JP2002029980A - Estrogenic agent and collagen production rpomoter, fibroblast proliferative agent, food for cosmetological use and skin cosmetic - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a new medicinal agent alternative to conventional moisturizers, serving as an agent capable of effectively preventing the aging of the skin and maintaining both the firmness and glossiness of the skin. SOLUTION: This new medicinal agent, an estrogenic agent, collagen production promoter or fibroblast proliferative agent, is obtained by subjecting the embryos (embyo buds) in the seeds of Nelumbo nucifera Gaertn. belonging to Nymphaea family to extraction with a hydrophilic organic solvent such as methanol, ethanol, 1,3-butylene glycol or glycerol, water or a water-based solvent such as a mixture thereof. The other objective foods for cosmetological use including candies, soft/refreshing drinks and tablets, or skin cosmetics including cream, milky lotions, lotions and pack are obtained by using the above estrogenic agent, collagen production promoter or fibroblast proliferative agent.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an estrogen-like agent, a collagen production promoter, a fibroblast proliferation agent,
The present invention relates to cosmetic foods and skin cosmetics. Specifically, a novel estrogen-like agent that has the same action as estrogen, a female hormone, a collagen production promoter that promotes the production of collagen that constitutes the skin, and activates fibroblasts in human skin The present invention relates to a fibroblast growth-promoting agent to be converted into a cosmetic, a cosmetic food and a skin cosmetic using the agent.

[0002]

2. Description of the Related Art One of the causes of skin aging associated with aging is a decrease in secretion of estrogen, a kind of female hormone. Therefore, a substance having the same action as estrogen is transdermally or orally administered to post-menopausal women in which estrogen secretion declines.
Conventionally, steroidal estrogens, non-steroidal estrogens, flavone compounds and the like have been used as estrogen-like agents for this purpose.

[0003] Here, the epidermis and dermis of the skin are composed of epidermal cells, fibroblasts, and extracellular matrices such as collagen outside these cells and supporting the skin structure.

[0004] In young skin, fibroblasts are actively proliferating, and the interaction of skin constituent tissues such as fibroblasts and collagen maintains homeostasis, thereby securing water retention, flexibility, elasticity, and the like. In addition, the skin is maintained in a fresh and crisp appearance.

However, under the influence of certain external factors, such as irradiation with ultraviolet rays, remarkable drying of air, and excessive skin washing, or as aging progresses, the proliferation of fibroblasts slows down, and collagen Production is also reduced. As a result, the skin loses its moisturizing function and elasticity, the keratin begins to peel off abnormally, and the skin loses its tone and luster, becomes rough, and exhibits aging symptoms such as wrinkles.

[0006] The most commonly used method for preventing and improving such skin aging is the natural moisturizing factor (NM).
F) is a moisturizing substance such as mucopolysaccharides such as sugar, amino acid, organic acid, pyrrolidone carboxylate, collagen, hyaluronic acid, glycerin, 1,3-butylene glycol, etc. to improve skin moisturizing property. It is to raise. However, humectants cannot be expected to improve the keratin condition of the epidermis. In addition, since it slows evaporation of water from the skin, the feeling of use is generally poor and long-term use may even cause skin damage.

Therefore, conventional moisturizers are insufficient to effectively prevent aging of the skin and prevent loss of firmness and luster, and have an effect of activating fibroblasts and promoting the production of collagen and the like. It is preferred to use an agent having

On the other hand, lotus has been eaten or used as a Chinese medicine since ancient times, and its safety has been established. For example, Japanese Patent Application Laid-Open No. 62-51606 discloses that this lotus is used to extract hot flashes after tanning, razor shade and rough skin, and is extracted from waterlily plants using a solvent such as water or a lower alcohol. The disclosed extract is disclosed. Further, as an example using a lotus seed germ, JP-A-63-66126 discloses that an extract extracted using water or a water-miscible organic solvent has a blood pressure lowering effect. Japanese Patent Application Laid-Open No. 64-90129 discloses that an extract similarly extracted from lotus germ using a solvent such as water or lower alcohol is used for circulatory diseases such as hypertension and respiratory diseases such as bronchial asthma. It is disclosed as having an effect on central nervous diseases such as insomnia.

