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Polyketone compound Lithocarpin E-G as well as preparation method and application thereof

A technology of compounds and cultures, applied in the field of medicine and biology, can solve the problems of expensive side effects, poor specificity, and high price of cancer patients, and achieve significant anti-tumor activity

Active Publication Date: 2021-04-02
GUANGDONG INST OF MICROBIOLOGY GUANGDONG DETECTION CENT OF MICROBIOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of the current anticancer drugs have defects such as poor specificity, strong side effects and high price, which makes cancer patients often give up treatment due to expensive drugs or cause accidental death due to high side effects

Method used

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  • Polyketone compound Lithocarpin E-G as well as preparation method and application thereof
  • Polyketone compound Lithocarpin E-G as well as preparation method and application thereof
  • Polyketone compound Lithocarpin E-G as well as preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0047] 1. Isolation, purification and identification of marine fungus Phomopsis lithocarpus FS508

[0048] The marine fungus Phomopsis lithocarpus FS508 of the present invention was isolated from deep-sea sediments in the Indian Ocean (16°50.508'N, 111°53.335'E, water depth 3606 meters) in May 2016, identified by ITS sequence analysis, and registered in GenBank The number is: MG686131. ​​After blast comparison and homology analysis, it was identified that the strain belongs to the fungus of the genus Phomopsis, and it was named Phomopsis lithocarpus FS508. It was deposited in Guangdong Microbial Culture Collection Center (GDMCC) on August 15, 2018, address : 5th Floor, Building 59, Compound, No. 100 Xianlie Middle Road, Guangzhou City, and its deposit number is GDMCCNo.60433.

[0049] 2. Solid fermentation of Phomopsis lithocarpus FS508

[0050] Inoculate the activated deep-sea fungus FS508 mycelium into potato glucose liquid medium (per liter of medium is prepared by the fol...

Embodiment 2

[0074] Antitumor activity of compound lithocarpin E-G was tested by SRB method (Skehan P, Storeng R, Dominic S. New colorimetric cytotoxicity assay for anticancer-drug screening [J]. J Natl Cancer Inst, 1990, 82:1107-1112.).

[0075] 1. Reagents for the test: the compound lithocarpin E-G prepared by the present invention was dissolved in dimethyl sulfoxide (DMSO) to obtain a mother solution with a concentration of 10 mg / mL, and then diluted to the required concentration with RPMI-1640 medium. The positive control was cisplatin aqueous solution.

[0076] The tumor cell lines used in this experiment were liver cancer cell HepG-2, breast cancer cell MCF-7, glioma cell SF-268 and non-small cell lung cancer cell A549.

[0077] 2. Experimental method: HepG-2, MCF-7, SF-268 and A549 cells in the logarithmic growth phase were digested with trypsin, counted by trypan blue staining, and after the trypan blue exclusion test detected that the cell viability was greater than 95%, Adjust t...

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Abstract

The invention discloses a polyketone compound Lithocarpin E-G as well as a preparation method and application of the polyketone compound Lithocarpin E-G. The compound Lithocarpin E-G is separated andprepared from a fermentation culture of a marine fungus Phomopsis lithocarpus FS 508. Proved by tests, the IC50value range of the compound Lithocarpin E-G on liver cancer cell HepG-2, breast cancer cell MCF-7, glioma cell SF-268 and non-small cell lung cancer cell A549 is 6.3-91.6 mu M, the anti-tumor activity is relatively obvious, and the compound Lithocarpin E-G can be used for preparing anti-tumor drugs.

Description

technical field [0001] The invention belongs to the technical field of medicine and biology, and in particular relates to a polyketide compound lithocarpin E-G and a preparation method and application thereof. Background technique [0002] Cancer is seriously threatening human health. At present, the number of people who die from cancer in the world is about 10 million every year, and the number of people who die from cancer in my country is about 2.5 million people every year, and this number is still increasing year by year. At present, the market share of anticancer drugs is also expanding, and anticancer drugs account for as much as 30% of the pharmaceutical market. However, most of the current anticancer drugs have defects such as poor specificity, strong side effects and high price, which makes cancer patients often give up treatment due to expensive drugs or cause accidental death due to high side effects. Therefore, improving the specificity of anticancer drugs and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/18A61K31/365A61P35/00C12P17/18C12R1/645
CPCC07D493/18A61P35/00C12P17/181
Inventor 刘洪新陈玉婵章卫民许建林李赛妮
Owner GUANGDONG INST OF MICROBIOLOGY GUANGDONG DETECTION CENT OF MICROBIOLOGY
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