Cyclic heptapeptide compound in Hsisha sponge and application thereof

A compound and cyclic heptapeptide technology, applied in the directions of cyclic peptide components, peptides, drug combinations, etc., can solve the problems of cyclic heptapeptide compounds with no anti-tumor activity, and achieve the effects of significant anti-tumor activity and simple preparation method.

Inactive Publication Date: 2009-09-02
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Abstract
  • Description
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AI Technical Summary

Problems solved by technology

All previous Phakellistatins cyclic peptide compounds were discovered by the Pettit group of Arizona State University from the sponge of the genus Phakellia, but so far there have been no reports on new cyclic heptapeptide compounds with antitumor activity

Method used

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  • Cyclic heptapeptide compound in Hsisha sponge and application thereof
  • Cyclic heptapeptide compound in Hsisha sponge and application thereof
  • Cyclic heptapeptide compound in Hsisha sponge and application thereof

Examples

Experimental program
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Embodiment 1

[0014] Embodiment 1. Preparation of compounds of the present invention

[0015] Take 15 kg of dried and pulverized brown flat sponge, extract by cold soaking in 50 L of 95% ethanol for 8 times, each time for one week, combine the extracts, concentrate the extracts under reduced pressure to obtain extracts, and extract with 50% ethyl acetate aqueous solution, To obtain the total ethyl acetate extract, suspend the total ethyl acetate extract with 90% methanol, degrease with petroleum ether, add water to adjust the methanol concentration of the suspension to 60%, extract 3 times with dichloromethane, and concentrate Extract, get crude extract 55g;

[0016] 55 g of the above-mentioned crude extract was passed through a Sephadex LH-20 gel column, and the 2 Cl 2 -MeOH=1:1 elution, according to the thin layer chromatography detection results, collect the eluate containing cyclic peptide compounds, and then perform reverse phase silica gel column chromatography, use methanol with a ...

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PUM

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Abstract

The invention relates to the technical field of medicaments, which is a novel cyclic heptapeptide compound with antineoplastic activity produced from a marine animal Phakellia fusca in the territorial waters near Hsisha Islands. The chemical structural formula of the novel cyclic heptapeptide compound is shown as the right formula. The in vitro activity test proves that the compound has certain inhibiting activity for various tumour cells, wherein the IC50 value of SPC-A-1 cells is only 31.4 mu g/ml and is superior to a positive control medicament vincristine, so the cyclic heptapeptide compound can be used for preparing antitumor medicaments. The invention provides a lead compound for developing a novel antitumor medicament.

Description

technical field [0001] The invention relates to the technical field of medicine, and is a novel cyclic heptapeptide compound with antitumor activity, which is produced in the marine animal brown flat sponge Phakellia fusca in the sea area near Xisha Islands. Background technique [0002] The sponge is a low-level multicellular animal, which is widely distributed but often contains many secondary metabolites with rare structures and anticancer activities. Therefore, it has always been the first choice of marine biological research objects for marine natural product chemists. The drug source material of the present invention, the Phakellia fusca sponge, belongs to the sponge family Axinellidae of the class Demospongiae and the order Halichondrida. In 2002, a new cyclic peptide phakelliastatin 12 was discovered from the P.fusca sponge collected from Yongxing Island, Xisha, South my country Sea, and a patent has been applied for (application number: 01113389.9). All previous Ph...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/64A61K38/12A61P35/00
Inventor 林厚文张红军杨帆陈万生
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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