However, only the above-mentioned effects and effects are known for the germ of the lotus (seed), and the anti-aging effect of the skin and the like are not known.

[0010]

SUMMARY OF THE INVENTION Accordingly, the present inventors have sought to find a new agent that can be used as a conventional moisturizer to effectively prevent skin aging and maintain firmness and luster. As a result of diligent efforts, the inventors have found that the extract of lotus germ has an estrogen action, a collagen production promoting action, and a fibroblast proliferation action, and completed the present invention.

[0011]

Means for Solving the Problems The estrogen-like agent, the collagen production promoter and the fibroblast proliferation agent according to the present invention are each characterized by comprising a lotus germ extract. In the present invention, an embryo (germ) in the seed of a lotus (Nelumbo nucifera Gaertn.) Belonging to the genus Lotus of the convulsive family is used. Embryos are usually green and rod-shaped, and are preferably used after being taken out of the collected seeds and immediately dried.

[0012] The lotus germ extract is prepared by converting the germ into water, various aliphatic lower alcohols such as methanol, ethanol and isopropanol; hydrophilic organic solvents such as 1,3-butylene glycol, ethylene glycol and glycerin; It is obtained by extraction using various aqueous solvents such as a mixture of solvents and a mixture of these hydrophilic organic solvents and water.

In the extraction, the obtained embryo can be used as it is, but it is preferable to use it after pulverization in order to increase the extraction efficiency. In addition, if the non-aqueous solvent (non-polar solvent) such as hexane is used in advance to perform a degreasing treatment, the content of impurities is reduced, and an extract with higher effect can be obtained.

[0014] The extraction can be carried out at room temperature or under heating using an arbitrary apparatus depending on the extraction solvent. For example, crushed lotus germ is put into a treatment tank filled with an extraction solvent, and a soluble component is eluted with occasional stirring. Thereafter, the residue is removed by filtration to obtain an extract. The amount of the solvent used at this time is preferably used so that the weight ratio is generally 1: 5 to 1:20 with respect to the lotus germ.

The extract (liquid) thus obtained can be used as it is as an estrogen-like agent, as a collagen production promoter, or as a fibroblast growth-promoting agent. It can also be provided as a concentrated extract or a dried product from which the extraction solvent and the like have been distilled off.

Since the extract of lotus germ has a peculiar smell and taste, it is preferable to purify the extract for the purpose of deodorizing and decoloring to the extent that physiological activity is not reduced. Of course, depending on the purpose of use, for example, when it is contained in the cosmetic food or skin cosmetic according to the present invention, since it is not used in large quantities, it can be practically used as it is.

Further, the estrogenic agent, collagen production promoter and fibroblast proliferation agent of the present invention include:
If necessary, the extract may be made to use various sugars such as sucrose and lactose, excipients such as protein and starch, and other optional auxiliaries in order to facilitate storage and handling thereof. . In addition, it can be provided in the form of an appropriate formulation, and can be provided as an arbitrary dosage form such as a powder, a granule, and a tablet.

These estrogen-like agents, collagen production promoters, and fibroblast proliferation agents can be orally added to any food or as a cosmetic food such as a dietary supplement containing them as a main component. It can be used in a practical way. Foods that can be added include, for example, various soft drinks and juice drinks, Japanese and Western confections, dairy products and other livestock processed products, fruit processed products, vegetable processed products, processed cereal products, processed marine products, seasonings, vitamins Many foods and drinks such as so-called various health foods mainly composed of such as foods. Also, as a dietary supplement, for example, it can be provided in the form of a liquid preparation or in the form of a tablet.
In this case, the addition rate varies depending on the form of the extract such as liquid or solid in consideration of the general intake of the cosmetic food to be added. It is suitable to add about 1 to 1000 mg in terms of amount, which is about 4 to 1200 mg in terms of dry material of lotus germ as a raw material.

