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KR-102962174-B1 - COMPOSITION FOR SKIN WHITENING COMPRISING ISOLINDLEYIN

KR102962174B1KR 102962174 B1KR102962174 B1KR 102962174B1KR-102962174-B1

Abstract

The present disclosure relates to a skin whitening composition comprising isorindelain or its stereoisomers, salts, hydrates, or solvates as an active ingredient. The skin whitening composition exhibits an excellent skin whitening effect by directly inhibiting melanin production through the inhibition of tyrosinase activity without side effects.

Inventors

  • 이지영
  • 노경태

Assignees

  • (주)아모레퍼시픽
  • 연세대학교 산학협력단

Dates

Publication Date
20260511
Application Date
20200316

Claims (10)

  1. A cosmetic composition for skin whitening comprising isolindleyin or its stereoisomers, salts, hydrates, or solvates as an active ingredient.
  2. A food composition for skin whitening comprising isolindleyin or its stereoisomers, salts, hydrates, or solvates as an active ingredient.
  3. In paragraph 1, A composition in which the concentration of isorindelain or its stereoisomer, salt, hydrate, or solvate in the above composition is 50 to 500 μM.
  4. In paragraph 1, A composition in which the above isorindelain or its stereoisomer, salt, hydrate, or solvate is administered at a dosage of 23 to 240 mg/kg/day.
  5. In paragraph 1, A composition in which the above active ingredient inhibits melanin production.
  6. In paragraph 1, A composition in which the above active ingredient inhibits the activity of tyrosinase.
  7. In paragraph 2, A composition in which the concentration of isorindelain or its stereoisomer, salt, hydrate, or solvate in the above composition is 50 to 500 μM.
  8. In paragraph 2, A composition in which the above isorindelain or its stereoisomer, salt, hydrate, or solvate is administered at a dosage of 23 to 240 mg/kg/day.
  9. In paragraph 2, A composition in which the above active ingredient inhibits melanin production.
  10. In paragraph 2, A composition in which the above active ingredient inhibits the activity of tyrosinase.

Description

Composition for skin whitening comprising isolindleyin This specification relates to a skin whitening composition having excellent skin whitening effects. Among the many factors that determine human skin color, the most important is melanin. This melanin is produced by melanocytes, which are melanin-forming cells. Melanin polymers are synthesized within melanosomes inside melanocytes, which then migrate to keratinocytes to determine the color of the skin's epidermis. While melanin functions to protect the body from ultraviolet rays and other factors, excessive production can lead to melanin deposition in the skin, potentially causing not only melasma and freckles but also skin cancer. In the past, arbutin and kojic acid have been used to inhibit melanin production, but these substances have the disadvantage of having very high active concentrations. In addition, hydroquinone, which is used to inhibit the activity of tyrosinase, a melanin-producing enzyme, causes toxicity when applied to the skin and can lead to problems such as vitiligo. Therefore, to solve these problems, it is necessary to develop skin whitening substances that are non-toxic to the skin while possessing high whitening activity. Figure 1 is a graph showing the cytotoxicity of isorindelain according to concentration. Figure 2 is a photograph showing the degree of pigmentation in melanocytes following isolindeline treatment. Figure 3 is a graph showing the amount of melanin produced according to isorindelain treatment. The present invention will be described in detail below. In one aspect, the present invention provides a skin whitening composition comprising isolindleyin or a stereoisomer, salt, hydrate, or solvate thereof as an active ingredient. In one embodiment, the isorindelain is [4,5-dihydroxy-6-(hydroxymethyl)-2-[4-(3-oxobutyl)phenoxy]oxan-3-yl] 3,4,5-trihydroxybenzoate, which can be represented by the following chemical formula 1. [Chemical Formula 1] In one embodiment, the concentration of isorindelain or its stereoisomer, salt, hydrate, or solvate in the composition may be 50 to 500 μM. If the concentration of isorindelain or its stereoisomer, salt, hydrate, or solvate is less than 50 μM, it is difficult to exhibit the effects according to the present invention, and if it exceeds 500 μM, it may cause skin irritation. Specifically, the concentration of isorindelain or its stereoisomer, salt, hydrate, or solvate in the composition is 50 μM or more, 55 μM or more, 60 μM or more, 65 μM or more, 70 μM or more, 75 μM or more, 80 μM or more, 85 μM or more, 90 μM or more, 95 μM or more, 100 μM or more, 110 μM or more, 120 μM or more, 130 μM or more, 140 μM or more, 150 μM or more, 160 μM or more, 170 μM or more, 180 μM or more, 190 μM or more, or 200 μM or more, and is 500 μM or less, 495 μM or less, 490 μM or less, 485 μM or less, 480 μM or less, 475 μM or less, 470 μM or less, It may be 465 μM or less, 460 μM or less, 450 μM or less, 440 μM or less, 430 μM or less, 420 μM or less, 410 μM or less, 400 μM or less, 390 μM or less, 380 μM or less, 370 μM or less, 360 μM or less, 350 μM or less, 340 μM or less, 330 μM or less, 320 μM or less, 310 μM or less, or 300 μM or less. In this specification, "stereoisomer" includes optical isomers, for example, essentially pure enantiomers, essentially pure diastereomers, or mixtures thereof. In this specification, "essentially pure" means that, for example, when used in relation to enantiomers or diastereomers, a specific compound that can be exemplified as an enantiomer or diastereomer is present in an amount of about 90% or more, preferably about 95% or more, more preferably about 97% or more, or about 98% or more, even more preferably about 99% or more, and even more preferably about 99.5% or more (w/w). In this specification, "salt" means a salt according to one aspect of the present invention that is acceptable in medicines, cosmetics and foods and has desirable activity of a parent compound. The salt is formed from (1) an inorganic acid such as hydrochloric acid, hydrobromide, sulfuric acid, nitric acid, phosphoric acid, etc.; or acetic acid, propionic acid, hexanoic acid, cyclopentanepropionic acid, glycolic acid, pyruvate, lactic acid, malonic acid, succinic acid, malic acid, maleic acid, fumaric acid, tartaric acid, citric acid, benzoic acid, 3-(4-hydroxybenzoyl)benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, 1,2-ethane-disulfonic acid, 2-hydroxyethanesulfonic acid, benzenesulfonic acid, 4-chlorobenzenesulfonic acid, 2-naphthalenesulfonic acid, 4-toluenesulfonic acid, camphorsulfonic acid, 4-methylbicyclo[2,2,2]-oct-2-en-1-carboxylic acid, glucoheptonic acid, 3-phenylpropionic acid, trimethylacetic acid, (2) may include an acid addition salt formed from an organic acid such as tert-butylacetic acid, lauryl sulfate, gluconic acid, glutamic acid, hydroxynaphthoic acid, salicylic acid, stearic acid, or muconic acid; or a salt formed when an acidic proton