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Lactone derivative derived from trichoderma citrinoviride and application thereof

A technology of application and medicine, applied in the field of lactone derivatives

Inactive Publication Date: 2013-08-28
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have found that the lactone compound has anti-tumor activity, but there is no report on the chemical structure of the compound and the inhibitory activity of tumor cell proliferation, so there is no drug related to this in the market.

Method used

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  • Lactone derivative derived from trichoderma citrinoviride and application thereof
  • Lactone derivative derived from trichoderma citrinoviride and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Fermentative production and separation and purification of the compound of embodiment 1

[0015] 1 Fermentation production

[0016] Fermentation culture of production bacteria: according to the conventional method of cultivating microorganisms, take Trichoderma auranthoderma ( Trichoderma citrinoviride. ) IBPT-4 (preserved in China Type Culture Collection Center on January 25, 2013, address: Wuhan University, Wuhan, China, deposit number is: CCTCC NO: M 2013055) appropriate amount, inoculated on PDA solid slant medium Cultivate for 4 days in a 28°C incubator.

[0017] Get the Trichoderma auranthoderma ( Trichoderma citrinoviride. ) appropriate amount of IBPT-4, inoculated into 400mL culture medium [Culture 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, NaCL 6.0 constant volume] in a 1000mL Erlenmeyer flask, after 30 days of static culture at 28°C, the mycelia and ferme...

Embodiment 2

[0029] Example 2 Test of anti-tumor activity in vitro

[0030] 1 Experimental samples and experimental methods

[0031] Preparation of the tested sample solution The test sample is the pure product of the compound separated and refined in the above-mentioned implementation 1. Accurately weigh an appropriate amount of sample, and prepare a solution with the required concentration with methanol for activity measurement.

[0032] Cell lines and cell subculture The human melanoma A375 cell line was used, and the A375 cells were subcultured in RPMI-1640 medium containing 10% FBS at 37°C in an incubator filled with 5% carbon dioxide.

[0033] Cell Proliferation Inhibitory Activity Test Method

[0034] Tetrazolium salt (MTT) method Take human melanoma A375 cells in the logarithmic growth phase, adjust the cell density to 2×10 per ml 5 Cells were inoculated into 96-well cell culture plates at 200 microliters per well, and filled with 5% CO at 37°C 2 for 4 hours in an incubator. A...

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Abstract

The invention relates to a lactone derivative derived from trichoderma citrinoviride and application thereof. The compound contains a molecular skeleton of hetero-oxygen atom pentacyclic lactone, and two methyls on the ring are located at the same side of the molecule. Verified by experiments, the lactone derivative has excellent anti-tumor activity. Besides, the lactone derivative can be applied to preparation of a cell proliferation inhibition drug or an anti-tumor drug and used for anti-tumor research.

Description

technical field [0001] The invention relates to a lactone derivative derived from Trichoderma aurantii and its application. Background technique [0002] In recent decades, during the research and development of new antineoplastic drugs, many natural lactones with anticancer activity have been discovered. Natural lactones with anticancer activity are mostly derived from marine organisms, with unique structures and novel mechanisms of action, which can not only provide lead compounds, but also provide a basis for the discovery of new targets. In addition, Iejimalides, anterior dinolides, and spongiolides, which have been studied more in recent years, have also played an important role in the discovery of new anti-tumor targets and the development of anti-cancer drugs with new mechanisms of action. , and become a tool for researching new antitumor drugs. [0003] The inventor's research has learned that Trichoderma auranthoderma ( Trichoderma citrinoviride. ) IBPT-4 (preser...

Claims

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Application Information

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IPC IPC(8): C07D317/34A61K31/365A61P35/00C12P17/04C12R1/885
Inventor 陈立张维维宫美维张其清
Owner FUZHOU UNIV
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