In order to exhibit the action of the lotus germ extract most effectively, it must be mixed with various skin cosmetics. Suitable skin cosmetics to be blended are, for example, ointments, creams, emulsions, lotions, packs, bath preparations and the like. In this case, the blending amount is about 0.01 to 10% by weight as a lotus germ extract, It is appropriate to add so as to be about 0.04 to 40% in terms of dry lotus germ.

The cosmetic foods and skin cosmetics according to the present invention include these cosmetic foods and skin cosmetics as long as any of these estrogenic effects, collagen production promoting effects and fibroblast proliferation effects are not hindered. It goes without saying that various raw materials usually used for the production of cosmetics can be used.

[0021]

EXAMPLES Next, examples of the present invention, estrogen-like agents, collagen production promoters and fibroblast proliferation agents, and cosmetic preparations and skin cosmetics as preparation examples of the present invention will be described. The invention will be described in detail.

(Example 1) 300 g of a crude lotus germ was put into each of 2000 ml of extraction solvents shown in Table 1, and extracted at 70 ° C for 3 hours with gentle stirring. Thereafter, the filtrate obtained by filtration is concentrated at 40 ° C. under reduced pressure, and further dried by a reduced-pressure drier to obtain a powdery lotus germ extract, estrogen-like agent, collagen production promoting agent, fibroblast. A cell growth agent was obtained. The yield is shown in Table 1.

[0023]

[Table 1]

Example 2 300 g of crushed lotus germ
Was poured into 2000 ml of a mixture of 1,3-butylene glycol and water (volume ratio 1: 1), and extracted at 80 ° C. for 3 hours with stirring. Thereafter, the mixture was filtered to obtain 1440 ml of an estrogen-like agent, a collagen production promoting agent, and a fibroblast proliferation agent, which are liquid lotus germ extracts.
This had a solid content of 4.0% by weight. The solid content concentration was determined by taking a small amount of the extract and evaporating it to dryness (the same applies hereinafter).

Example 3 1540 ml of a liquid lotus germ extract was obtained in the same manner as in Example 2 except that a mixed solution of glycerin and water (volume ratio 1: 1) was used as an extraction solvent. This had a solid content of 3.5% by weight.

Example 4 1540 ml of a liquid lotus germ extract was obtained in the same manner as in Example 2 except that 2,000 ml of a mixed solution of propylene glycol and water (volume ratio 1: 1) was used as the extraction solvent. . Its solids concentration is 3.3
% By weight.

Next, using the various estrogen-like agents, collagen production promoting agents and fibroblast proliferation agents obtained in Examples 1 to 4, the skin cosmetics and cosmetic foods according to the present invention were used. Were prepared in various ways. (Formulation Example 1) [Emulsion 100 ml] Lotus germ ethanol / water mixture (1: 1) extract 1.0 g Stearyl glycyrrhetinate 0.2 g Cetyl alcohol 0.5 g Magnesium ascorbate 3.0 g Beeswax 2.0 g Polyoxyethylene sorbitan oleate (10E.O.) 1.0 g Glyceryl monostearate 1.0 g Hyaluronic acid 0.1 g Propylene glycol 5.0 g Ogon extract 1.0 g Pea seed extract 1.0 g Ethanol 3.0 g Paraoxy Methyl benzoate 0.3 g Fragrance 0.03 g Remaining amount of purified water The above component amounts were taken to prepare an emulsion, which is a skin cosmetic according to the present invention, according to a conventional method.

