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WO2014178681A1 - Composition topique pour la peau contenant du ginsenoside y - Google Patents

Composition topique pour la peau contenant du ginsenoside y Download PDF

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Publication number
WO2014178681A1
WO2014178681A1 PCT/KR2014/003953 KR2014003953W WO2014178681A1 WO 2014178681 A1 WO2014178681 A1 WO 2014178681A1 KR 2014003953 W KR2014003953 W KR 2014003953W WO 2014178681 A1 WO2014178681 A1 WO 2014178681A1
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WO
WIPO (PCT)
Prior art keywords
composition
skin
ginsenoside
external
effect
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/KR2014/003953
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English (en)
Korean (ko)
Inventor
김동현
류권렬
이옥찬
염명훈
조준철
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Amorepacific Corp
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Amorepacific Corp
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Priority to HK16105231.0A priority Critical patent/HK1217286B/zh
Priority to CN201480025030.6A priority patent/CN105163742B/zh
Publication of WO2014178681A1 publication Critical patent/WO2014178681A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60—Sugars; Derivatives thereof
    • A61K8/602—Glycosides, e.g. rutin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/02—Local antiseptics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/08—Anti-ageing preparations
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00—Preparations for affecting hair growth
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/06—Preparations for care of the skin for countering cellulitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00—Preparations for care of the hair

Definitions

  • the present invention relates to an external composition for skin containing ginsenoside Y, and more particularly, by containing ginsenoside Y, having excellent antioxidant power, improving skin moisturizing effect, anti-inflammatory effect, acne and atopy. Improvement of scalp and hair condition such as anti-dandruff effect, hair growth effect and white hair prevention effect as well as overall skin condition improvement effect such as skin trouble improvement effect, whitening effect, sebum control effect, pore contraction effect, improvement of complexion through blood circulation improvement It relates to a composition capable of providing an effect.
  • Human skin is the body's primary protective barrier, which protects the body's organs from changes in temperature and humidity, and from external environmental stimuli such as ultraviolet rays and pollutants. Undergo a change. That is, internally, the secretion of various hormones that regulate metabolism decreases, and the function of immune cells and the activity of cells decreases, thereby reducing the biosynthesis of immune proteins and constituent proteins necessary for living organisms.
  • free radicals and free radicals increase, thereby reducing the thickness of the skin, increasing wrinkles, reducing elasticity, Skin color becomes dull, skin problems frequently occur, blemishes, freckles and blotch also increase, the color becomes worse and the skin tone becomes darker.
  • the skin condition is improved by adding bioactive substances obtained from various known animals, plants, and microorganisms to cosmetics.
  • Efforts have been made, and research and development of cosmetics using ginseng (Panax ginseng C. A Meyer) in particular has been conducted.
  • Ginseng has been widely used in cosmetic compositions since its efficacy in the skin has been proven early, and ginseng root or leaf extract, ginseng saponin (ginsenoside), ginseng aglycon and ginseng polysaccharides have been used.
  • the cosmetics containing such ginseng extract, extract, polysaccharides, etc. contain a very small amount of the active substance has a disadvantage that the effect is not significantly superior to other raw materials.
  • the inventors of the present invention can provide the ginsenoside Y contained in ginseng to improve the whitening, moisturizing effect, as well as to improve acne and skin troubles, atopic symptoms, such as the effect of improving skin color, sebum control, pore contraction effect, etc.
  • the present invention has been found to be able to provide a skin condition improving effect, and also to provide a scalp and hair condition improving effect such as anti-dandruff, hair growth and white hair prevention.
  • an object of the present invention to provide an external preparation composition for skin containing ginsenosides Y which can improve the overall condition of the skin.
  • the present invention provides an external composition for skin containing ginsenoside Y as an active ingredient.
  • the present invention also provides a whitening skin external composition comprising ginsenoside Y as an active ingredient.
  • the present invention also provides a moisturizing skin external composition comprising ginsenoside Y as an active ingredient.
  • the present invention provides a topical composition for improving acne containing ginsenoside Y as an active ingredient.
