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Method for preparing icariside II, cosmetic composition containing the same and the use thereof for skin whitening

A cosmetic composition, icariin technology, applied in the direction of medical preparations containing active ingredients, cosmetics, cosmetic preparations, etc., can solve the problems of insufficient whitening effect, use restrictions, etc., to achieve excellent skin whitening Effect, effect of suppressing melanin production

Inactive Publication Date: 2009-08-26
AMOREPACIFIC CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, their use is limited due to insufficient whitening effects and various problems arising when adding them to cosmetics, such as skin safety, and formulation and stability

Method used

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  • Method for preparing icariside II, cosmetic composition containing the same and the use thereof for skin whitening
  • Method for preparing icariside II, cosmetic composition containing the same and the use thereof for skin whitening
  • Method for preparing icariside II, cosmetic composition containing the same and the use thereof for skin whitening

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Preparation of Icariside II by Extraction

[0040] 2 kg of dried leaves of Epimedium korean were added to 6 liters of hexane, and extracted three times at room temperature with stirring. 1 kg of defatted plant leaves was added to 4 liters of methanol, extracted three times under reflux, and then settled at 15 °C for 1 day. Afterwards, the settled material is filtered through a filter cloth and centrifuged into a residue and a filtrate. The filtrate was concentrated under reduced pressure. The obtained extract was suspended in water and extracted 5 times with ether to remove the pigment, and the aqueous layer was extracted once with 500 ml of 1-butanol. The resulting entire 1-butanol layer was concentrated under reduced pressure to obtain a 1-butanol extract, which was then dissolved in a small amount of methanol. This solution was added to a large amount of ethyl acetate, and the formed precipitate was dried, thereby obtaining an extract containing icariin...

Embodiment 2

[0041] Example 2: Preparation of Icariside II Using Cellulase

[0042] 10 g of icariin was dissolved in 500 ml of 0.1 M acetate buffer solution (pH 4.5), and 0.5 g of cellulase (Sigma) was added thereto. The solution was stirred in a water bath at 37°C for 48 hours while it was checked periodically by thin layer chromatography. When icariin completely disappeared, the reaction solution was heated in hot water (80-100° C.) for 10 minutes to terminate the reaction, and then concentrated under reduced pressure to remove the solvent. The residue was added to 200 ml of ethanol, the solution was stirred three times, and filtered to remove a precipitate, and the filtrate was concentrated under reduced pressure to obtain a crude product. The crude product was separated by silica gel column chromatography (chloroform:methanol=8:1-4:1), thereby obtaining 7.5 g of icariin II.

Embodiment 3

[0043] Example 3: Preparation of Icariside II using β-glucosidase

[0044] 10 g of icariin was dissolved in 500 ml of 0.1 M acetate buffer solution (pH 5.5), and 0.5 g of β-glucosidase (Sigma) was added thereto. The solution was stirred in a water bath at 25°C for 48 hours while periodically checking it by thin layer chromatography. When icariin completely disappeared, the reaction solution was heated in hot water (80-100° C.) for 10 minutes to terminate the reaction, and then concentrated under reduced pressure to remove the solvent. The residue was added to 200 ml of ethanol, the solution was stirred three times, and filtered to remove the precipitate. The filtrate was concentrated under reduced pressure to obtain a crude product. The crude product was separated by silica gel column chromatography (chloroform:methanol=8:1-4:1), thereby obtaining 6.9 g of icariin II.

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Abstract

The present invention relates to a method for preparing icariside II and a skin whitening cosmetic composition containing the same. More specifically, the invention relates to a method for preparing icariside II represented by Formula I, which inhibits the glycosylation of glycoprotein enzyme tyrosinase by inhibiting the enzymatic activity of alpha-glucosidase, which is an important enzyme in the glycosylation of tyrosinase, as well as a skin whitening composition.

Description

technical field [0001] The present invention relates to the method for preparing icariside II (icariside II), the cosmetic composition containing icariside II, and the purposes of this composition for skin whitening, more specifically, the present invention relates to Process for preparing icariside II represented by formula 1, cosmetic composition and use of the composition for skin whitening, icariside II inhibits by inhibiting the enzymatic activity of α-glucosidase Glycosylation of glycoproteinase (tyrosinase), α-glucosidase is an important enzyme in the glycosylation of tyrosinase: [0002] Formula 1 [0003] [0004] Wherein, R1 is rhamnopyranose. Background technique [0005] Factors that determine the color of a person's skin include various aspects, and among these factors, such as the activity of melanin-producing melanocytes in the human body, the distribution of blood vessels, the thickness of the skin, and the presence or absence of pigments (for example, c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/49A61Q19/02
CPCA61K8/602A61K2800/782A61K8/97A61Q19/02A61K8/9789A61K8/49
Inventor 朴葰星朴惠胤卢浩植安秀美金德姬
Owner AMOREPACIFIC CORP
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