermatoglyph under concentration improves superior activity, but the ability of absorbing transmission from skin is low, it is difficult to be applied to reality On the skin on border.In addition, other active components are low due to hydrophily, medicine is turned to therefore, it is difficult to formulation Or cosmetics.In addition, some improve the composition of dermatoglyph when in heat, light or oxygen, deposit In above-mentioned active component other compounds are decomposed or are changed into so as to failed before skin is applied to Situation.
By following embodiments, can confirm:Rutin also shows that extremely excellent skin-color at low concentrations Improvement is adjusted, therefore can be as the medicine for improving dermatoglyph, cosmetics, health food etc. Active ingredient use.
Therefore, the present invention provide a kind of pharmaceutical composition for improving dermatoglyph, its as effectively into Subpackage contains the compound represented by following chemical formula 1.
Chemical formula 1:
The compound name of the compound of above-mentioned chemical formula 1 is 2- (3,4- dihydroxy phenyls) -5,7- dihydroxy - 3- [α-L- rhamnopyranosyls-(1 → 6)-β-D- glucopyras glycosyloxy] -4H- chromene -4- ketone (2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-3-[α-L-rhamnopyranosyl-(1→ 6)-β-D-glucopyranosyloxy] -4H-chromen-4-one), have another name called for rutin (Rutin), Lu Ding, Road fourth powder, rutin, Lu Tong, network are logical, Rutin, rue leaf glycosides, Rutoside, Phytomelin, Sophorin、Birutan、Eldrin、Birutan Forte、Rutin trihydrate、Globularicitrin、 Violaquercitrin。
The compound of above-mentioned chemical formula 1 can synthesize and use or can use commercially available compound.
Pharmaceutical composition for improving dermatoglyph of the invention can be comprising shownization of above-mentioned chemical formula 1 The pharmaceutically acceptable salt of compound.
The pharmaceutically acceptable salt of compound shown in above-mentioned chemical formula 1 can be to use organic acid or inorganic Acid formed acid-addition salts, above-mentioned organic acids can such as enumerate formic acid, acetic acid, propionic acid, lactic acid, butyric acid, Isobutyric acid, trifluoroacetic acid, malic acid, maleic acid, malonic acid, fumaric acid, butanedioic acid, mono succinate Acid amides, glutamic acid, tartaric acid, oxalic acid, citric acid, hydroxyacetic acid, glucuronic acid, ascorbic acid, Benzoic acid, phthalic acid, salicylic acid, ortho-aminobenzoic acid, dichloroacetic acid, AOAA, benzene sulfonic acid, P-methyl benzenesulfonic acid and the salt of methanesulfonic acid system, above-mentioned inorganic acid can for example enumerate hydrochloric acid, bromic acid, sulfuric acid, The salt of phosphoric acid, nitric acid, carbonic acid and boric acid system.It is preferred that can be the form of hydrochloride or acetate, More preferably hydrochloride form.
The above-mentioned acid-addition salts for referring to can be manufactured by following conventional salt manufacture method:A) will be above-mentioned The compound of chemical formula 1 and acid directly mix;Or one kind therein b) is dissolved in solvent or aqueous solvent In after mixed;Or c) compound of chemical formula 1 is placed in solvent or aquation solvent in acid in, will They mix.
Form as other acceptable salt unlike those described above has GABA salt, Gabapentin Salt, Pregabalin salt, nicotinate, adipate, half malonate, cysteine salt, the Guang of acetyl half Propylhomoserin salt, methionine salt, arginine salt, lysine salt, ornithine salt, aspartate etc..
In addition, when the compound of above-mentioned chemical formula 1 of the invention is used as into medicine, a kind can also be contained More than show the active ingredient of same or similar function.For example, also skin can be improved comprising known The composition of texture.When composition is improved comprising other additional dermatoglyphs, can more promote of the invention The dermatoglyph improvement of composition.In additional mentioned component, it may be considered that what compound use caused Stability between cutaneous safety, the easiness of formulation and active ingredient.Add containing for composition Amount can be 0.0001 weight %~10 weight % relative to composition total weight, and above-mentioned content range can be according to skin The essential conditions such as skin security, the easiness of the compound in formulation of above-mentioned chemical formula 1 are adjusted.
