JP7246125B2 - Epidermal cell activator - Google Patents

Description

The present invention relates to an epidermal cell activator, an epidermal growth factor production promoter, and an epidermal growth factor receptor production promoter containing one or two selected from purple extract and valerian extract as active ingredients.

Areas exposed to ultraviolet rays, such as the face, back, and hands and feet, progress in aging, and localized pigmentation, so-called "blemishes", is formed. As for the formation mechanism of spots, it is said that spots appear when the balance between the enhancement of melanin production due to stimuli such as ultraviolet rays and aging and the excretion of transferred melanin is disturbed. Therefore, as an approach applied to skin-whitening agents, a method of suppressing the accelerated melanin production and a method of restoring the regressed melanin excretion are conceivable. Many studies have been conducted so far on whitening agents that suppress the former melanin production, but little research has been conducted on whitening agents that restore and promote the latter melanin excretion (Non-Patent Document 1).

In order to prevent such aging symptoms, sesame extract, rhubarb extract, peach extract, licorice extract, Houttuynia cordata extract, and cactus extract are used as ingredients that promote the production of epidermal growth factor (EGF). An extract, a wheat germ extract, a cat's claw extract, a perilla extract, and a loquat extract are known (Patent Document 1).

It is also known that epidermal growth factor exerts its effects only after it is taken up into cells by its receptor (epidermal growth factor receptor, EGFR) (Patent Document 2).

Cosmetic Journal, 24(1): 21-28, 2000)

JP 2008-247783 A JP 2009-155329 A

So far, no studies have been made on ingredients having both epidermal cell growth (EGF) production-promoting action and epidermal growth factor receptor (EGFR) production-promoting action. By combining the EGF production promotion action and the EGFR production promotion action, the turnover of epidermal cells caused by aging etc. is activated, and the anti-aging effect and skin beautifying effect that prevent dullness and skin aging are expressed, and the skin is healthy. An object of the present invention is to provide an epidermal cell activator, an epidermal cell growth factor production promoter, and an epidermal cell growth factor receptor production promoter, which can maintain the

The present invention provides an epidermal cell activator, an epidermal cell growth factor production promoter, and an epidermal cell growth factor receptor production promoter containing one or two selected from purple extract and valerian extract as active ingredients. do.

Murasaki extract and valerian extract exhibit high epidermal cell activating effect, epidermal cell growth factor production promoting effect, and epidermal cell growth factor receptor production promoting effect, and anti-aging and skin beautifying effects to prevent dullness and skin aging. can be expressed and the skin can be kept healthy.

A mode for carrying out the present invention will be described below.

The purple extract used in the present invention uses the root of purple (Lithospermum officinale).

Valeriana fauriei extracts used in the present invention can be the leaves, stems, flowers, roots and other parts of valeriana fauriei and the whole plant, but preferably the roots and rhizomes.

In the present invention, each of the above plant extracts may be used for extraction in its raw state, but in consideration of extraction efficiency, it is preferable to perform extraction after treatment such as chopping, drying, and pulverization. Extraction is performed by immersion in an extraction solvent. Stirring or homogenization in an extraction solvent may be performed to increase extraction efficiency. A suitable extraction temperature is from about 5° C. to a temperature below the boiling point of the extraction solvent. Although the extraction time varies depending on the type of extraction solvent and the extraction temperature, it is suitable to be about 4 hours to 14 days.

Extraction solvents include water, lower alcohols such as methanol, ethanol, propanol and isopropanol, polyhydric alcohols such as 1,3-butylene glycol, propylene glycol, dipropylene glycol and glycerin, and ethers such as ethyl ether and propyl ether. , esters such as ethyl acetate and butyl acetate, and ketones such as acetone and ethyl methyl ketone. Physiological saline, phosphate buffer, phosphate buffered saline, etc. may also be used.

