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Compound lithocarolsA-F, preparation method and application thereof in preparation of antitumor drugs

A technology of anti-tumor drugs and compounds, applied in the field of medicine and biology, can solve the problems of accidental death, high price, strong toxic and side effects, etc.

Active Publication Date: 2019-02-15
东岱(济南)智能技术有限公司
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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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  • Compound lithocarolsA-F, preparation method and application thereof in preparation of antitumor drugs
  • Compound lithocarolsA-F, preparation method and application thereof in preparation of antitumor drugs
  • Compound lithocarolsA-F, preparation method and application thereof in preparation of antitumor drugs

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Effect test

Embodiment 1

[0052] 1. Isolation, purification and identification of marine fungus Phomopsis lithocarpus FS508

[0053] 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.

[0054] 2. Solid fermentation of Phomopsis lithocarpus FS508

[0055] Inoculate the activated deep-sea fungus FS508 mycelium into potato glucose liquid medium (per liter of medium is prepared by the fol...

Embodiment 2

[0087] The antitumor activity of compounds lithocarols A-F 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.).

[0088] 1. Reagents for the test: Dissolve the compounds lithocarols A-F prepared by the present invention in dimethyl sulfoxide (DMSO) to obtain a mother solution with a concentration of 10 mg / mL, and then dilute to the required concentration with RPMI-1640 medium. The positive control was cisplatin aqueous solution.

[0089] 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.

[0090] 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 compound lithocarolsA-F, a preparation method and application thereof in preparation of antitumor drugs. The compound lithocarolsA-F is isolated from a fermentation culture of marine fungi Phomopsis lithocarpus FS508. Experiments prove that the IC50 values of the compound lithocarolsA-F on liver cancer cells HepG-2, breast cancer cells MCF-7, glioma cells SF-268 and non-small cell lung cancer cells A549 are 10.5-87.7 muM, showing that the compound lithocarolsA-F has relatively significant antitumor activity and can be used for preparing antitumor drugs.

Description

technical field [0001] The invention belongs to the field of medical biotechnology, and in particular relates to compounds lithocarolsA-F, a preparation method thereof and an application in preparation of antitumor drugs. 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 anticanc...

Claims

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Application Information

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IPC IPC(8): C07D407/04C07D407/12A61K31/343A61K31/357C12P17/16A61P35/00C12R1/645
CPCA61P35/00C07D407/04C07D407/12C12P17/162
Inventor 刘洪新章卫民许建林陈玉婵谭海波李赛妮李浩华刘昭明
Owner 东岱(济南)智能技术有限公司
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