In addition, the pharmaceutical composition for improving dermatoglyph of the invention can also be included can pharmaceutically connect The carrier received.
Pharmaceutically acceptable carrier can contain such as cushioning liquid, sterile water for injection, common life Manage the various composition of salt solution or phosphate buffered saline (PBS), sucrose, histidine, salt and polysorbate etc..
Pharmaceutical composition of the invention can be administered by oral or parenteral mode, can be with common drug Oral and parenteral various formulations administration during the form, such as clinical administration of product preparation, formulation When, it is possible to use usually used filler, extender, adhesive, wetting agent, disintegrant, surface The diluent or excipient of activating agent etc. is adjusted.
For be administered orally solid pharmaceutical preparation including tablet, pill, powder, granule, capsule etc., Such solid pharmaceutical preparation can be by the figuration that is mixed into pharmaceutical composition of the invention more than at least one Agent, such as starch, calcium carbonate (Calcium carbonate), sucrose (Sucrose) or lactose (Lactose), Gelatin etc. is adjusted.
In addition to simple excipient, lubricant of magnesium stearate, talcum etc. etc. can also be used.Make It is that, for oral liquid preparation, suspending agent, oral solution (oral solutions), breast can be enumerated Agent, syrup etc., except be commonly used the water as simple diluent, in addition to atoleine, can be with Comprising various excipient, such as wetting agent, sweetener, aromatic, antistaling agent etc..
For in the preparation of non-oral administration can comprising bactericidal aqueous solution, non-aqueous solvent, suspending agent, Emulsion, freeze-dried preparation, suppository.As non-aqueous solvent, suspension agent, it is possible to use propane diols The injectable of the vegetable oil of (Propylene glycol), polyethylene glycol, olive oil etc., ethyl oleate etc. Ester etc..As the matrix of suppository, it is possible to use witepsol, polyethylene glycol, tween (tween) 61, Cocoa butter, laurin fat (Laurin butter), glycerin gelatine (glycerogelatin) etc..
In the present invention, " dermatoglyph improvement " refers to by suppressing or hindering due to aging, pressure Deng influence caused by the roughening phenomenon of skin surface so that skin surface becomes smooth, assigns light Pool, the improvement colour of skin brighten.
Pharmaceutical composition of the invention in the compound of the above-mentioned chemical formula 1 comprising effective dose, Ke Yiti For preferable dermatoglyph improvement.In the present invention, " effective dose " refers to that can show that skin line Manage the amount of the compound of improvement.The compound of the above-mentioned chemical formula 1 included in composition of the invention Form of effective dose when being made into product according to composition, above-claimed cpd be applied to the method for skin with And rest on time of skin etc. and different.For example, when above-mentioned composition is made into medicine, it is logical with being made Compared when often suitable for the cosmetics of skin, can be with compound of the higher concentration comprising above-mentioned chemical formula 1. Thus, it is 0.1~100mg/kg when the dosage of a day is on the basis of the amount of the compound of above-mentioned chemical formula 1, Preferably 30~80mg/kg, more preferably 50~60mg/kg, can be administered 1~6 time daily.
Pharmaceutical composition of the invention can be used alone or with operation, radiation cure, hormone therapy, Chemotherapy and the method using BRM etc. are applied in combination.
The present invention can also be provided as compound of the active ingredient comprising above-mentioned chemical formula 1 for changing The formulation of the skin preparations for extenal use of kind dermatoglyph.
When the compound of above-mentioned chemical formula 1 is used as into skin preparations for extenal use, lipid material can also be contained, had Machine solvent, solubilizer, concentrating agents and gelling agent, softening agent, antioxidant, suspending agent, stabilizer, hair Infusion (foaming agent), aromatic, surfactant, water, ionic or nonionic emulsifier, Filler, metal ion block agent and chelating agent, antistaling agent, vitamin, blocking agent, wetting agent, essence Oil, dyestuff, pigment, hydrophily or lipophile activating agent, lipid vesicle are generally used for skin external application The usually used adjuvant (adjuvant) in Dermatology field such as arbitrary other compositions of agent.In addition, Mentioned component can be imported with amount usually used in Dermatology field.
