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Wrinkle reduction agent, lipolysis accelerator, composition for external use on skin, and food or beverage composition

a technology of lipolysis accelerator and composition, applied in the field of anti-wrinkle agent, can solve the problems of reducing affecting the effect of anti-aging, and aesthetically undesirable, and achieve the effect of increasing or reinforcing the effect of the

Inactive Publication Date: 2009-06-11
KAO CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0036]In the case of formulating a compound represented by the aforementioned general formula (1), and an extract obtained from guinea ginger, and particularly from the seeds thereof, and / or an acylation treatment product of said extract into an external composition for skin and food and beverage composition as a lipolysis promoter, although unable to be uniformly defined as a result of varying according to the preparation form, the formulated amount in terms of paradol is preferably, for example, 0.001 to 10.0% by mass (hereinafter simply abbreviated as %), particularly preferably 0.01 to 8.0%, more preferably 0.05 to 5% and most preferably 0.1 to 3% based on the total weight of said composition. If the formulated amount is less than 0.001% by mass, the effects of the invention may not be demonstrated, while if the formulated amount exceeds 10% by weight, pungency increases which may result in impairment of sensory characteristics and likeability. In addition, the amount consumed by an adult of the food and beverage composition is 20 to 1000 mg, and preferably 100 to 200 mg, in terms of paradol.
[0037]In addition, other components having obesity inhibitory or preventive action such as raspberry ketone, zingerone, 4-(3′,4′-dihydroxyphenyl)-2-butanone or synephrine may be suitably combined and formulated into an external composition for skin or food and beverage composition used as a lipolysis promoter of the present invention for the purpose of increasing or reinforcing the effects thereof.
[0038]In addition, stimulants of β-adrenalin action such as butopamine and isoproterenol, inhibitors of α2-adrenalin action such as yohimbine and ergotoxin, xanthin derivatives such as theophylline and caffeine, or bipyridine derivatives such as milrinone and aminone can also be formulated into an external composition for skin or food and beverage composition used as a lipolysis promoter of the present invention.
[0039]Moreover, various other ordinarily used components can also be formulated as necessary into an external composition for skin or food and beverage composition of the present invention within a range that does not impair the effects thereof. Examples of components that can be formulated into an external composition for skin include components ordinarily formulated into external compositions such as oils, pigments, fragrances, surfactants, moisture retainers, ultraviolet absorbers, anti-inflammatory agents, bacteriocides, dyes, preservatives, and antioxidants, while examples of components that can be formulated into food and beverage compositions include components such as vehicles, binders, thickeners, emulsifiers, colorants, fragrances, food additives, and flavorings.
[0040]An external composition for skin of the present invention corresponds to not only a skin cosmetic, but also a pharmaceutical or bath additive. Although there are no particular limitations on the form, in the case of an external composition for skin, examples of forms include skin toners (lotions), skin creams, bathing creams and washing creams, milky lotions, gels, packs, sticks, sheets, adhesive skin patches, powders, liquids and granules. In the case of a food and beverage composition, examples of forms include tablets, hard candies, pills, sugar-coated tablets, powders, granules, leaves, tea bags, hard capsules, soft capsules, chewing gum, chocolate, candies, jellied candies, beverages, soups, ice cream, noodles and bakery products.EXAMPLES
[0041]The following provides a detailed explanation of the present invention based on Examples and Comparative examples thereof, but the present invention is not limited to these examples. Furthermore, unless specifically indicated otherwise, “%” in Examples refers to “% by mass”.Production

Problems solved by technology

As aging of the skin progresses, the skin's defensive abilities against stimulation by oxidative stress and so forth diminish, and this causes a disturbance of the conditions inside the skin, which in turn further accelerates aging.
This progressive change in the skin is referred to as photo-aging, and in skin suffering from photo-aging, collagen, which is a constituting component that accounts for the majority of the dermis, decreases, thereby resulting in an aesthetically undesirable state such as deep, large wrinkles in the surface of the skin.
Although retinoic acid is used as a prescription drug in the US as a substance having ameliorative effects on wrinkles formed as a result of the progression of photo-aging, since it has problems in terms of safety to the occurrence of significant adverse side effects, it has not been approved for use in Japan.
Thus, there has previously not been a substance for use as an antiwrinkle agent capable of demonstrating sufficiently satisfactory effects while also being safe to use.
In addition, many conventional antiwrinkle agents are chemically synthesized, and have numerous problems in terms of safety.
On the other hand, with respect to naturally-occurring substances which have few problems in terms of safety, there are hardly any such substances known which can be used as antiwrinkle agents other than vitamins, and what is more, none of them have been obtained which adequately demonstrate ameliorative effects.
Moreover, most of natural antiwrinkle agents such as retinol significantly lack photostability, and even if such antiwrinkle agents are effective, nearly all are difficult to formulate into preparations since they are rapidly decomposed in the preparations.
What is called obesity, in which body fat has accumulated in excess, is not only aesthetically undesirable, but also causes various diseases such as arteriosclerosis, thus making it undesirable in terms of health as well.
Recently, there has been an increase in the incidence of obesity caused by such factors as overeating, lack of exercise and stress, and the reduction of body fat or prevention of accumulation thereof is becoming an important issue.
However, since capsaicins exhibit potent stimulation, they have had the problems of limitations on their applications and amounts used.
However, since raspberry ketone and zingerone have distinctive aroma, they were not necessarily satisfactory with respect to formulated amount and universality.
Although Guinea ginger is used as a food seasoning or flavoring, studies have not been conducted on antiwrinkle agents or external compositions for skin using an extract thereof.

