Use of saponins compound echinoside A in sea pumpkin in preparing tumor topoisomerase II inhibitor

A technology of topoisomerase and compound, applied in the field of medicine

A technology of topoisomerase and compound, applied in the field of medicine

CN101336928AInactive Publication Date: 2009-01-07SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY +1
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  • Use of saponins compound echinoside A in sea pumpkin in preparing tumor topoisomerase II inhibitor
  • Use of saponins compound echinoside A in sea pumpkin in preparing tumor topoisomerase II inhibitor
  • Use of saponins compound echinoside A in sea pumpkin in preparing tumor topoisomerase II inhibitor

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Experimental program
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Effect test

Embodiment 1

[0033] Embodiment 1: the separation and preparation of echinoside A

[0034] Select 7,500 grams of black milk sea cucumber dry product grown in Dongshan sea area, Fujian, China, wash and chop, soak and extract with 5 times the weight of 70% ethanol successively for 3 times, each soaking for 7 days. The ethanol extracts were combined, and the ethanol was recovered under reduced pressure to obtain a liquid extract. The fluid extract was dissolved in 3 times the volume of water, and extracted 4 times with petroleum ether and water-saturated n-butanol successively, each time 2500ml of the extract. Combine the n-butanol extracts, recover the solvent until nearly dry, and evaporate to dryness in a water bath at 70°C to obtain 62 g of the total n-butanol extract of sea cucumber black milk.

[0035] The total extract was dry-loaded as usual, separated by silica gel column chromatography, eluted with about 3000ml of a mixed solvent of chloroform:methanol:water=8~6.5:2~3.5:1, collected...

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Abstract

The invention relates to an application of a saponin compound echinoside A extracted from sea cucumber in preparing tumor topoismerase II inhibitors, belonging to the technical field of pharmaceuticals. The compound echinoside A has a molecular formula of C54H87O26SNa, and the chemical structure and the spatial configuration of the compound are determined through analysis of multiple modern spectra including advanced two-dimensional nuclear magnetic resonance spectra. In vitro tests indicate that the compound has distinct inhibitory effect on tumor topoismerase II (Topo II), and is an effective Topo II inhibitor. The invention provides a lead compound for developing Topo II inhibitors, and is important for developing and unitizing Chinese ocean medicinal biological resources.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a new application of echinoside A, a sea cucumber triterpene saponin compound isolated from sea cucumber black milk sea cucumber, for the preparation of tumor topoisomerase II inhibitors and a preparation method thereof. Background technique [0002] Black Milk Sea Cucumber (Holothuria nobilis Selenka) is a species of Holothuria nobilis Selenka that grows in large numbers in the waters from Dongshan, Fujian, my country to Hainan Island. It belongs to the large species of Holothuria nobilis. blunt round. Black milk sea cucumber is one of the important edible sea cucumbers (edited by Liao Yulin, Chinese Zoology, Echinodermata, Sea Cucumber. Beijing: Science Press, 1997, 121-122), and it is often used as medicine in the folk, with nourishing and therapeutic properties Gynecological diseases and other functions. [0003] echinoside A is a sea cucumber triterpenoid saponin compound. K...

Claims

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Application Information

Patent Timeline
07 Jan 2009
Publication
CN101336928A
IPC
A61K31/7048; A61P35/00; C07J71/00; A61K35/56; A61K35/616
Inventors
易杨华; 丁健