When the compound of above-mentioned chemical formula 1 is provided with the formulation of skin preparations for extenal use, can using ointment, The formulation of patch (Patch), gel, creams or spray etc., but not limited to this.
The present invention can also be provided as compound of the active ingredient comprising above-mentioned chemical formula 1 for changing The formulation of the cosmetics of kind dermatoglyph.
When the compound of above-mentioned chemical formula 1 is used as into cosmetics, above-mentioned chemical formula 1 is contained as active ingredient Compound the form of common emulsification formulation and solubilized formulation is can be made into the cosmetics that manufacture. For example, can be:The toner such as soft toner or nutrition toner, facial emulsion (Facial Lotion), The creams of the emulsion of beauty body lotion liquid (Body Lotion) etc., nourishing cream, moisturiser, eye cream etc., Elite, cosmetic ointment, spraying, gel, facial mask, suncream, sun screen (Makeup Base), liquid The makeup removing agent of the vanishing cream of state or solid-state or aerosol type, muffin, washing cream, mildy wash, face cleaning oil etc., The formulations such as the lotion of face cleaning foam, soap, shower cream etc..
In addition, above-mentioned cosmetics can also contain lipid except the chemical combination beyond the region of objective existence containing above-mentioned chemical formula 1 Matter, organic solvent, solubilizer, concentrating agents and gelling agent, softening agent, antioxidant, suspending agent, stabilization Agent, foaming agent (foaming agent), aromatic, surfactant, water, ionic or nonionic It is emulsifying agent, filler, metal ion block agent and chelating agent, antistaling agent, vitamin, blocking agent, wet Profit agent, essential oil, dyestuff, pigment, hydrophily or lipophile activating agent, lipid vesicle or being generally used for The usually used adjuvant (adjuvant) in cosmeceutical field such as arbitrary other compositions of cosmetic.
When the compound of above-mentioned chemical formula 1 is made into cosmetics, if being rested in the active ingredient short time Makeup removal products, the lotion of skin etc. clean (wash-off) type cosmetics in the case of, can include compared with The compound of the above-mentioned chemical formula 1 of high concentration.If conversely, active ingredient rests on skin for a long time In the case of the cosmetics of maintenance (leave-on) type such as toner, emulsion, creams, elite, can wrap Compound containing the above-mentioned chemical formula 1 less than clean type cosmetics concentration.In a concrete example of the invention In, the content of the compound of above-mentioned chemical formula 1 can be relative to composition total weight in above-mentioned composition 0.0001 weight %~10 weight % (preferably 0.0001 weight %~1 weight %), but not limited to this.This If compound of the composition of invention comprising the above-mentioned chemical formula 1 less than 0.0001 weight %, can not the phase Sufficient dermatoglyph improvement is treated, if comprising more than 10 weight %, it is likely that allergy etc. occur no Wish the reaction that occurs or there is problem on cutaneous safety, thus above range setting be in order to Prevent the generation of problems.
The invention further relates to the food of the health care for improving dermatoglyph of the compound comprising above-mentioned chemical formula 1 Product.
In this specification, " health food " refers to, by the compound of above-mentioned chemical formula 1 be added to beverage, Food in the raw-food material of teas, spices, chewing gum, Biscuits etc., or be manufactured into it is encapsulated, The food of powdered, suspension etc., certain effects are brought when these food are absorbed in health, but with General medicine is different, may occur with food as raw material, thus during with the absence of long-term taking medicine Side effect the advantages of.
The health food of the invention for obtaining by this way in daily middle intake, therefore be able to can be expected Dermatoglyph improvement high, thus it is highly useful.
