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Composition containing obacunone and method for using obacunone in skin whitening

A technology of skin whitening and composition, applied in the field of composition including phellodendron and its use in skin whitening application, capable of solving problems such as acute dermatitis and skin irritation

Inactive Publication Date: 2016-08-03
ACCESS BUSINESS GRP INT LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] One problem with using synthetic skin lightening agents such as hydroquinone or kojic acid is that they may cause skin irritation or acute dermatitis

Method used

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  • Composition containing obacunone and method for using obacunone in skin whitening
  • Composition containing obacunone and method for using obacunone in skin whitening
  • Composition containing obacunone and method for using obacunone in skin whitening

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Embodiment 1: by in B16F10 cell (CTG) Luminescent Cell Storage Cytotoxicity / safety of Phellodendrones carried out by Luminescent Cell Viability Assay full assessment

[0076] In order to determine the cellular safety of phellodendron, the following experiment was carried out.

[0077] Should (CTG) Luminescence cell viability assay (from Promega) was performed according to the manufacturer's instructions to determine the number of surviving cells in culture based on the quantification of ATP present, an indicator of metabolically active cells. In this experiment, 99.99% pure phellodendron was used (at 100.00 μg / mL, 33.333 μg / mL, 11.111 μg / mL, 3.704 μg / mL, 1.235 μg / mL, 0.412 μg / mL, 0.137 μg / mL, 0.046 μg / mL, 0.015μg / mL) and hydroquinone (used as reference, with the same gradient concentration). This experiment was performed using B16F10 cells.

[0078] According to the cell-based safety assessment using CTG, Phellodendron showed no cytotoxicity (see Table 1)....

Embodiment 2

[0082] Embodiment 2: In B16F10 cell, the agent of enzymatic activity to tyrosinase is carried out with cortex ketone Quantity-dependent inhibition

[0083] In order to determine whether phellodendron affects the enzymatic activity of tyrosinase, the following experiment was carried out.

[0084] On day 1, B16F10 cells were plated into 24-well assay plates at a density of approximately 18,000 cells / ml. Assay plate at 37°C, 5% CO 2 , Incubate for 24 hours under humid conditions.

[0085] On the second day, the reference substance (arbutin) and the test compound (phellodine) were added (the compound on the assay plate was 5 μl (final concentration: 1×)) to the plate and the plate was incubated at 37 °C, 5% CO 2 . Incubate for an additional 2 days under humidified conditions.

[0086] On day 5, plates were imaged. The inverted plate was shaken on a medium waste receptacle and blotted with a clean paper towel. 80 μl of 0.05 mMPBS (0.1% Triton-X) was added and the plate wa...

Embodiment 3

[0098] Example 3: Phellodendrones Shows Dose-Dependent Reduction of Melanin Production

[0099] In order to determine whether phellodendron affects the production of melanin, the following experiment was carried out.

[0100] 100 ug / mL of phellodendron was tested. Arbutin, a well-known tyrosinase inhibitor, was used as a positive control inhibitor in the experiments.

[0101] Phellodendron was dissolved in DMSO and added to B16F10 cells seeded at a density of 18,000 cells / mL in 24-well plates for 24 hours prior to treatment. The final concentration of test compound is 1X. The cytosolic pH of B16F10 cells in this experiment was approximately 5-7. Each dose of phellodendron was added to the cells in triplicate. Plates were then incubated at 37 °C, 5% CO 2 , Incubate for 72 hours under humid conditions.

[0102] On day 5, the medium was removed from the cells, 150 μl of 1 M NaOH was added to each well of the assay plate and the plate was incubated at 80° C. for 30 minutes...

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Abstract

The invention relates to a composition for partial usage and having melanin synthesis inhibition activity and tyrosinase inhibition activity, which contains 75-100% of pure obacunone, and the obacunone amount can effectively reduce melanin synthesis and / or inhibit tyrosinase activity. The invention also relates to a method for inhibiting melanin synthesis, inhibiting tyrosinase activity and whitening skin.

Description

technical field [0001] Compositions comprising phellodendrones and their use in methods of inhibiting tyrosinase activity and melanin synthesis in skin and methods of skin lightening are described. Background technique [0002] Skin color is mainly determined by the amount of melanin in the skin. Melanin is a brown-black pigment present in the skin. Since this pigment is dark, lower amounts of melanin result in lighter skin tones, while higher amounts result in darker skin tones. Melanin is formed by oxidation of the amino acid tyrosine to dihydroxyphenylalanine in melanocytes. This reaction is catalyzed by tyrosinase. [0003] The causes of excessive skin pigmentation may be: hormone abnormalities in the human body unrelated to ultraviolet rays, genetic diseases, etc.; or excessive melanin production and uneven distribution of melanin caused by excessive ultraviolet radiation. Having an appropriate amount of melanin in the skin has positive effects such as keeping the s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/49A61K8/97A61Q19/02A61Q19/08A61Q19/00
CPCA61K8/9789A61Q19/00
Inventor 韩强张翌李廷钊杜军李波
Owner ACCESS BUSINESS GRP INT LLC