The extract of the above-mentioned plant with the above-mentioned solvent can be contained in the composition according to the present invention as it is. It may be used after purification treatment such as decolorization, deodorization, and desalting, or fractionation treatment by column chromatography, as long as the action is not impaired. For storage, it can also be freeze-dried after purification and dissolved in a solvent before use. It can also be used by encapsulating it in vesicles such as liposomes or microcapsules.

In particular, by encapsulating it in vesicles such as liposomes, microcapsules, or the like, percutaneous absorption is enhanced and higher effects are exhibited.

One or two selected from purple extract and valerian extract have excellent epidermal cell activating effect, epidermal cell growth factor production promoting effect, and epidermal cell growth factor receptor production promoting effect. , epidermal growth factor production promoter, and epidermal growth factor receptor production promoter.

The epidermal cell activator, epidermal cell growth factor production promoter, and epidermal cell growth factor receptor production promoter characterized by containing one or two selected from purple extract and valerian extract can be used alone It can be used as an epidermal cell activator, an epidermal cell growth factor production promoter, and an epidermal cell growth factor receptor production promoter in various compositions such as pharmaceuticals, quasi-drugs, food and drink, and cosmetics. As a result, a composition having an epidermal cell activating action, an epidermal cell growth factor production promoting action, and an epidermal cell growth factor receptor production promoting action can be obtained.

An epidermal cell activator, an epidermal cell growth factor production promoter, and an epidermal cell growth factor receptor production promoter characterized by containing one or two selected from purple extract and valerian extract, and the presence or absence of other ingredients, etc., are not limited at all. Regarding the form, any form such as liquid, paste, gel, solid, powder, etc. can be selected according to the application, etc., and the vehicle (excipient), solvent, Other common additives (antioxidants, colorants, dispersants, etc.) can optionally be included.

A composition containing an epidermal cell activator, an epidermal cell growth factor production promoter, and an epidermal cell growth factor receptor production promoter, characterized by containing one or two selected from purple extract and valerian extract. The product can take any dosage form. When the composition is a skin cosmetic, hair cosmetic, cleanser or the like, it can be provided as a solubilized system such as lotion, a dispersed system such as calamine lotion, or an emulsified system such as cream or milky lotion. Furthermore, it can be provided in various dosage forms such as an aerosol form filled with a propellant, an ointment, and a poultice.

Specifically, various cosmetics such as emulsions, creams, lotions, lotions, packs, serums, cleansers, and make-up cosmetics; Various forms of cosmetics, quasi-drugs, topical drugs, and the like can be exemplified.

In the case of oral pharmaceuticals, general dosage forms such as liquids such as drinks and infusions, solids such as gums and candies, capsules, powders, granules, and tablets can be used.

A composition containing one or two selected from a purple extract and a valerian extract characterized by containing one or two selected from a purple extract and a valerian extract, these In addition, depending on the application and need, optional ingredients that are usually blended in pharmaceuticals, quasi-drugs, skin cosmetics, hair cosmetics, cleansers, and oral pharmaceuticals, such as water, oily ingredients, Humectants, powders, pigments, emulsifiers, solubilizers, gelling agents, detergents, UV absorbers, anti-inflammatory agents, thickeners, pH adjusters, chelating agents, drugs (medicinal ingredients), fragrances, resins, Antibacterial and antifungal agents, antioxidants, alcohols and the like can be appropriately added. Furthermore, other moisturizing agents, anti-aging agents, whitening agents, antioxidants, slimming agents, various plants/fungi, or extracts thereof can be used in combination, as long as the effects of the present invention are not impaired.

The amount of one or two selected from purple extract and valerian extract in various compositions can be adjusted depending on the type and purpose of the composition, but from the viewpoint of effect and stability. , preferably 0.0001 to 10.0% by mass, more preferably 0.001 to 5.0% by mass, still more preferably 0.01 to 5.0% by mass, based on the total amount.

EXAMPLES The present invention will be specifically described below with reference to examples, but the scope of the present invention is not limited by these examples.