(Formulation Example 2) [Emulsion 100 ml] Lotus germ ethanol extract 0.1 g Lotus germ 1,3-butylene glycol / water mixture (1: 1) extract 1.0 g Jojoba oil 4.0 g olive oil 2 1.0 g Squalane 2.0 g Cetanol 2.0 g Tocopherol acetate 0.2 g Glyceryl monostearate 2.0 g Polyoxyethylene cetyl ether (20 EO) 2.5 g Polyoxyethylene sorbitan oleate (20 EO) 0 g 1,3-butylene glycol 3.0 g methyl paraoxybenzoate 0.15 g birch bark extract 0.5 g oil-soluble licorice extract 0.05 g cinnabar extract 0.5 g flavoring 0.05 g purified water balance Then, an emulsion, which is a skin cosmetic according to the present invention, was prepared according to a conventional method.

(Formulation Example 3) [In 100 ml of lotion] Lotus germ water extract 0.2 g Lotus germ 1,3-butylene glycol / water mixture (1: 1) extract 2.0 g glycerin 3.0 g 1,3 -Butylene glycol 3.0 g polyoxyethylene sorbitan oleate (20E.O.) 0.5 g methyl paraoxybenzoate 0.15 g citric acid 0.1 g sodium citrate 0.1 g dipotassium glycyrrhizinate 0.3 g lindane extract 0.0 5 g Loquat extract 0.5 g Yeast extract 0.3 g Hyaluronic acid aqueous solution (solid content 1%) 3.0 g Fragrance 0.05 g Purified water Remaining amount The amount of the above components is taken, and is a skin cosmetic according to the present invention according to a conventional method. A lotion was prepared.

(Formulation Example 4) [In 100 g of cream] Lotus germ ethanol extract 0.1 g Lotus germ 1,3-butylene glycol / water mixture (1: 1) extract 1.0 g Carrot extract 0.2 g Extract 0.5 g Tormentilla extract 0.5 g Hydrolyzed conchiolin 0.1 g Liquid paraffin 5.0 g Wheat ceramide 0.1 g Salami beeswax 4.0 g Cetanol 3.0 g Squalane 10.0 g Lanolin 2.0 g Stearic acid 1.0 g Oleic acid Polyoxyethylene sorbitan (20E.O.) 1.5 g Glyceryl monostearate 3.0 g 1,3-butylene glycol 6.0 g Methyl parahydroxybenzoate 1.5 g Perfume 0.1 g Residual water According to a conventional method, a W / O type cream, which is a skin cosmetic according to the present invention, is prepared. It was.

(Formulation Example 5) [In 100 g of pack] Lotus germ 1,3-butylene glycol / water mixture (1: 1) extract 5.0 g Polyvinyl alcohol 15.0 g Placenta extract 1.0 g Ascorbic acid 0.02 g Pueraria Extract 0.2 g Potato trifoliatum extract 1.0 g Polyethylene glycol 3.0 g Propylene glycol 7.0 g Ethanol 10.0 g Methyl parahydroxybenzoate 0.05 g Perfume 0.05 g Residual water A pack as the skin cosmetic according to was prepared.

(Formulation Example 6) [Tablet-shaped cosmetic food] Lotus germ Ethanol / water mixture (1: 1) extract 100 (parts by weight) Collagen 30 Mucopolysaccharide / protein (chondroitin) 10 Hyaluronic acid Products 33 Black rice extract (including polyphenols) 33 Licorice extract (including glycyrrhizin) 10 Milk protein hydrolyzate (including amino acids and low molecular weight peptides) 10 Vitamin B group mixed powder (including all vitamin B groups) 4 Vitamin C 10 Powdered sugar (sucrose) 47 Glycerin fatty acid ester 12 The above component amounts were taken, and a tablet-shaped health and nutritional supplement, which is a cosmetic food according to the present invention, was produced according to a conventional method.