When the compound of above-mentioned chemical formula 1 is used as into food additives, can be by the change of above-mentioned chemical formula 1 Compound is directly added or is used together with other food or food composition, can be suitable according to conventional methods Use.The combined amount of active ingredient can be according to its application target (prevention, health or metacheirisis) And suitably determine.Generally, when Foods or drinkses are manufactured, below relative to the weight portion of raw material 15, It is preferred that the amount below 10 weight portions adds composition of the invention.However, for the purpose of health and health Or for the purpose of health regulation and in the case of taking in for a long time, above-mentioned amount can for below above range, by In not existing any problem in terms of security, therefore active ingredient can also be with amount more than above range To use.
Species to above-mentioned food is not particularly limited.As the food that can add above-mentioned substance Example has meat, sausage, bread, chocolate, confectionery, snack categories, Biscuits, pizza, side Just face, other noodles, chewing gum class, the dairy products including ice cream, all kinds of soup, beverage, tea, Freshener, alcoholic beverage and compound vitamin etc., the health food on ordinary meaning are then all wrapped Include.
Health beverage composition of the invention ground identical with common beverage can contain various fumet or day Right carbohydrate etc. is used as additional composition.Above-mentioned natural carbohydrate can use glucose, fructose Deng monose, the disaccharides of maltose, sucrose etc., and dextrin, the polysaccharide of cyclodextrin etc., xylitol, The sugar alcohols such as D-sorbite, antierythrite.As sweetener, it is possible to use Talin (Thaumatin), sweet The natural sweetener of leaf chrysanthemum extract etc., or saccharin, Aspartame etc. synthetic sweetener etc..On generally The ratio for stating natural carbohydrate is that about 0.01~0.04g is included per composition 100mL of the invention, excellent Elect about 0.02~0.03g as.
In addition to the foregoing, health food of the invention can contain various nutritional agents, vitamin, electrolysis Matter, flavor enhancement, colouring agent, pectic acid and its salt, alginic acid and its salt, organic acid, protective colloid Thickener, pH adjusting agent, stabilizer, preservative, glycerine, alcohol, the carbonating for soda Agent etc..In addition, health food of the invention can containing for manufacture fruit juice, fruit drink, And the pulp of vegetable beverage.Such composition can be used alone or mix and use.This addition It is 0.01~0.1 typically relative to the weight portion of composition of the invention 100 though the ratio of agent is inessential The scope of weight portion.
The present invention also provides a kind of composition for promoting Stem Cell Activity, and it is included as active ingredient The compound of above-mentioned chemical formula 1.
In the present invention, term " stem cell " can voluntarily to carry out cell division, with can be divided into The cell of the ability of the particular cell types (specific cell type) of extremely various form.To this dry The species of cell is not particularly limited, and in a concrete example, above-mentioned stem cell can be skin progenitor cell. Above-mentioned " skin progenitor cell " is to refer to be divided into composition skin (epidermis, corium and subcutaneous layer of fat) Cell stem cell.Constituting the cell of above-mentioned skin includes being present in the keratinocyte of epidermis (keratinocyte), melanocyte (melanocyte) and be present in corium fibroblast it is (main It is responsible for the biosynthesis of collagen and elastin laminin).
Species to above-mentioned skin progenitor cell is not particularly limited.The skin progenitor cell that is used in the present invention with It is independently available that it comes from where.For example, skin progenitor cell may be from known skin does thin Born of the same parents originate, for example, can be obtained from the basalis of hair follicle or epidermis, can feed as the animal of acquisition target Newborn animal.In a concrete example, mammal can include people, mouse, rat, cavy, rabbit, Monkey, pig, horse, ox, sheep, antelope, dog or cat, but not limited to this.Preferably, mammal can be with It is people.Method for obtaining skin progenitor cell from above-mentioned skin progenitor cell source, is known in this area 's.
In the present invention, " Stem Cell Activity facilitation effect " refer to stem cells hyperplasia facilitation effect and/or Dryness maintains effect.
