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Terrein compound having melanin biosynthesis inhibitors and its preparation

A technology of biosynthesis and terreus, applied in biochemical equipment and methods, methods based on microorganisms, organic active ingredients, etc., can solve problems such as death, deterioration of chromaffin cells, damage to original cell functions, etc.

Inactive Publication Date: 2007-03-07
KOREA RES INST OF BIOSCI & BIOTECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, 4-hydroxyanisole and hydroquinine, which have been used topically to treat hypermelanosis such as discoloration, freckles, spots, hyperpigmentation during pregnancy, etc., although they have strong melanin biosynthesis inhibitory activity, But it can also induce the deterioration or even death of chromaffin cells and impair the original function of cells

Method used

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  • Terrein compound having melanin biosynthesis inhibitors and its preparation
  • Terrein compound having melanin biosynthesis inhibitors and its preparation
  • Terrein compound having melanin biosynthesis inhibitors and its preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] preparation of terreinone compound of the present invention

[0049] The melanin biosynthesis inhibitor of the present invention can be isolated from the broth medium of Penicillium sp strain isolated from soil.

[0050] Specifically, in a 500 ml Erlenmeyer flask, Penicillium sp F020135 (Accession No.: KCTC 26245) (a fungal strain isolated from soil) was placed on 100 ml of yeast-malt extract (YM) medium at 140 rpm Cultured at 28°C for 8 days. Cells and culture medium were separated from each other using filter paper, and cells were placed in an equal volume of acetone overnight. Cells were removed by filtration with filter paper, and concentrated under reduced pressure to obtain an acetone extract. The acetone extract and the culture medium were placed in an equal amount of ethyl acetate for further extraction. The mixture was concentrated under reduced pressure to obtain ethyl acetate extract.

[0051] Fractions were obtained from the prepared ethyl acetate extra...

preparation Embodiment 1

[0060] Preparation of a cream containing the terrein compound of the present invention

[0061] Put stearic acid, cetostearyl alcohol, caprylic / capric triglyceride, mineral oil and butylene glycol into a beaker placed in a water bath, and heat to 75°C to form an oil phase. Mix the terreinone compound prepared in the above-mentioned Example 1, water, glycerin, Tween 60, Tween 80 and potassium hydroxide to form a water phase, and add the above-mentioned oil phase to the water phase. The reaction solution was stirred at 1200-1500 rpm for 10-20 minutes and then cooled. The solution was left at room temperature for 1-2 days. The contents of the substances contained in the cream are shown in Table 1 below (the total weight is 100 g).

[0062] substance

experiment Embodiment 1

[0063] Cytotoxicity test of the compound of the present invention

[0064] To study the cytotoxicity of the terreinone compounds of the present invention, Mel-Ab cells were treated with the terreinone compounds.

[0065] Specifically, at 5% CO 2 , Under the condition of 37°C, Mel-Ab melanocytes were cultivated with DMEM medium supplemented with 10% fetal bovine serum (FBS), 100nM phorbol 12-myristate 13-acetate (phobol 12-myristate 13-acetate), 1 nM cholera toxin, 50 μg / ml streptomycin and 50 U / ml penicillin.

[0066] The Mel-Ab melanocytes cultured above were treated with terreinone compound at different concentrations (0, 10, 25, 50, 75, 100 μM) for 24 hours, and then further cultured. The medium is then removed. Cells were stained with 0.5 ml 0.1% crystal violet and checked for Mel-Ab melanocytes. Crystal violet was removed by washing several times. Use 1.0 ml of 95% ethanol to extract the remaining crystal violet in the cells. Measure the OD of the extracted crystal...

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PUM

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Abstract

The present invention relates to a melanin biosynthesis inhibitor containing terrein compound as an effective ingredient. The terrein compound can be easily separated from Penicillium sp KCTC 26245, a fungal strain inhabited in domestic soil. It does not directly inhibit tyrosinase but inhibits the expression of MITF (microphthalmia-associated transcription factor) by activating ERK (extracellular signal-regulated kinase) in melanin chromatocytes to give whitening effect. So, the melanin biosynthesis inhibiting effect of the compound is much greater than that of any other conventional inhibitors, and further the effect can be raised when the compound is used together with other inhibitors, owing to their different mechanisms. Thus, the compound of the present invention can be effectively used as a skin trouble treating agent, a skin whitening agent and a browning inhibitor.

Description

technical field [0001] The present invention relates to a new use of a fungus-derived compound having melanin biosynthesis inhibitory activity and a preparation method thereof. Background technique [0002] Melanin is a phenolic biopolymer widely distributed in nature. It is a complex of melanin and protein and has the activity of increasing the ability to survive against any environment and competition. However, overproduction of melanin can cause discoloration and freckles, cause skin aging or even lead to skin cancer. The reason for the excessive biosynthesis of melanin is the severe exposure to UV light due to the destruction of the ozone layer, and excessive biosynthesis can cause harm to humans, especially to the skin. Therefore, various attempts have been made to develop new substances having strong melanin biosynthesis inhibitory activity. [0003] In terms of skin cancer, melanin biosynthesis has become a major target of research, and various melanin biosynthesis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61K8/99A61K8/02A61K8/35A61Q19/02C12P7/38
CPCC12P7/38A61K8/35A61K2800/782A61Q19/02A61K31/122A61P17/00A61P17/16A61P43/00C12N1/145C12R2001/80
Inventor 俞益东金元坤柳仁子金钟平李相龟朴曙亨金东锡朴景赞
Owner KOREA RES INST OF BIOSCI & BIOTECH
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