Composition for whitening skin comprising dihydro-5-methylfuran-2 (3h)-one derivatives

A skin-whitening and cosmetic composition technology, which is applied in the directions of drug combinations, skin-care preparations, active ingredients of hydroxy compounds, etc., can solve problems such as inhibition of melanin production by undisclosed marliolide, and achieve prevention or treatment of hypermelanosis diseases, reduction of Melanin, low risk effect

Pending Publication Date: 2022-04-05
艾弼生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above documents do not disclose whether marliolide and its derivatives are involved in melanogenesis inhibition or melanosome breakdown

Method used

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  • Composition for whitening skin comprising dihydro-5-methylfuran-2 (3h)-one derivatives
  • Composition for whitening skin comprising dihydro-5-methylfuran-2 (3h)-one derivatives
  • Composition for whitening skin comprising dihydro-5-methylfuran-2 (3h)-one derivatives

Examples

Experimental program
Comparison scheme
Effect test

reference example 1

[0095] cell culture

[0096] B16 melanoma cells were diluted with 0.25% trypsin solution and separated. The separated cells were added to Dulbecco's modified eagle's medium (Dulbecco's modified eagle's medium) supplemented with 10% fetal bovine serum (FBS) and 1% penicillin / streptomycin (100 U / ml). , DMEM), at 37°C, 5% CO 2 Adapted and cultured in an incubator.

Embodiment 1

[0098] Analysis of Effects on Cell Survival

[0099] The method of measuring cytotoxicity by MTT assay (MTT assay) using B16 melanoma cells is as follows.

[0100] 200 μL of B16 melanoma cells in 2.7 × 10 3 Cells / well (cells / well) were seeded in a 96-well plate (96well plate), and then incubated at 37°C, 5% CO 2 incubator for 24 hours. Compounds 1 to 5 were treated with B16 melanoma cells at concentrations of 0.3 μM, 1 μM, 3 μM, and 10 μM for 2 hours.

[0101] Then, α-MSH was treated with a concentration of 100nM for 76 hours, and the absorbance at 590nm was measured by the MTT method, and the results were as follows: figure 1 shown. And, for the racemic mixture of Compound 1 at 1 μM, 3 μM, and 10 μM, the absorbance was measured by the same method, and the results were as follows: figure 2 shown.

[0102] Such as figure 1 and figure 2 As shown, compared with the control group, the compounds of the present invention all exhibited the same level of cell viability, thus...

Embodiment 2

[0104] Melanin production inhibition and melanosome decomposition effect

[0105] Using B16 melanoma cells, the effects of melanin production inhibition and melanosome decomposition were confirmed by the following method.

[0106] B16 melanoma cells in 2.7×10 3cells / well were seeded in a 96-well culture plate. After 24 hours, the culture medium of the 96-well was removed, and the DMEM medium containing 10% FBS and compound 1 to compound 5 were treated at concentrations of 0.3 μM, 1 μM, 3 μM, and 10 μM for 2 hours. Then, α-MSH was treated at a concentration of 100 nM for 72 hours.

[0107] After 72 hours, measure the amount of melanin released into the culture medium by measuring the absorbance at 405 nm, the results are as follows image 3 shown. And, for the racemic mixture of Compound 1 at 1 μM, 3 μM, 10 μM, and 30 μM, the absorbance was measured by the same method, and the results were as follows: Figure 4 shown.

[0108] Such as image 3 and Figure 4 As shown, co...

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PUM

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Abstract

The present invention relates to a composition for whitening skin, comprising a dihydro-5-methylfuran-2 (3H)-one derivative having melanogenesis inhibition and melanosome decomposition activity, an isomer thereof, or a pharmaceutically acceptable salt thereof. Specifically, the composition according to the present invention is characterized by inhibiting melanogenesis and promoting melanosome decomposition by the action of a dihydro-5-methylfuran-2 (3H)-one derivative on a melanin biosynthesis signal transduction pathway induced by an alpha-melanocyte stimulant (alpha-MSH), and in that the composition according to the present invention is a composition for inhibiting melanogenesis and promoting melanosome decomposition by means of the action of a dihydro-5-methylfuran-2 (3H)-one derivative on a melanin biosynthesis signal transduction pathway induced by alpha-MSH.

Description

technical field [0001] The present invention relates to a composition for whitening skin comprising a dihydro-5-methylfuran-2(3H)-one derivative having melanin production inhibitory activity or a pharmaceutically acceptable salt thereof. Specifically, the composition is characterized in that the compound of the present invention acts on the melanin biosynthesis signal transduction pathway induced by α-Melanocyte-stimulating hormone (α-MSH) to prevent or Treatment of hyperpigmentation disorders. Background technique [0002] Melanin (melanin) is a black pigment found in animals, plants, microorganisms, etc., and is not essential for growth or development, but it is a substance that improves viability and competitiveness against the environment. Melanin is a stable pigment among the pigments found in living organisms, which is almost insoluble in all solvents, and the process of melanogenesis occurs in melanosomes, which are melanocytes ( melanocytes) are small organs of spe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/49A61K8/58A61K8/34A61K31/365A61K31/695A61P17/00A61P17/16A61P29/00A61Q19/02A23L33/10A61K31/05
CPCA23L33/10A23V2200/318A61Q19/02A61K8/4973A61K8/347A61K31/365A61P17/00A23V2002/00A23V2250/30A61K2800/92
Inventor 成钟赫金炫周尹清镛
Owner 艾弼生物科技有限公司
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