  • the present invention also provides a topical skin external composition for improving atopy containing ginsenoside Y as an active ingredient.
  • the present invention also provides a skin external preparation composition for improving color and skin tone containing ginsenoside Y as an active ingredient.
  • the present invention also provides a skin external preparation composition for reducing pores containing ginsenoside Y as an active ingredient.
  • the present invention also provides a skin external composition for controlling sebum containing ginsenoside Y as an active ingredient.
  • the present invention also provides a topical anti-dandruff composition containing ginsenoside Y as an active ingredient.
  • the present invention also provides a composition for external application for hair growth comprising ginsenoside Y as an active ingredient.
  • the present invention also provides a topical composition for preventing white hair, comprising ginsenoside Y as an active ingredient.
  • the present invention also provides an external composition for skin using ginsenoside Y as a natural preservative.
  • composition of the present invention has an excellent antioxidant power by containing ginsenoside Y, while improving skin moisturizing effect, anti-inflammatory effect, skin trouble improvement effect such as acne and atopy, whitening effect, sebum control effect, pore contraction effect, blood circulation improvement
  • skin moisturizing effect such as acne and atopy
  • skin trouble improvement effect such as acne and atopy
  • whitening effect such as acne and atopy
  • sebum control effect skin trouble improvement effect
  • pore contraction effect such as acne and atopy
  • blood circulation improvement In addition to improving the overall skin condition, such as improving the complexion through it can provide a scalp and hair condition improvement effect such as anti-dandruff effect, hair growth effect and white hair prevention effect.
  • the external preparation composition for skin according to the present invention contains ginsenoside Y as an active ingredient, and in particular, the ginsenoside Y may be extracted from ginseng.
  • Ginsenoside Y used in the present invention has a structure represented by the following Chemical Formula 1.
  • Ginseng belongs to the genus Ginseng of Araliace and is a herbaceous plant as a perennial ring-negative root. It is produced in many parts of the world, including Korea, China, Japan, and the United States, and is mainly cultivated at 85-140 degrees east, 22-49 degrees north latitude, 70-97 degrees west latitude, and 34-47 degrees north latitude in North America. As described above, ginseng produced in different parts of the world is different in its composition, and ginseng saponin, which is the most important ginsenoside, is used in Korean ginseng to represent various physiological and pharmacological effects of ginseng.
  • ginsenosides About 34 kinds have been isolated so far, and the pharmacological efficacy differs depending on the type of sugars bound to the aglycone, the number of the sugars bound thereto, or the binding sites thereof. According to the structural characteristics, it is divided into diols, triols and oleanes. In addition, it contains panacen, a polyacetylene compound, a polyphenol compound, flavonoids and vitamins, which are inherent fragrance components of ginseng.
  • Ginseng has long been recognized for its efficacy and has been used for the treatment of various diseases.
  • the herbal efficacy of ginseng is known to improve stamina, improve metabolism, relieve stress, treat diabetes, improve respiratory diseases, improve digestive system, and anti-cancer activity.
  • ginseng has anti-complement activity, anti-ulcer activity, immune boosting effect, It has been reported to have anticancer action and hypoglycemic action.
  • Skin-related effects include anti-inflammatory activity (Korean J. Dermatol. 18 (1): 39-42 (1980), Korean J. Dermatol. 14 (4): 335-339 (1976)), prevention of hyperkeratosis (Korean J. Dermatol. Dermatol.
  • Ginsenoside Y of the present invention may be extracted from plants, synthesized according to methods known in the art, and may be commercially available.
  • derivatives obtained by the addition or substitution reaction of the substituents commonly performed in the art with ginsenoside Y derivatives showing skin, hair improvement effect and antiseptic effect are included in the scope of the present invention. It is clear to those skilled in the art in consideration of this.
  • Ginsenoside Y used in the present invention can be obtained especially from ginseng extract.
  • the type of ginseng used at this time is not particularly limited, and ginseng, red ginseng, white ginseng, taeguksam, misam and the like can be used.
