Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Cyclic octapeptide compound in Hsisha sponge and application thereof

A compound and cyclic octapeptide technology, which can be applied to cyclic peptide components, peptides, drug combinations, etc., can solve the problems of cyclic octapeptide 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
View PDF1 Cites 10 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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 octapeptide compounds with anti-tumor activity

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Cyclic octapeptide compound in Hsisha sponge and application thereof
  • Cyclic octapeptide compound in Hsisha sponge and application thereof
  • Cyclic octapeptide compound in Hsisha sponge and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1. Preparation of compounds of the present invention

[0027] 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;

[0028] 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 ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to the technical field of medicaments, which is a novel cyclic octapeptide 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 octapeptide compound is shown as a formula (I), wherein a group R1 is expressed as a formula (II), R2 represents CH (CH3)2or CHCH3(CH2CH3), R3 represents CH2CH (CH3)2, R4 represents CHCH3(CH2CH3)or CHOH (CH3), and R5 represents CHCH3(CH2CH3)or CH2CH (CH3)2. The in vitro activity test proves that the compound has certain inhibiting activity for various tumour cells, wherein the IC50 value of a mouse P388 is only 7.8 mu g / ml and is superior to a positive control medicament vincristine, so the cyclic octapeptide 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 octapeptide compound with antitumor activity 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 anti-cancer activities, so 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 Phakellistatins cyc...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07K7/64A61K38/12A61P35/00
Inventor 林厚文张红军杨帆朴淑娟陈万生
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com