(Formulation Example 7) [Granular cosmetic food] Lotus germ water extract 200 (parts by weight) Pearl protein hydrolyzate (including various amino acids and peptides) 15 Silk protein hydrolyzate 15 Soy isoflavone 10 Purple rice Extract (including polyphenols) 100 Red wine extract powder (including procyanidin) 30 Yeast extract (including glutathione, nucleic acids, amino acids, and vitamins) 10 Pomegranate seed extract 10 Wheat germ extract (including vitamins, chromium, selenium, and molybdenum) 10) DNA 30 Beet oligosaccharide 1060 Stevia extract 10 The above component amounts were taken, and a granular health and nutritional supplement, which is a cosmetic food according to the present invention, was produced according to a conventional method.

(Formulation Example 8) [Capsule-shaped cosmetic food] Lotus germ Ethanol / water mixture (1: 1) extract 50 (parts by weight) Ceramide 30 Phospholipid (lecithin) 10 Vitamin E (tocopherol) 17 Multicarotene ( α and β carotene, lutein, lycopene 10 Red rice extract (including cycloartenol ester) 33 Octacosanol 1 Plant sterol 5 Perilla oil (including α-linolenic acid) 20 Refined fish oil (including DHA, EPA) REFERENCE SIGNS LIST 20 Sesame oil (including lignan compound) 20 Olive oil 10 Soybean and rapeseed mixed oil 62 Glycerin fatty acid ester 12 Take the above component amounts, gelatin capsule according to a conventional method, and obtain capsule-shaped health and beauty food according to the present invention.
Dietary supplements were manufactured.

(Preparation Example 9) [100 parts by weight of soft drink water-based cosmetic food] Lotus germ water extract 1 (parts by weight) Royal jelly 3 Water-soluble collagen 8 Barley extract 1 Ginseng extract (including saponin) 1 Placenta Extract 1 Pueraria extract (including flavonoids) 1 Purple yam extract 1 Oligosaccharide 5 Sucrose 10 Prune juice 2 Pomegranate juice 5 Grapefruit juice 10 Vitamin C 1 Grapefruit flavor 0.7 Water residue Take the above component amounts, stir and dissolve A soft drink-like health / dietary supplement, which is a cosmetic food according to the present invention, was produced.

(Preparation Example 10) [Candy-like beauty food] Lotus germ Ethanol / water mixture (1: 1) extract 2 (parts by weight) Mizuna 30 Licorice extract 3 Tengcha extract 1 Blueberry extract (including anthocyan) 1 Green tea Extract (including plant polyphenols) 3 Strawberry 1/5 concentrated juice 1 Red cabbage pigment 0.05 Lemon juice 0.5 Water 5 Take the above component amounts and take a candy-like health that is a cosmetic food according to the present invention according to a conventional method. -Made dietary supplements.

(Effect test) [Estrogen-like action] The method of Thomas et al. (In Vitr) for examining the effect of various Lotus germ extracts obtained in Examples 1 to 4 on the growth of estrogen-dependent cells was examined.
o Cell. Dev. Biol. 28A, 595-602, 199
According to 2), the estrogenic effect was examined. Table 2 shows the results. The control value using water was 10
Shown as 0.

[0038]

[Table 2]

[Collagen production promoting action]
Each of the extracts obtained in (1) to (4) was analyzed by the method of Webster et al. (Anal.
Biochem., Vol 96, 220, 1979), the amount of collagen produced by fibroblasts cultured in a medium to which each extract was added was measured. On the other hand, the radioactivity produced in the medium to which each extract was not added was measured, and this collagen amount was reduced to 1
The collagen production ratio when the value was set to 00 was determined. Specific test methods are shown below, and the results are shown in Table 3. Test method: Human fibroblasts were seeded on a plate and
After culturing in two types of sample-added media (sample concentration: 200 ppm and 50 ppm) for several days at 5 ° C. and 5% carbon dioxide, β-aminopropionitrile and [ ³ H] -proline were added, and further 24 hours Cultured. A pepsin / acetic acid solution was added to the whole culture solution and digested at 4 ° C. for 16 hours.
Next, a carrier was added to the digested solution, precipitated with 0.7 M saline, and redissolved under neutral conditions.
Reprecipitated with 2M saline. 20 v /
After washing with v% ethanol, the radioactivity of the precipitate was measured.