  • the ginseng extract is contained not only in the leachate obtained by leaching and transferring from ginseng, but also in the concentrate obtained by partially or fully concentrating the leachate, or in stagnation, whole, regular, liquid extract and ginseng prepared by drying the concentrate again.
  • the chemicals that exert the main effect include all of the plant itself, and extracts from all parts of ginseng, such as stems, roots, leaves, flowers, fruits, can be used and are not limited to extracts of any particular part.
  • a method for extracting ginsenoside Y from ginseng extract may use a known method.
  • the ginsenoside Y may be separated from the ginseng extract by preparing a ginseng extract with water or an organic solvent by a method well known in the art.
  • the organic solvent used in the present invention may be selected from the group consisting of ethanol, methanol, butanol, ether, ethyl acetate, chloroform and a mixed solvent of these organic solvents and water, and preferably 80% ethanol is used.
  • the extraction temperature is preferably 10 ⁇ 80 °C, it can be extracted for 3 to 24 hours. If the extraction temperature and extraction time is out of the extraction efficiency may decrease or change of components may occur.
  • the composition according to the present invention may contain ginsenoside Y in an amount of 0.001 to 50% by weight, preferably 0.01 to 30% by weight, more preferably 0.1 to 10% by weight, based on the total weight of the composition. If the content of ginsenoside Y is less than 0.001% by weight, the efficacy and effect by the above components are insignificant. If the content of the ginsenoside Y exceeds 50% by weight, there is a problem in skin safety or formulation.
  • composition of the present invention containing ginsenoside Y provides excellent antioxidant power to the skin.
  • composition of the present invention can be used as a composition for whitening, which can provide an excellent whitening effect by inhibiting tyrosinase activity and inhibiting melanin production.
  • the composition of the present invention can be used as a moisturizing skin external preparation composition, which can enhance skin barrier function and induce differentiation of skin keratinocytes. Therefore, it can be usefully used as an external composition for skin to prevent or improve skin dryness, atopic dermatitis, contact dermatitis, or psoriasis caused by incomplete epidermal differentiation.
  • composition of the present invention can be used as an external preparation composition for improving acne, which is excellent in antibacterial effect, in particular, antibacterial effect against acne causing bacteria, and also provides an anti-inflammatory effect.
  • composition of the present invention can be used as an external skin composition for improving color and skin tone, and when applied to the skin, it smoothly supplies nutrients to the skin by promoting capillaries and promotes blood circulation and inhibits skin aging to improve color and skin tone. The effect is excellent.
  • the composition of the present invention can be used as a skin external preparation composition for pore reduction, sebum control and skin trouble improvement, which suppresses excessive secretion of sebum when applied to the skin, and reduces pores by promoting free radical removal and collagen synthesis.
  • the effect of suppressing skin problems is excellent by reducing the expression of inflammatory factors.
  • composition of the present invention can be used as an anti-dandruff skin external composition, which effectively discharges toxins accumulated in the hair and scalp to cleanse the scalp, inhibit the growth and growth of dandruff bacteria, and prevent the scalp inflammatory reaction, and also active It has an excellent antioxidant effect that inhibits the production and action of oxygen, so it can provide the effect of calming and strengthening the scalp and strengthening its natural defense.
  • composition of the present invention can be used as a skin external preparation composition for hair growth, which can promote the growth of hair and prevent hair loss by promoting the transition from the resting hair cycle to the growing hair cycle.
  • composition of the present invention can be used as a topical anti-skin composition for white hair, which can significantly increase the expression of MITF in melanocytes, inhibit white hair and promote the induction of black hair.
  • ginsenoside Y used in the external preparation composition for skin of the present invention can provide an effect as a natural preservative.
  • the external preparation composition for skin of the present invention described above may be formulated as a cosmetic composition, and may be formulated containing a cosmetically or dermatologically acceptable medium or base.
  • a cosmetically or dermatologically acceptable medium or base for example emulsions, suspensions, microemulsions, microcapsules, microgranules or ionic (liposomes) and non-obtained by dispersing an oil phase in solution, gels, solids, pasty anhydrous products, aqueous phases.