Skin progenitor cell plays weight for the shape constancy in the health and physiology and biochemistry that maintain skin The effect wanted.Being present in the stem cell of skin can also be subject to aging influence and exception functionally occurs, Thus the shape constancy of skin is broken, and produces various problems.Can be improved by the activity of this stem cell The various phenomenons [non-patent literature 4] of skin aging, to confirming that dermatoglyph improves effect in this present invention Really.
Thus, the present invention can be provided comprising the above-mentioned cosmetics for promoting the composition of Stem Cell Activity Composition.For this State of cosmetics, previously with regards to the cosmetics of the compound comprising chemical formula 1 Content described in the explanation of formulation is identical.
Below, by embodiment to the detailed description of the invention.But, following embodiments are merely exemplary this hair Bright, present disclosure is not limited to following embodiments.
Reference example 1:Rutin (Rutin) material information
Chemical formula 1:
CAS No.:153-18-4
Supplier:Sichuan Hongjie Import&Export CO., LTD
Reference example 2:The culture of the skin progenitor cell under the conditions of serum free medium
Using 48- orifice plates (6 × 103Cells/well it is added with) and hyclone (fetal bovine serum) The CNT-57 culture mediums (Cellntec companies) of similar BPE (Bovine pituitary extract), In 5%CO2With 37 DEG C under the conditions of the application on human skin stem cell bought from Cellntec companies for 24 hours of culture (Human epidermal stem cell).Afterwards, after suction line removes nutrient solution, using PBS Solution (GibcoBRL companies) removes medium component, with the CNT-57 culture mediums not comprising BPE The μ g/mL of compound 20 of chemical formula 1 are processed, in 5%CO2With 37 DEG C under the conditions of cultivated 72 hours.
Experimental example 1:Skin progenitor cell using CCK-8 evaluation assessments breeds facilitation effect
Skin progenitor cell to being cultivated in above-mentioned reference example 2 carries out CCK-8 (Cell counting kit-8) and comments Valency.It is that the dehydrogenase (Dehydrogenase) in intracellular electron transport system is decomposed that CCK-8 is evaluated Tetrazolium salts (Tetrazolium Salt) and generate first(Formazan) absorbance is measured, from And the analysis method of the density of the cell of survival is shown indirectly.
After being processed 2 hours cell with CCK-8 solution (the 1/10 for the treatment of culture volume) at 37 DEG C, Spectroscopy determining is carried out by determining the absorbance under wavelength 450nm.For the compound of chemical formula 1 Skin progenitor cell propagation facilitation effect, (be with the addition of according to the absorbance that will be determined and control group The CNT-57 culture mediums of BPE) following mathematical expressions 1 for being compared, proliferation rate (%) is obtained, by it Value is shown in table 1 below.
Mathematical expression 1:
Proliferation rate (%)=(absorbance of the absorbance/control group of sample pretreating group) × 100
Table 1
The propagation facilitation effect of skin progenitor cell
Addition sample Concentration The cell proliferation rate (%) compared with control group
The compound of chemical formula 1 20μg/mL 144%
Control group - 100%
The culture of the compound treatment with chemical formula of the invention 1 is can be seen that by the result of above-mentioned table 1 Skin progenitor cell under the conditions of base shows excellent propagation facilitation effect.
Experimental example 2:The dryness (stemness) of skin progenitor cell maintains effect to confirm
In order to the dryness for confirming the skin progenitor cell cultivated in above-mentioned reference example 2 maintains effect, p63 is evaluated Expression degree.P63 is as the Intracellular transcription factor and known as the maintenance mark of skin progenitor cell. The RNA of cell is separated and after synthesizing cDNA, implemented with Taqman dyeing liquors in real time-PCR come Determine the expression degree of p63.In this experiment, the concentration of RNA is carried out with S16 rRNAs Standardization.
Above-mentioned experimental result is shown in table 2 below.The numerical value that p63 in table 2 below increases multiple is represented The multiple compared with control group (with the addition of the CNT-57 culture mediums of BPE).