[0040]

[Table 3]

[Proliferation of fibroblasts] The above Examples 1-4
The various lotus germ extracts obtained in
According to the T method (J. Immunol. Medhods. 93, 157, 1986), the fibroblast proliferation activity was measured using human normal neonatal skin fibroblasts (NBIRGB). Table 4 shows the results.
Shown in The control value using water is shown as 100.

[0042]

[Table 4] (Evaluation results) As shown in Tables 2 to 4, the lotus germ extracts using various water-based solvents such as water, ethanol, a mixed solution of isopropanol and water, and a mixed solution of 1,3-butylene glycol and water are excellent respectively. An estrogenic effect, a collagen production promoting effect and a fibroblast proliferation effect were observed.

[Effect of Improving Skin Roughness] Next, the following evaluation test was performed on the emulsion shown in Formulation Example 1 above. As a comparative example, an emulsion containing no lotus germ extract was prepared and used.・ Subject: From a large number of healthy women aged 22 to 43 years,
According to the following evaluation criteria, 20 persons judged to have rough skin corresponding to the score 1 or 2 were selected as subjects. Application test: Each subject was asked to apply an appropriate amount of the emulsion shown in Formulation Example 1 on the right half of the face and the emulsion of the comparative example once on the left half for 30 days in the morning and evening.・ Evaluation: After application test, Sylflo (Flexicl Developm
A replica of the face was taken using a replica method manufactured by ents Ltd., and the skin crest state and exfoliation state were observed with an optical microscope at a magnification of 50 times, and the skin state was determined according to the following evaluation criteria. Table 5 shows the results of the determination.

Judgment Criteria Score 1: Skin crevices and crusts have disappeared, and a wide range of keratin has been turned over.
(Rough skin condition) 2: Skin grooves / skins are unclear. The keratin is partially turned up. (Rough skin condition) 3: Skin grooves / skins are recognized but flat. (Normal skin) 4: Skin grooves and skin ridges are clear. (Relatively beautiful skin) 5: The skin sulcus / skin is extremely clear and tidy. (Beautiful skin)

[0045]

[Table 5]

As shown in Table 5, it can be seen that in the area where the emulsion of the present invention was applied, the skin roughness was remarkably improved as compared with the case where the emulsion of the comparative example was applied.

[0047]

Industrial Applicability According to the present invention, a novel estrogen-like agent having high safety and an action similar to estrogen, a collagen production promoter for promoting the production of collagen constituting skin, and a human skin An agent for promoting fibroblast proliferation that activates fibroblasts can be provided. By applying these to cosmetic foods and skin cosmetics, aging of the skin can be effectively prevented, and it can greatly contribute to maintaining tension and luster.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI theme coat ゛ (reference) A61P 43/00 105 A61P 43/00 105 111 111 111 F term (reference) 4B018 MD61 ME10 ME14 4C083 AA032 AA082 AA111 AA112 AA122 AB052 AC012 AC022 AC072 AC102 AC122 AC182 AC242 AC392 AC402 AC482 AD042 AD332 AD532 AD642 AD662 CC02 CC05 DD31 EE12 4C088 AB39 AC04 CA03 ZA91 ZB21 ZC03 ZC11

Claims (5)

[Claims] 1. An estrogen-like agent comprising a lotus germ extract. 2. A collagen production promoter comprising a lotus germ extract. 3. A fibroblast growth-promoting agent comprising a lotus germ extract. 4. A cosmetic composition comprising the estrogen-like agent according to claim 1 and / or the collagen production promoter according to claim 2 and / or the fibroblast proliferation agent according to claim 3. Food. 5. A skin cosmetic comprising the estrogen-like agent according to claim 1 and / or the collagen production promoter according to claim 2 and / or the fibroblast proliferation agent according to claim 3. Fees.