  • It may be provided in the form of an ionic vesicle dispersant or in the form of a cream, skin, lotion, powder, ointment, spray or cone stick. It may also be used in the form of a foam or in the form of an aerosol composition further containing a compressed propellant.
  • These compositions can be prepared according to conventional methods in the art.
  • topical skin composition of the present invention when used for the prevention of dandruff, hair growth or white hair, it may be formulated as a composition for scalp and hair, and the formulation is not particularly limited, for example, hair tonic, hair nourishing cosmetics, scalp It can be formulated as a treatment, hair treatment, hair shampoo, hair rinse, hair lotion or scalp hair combination treatment and the like.
  • the composition according to the present invention is a fatty substance, an organic solvent, a dissolving agent, a thickening agent, a gelling agent, a softening agent, an antioxidant, a suspending agent, a stabilizer, a foaming agent, a fragrance, a surfactant, water, an ionic or nonionic.
  • a fatty substance an organic solvent, a dissolving agent, a thickening agent, a gelling agent, a softening agent, an antioxidant, a suspending agent, a stabilizer, a foaming agent, a fragrance, a surfactant, water, an ionic or nonionic.
  • adjuvants conventionally used in the
  • composition of the present invention may contain a skin absorption promoting substance to increase the skin improving effect.
  • test examples and formulation examples are provided only for the purpose of illustration to help the understanding of the present invention is not limited to the scope and scope of the present invention by the following examples.
  • Ginsenoside Y for testing the efficacy of the composition of the present invention was purchased from Ambo laboratory.
  • the keratinocytes (keratinocyte) isolated from the skin tissue of the person into a 5 ⁇ 10 4 are in each well of a 24-well plate was attached for 24 hours. After 16 hours, ginsenoside Y was treated with 1%. At this time, the control group was not treated with ginsenoside Y for comparison. After 2 hours, the culture solution was removed, and 100 ⁇ l of phosphate buffered saline (PBS) was added to each well. The keratinocytes were irradiated with UV 30mJ / cm 2 using an ultraviolet B (UVB) lamp (Model: K5T8, UV B 15 W, Sankyo Dennki, Japan), and then PBS was removed and each cell was treated with keratinocyte culture solution 200.
  • UVB ultraviolet B
  • ginsenoside Y according to the present invention effectively inhibits the production of ROS known to cause skin cell damage by ultraviolet rays, and ROS to a level above that when the amount of ROS after ultraviolet stimulation is not irradiated with ultraviolet rays. It can be seen that the antioxidant effect is very excellent by inhibiting the production of. Therefore, it was confirmed that ginsenoside Y according to the present invention can prevent pores from widening by inhibiting oxidation and preventing aging, and can improve skin trouble by defending the generation of skin irritation.
  • Tyrosinase enzyme was extracted from the mushroom (Mushroom) was used as the Sigma (SIGMA). First, the substrate tyrosine was dissolved in distilled water to make a solution of 0.3 mg / ml, and the solution was added to the test tube by 1.0 ml. Then, 1.0 ml of potassium-phosphate buffer solution (0.1 mol concentration, pH 6.8) and 0.7 ml of distilled water were added thereto. Added.
  • 0.2 ml of the sample solution prepared by mixing ginsenoside Y of the present invention in an appropriate concentration in an ethanol solution was added to the reaction solution and then reacted for 10 minutes in a 37 ° C thermostat.
  • the control group was prepared by adding only 0.2 ml of solvent instead of each sample solution, and ascorbic acid was used as a positive control group.
  • 0.1 ml of a tyrosinase solution of 2500 units / ml was added to the reaction solution and reacted for 10 minutes in a 37 ° C thermostat.
  • the test tube containing the reaction solution was placed in iced water and quenched to stop the reaction, and the absorbance at 475 nm was measured with a photospectrometer. The results are shown in Table 2 below.
  • Each tyrosinase inhibitory effect was calculated by the following equation.
  • Nutritional cream was prepared in a conventional manner according to the composition of Table 4 (unit: wt%).
