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Kojic acid and kojic acid derivative, and preparation method and application thereof

A technology of kojic acid and medicine, applied in the field of kojic acid and kojic acid derivatives and their anti-inflammatory uses, can solve the problems of few reports on the anti-inflammatory activity of kojic acid and its derivatives, etc.

Active Publication Date: 2021-10-08
ZHENGZHOU UNIVERSITY OF LIGHT INDUSTRY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, there are few reports on the anti-inflammatory activity of kojic acid and its derivatives

Method used

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  • Kojic acid and kojic acid derivative, and preparation method and application thereof
  • Kojic acid and kojic acid derivative, and preparation method and application thereof
  • Kojic acid and kojic acid derivative, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Fermentation and extraction of embodiment 1 bacterial classification

[0034] Aspergillus versicolor (Aspergillus versicolor), purchased from the American Type Culture Collection (ATCC), the preservation number is ATCC 28286. The strain was revived by streaking, inoculated into PDA solid medium, and activated in a 28°C incubator for 5 days. Use a scalpel to cut out small pieces of colonies from the PDA medium, inoculate them into PDB liquid medium, and cultivate them on a shaker at 28° C. and 160 rpm for 5 days to obtain seed liquid. Then the seed solution was inoculated into rice solid medium, and cultured statically for 30 days in a constant temperature and humidity chamber at 28°C. Take the fermented product of rice, add 400 mL of ethyl acetate for every 200 g of the fermented product, cold-soak and extract twice, combine the extracts and concentrate under reduced pressure until there is no ethyl acetate smell to obtain ethyl acetate extract.

Embodiment 2

[0035] The separation and identification of embodiment 2 trexone A

[0036] The extractant was chromatographed on a macroporous resin column, adsorbed overnight, and eluted with 10%, 30%, 50%, 70%, 90%, 100% methanol-water gradient, and each gradient was combined and spin-dried until there was no liquid to obtain 6 a subcomponent. The fourth subcomponent (70% part) was separated and purified by semi-preparative high performance liquid chromatography, mobile phase: 65% MeOH, flow rate 4mL / min, detection wavelength 210nm, peak time 34.8-35.6min. The peak was picked up and evaporated to complete dryness to obtain 12.5 mg of white solid. The white solid was subjected to high-resolution mass spectrometry and one-dimensional two-dimensional NMR analysis results as follows Figure 1-8 , the structure of the compound is determined to be High resolution mass spectrometry [M-H] – m / z 419.1339, calculated to be 419.1348 (C 21 h 23 o 9 ), the molecular formula of the compound is C...

Embodiment 3

[0039] Example 3 NO release inhibition experiment

[0040] Mouse macrophage cell line RAW 264.7 was cultured in high glucose DMEM medium supplemented with 1% penicillin and streptomycin at 37°C, 5% CO 2 cultivated under conditions. First, the MTT method was used to test the cytotoxicity of the compounds on RAW 264.7 cells. Both compounds had no cytotoxicity, IC 50 >100 μM. RAW 264.7 cells were counted with a hemocytometer, and the cell concentration was adjusted to 5×10 3 cells / well and cultured on a 96-well plate for 24 hours. After that, LPS (1.0 μg / mL) was added, and the compounds were diluted with culture medium to a final concentration of 50, 25, 12.5, 6.25, and 3.125 μM, respectively, and three replicate wells were set up in the sample addition group and the blank group. After continuing to culture for 24 hours, the amount of NO released was tested with a NO kit, and the OD value of each well was measured with a microplate reader at a wavelength of 550 nm. Inhibitio...

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Abstract

The invention discloses a kojic acid and a kojic acid derivative, and a preparation method and application thereof. The invention provides a kojic acid derivative trexone A. In an anti-inflammatory activity test, the median inhibitory concentrations of the trexone A and a precursor compound kojic acid for inhibiting mouse macrophages RAW264.7 are 15.5 + / -1.2 [mu]M and 40.8 + / -3.1 [mu]M respectively, the trexone A and the kojic acid can inhibit the expression of inflammatory factors IL-1beta, IL-6, TNF-alpha and iNOS of the mouse macrophages RAW264.7, the kojic acid can be used for treating dextran sodium sulfate induced mouse colitis, the effect of the kojic acid is equivalent to that of a positive drug mesalazine, the tradone A and the kojic acid can be applied to preparation of anti-inflammatory drug precursors, and a material basis is laid for further research and application of cosmetics and medicines of anti-inflammatory drugs.

Description

technical field [0001] The invention belongs to the technical field of natural medicines, and in particular relates to kojic acid and kojic acid derivatives and their anti-inflammatory application. Background technique [0002] The chemical name of kojic acid is 5-hydroxy-2-hydroxymethyl-4-pyrone, which has significant tyrosinase inhibitory activity and can inhibit the production of skin melanin. It is widely used in the fields of medicine and cosmetics, and the market value huge. Kojic acid, a key whitening ingredient, is added to a variety of high-end whitening cosmetics, such as Longsea Neaton, Cosmetic, and Langsi Dongxing. Clinically, creams containing 1% kojic acid can be used for the treatment of melasma, dark spots, sun spots and freckles. In addition, kojic acid is an ideal new food antioxidant and industrial raw material. [0003] At present, there are few reports on the anti-inflammatory activity of kojic acid and its derivatives. Through the research on the a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/04A61P29/00A61P1/00C12P17/18C12R1/66
CPCC07D493/04A61P29/00A61P1/00C12P17/18C07B2200/07Y02A50/30
Inventor 李天笑贾学伟王颖许春平梁佳欣熊亚妹袁梦
Owner ZHENGZHOU UNIVERSITY OF LIGHT INDUSTRY
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