[Purple extract 1]
After drying, the roots of purple (Lithospermum officinale) were cut into small pieces, immersed in a 20-fold mass ethanol/BG mixture (9:1), the filtrate was collected, the solvent was distilled off, and purple extract 1 was obtained. bottom.

[Murasaki extract 2]
Murasaki extract 1 was dissolved in a glycerin/ethanol mixed solution (25:75) to a concentration of 1% by mass, aged, and filtered again to obtain Murasaki extract 2.

[Valeriana extract 1]
After drying, the roots and rhizomes of valerian were finely chopped, immersed in 20 times the mass of purified water, the filtrate was collected, and the solvent was distilled off to obtain valerian extract 1.

[Valeriana extract 2]
Valerian extract 1 was dissolved in a 20% by mass 1,3-butylene glycol aqueous solution, aged, and filtered again to obtain valerian extract 2.

[Epidermal keratinocyte activating action]
Normal human epidermal keratinocytes manufactured by Kurabo Co., Ltd. (Kurashiki Boseki Co., Ltd.) were seeded in a 96-well microplate at 2.0×10 ⁴ per well. Commercially available Humedia KG2 (manufactured by Kurabo Industries) was used as a seeding medium. After culturing for 24 hours, the cells were replaced with Humedia KG2 to which the sample (extract) was added at each concentration, and cultured for another 24 hours. After removing the supernatant, the medium was replaced with a medium containing 100 μg/mL of 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide (MTT) and cultured for about 1 hour. Thereafter, formazan produced by opening the tetrazolium ring was extracted with 2-propanol, and the absorbance at 550 nm was measured using a microplate reader. At the same time, the absorbance at 650 nm was measured as turbidity, and the difference between the two measured values was used to evaluate the cell activation action. Humedia KG2 was used as a control in addition to the medium containing the sample in the evaluation. The results are shown in Tables 1 and 2.

As shown in Tables 1 and 2, purple extract 1 and valerian extract 1 were found to have an activation effect on epidermal keratinocytes in a concentration-dependent manner.

[Epidermal Growth Factor Production Promoting Action, Epidermal Growth Factor Receptor Production Promoting Action]
Human epidermal keratinocytes were seeded in a 6-well plate at 5×10 ⁵ cells/well and cultured overnight in Humedia KG2 medium. The medium in which the plant extract was dissolved was replaced and cultured for 24 hours in a 37°C, 5% CO2 incubator. Total RNA was extracted from the cells using Trizol reagent and prepared according to the Life Technologies protocol. After cDNA synthesis, gene expression was confirmed by real-time PCR by the Cybergreen method using the following primers. GAPDH was used as an internal standard. Table 4 shows the results.

As shown in Table 4, purple extract 1 and valerian extract 1 exhibited high epidermal growth factor production-promoting action and epidermal growth factor receptor production-promoting action.

[Example 1] Emulsion (1) Squalane 10.0 (mass%)
(2) Methylphenylpolysiloxane 4.0
(3) Hydrogenated palm kernel oil 0.5
(4) Hydrogenated soybean phospholipid 0.1
(5) Polyoxyethylene monostearate
Sorbitan (20 E.O.) 1.3
(6) Sorbitan monostearate 1.0
(7) Glycerin 4.0
(8) Methyl paraoxybenzoate 0.1
(9) carboxyvinyl polymer 0.15
(10) Remainder of purified water 100 (11) Arginine (1% by mass aqueous solution) 20.0
(12) Murasaki extract 2 1.0
Production method: The oil phase components (1) to (6) are heated and dissolved at 80°C. On the other hand, the water phase components (7) to (10) are heated and dissolved at 80°C. The oil phase components are added to this while stirring, and uniformly emulsified with a homogenizer. After cooling, at 40° C., (11) and (12) are sequentially added and uniformly mixed.