  • Formulation Example 1 In order to measure the effect of ginsenoside Y on increasing skin moisturizing power, Formulation Example 1 and Comparative Formulation Example 1 were used, and evaluated as follows.
  • the amount of CE (Cornified Envelop) generated during the differentiation of keratinocytes was measured using absorbance.
  • the keratinocytes of the primary cultured humans isolated from the epidermis of the newborn were put in a culture flask and adhered to the bottom. After treatment with ginsenoside Y at 5 ppm concentration in the culture medium, the cells were approximately 70-80% of the floor area. Incubate for 5 days until growth. At this time, the low calcium (0.03mM) treated group and the high calcium (1.2mM) treated group were used as negative and positive controls, respectively.
  • the cultured cells were harvested and washed with PBS (Phosphate buffered saline), and then 10 mM Tris-HCl buffer containing 2% SDS (sodium dodecyl sulfate) and 20 mM DTT (Dithiothreitol). pH 7.4) 1 ml was added to sonication, boiling and centrifugation, and the precipitate was suspended in 1 ml of PBS again to measure absorbance at 340 nm. Separately, a portion of the solution after the sonication was taken to measure the protein content and used as a reference when evaluating the degree of cell differentiation. The results are shown in Table 6 below.
  • LDPI Laser Doppler Perfusion Imager
  • the cosmetic composition according to the present invention significantly increased the skin blood flow than Comparative Formulation Example 1 containing no ginsenoside Y, it was confirmed that the blood color is improved through the blood circulation. . This ultimately suggests that the cosmetic composition containing ginsenoside Y according to the present invention can contribute effectively to the skin's nutrient delivery, inhibit skin aging and delay.
  • Comparative Formulation Example 1 which does not contain ginsenoside Y according to the present invention, does not show a significant skin tone improvement effect, whereas Formulation Example 1 containing ginsenoside Y as an active ingredient is used. It was confirmed that the skin tone after use is much improved than before use.
  • Ginsenoside Y according to the present invention was measured by comparing collagen biosynthesis promoting effect with TGF- ⁇ .
  • fibroblasts were seeded by 10 5 per hole in 24 wells and cultured to about 90% growth. This was incubated in serum-free DMEM medium for 24 hours, and then treated with 10 ng / ml of ginsenoside Y and TGF- ⁇ of the present invention dissolved in serum-free medium, and incubated in a CO 2 incubator for 24 hours. These supernatants were removed and procollagen increased or decreased using procollagen type I ELISA kit (procollagen type (I)). The results are shown in Table 11 below, and the synthetic ability of collagen was compared with the non-treated group as 100.
  • ginsenoside Y according to the present invention was confirmed to exhibit a higher level of collagen synthesis than the positive control group TGF- ⁇ . Therefore, it was confirmed that ginsenoside Y according to the present invention can reduce the enlarged pores by increasing the amount of collagen production around the pores.
  • Comparative Formulation Example 1 does not have a pore reduction effect, but in the case of Formulation Example 1 shows a pore reduction effect that can be visually confirmed, ginsenoside Y according to the present invention reduces the size of the pores It was found that the effect was excellent.
  • HEK293 cells were transfected with p3 ⁇ FLAG-CMV-5 ⁇ R2 and cultured in a 24 well plate at 2.5 ⁇ 10 5 cells per well (Park et al., 2003, JDS. Vol. 31, pp. 191-98). The next day, a new medium with enzyme substrate and inhibitor was added. 0.05 ⁇ Ci [ 14 C] testosterone (Amersham Pharmacia biotech, UK) was used as the substrate of the medium.
  • ginsenoside Y was added and incubated for 2 hours at 37 ° C. in a 5% CO 2 incubator. In this case, the ginsenoside Y was not used as the negative control group, and the finasteride was used as the positive control group. Thereafter, the culture medium was collected, the steroid was extracted with 800 ⁇ l ethyl acetate, the organic solvent layer was separated, dried, and the remaining residue was dissolved in 50 ⁇ l ethyl acetate.
