JP3835609B2 - Melanin production inhibitor - Google Patents

Description

表１の結果から明らかなように、本発明のメラニン生成抑制剤を添加した溶液において、メラニンの生成は抑制された。さらにその効果は、既知の物質のアルブチンやコウジ酸と同等のものであった。
【００２１】
【発明の効果】
本発明のイソクロマン−１，３−ジオンは、高いメラニン生成抑制効果を有し、それ自身の香気強度が低いため、香粧品の品質を損なったり、香粧品の香りのバリエーションを限定することがなく、任意の量を配合することが可能であり、香粧品中に安全に用いることができる。[0001]
BACKGROUND OF THE INVENTION
The present invention relates to melanin production inhibitors and cosmetics containing them.
[0002]
[Prior art]
Conventionally, the suppression of melanin production is due to cytotoxicity to melanocytes, the suppression of tyrosinase activity in melanocytes, the suppression of tyrosinase expression, the autooxidation from dopaquinone generated by tyrosinase activity There is known a method for preventing oxidation through a route leading to melanin. And hydroquinone etc. are known as what shows the melanin production suppression effect by cytotoxicity. They have been used to treat pigmentation for the purpose of reducing skin pigmentation, but have safety issues. Arbutin (Non-patent Document 1), which is generally known as a derivative thereof, is generally used in cosmetics and the like as a substance that reversibly suppresses the production of melanin.
[0003]
Other melanin production inhibitors include, for example, cysteine, glutathione, vitamin C (non-patent document 2), kojic acid (non-patent document 3), products of microorganisms belonging to the genus Trichoderma (patent document 1), and alkalis of milk proteins. Decomposed product (Patent Document 2), milk protein hydrolyzate (Patent Document 3), amino acid derivative and peptide derivative of kojic acid (Patent Document 4), fragrance compound group having melanin production inhibitory function (Patent Document 5), tyrosinase A group of perfume compounds having an activity-inhibiting function (Patent Documents 6 and 7), various plant extracts, and the like are known.
[0004]
However, these conventional melanin production inhibitors, such as hydroquinone, have safety problems and are unsatisfactory in practical use and cannot be said to be truly satisfactory.
[0005]
[Patent Document 1]
Japanese Patent Laid-Open No. 2-145189 [Patent Document 2]
Japanese Patent Publication No.58-17773 [Patent Document 3]
JP-A-5-320068 [Patent Document 4]
JP-A-4-187618 [Patent Document 5]
JP 2000-302642 A [Patent Document 6]
JP 2001-163719 A [Patent Document 7]
JP 2001-240528 A [Non-Patent Document 1]
Kenichi Tomita, 20th FJ Seminar Proceedings, Page 21, Fragrance Journal, March 14, 1990 [Non-Patent Document 2]
Mishima Yutaka et al., Basic Dermatology, page 258, Asakura Shoten, 1973 [Non-patent Document 3]
Nikkei Business Daily, May 24, 1988 [0006]
[Problems to be solved by the invention]
An object of the present invention is to provide a melanin production inhibitor that is safe and can be incorporated in an arbitrary amount in a cosmetic product without impairing the quality of the cosmetic product.
[0007]
[Means for Solving the Problems]
The melanin production inhibitor of the present invention is a melanin production inhibitor containing isochroman-1,3-dione as an active ingredient, and is extremely useful as a whitening component for cosmetics and the like.
[0009]
DETAILED DESCRIPTION OF THE INVENTION
The melanin production inhibitor of the present invention contains isochroman-1,3-dione as an active ingredient.
[0011]
The melanin production inhibitor of the present invention can be produced by a known method and can be easily obtained because some compounds are commercially available.
[0012]
Examples of the melanin production inhibitor of the present invention include emulsions, lotions, creams, powders, packs, skin cleansers, pastes, foundations, lotions, gels, and other cosmetics, shampoos, rinses, body soaps, facial cleansers, etc. It can be suitably used for cosmetics such as soaps and other body cleansing agents and other skin external preparations.
[0013]
The blending ratio of the melanin production inhibitor of the present invention into the cosmetic can be arbitrarily set, but is preferably 0.00001% to 10% by weight (hereinafter simply referred to as “%”). More preferably, the content is 0.0001 to 5%, particularly preferably 0.1 to 1%. The melanin production inhibitor of the present invention can be used in combination with other melanin production inhibitors such as arbutin, kojic acid, and ascorbic acid. In addition, other active ingredients such as vitamins, antioxidants, antibacterial agents, anti-inflammatory agents, ultraviolet absorbers, and cooling agents can also be blended.
