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Preparation method of compound endecaphyllacins B and application thereof in preparation of anti-tumor drugs

A technology of anti-tumor drugs and compounds, applied in the field of medicine and biology

Active Publication Date: 2013-04-03
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

But so far, in domestic and foreign literature reports, there is no report that the compound endecaphyllacins B has anti-tumor activity

Method used

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  • Preparation method of compound endecaphyllacins B and application thereof in preparation of anti-tumor drugs
  • Preparation method of compound endecaphyllacins B and application thereof in preparation of anti-tumor drugs
  • Preparation method of compound endecaphyllacins B and application thereof in preparation of anti-tumor drugs

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Experimental program
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Effect test

Embodiment 1

[0024] One, the preparation of compound endecaphyllacins B

[0025] After crushing 10Kg of the fruit peel of Akiras sinensis, extract it by cold immersion with 98% ethanol aqueous solution for several times until the extract is basically colorless, combine the extracts, concentrate under reduced pressure until there is no alcohol smell, add 500mL of water to suspend, and then dilute the suspension with ethyl acetate The ester was extracted 5 times until the suspension was basically colorless. The ethyl acetate extracts were combined and concentrated under reduced pressure at 40°C to obtain 167.9 g of extract.

[0026] The extract is subjected to silica gel column chromatography (silica gel 200-300 mesh), and petroleum ether-ethyl acetate is used as the eluent for elution, and petroleum ether-ethyl acetate is eluted from a volume ratio of 100:0~1:1. Use thin-layer chromatography (TLC) to detect (the color reagent is anisaldehyde-concentrated sulfuric acid reagent), and combine ...

Embodiment 2

[0034] The antitumor activity of compound endecaphyllacins B was tested by SRB method [Skehan P, Storeng R, Dominic S. New colorimetric cytotoxicity assay for anticancer-drug screening [J]. J Natl Cancer Inst,].

[0035] 1. Experimental reagents: Dissolve endecaphyllacins B, a compound prepared by the present invention, in dimethyl sulfoxide (DMSO) to obtain a mother solution with a concentration of 10 mmol / L, and then dilute it to the required concentration with RPMI-1640 medium. The positive control was cisplatin aqueous solution.

[0036] The tumor cell lines used in this experiment were glioma cell SF-268, breast cancer cell MCF-7, non-small cell lung cancer cell NCI-H460 and liver cancer cell HePG-2.

[0037] 2. Experimental method: Take NCI-H460, SF-268, MCF-7 and HePG-2 cells in the logarithmic growth phase, digest with trypsin, count by trypan blue staining, and trypan blue exclusion test detects that the cell viability is greater than 95% Afterwards, adjust the cell ...

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Abstract

The invention discloses a preparation method of a compound endecaphyllacins B and an application thereof in the preparation of anti-tumor drugs. According to the preparation method, the compound endecaphyllacins B is obtained through preparative separation of aquilaria sinensis (Lour.) Gilg.) pericarps, has obvious anti-tumor activity and can be used for preparing the anti-tumor medicines. Therefore, the realization of the compound endecaphyllacins B provides a candidate compound for the research and development of the new anti-tumor medicines and a scientific basis for the development and utilization of aquilaria sinensis plant resources.

Description

technical field [0001] The invention belongs to the field of medical biotechnology, and in particular relates to a preparation method of compound endecaphyllacins B and its application in the preparation of antitumor drugs. Background technique: [0002] Malignant tumor, also known as cancer, is one of the major diseases that endanger human life and quality of life. According to the statistics of the World Health Organization, 10 million people in the world suffer from cancer every year, and about 6 million people die of cancer, accounting for 12% of the global death toll. And due to the increase in the number of smokers, the reduction in physical activity, the lack of fruits and vegetables in the diet and other bad habits may lead to an increase in the number of people suffering from cancer. The incidence of cancer in my country is in a period of rapid increase, with about 2.6 million cancer cases and 1.8 million deaths each year. Therefore, finding effective anticancer d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J1/00A61K31/565A61P35/00
Inventor 章卫民张兴陈玉婵李浩华陶美华
Owner GUANGDONG INST OF MICROBIOLOGY GUANGDONG DETECTION CENT OF MICROBIOLOGY