  • the silica plastic sheet kieselgel 60 F254 was developed using ethyl acetate-hexane (1: 1) as a solvent.
  • 5 ⁇ -reductase which converts testosterone to dihydrotestosterone, binds to a receptor protein in the cytoplasm, enters the nucleus, activates sebaceous gland cells, promotes differentiation, and hypersecretes sebum in sebaceous glands.
  • ginsenoside Y effectively inhibits the conversion of testosterone to dihydrotestosterone, and has a superior inhibitory effect than finasteride, which is known to inhibit the activity of 5 ⁇ -reductase.
  • finasteride which is known to inhibit the activity of 5 ⁇ -reductase.
  • ginsenoside Y can suppress sebum hypersecretion by effectively inhibiting the activity of 5 ⁇ -reductase.
  • Formulation Example 3 and Comparative Formulation Examples 3 to 4 were prepared according to the ingredients and the contents (% by weight) shown in Table 15 below. Specifically, Formulation Example 3 is a formulation of ginsenoside Y, Comparative Formulation Example 3 does not contain any active ingredients for improving acne skin, Comparative Formulation Example 4 is a standard to be used as a reference for antimicrobial activity As an anti-acne treatment, it contains erythromycin.
  • the preparation method of Formulation Example 3 and Comparative Formulation Examples 3-4 is as follows.
  • the components of phase A in Table 15 were completely dissolved and the components of phase B were completely dissolved in a separate dissolution bath, followed by mixing solubilization by adding phase B to phase A.
  • the ingredients of phase C were added thereto according to the blending ratios described in Table 15 to homogenize the mixing and then filtered to prepare the compositions.
  • Antibacterial activity was tested against propionibacterium acnes (ATCC 6919: Medium-BHI broth), which is an acne-causing strain, with each cosmetic composition prepared in the formulation of Formulation Example 3 and Comparative Formulation Examples 3-4. .
  • the antibacterial test method for acne bacteria was as follows.
  • Propionibacterium acnes was used as a culture broth inoculated in BHI broth and anaerobic culture.
  • test bacteria 0.15 ml of the test bacteria was added to 15 ml of BHI broth (pH 6.8) or LB broth (pH 4.5) and mixed well as a dilution solution.
  • the antimicrobial activity test results for acne bacteria are shown in Table 16 below. MIC is expressed in terms of the concentration of the active ingredient contained in the formulation.
  • 3T3-L1 cells a mouse fibroblast cell line
  • DMEM Dulbecco's modified eagle's medium, GIBCO BRL, Life Technologes
  • FBS fetal bovine serum
  • the well culture plate was attached at 1 ⁇ 10 5 cells / well. After 2 days, it was again exchanged with fresh DMEM (containing 10% FBS) medium and incubated for 2 days. The cultured cells were then induced to differentiate into DMEM (containing 10% FBS) containing 1 ⁇ g / ml insulin, 0.5 mM IBMX and 0.25 ⁇ M dexamethasone, and ginsenoside Y and caffeine. After 2 days of treatment 50 ⁇ M was exchanged for DMEM containing insulin and incubated for 5 days. After 5 days, the cells were exchanged with normal medium (DMEM, containing 10% FBS) and cultured while observing until the cells changed to fat cells.
  • DMEM normal medium
  • the ginsenoside Y used in the present invention not only has a small amount of fat accumulated in adipocytes, but also has a superior lipid synthesis inhibitory effect than caffeine, a known lipid synthesis inhibitor. have. Therefore, sebum is reduced by inhibiting lipid synthesis, thereby suppressing the occurrence of acne.
  • Formulation Example 3 did not recur acne compared to Comparative Formulation Example 3, it can be seen that there is an excellent effect on the overall acne improvement.
  • Comparative Formulation Example 4 containing an antimicrobial activity standard shows an acne improvement effect, but in use, the skin irritation seems to be unsuitable for long-term use due to the strong skin irritation, the composition according to the present invention does not have a stimulus for long-term use Even appeared to be appropriate.