Table 2
Dryness (stemness) maintains effect (repeat number=3)
Addition sample Concentration P63 increases multiple (again)
The compound of chemical formula 1 20μg/mL 1.455
Control group - 1.0
The culture of the compound treatment with chemical formula of the invention 1 is can be seen that from the result of above-mentioned table 2 Base condition promotes the p63 expression of skin progenitor cell, therefore dryness maintains excellent effect.
Embodiment 1:The both effectiveness of (turn-over) improvement is peeled off for cutin
Women with 20 years old to 50 years old of health is object, and following preparation examples 2 are tested as follows Nutrition creams cutin peel off improvement.
To the experiment position of the women 20 of 20 years old to 50 years old, with DHA (Dihydroxyacetone, Sigma Aldrich, USA) 1.5% solution carry out 8 hours closing patch (Closed Patch) make its sink After product, by the nutrition creams of Production Example 2 times a day be coated to experiment position on.After coating 4 days, apply Apply 8 days after and coating 12 days after, using Chromameter CR-400 (Minolta, Japan) Instrument measuring is carried out to the skin color of deposition site and photograph taking is carried out using DSLR.Measured value Evaluated by obtaining 3 average values in addition to maximum and minimum value, the skin of deposition site The colour of skin is adjust and reform kind higher, and it is better that display cutin peels off improvement.
Result is shown in Table 3 below.
Table 3
Skin color improvement
Distinguish After coating 4 days After coating 8 days After coating 12 days
Improvement rate (%) 1.26 4.38 11.82
By above-mentioned table 3 as can be seen that when using the nutrition creams of preparation example of the invention, being obtained in that angle Matter peels off improvement.
Preparation example 1:The manufacture of pharmaceutical preparation
1. the manufacture of tablet
The compound 0.2mg of chemical formula 1
Cornstarch 100mg
Lactose 100mg
Magnesium stearate 2mg
After mixing mentioned component, the manufacture method according to conventional tablet carries out compressing tablet, has manufactured tablet.
Preparation example 2:The manufacture of cosmetics
1. the manufacture of nutrition creams
Constitute as follows, manufactured according to conventional methods as change of the active ingredient comprising chemical formula 1 The nutrition creams of compound.
The weight % of compound 0.2 of chemical formula 1
The weight % of beta-1,3-dextran 5.0
The weight % of beeswax 10.0
The weight % of polysorbate 601.5
The weight % of PEG60 rilanit specials 2.0
The weight % of sorbitan sesquialter isostearate 0.5
The weight % of atoleine 10.0
The weight % of saualane 5.0
The weight % of caprylic/capric triglyceride 5.0
The weight % of glycerine 5.0
The weight % of butanediol 3.0
The weight % of propane diols 3.0
The weight % of triethanolamine 0.2
The weight % of preservative 0.05
The weight % of pigment 0.05
The weight % of spices 0.05
Pure water adds to 100 weight %
Preparation example 3:The manufacture of skin preparations for extenal use
1. the manufacture of ointment
Constitute as follows, manufacture according to conventional methods as chemical combination of the active ingredient comprising chemical formula 1 The ointment of thing.
The weight % of compound 0.5 of chemical formula 1
The weight % of beta-1,3-dextran 10.0
The weight % of beeswax 10.0
The weight % of polysorbate 605.0
The weight % of PEG60 rilanit specials 2.0
The weight % of sorbitan sesquialter isostearate 0.5
The weight % of vaseline 5.0
The weight % of atoleine 10.0
The weight % of saualane 5.0
The weight % of sher butter (Shea Butter) 3.0
The weight % of caprylic/capric triglyceride 5.0
The weight % of glycerine 10.0
The weight % of propane diols 10.2
The weight % of triethanolamine 0.2
The weight % of preservative 0.05
The weight % of pigment 0.05
The weight % of spices 0.05
Pure water adds to 100 weight %

Claims (5)

1. a kind of skin preparations for extenal use for improving dermatoglyph, it is included by followingization as active ingredient The compound that formula 1 is represented,
Chemical formula 1:
2. a kind of cosmetic composition for improving dermatoglyph, it is included by following as active ingredient The compound that chemical formula 1 is represented,
Chemical formula 1:
3. a kind of composition for promoting Stem Cell Activity, it is included by following chemistry as active ingredient The compound that formula 1 is represented,
Chemical formula 1:
4. the composition for promoting Stem Cell Activity according to claim 3, it is characterised in that Above-mentioned Stem Cell Activity is the activity for promoting stem cells hyperplasia or maintaining dryness.