[Example 2] Lotion (1) Ethanol 15.0 (mass%)
(2) Polyoxyethylene (40E.O.) hydrogenated castor oil 0.3
(3) Perfume 0.1
(4) Remainder of purified water 100 (5) Citric acid 0.02
(6) sodium citrate 0.1
(7) Glycerin 1.0
(8) hydroxyethyl cellulose 0.1
(9) valerian extract 2 1.0
Preparation method: (2) and (3) are dissolved in (1). Further, after sequentially adding (4) to (8), the mixture is sufficiently stirred, and (9) is added and mixed uniformly.

[Example 3] Cream (1) Squalane 10.0 (% by mass)
(2) stearic acid 2.0
(3) Hydrogenated palm kernel oil 0.5
(4) Hydrogenated soybean phospholipid 0.1
(5) Cetanol 3.6
(6) Lipophilic glyceryl monostearate 2.0
(7) Glycerin 10.0
(8) Methyl paraoxybenzoate 0.1
(9) Arginine (20% by mass aqueous solution) 15.0
(10) Remainder of purified water 100 (11) Carboxyvinyl polymer (1% by mass aqueous solution) 15.0
(12) Murasaki extract 2 0.5
Production method: The oil phase components (1) to (6) are heated and dissolved at 80°C. On the other hand, the water phase components (7) to (10) are heated and dissolved at 80°C. The oil phase components are added to this while stirring, and uniformly emulsified with a homogenizer. After (11) is added and stirred, the mixture is cooled, and (12) is added at 40° C. and mixed uniformly.

[Example 4] Essence (1) Remainder of purified water 100 (% by mass)
(2) Glycerin 10.0
(3) Sucrose fatty acid ester 1.3
(4) Carboxyvinyl polymer (1% by mass aqueous solution) 17.5
(5) Sodium alginate (1% by mass aqueous solution) 15.0
(6) Polyglyceryl monolaurate 1.0
(7) macadamia nut oil fatty acid phytosteryl 3.0
(8) N-lauroyl-L-glutamic acid di(phytosteryl-2-octyldodecyl) 2.0
(9) Hydrogenated palm oil 2.0
(10) Squalane (derived from olive) 1.0
(11) behenyl alcohol 0.75
(12) Beeswax 1.0
(13) Jojoba oil 1.0
(14) 1,3-butylene glycol 10.0
(15) L-arginine (10 wt% aqueous solution) 2.0
(16) valerian extract 2 0.3
Production method: The water phase components (1) to (6) are mixed and dissolved by heating at 75°C. On the other hand, the oil phase components (7) to (14) are mixed and dissolved by heating at 75°C. Next, the oil phase component is added to the water phase component and pre-emulsified, followed by uniform emulsification with a homomixer. After cooling, add (15) at 50°C and add (16) at 40°C, and mix uniformly.

[Example 5] Aqueous gel (1) Carboxyvinyl polymer 0.5 (mass%)
(2) Remaining purified water 100 (3) Sodium hydroxide (10% by mass aqueous solution) 0.5
(4) Glycerin 10.0
(5) 1,3-butylene glycol 10.0
(6) Ethanol 10.0
(7) methyl paraoxybenzoate 0.1
(8) Perfume 0.1
(9) Murasaki extract 2 0.3
(10) valerian extract 2 0.3
(11) Polyoxyethylene (60E.O.) hydrogenated castor oil 1.0
Production method: Add (1) to (2), stir uniformly, and then add (3). After uniformly stirring, (5) dissolved in advance in (4) is added. After uniformly stirring, (6) to (11) mixed in advance are added and uniformly stirred and mixed.

Claims (2)

An epidermal cell growth factor production promoter containing one or two selected from purple extract and valerian extract as active ingredients (excluding cosmetics containing both kinetin and lichen extract). An epidermal growth factor receptor production-enhancing agent containing, as active ingredients, one or two selected from purple extract and valerian extract (excluding cosmetics containing both kinetin and lichen extract).