  • normal human skin keratinocytes (NHEK, obtained from Lonza) were dispensed in 96-well plates at 5x10 4 cells / well, and then in a 37 ° C, 5% CO 2 incubator. Incubated for 24 hours. After 24 hours, the cells were washed twice with PBS and changed to serum-free keratinocyte basement media (KBM). Each well was treated with ginsenoside Y by the concentrations shown in Table 19 for 30 minutes, followed by PGSA (10 ⁇ g / ml), PGSA (50 ⁇ g / ml), and PGSA (50 ⁇ g / ml) + LPS (1). [Mu] g / ml) was treated respectively.
  • PGSA peptidoglycan from S. aureus
  • Staphylococcus aureus a peptidoglycan extracted from Staphylococcus aureus
  • a major component of the Gram-positive (+) cell wall and bacterial membrane components are known to cause inflammation
  • staphylococci about 90% of patients with atopic dermatitis have been reported to cause secondary infection.
  • Lypopolysaccaride (LPS) is a major component of the cell membrane of Gram-negative bacteria and is known to be a major cause of inflammation.
  • the topical skin composition of the present invention can provide an excellent anti-inflammatory effect by significantly reducing the secretion of IL-8 increased by PGSA and LPS.
  • the keratinocytes (Cell name: HaCaT obtained from ATCC) were dispensed into 96 well plates at 4x10 4 cells / well, followed by incubation for 24 hours in a 37 ° C, 5% CO 2 incubator. It was. After 24 hours, wash the 96 well plate twice with Hanks'Balanced Salt solution (HBSS) buffer, and then add reaction buffer (2 ⁇ M Fluo-4-AM, 20% pluronic acid, 2.5 mM probenecid) to the cells. gave. After reaction at 37 ° C., 5% CO 2 incubator for 30 minutes, and at room temperature for 30 minutes, the cells were washed twice with HBSS buffer and treated with ginsenoside Y at a concentration (%) as shown in Table 20 below.
  • HBSS Hanks'Balanced Salt solution
  • Inhibition rate (%) of calcium ions in the cellular influx compared to the difference between the minimum value and the maximum value when treated with 2 U / ml trypsin or 5 ⁇ M PAR-2 active peptide (SLIGKV) is shown in Table 20 below.
  • the external preparation composition for skin containing ginsenoside Y of the present invention can provide an excellent antipruritic effect by effectively inhibiting PAR-2 activity causing itching.
  • a shampoo in the composition of Table 21 To prepare a shampoo in the composition of Table 21. Specifically, the surfactant and ethylene glycol distearate are added to purified water, heated to 80 ° C., uniformly dissolved, and then slowly cooled to 40 ° C. under stirring, and the active ingredient and preservative according to the present invention are added to the mixture. A viscosity modifier, a perfume, and a hair conditioner were added and mixed, followed by cooling to room temperature under stirring.
  • the keratin proteins that make up hair are produced in hair root keratinocytes, which are differentiated from dermal papilla cells.
  • a rat immortalized dermal papilla cell (DP6) cell line was used in the present invention (Wendy Filsell, Journal of Cell Science 107, 1761-1772 (1994)).
  • This dermal papilla cell line was cultured by microdissection from the hair roots of male PVG rat whiskers and cultured with DMEM (Dulbecco's modified Eagle's medium, Gibco BRL, Gaithersburg, MD, USA) was incubated for 24 hours in an incubator maintained at 5% CO 2 , 37 °C.
  • DP6 was placed in a 96 well plate and incubated in a 37 ° C. incubator for 24 hours and then treated with ginsenoside Y at concentrations of 5 ppm, 10 ppm and 20 ppm, respectively. After 24 hours of drug treatment, cell proliferation was measured using the WST-1 kit (Roche). The results are shown in Table 24 below.
  • Hair loss treatment of minoxidil is known as mitochondrial potential potassium ion channel openers (K ATP channel opener), a representative drug used in the treatment of androgenetic alopecia.
  • K ATP channel opener mitochondrial potential potassium ion channel openers
  • To evaluate the mechanism of minoxidil the treatment of toltamide (SIGMA AlDRICH, T0891), which blocks the K ATP channel in fibroblasts constituting the dermis of the scalp, inhibits cell proliferation, and then opens potassium ion channels to allow cell proliferation. A recovering test method was used.