5. a kind of cosmetic composition, its include described in claim 3 for promoting Stem Cell Activity Composition.
CN201510424067.2A 2015-07-17 2015-07-17 Composition for improving skin Pending CN106691880A (en)

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CN106691880A true CN106691880A (en) 2017-05-24

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Country Status (1)

Country Link
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Citations (11)

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EP0648496A1 (en) * 1993-10-15 1995-04-19 Bristol-Myers Squibb Company Therapeutic compositions for use in the treatment of skin lesions and method of making same
JPH0899861A (en) * 1994-09-30 1996-04-16 Kose Corp Skin external agent
JPH0899860A (en) * 1994-09-30 1996-04-16 Kose Corp Skin external agent
JPH0899820A (en) * 1994-09-30 1996-04-16 Kose Corp Skin external agent
JP2000319154A (en) * 1999-05-06 2000-11-21 Nippon Menaade Keshohin Kk Phototoxicity inhibitor
JP2002370922A (en) * 2001-06-15 2002-12-24 Azuma Noen:Kk Cosmetic containing japanese plum extract
US20060018861A1 (en) * 2004-07-23 2006-01-26 Minghua Chen Skin care composition
CN1988881A (en) * 2004-07-23 2007-06-27 宝洁公司 Skin care composition containing a flavonoid and vitamin b3
US7544375B1 (en) * 2006-06-12 2009-06-09 Swiss Skin Repair, Inc. Composition
EP2119434A1 (en) * 2008-05-13 2009-11-18 Institut National De La Sante Et De La Recherche Medicale (Inserm) Use of heterosidic flavonoid derivatives for therapy of stem cell cancers
FR2944794A1 (en) * 2009-04-28 2010-10-29 Rocher Yves Biolog Vegetale Preparing flavonoid glycoside oligomer comprises solubilizing flavonoid glycoside in mixture comprising glycerin, ethanol and aqueous solution to obtain solution having flavonoid and polymerizing solubilized flavonoid glycoside by laccase

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EP0648496A1 (en) * 1993-10-15 1995-04-19 Bristol-Myers Squibb Company Therapeutic compositions for use in the treatment of skin lesions and method of making same
JPH0899861A (en) * 1994-09-30 1996-04-16 Kose Corp Skin external agent
JPH0899860A (en) * 1994-09-30 1996-04-16 Kose Corp Skin external agent
JPH0899820A (en) * 1994-09-30 1996-04-16 Kose Corp Skin external agent
JP2000319154A (en) * 1999-05-06 2000-11-21 Nippon Menaade Keshohin Kk Phototoxicity inhibitor
JP2002370922A (en) * 2001-06-15 2002-12-24 Azuma Noen:Kk Cosmetic containing japanese plum extract
US20060018861A1 (en) * 2004-07-23 2006-01-26 Minghua Chen Skin care composition
CN1988881A (en) * 2004-07-23 2007-06-27 宝洁公司 Skin care composition containing a flavonoid and vitamin b3
US7544375B1 (en) * 2006-06-12 2009-06-09 Swiss Skin Repair, Inc. Composition
EP2119434A1 (en) * 2008-05-13 2009-11-18 Institut National De La Sante Et De La Recherche Medicale (Inserm) Use of heterosidic flavonoid derivatives for therapy of stem cell cancers
FR2944794A1 (en) * 2009-04-28 2010-10-29 Rocher Yves Biolog Vegetale Preparing flavonoid glycoside oligomer comprises solubilizing flavonoid glycoside in mixture comprising glycerin, ethanol and aqueous solution to obtain solution having flavonoid and polymerizing solubilized flavonoid glycoside by laccase

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