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Gamma-butyrolactone polyketone compounds having antineoplastic activity

A kind of polyketone compound, butyrolactone technology, applied in the field of medicine

Inactive Publication Date: 2012-08-01
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far there is no report on the isolation of γ-butyrolactone polyketide compounds simplexolides A and B with antitumor activity from sponges of this genus

Method used

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  • Gamma-butyrolactone polyketone compounds having antineoplastic activity
  • Gamma-butyrolactone polyketone compounds having antineoplastic activity
  • Gamma-butyrolactone polyketone compounds having antineoplastic activity

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Experimental program
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Embodiment 1

[0020] Example 1. Preparation of compounds simplexolides A and B

[0021] 1. Preparation of simple plank sponge extract extract

[0022] (1) Preparation of extract:

[0023] Take 2.0 kg of dried and pulverized simple flat plate sponge (Plakortis simplex), extract by percolating with 15L of methanol 4 times, each percolating for 3 days, and combine the extracts;

[0024] (2) Preparation of extract extract

[0025] The above-mentioned extract was concentrated under reduced pressure to obtain 500 g of extract extract;

[0026] 2. Separation and purification

[0027] 1) Disperse the above-mentioned extract extract in water to form a suspension, extract the suspension with n-hexane, dichloromethane, ethyl acetate and n-butanol in sequence, and concentrate the extract respectively to obtain 105 g of n-hexane extract extract; Dichloromethane extraction extract 41g; ethyl acetate extraction extract 1.2g and n-butanol extraction extract 22g;

[0028] 2) Extract the dichloromethane...

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Abstract

The invention relates to the technical field of medicines, in particular to novel gamma-butyrolactone polyketone compounds simplexolide A and simplexolide B having antineoplastic activity which are extracted from marine animal sponges and a preparation process and purposes of compounds. External antineoplastic experiments indicate that compounds simplexolide A and simplexolide B have obvious effects on activity inhibition of human colon cancer cells HCT-116 and SW480, so that compounds can be used for preparing antineoplastic medicines. According to the gamma-butyrolactone polyketone compounds having the antineoplastic activity, novel lead compounds are provided for preparing antineoplastic medicines and scientific evidences are provided for developing and using Chinese marine medicinal resources.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to gamma-butyrolactone polyketide simplexolides A and B isolated from marine animal sponges and having antitumor activity, as well as its preparation method and application. Background technique [0002] The sponge is a low-level multicellular animal that lives in an environment of low temperature, high pressure, high salt, and lack of sunlight. It often contains many metabolites with rare structures and strong biological activities. It can provide potential resources for the research of natural medicines. The simple flat sponge (Plakortis simplex) belongs to the class Demospongiae (Demospongiae) and the order Hamosclerophorida (Plakinidae) sponge. A large number of polyketide secondary metabolites have been isolated from sponges of this genus, the most characteristic of which are polyketide cyclic peroxides (Rahm F, Hayes P. Kitching W Metabolites from marine sponges of the genus P...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/33A61K31/365A61P35/00
Inventor 林厚文刘香芳杨帆郎俊慧刘彦儒陈万生
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY