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Linear chain polyketone compounds and application thereof

A technology of polyketide compounds and compounds, applied in the field of medicine

Inactive Publication Date: 2011-10-19
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, no chain polyketide C with anti-tumor or protein tyrosine phosphatase (protein tyrosinephosphatase, PTP1B) activity has been isolated from this genus of sponges so far. 17 h 32 o 4 report

Method used

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  • Linear chain polyketone compounds and application thereof
  • Linear chain polyketone compounds and application thereof
  • Linear chain polyketone compounds and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1. Preparation of Compound C 17 h 32 o 4

[0017] 1. Preparation of simple plank sponge extract extract

[0018] (1) Preparation of extract:

[0019] Take 2.0 kg of dry and pulverized simple flat plate sponge (Plakortis simplex) and use 15L methanol to percolate and extract 4 times, each time percolating for 3 days, and combine the extracts;

[0020] (2) Preparation of extract extract

[0021] The above-mentioned extract was concentrated under reduced pressure to obtain 500 g of extract extract;

[0022] 2. Separation and purification

[0023] 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;

[0024] 2) Extract the dichloromethane e...

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Abstract

The invention relates to the technical field of medicines, in particular to linear chain polyketone compounds separated from marine poriferans and application thereof in preparation of medicines for treating tumors, diabetes and obesity or inhibitors for protein tyrosine phosphatase-1B(PTP1B). The in vitro anti-tumor tests and the PTP1B inhibition tests show that the compound C17H32O4 has obvious inhibiting activity on human colon cancer cells HCT-116 and PTP1B, so that the compound can be used for preparing anti-tumor medicines or PTP1B inhibitors and medicines for treating diabetes, obesity and complications caused by diabetes and obesity. The invention provides novel lead compounds for developing new anti-tumor medicines or medicines for treating diabetes and obesity, and has great significance for the development and the utilization of Chinese marine medical biological resources.

Description

technical field [0001] The invention relates to the technical field of medicine, and is a chain polyketide compound isolated from marine animal sponges and its use in the preparation of drugs for treating tumors, diabetes, obesity or protein tyrosine phosphatase (PTP1B) inhibitors Applications. 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 drug source material Plakortis simplex of the present invention belongs to the sponge family Plakinidae of the class Demospongiae and the order Hamosclerophorida. A large number of polyketide secondary metabolites have been isolated from sponges of this genus, the most characteristic of which is the polyketide cyclic peroxide (Rahm F, Hayes P. Kit...

Claims

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Application Information

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IPC IPC(8): C07C59/42C07C51/43A61K31/201A61P35/00A61P3/10A61P3/04
Inventor 林厚文刘香芳于豪冰徐影王茹萍焦伟华陈万生
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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