Method used

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  • Wrinkle reduction agent, lipolysis accelerator, composition for external use on skin, and food or beverage composition
  • Wrinkle reduction agent, lipolysis accelerator, composition for external use on skin, and food or beverage composition
  • Wrinkle reduction agent, lipolysis accelerator, composition for external use on skin, and food or beverage composition

Examples

Experimental program
Comparison scheme
Effect test

production example 1

Production of Guinea Ginger Extract

[0042]After crushing 2 g of dried guinea ginger (Aframomum melegueta) seeds with a mixer, the crushed seeds were extracted by immersing in 20 ml of acetone for 24 hours. The resulting extract was concentrated and dried under reduced pressure to obtain 0.1 g of an extract from guinea ginger seeds. This extract is referred to as “guinea ginger extract”. According to the results of HPLC analysis, this guinea ginger extract contained 55% paradol.

production example 2

Production of Paradol

[0043]After crushing 100 g of dried guinea ginger (Aframomum melegueta) seeds with a mixer, the crushed seeds were immersed in 2 liters of hexane for 24 hours. The resulting extract was concentrated and dried under reduced pressure to obtain 2.0 g of extract. This extract was fractionated by silica gel chromatography (hexane / ethyl:acetate (9:1)) using Silica Gel 60N (100 to 210 μm, Kanto Chemical) to obtain about 500 mg of purified paradol.

(Identification of Paradol)

[0044]The purified paradol was confirmed by GC-MS and 13C-NMR (100 MHz, CDCl3). Those results are shown below.

[0045]Molecular ion peak (M+) (m / z: 278) was detected by GC-MS (see FIG. 1). The following signals were detected by 13C-NMR [δ(ppm): 14.0, 22.5, 23.7, 29.1, 29.4, 31.2, 43.0, 44.5, 55.7, 111.1, 114.3, 120.6, 133.0, 143.8, 146.4, 210.7] (see FIG. 2).

production example 3

Production of Acetylated Guinea Ginger Extract

[0046]1.0 g of the guinea ginger extract obtained in Production Example 1, 1.0 ml of pyridine and 30 ml of acetic anhydride were mixed and stirred at room temperature for 24 hours. Then, after water was added thereto, the mixture was extracted with ethyl acetate to obtain 1.2 g of acetylation treatment extract. This treated product was referred to as “acetylated guinea ginger extract”.

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Abstract

An antiwrinkle agent, lipolysis promoter, external composition for skin, and food and beverage composition having for an active ingredient thereof a compound represented by general formula (1):(wherein R represents a hydrogen atom or an acyl group having 2 to 20 carbon atoms)or an extract obtained from guinea ginger and / or an acylation treatment product of said extract.

Description

[0001]The present application is a divisional of U.S. application Ser. No. 11 / 661,401, filed Feb. 28, 2007, the entire contents of which is incorporated herein by reference.TECHNICAL FIELD[0002]The present invention relates to an antiwrinkle agent having superior ameliorative effects on wrinkles occurring with aging, and particularly at sites exposed to sunlight, which maintains the skin in a dermatologically and aesthetically healthy state, and an external composition for skin formulating said antiwrinkle agent.[0003]The present invention also relates to an external composition for skin and food and beverage composition effective for improving an obese constitution by promoting a systemic or local reduction of adipose tissue, or effective for inhibiting or preventing obesity by preventing increases in adipose tissue.BACKGROUND ART[0004]The organs of all living things, including humans, gradually decline with age following birth and growth, and death occurs when their function stops...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K8/35A61K31/12A61Q19/08A23L33/00
CPCA23L1/3002A23V2002/00A61K8/35A61K8/97A61K36/906A61Q19/08A23V2250/21A23V2200/318A23V2200/332A23L33/105A61K8/9794A61P3/00A61P3/04A61P17/00A61P43/00
Inventor SUGITA, JUNIKEMOTO, TAKESHIAKAZAWA, YUMIKOKOBAYASHI, YURIEMITANI, MITSUMASAHARATAKE, AKINORIKOMIYA, AYA
Owner KAO CORP