[0014]
The melanin production inhibitor of the present invention can be appropriately selected from general dispersion and solubilization techniques depending on the combination of the melanin production inhibitor and the base. Specifically, it can be stably dispersed or solubilized by, for example, a method using a surfactant or other solubilizer, or a means such as reducing the fluidity of the preparation with a thickener or the like.
[0015]
【Example】
EXAMPLES Hereinafter, the present invention will be specifically described with reference to examples, but the present invention is not limited to these examples.
[0016]
[Example 1] Melanin production inhibitory effect (test method)
0.1 mol / LM phosphate buffer (potassium dihydrogen phosphate: manufactured by Kanto Chemical Co., Inc., potassium phosphate: manufactured by Wako Pure Chemical Industries, Ltd.) 1.5 ml, 1.5 mmol / LM tyrosine (manufactured by Tokyo Chemical Industry Co., Ltd.) ) 0.3 ml and 0.5 ml of activator were added and stirred, and 0.2 ml of each sample shown in Table 1 diluted 20-fold with ethanol was added. Stir until the solution becomes clear, add 0.3 ml of mushroom tyrosinase (Sigma) adjusted to 3000 units / ml with pure water, quickly stir, and then incubate at 37 ° C for 100 minutes in a shaking thermostat. did. After 100 minutes, the amount of melanin produced was determined by measuring the absorbance at a wavelength of 640 nm using a UV spectrophotometer (JASCO: UVIDEC-610C). A sample obtained by adding 0.3 ml of buffer instead of tyrosinase was measured for each sample and used as a blank, and as a control, ethanol was added instead of the sample solution and the same measurement was performed as a control.
[0017]
(Suppression rate calculation formula)
Melanin inhibition rate (%) = (A− (CB)) / A × 100 (A: absorbance of control, B: absorbance of blank, C: absorbance of sample)
The results are shown in Table 1.
[0018]
[Example 2] Measurement of IC50 (test method)
0.1 mol / LM phosphate buffer (potassium dihydrogen phosphate: manufactured by Kanto Chemical Co., Inc., potassium phosphate: manufactured by Wako Pure Chemical Industries, Ltd.) 1.5 ml, 1.5 mmol / LM tyrosine (manufactured by Tokyo Chemical Industry Co., Ltd.) ) 0.3 ml and 0.5 ml of activator were added and stirred, and 0.2 ml of a sample diluted with ethanol was added to adjust the sample concentration. These were stirred until the solution became transparent, 0.3 ml of mushroom tyrosinase (manufactured by Sigma) adjusted to 3000 units / ml with pure water was added, and after rapid stirring, 100 ° C. at 37 ° C. with a shaking constant temperature bath. Incubated for minutes. After 100 minutes, the absorbance at a wavelength of 640 nm was measured using a UV spectrophotometer (JASCO: UVIDEC-610C). A sample obtained by adding 0.3 ml of buffer instead of tyrosinase was measured for each sample and used as a blank, and as a control, ethanol was added instead of the sample solution and the same measurement was performed as a control.
[0019]
(IC50 calculation formula)
Melanin inhibition rate (%) = (A− (CB)) / A × 100 (A: absorbance of control, B: absorbance of blank, C: absorbance of sample)
A graph was prepared by plotting the concentration on the horizontal axis and the melanin production inhibition rate on the vertical axis, and the concentration at which melanin production was inhibited by 50% (hereinafter referred to as IC50) was determined from this graph.
The results are shown in Table 1.
[0020]
[Table 1]

As is apparent from the results in Table 1, the production of melanin was suppressed in the solution to which the melanin production inhibitor of the present invention was added. Furthermore, the effect was equivalent to the known substances arbutin and kojic acid.
[0021]
【The invention's effect】
Since the isochroman-1,3-dione of the present invention has a high melanin production inhibitory effect and its own fragrance intensity is low, it does not impair the quality of the cosmetic product or limit variations in the fragrance of the cosmetic product. Any amount can be blended and can be used safely in cosmetics.

Claims (2)

A melanin production inhibitor containing isochroman-1,3-dione as an active ingredient. A cosmetic comprising the melanin production inhibitor according to claim 1.