  • a mouse embryonic fibroblast cell line (NIH3T3) cell line was used.
  • the cell line is a cell line in which the fibroblast cell line isolated from NIH Swiss mouse embryo was naturally immortalized by 3T3 protocol.
  • the cell line was incubated in DMEM (Gibco BRL, Gaithersburg, MD, USA) containing 10% FBS for 24 hours in an incubator maintained at 5% CO 2 , 37 °C.
  • NIH3T3 was placed in a 96-well plate and incubated in a 37 ° C.
  • Table 26 sample Melanin Synthesis (%) DMSO (0.1%) 100 IBMX (100 ⁇ M) 120 Ginsenoside Y (10 ppm) 108 Ginsenoside Y (50 ppm) 118
  • ginsenoside Y promotes melanin synthesis of melanocytes, thereby increasing melanin production, showing an excellent melanin production promoting effect.
  • Y was treated with 10 ppm, and the protein was obtained after incubating at 37 ° C. for 24 hours, 48 hours and 72 hours.
  • the protein thus obtained was subjected to western blot using MITF and tyrosinase antibody. Protein extraction and Western blot were usually performed by standard methods used by those skilled in the art. After Western blot the results are shown in Table 27 below by comparing the negative control to 100.
  • ginsenoside Y increases the expression of MITF and tyrosinase protein in melanocytes.
  • Antimicrobial experiments were conducted to evaluate the antimicrobial activity of ginsenoside Y.
  • the specific experimental method is as follows.
  • Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa strains used in the experiment were tested on Tryptic Soy Broth.
  • Candida albicans and Aspergillus niger strains were cultured in Sabouraud Dextrose Broth. Incubate 1/100 (Candida albicans) in each medium The strain was diluted 1/10) was used as the test bacteria.
  • Aspergillus niger used a spore suspension prepared to be 2 ⁇ 10 8 cfu / ml as the test cell solution.
  • test bacteria 0.15 ml of the test bacteria was added to 15 ml of each medium, and a well mixed solution was used as a diluting solution.
  • 16 ⁇ l of the sample was added to the first row of a 96 well plate, and 184 ⁇ l of the diluted solution was added thereto. The remaining wells were added with 100 ⁇ l of dilution solution. After mixing well the mixture of the first row, 100 ⁇ l was taken in the second row, mixed well, and then diluted 100 times by taking 100 ⁇ l again in the third row.
  • Staphylococcus aureus Escherichia coli, Pseudomonas aeruginosa, in a 32 C thermostat, Candida albicans, Aspergillus niger niger) was incubated in a 25 °C thermostat.
  • ginsenoside Y exhibits antibacterial activity against various strains, through which it can be predicted that ginsenoside Y can act as a natural preservative, or antimicrobial agent in the composition.

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Abstract

La présente invention concerne une composition contenant du ginsenoside Y, et plus spécifiquement, une composition contenant du ginsenoside présentant un meilleur effet antioxydant pour produire des effets tels qu'une meilleure hydratation, un effet anti-inflammatoire, une amélioration des problèmes de la peau tels que l'acné et les symptômes de la dermatite atopique, en plus de fournir des effets d'amélioration générale de la peau, tels que le blanchiment de la peau, la régulation du sébum, le raffermissement des pores et l'amélioration du teint de la peau due à l'amélioration de la circulation, ainsi que des effets d'amélioration des cheveux et du cuir chevelu tels que des effets anti-pelliculaires, la favorisation de la croissance des cheveux et la prévention des cheveux gris.
PCT/KR2014/003953 2013-05-03 2014-05-02 Composition topique pour la peau contenant du ginsenoside y Ceased WO2014178681A1 (fr)

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CN109010112B (zh) 2021-06-04
CN105163742A (zh) 2015-12-16
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TW201521738A (zh) 2015-06-16
KR20140131026A (ko) 2014-11-12

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