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Alkyl pyranone compound and preparation process and application

A kind of compound and application technology, applied in the field of alkylpyrone compounds and their preparation and application

Inactive Publication Date: 2014-12-17
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The study found that the indicated alkylpyrone compounds have anti-tumor activity, but there is no report on the chemical structure of the compound and the anti-proliferation activity of cancer cells, so there is no related drug on the market

Method used

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  • Alkyl pyranone compound and preparation process and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Fermentative production and separation and purification of the compound of embodiment 1

[0013] 1 Fermentation production

[0014] Fermentation culture of production bacteria: according to the routine method of cultivating microorganisms, get Trichoderma aculeatus ( Trichoderma asperellum ) (preserved on October 30, 2012 in the China Type Culture Collection Center of Wuhan University, the deposit number is: CCTCC NO: M 2012438) appropriate amount, inoculated on the PDA solid slant medium and cultivated in a 28°C incubator for 4 days.

[0015] Take an appropriate amount of strains cultured on a slant for 4 days, and inoculate them into 400mL of culture medium [medium composition (g / L): mannitol 20.0, yeast extract 3.0, maltose 20.0, monosodium glutamate 10.0, glucose 10.0, KH 2 PO 4 0.5, MgSO 4 0.3] in a 1000 mL Erlenmeyer flask, after static culture at 28°C for 30 days, mycelium and fermentation broth were obtained.

[0016] 2 Obtaining the extract

[0017] Aft...

Embodiment 2

[0026] Example 2 Test of anti-tumor activity in vitro

[0027] 1 Experimental samples and experimental methods

[0028] Preparation of the test sample solution: the test sample is the pure product of the compound separated and purified in the above-mentioned implementation 1. Accurately weigh an appropriate amount of sample, add 50 mu L DMSO, after one hour of UV irradiation, add 950 mu L cell culture medium containing 10% FBS, obtained 1 mg.mL containing 5% DMSO -1 Sample stock solution. Dilute with cell culture medium to obtain concentrations of 0.1, 0.05, 0.02, 0.01 mg.mL -1 sample.

[0029] Cell lines and subculture of cells adopt human lymphoma cell line RAJI. Cells were subcultured in RPMI-1640 medium containing 10% FBS at 37°C in an incubator blown with 5% carbon dioxide.

[0030] Cancer cell proliferation inhibitory activity test method

[0031] Take the tumor cells in the logarithmic growth phase, dilute them with culture medium containing 10% FBS, and adjus...

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Abstract

The invention relates to an alkyl pyranone compound and its preparation process and application. The alkyl pyranone compound belongs to an active pyranone compound and contains an alpha-pyranone structure. According to the preparation method, through fermental cultivation of Trichodermaasperellum, a crude extract of metabolite in mycelium is obtained, and the compound provided by the invention is prepared by separation and purification. There is no report about a chemical structure of the compound and its cancer cell proliferation inhibition activity. It is verified through tests that the compound can be used as a cancer cell proliferation inhibitor or an antitumor agent.

Description

technical field [0001] The invention relates to an alkylpyrone compound and its preparation method and application. Background technique [0002] Alkyl pyrones (Alkyl pyrones) are a class of derivatives of pyrones, which are characterized by containing six-membered ring unsaturated lactones, and are often reported to have a wide range of biological activities, such as cytotoxicity, neurotoxicity, toxicity and phytotoxicity. The inventor's research has learned that Trichoderma aculeatus ( Trichoderma asperellum ) IBPT-2 (preserved in the Chinese Type Culture Collection Center of Wuhan University on October 30, 2012, and the preservation number is: CCTCC NO: M 2012438) The crude extract of metabolites in mycelium has better inhibitory activity on cancer cell proliferation , and its active ingredients were studied. The study found that the indicated alkylpyrone compounds have anti-tumor activity, but there is no report on the chemical structure of the compound and the anti-p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P35/00C12P17/06C12R1/885C07D309/38A61K31/366
CPCC07D309/38C12P17/06
Inventor 陈立钟萍夏其文张其清
Owner FUZHOU UNIV
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