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Cytospolides with anti-tumor and antibacterial activity

A technology of ester compounds and anti-tumor drugs, applied in the field of medicine

Active Publication Date: 2013-01-23
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

But so far there is no report on the isolation of ten-membered ring lactone compounds Cytospolides A~P with antitumor and antibacterial activities from the endophytic fungus Cytospora sp.

Method used

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  • Cytospolides with anti-tumor and antibacterial activity
  • Cytospolides with anti-tumor and antibacterial activity

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Experimental program
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Embodiment 1

[0055] Embodiment 1. preparation compound Cytospolides A~P

[0056] 18.7g of the endophytic fungus Cytospora sp. fermentation product (provided by the University of Braunschweig, Germany) was completely dissolved in 10ml of chloroform, separated by normal phase silica gel chromatography (200-300 mesh) as usual, and separated by dichloromethane: acetone volume ratio Carry out gradient elution for 100:1, 80:20, 50:50, 30:70, 1:100 eluents, and collect 18 partial elutions according to the difference in polarity from small to large according to TLC monitoring Liquid Fr 1 ~ Fr18. Each part was separated by normal phase silica gel, reversed phase silica gel, Sephadex LH-20 and HPLC and other modern chromatographic separation techniques to obtain 16 new compounds: Cytospolide A (5.0 mg), Cytospolide B (2.4 mg), Cytospolide C ( 600.0mg), Cytospolides D (9.3mg), Cytospolides E (6.0mg), Cytospolides F (10.0mg), Cytospolides G (5.4mg), Cytospolides H (0.9mg), Cytospolides I and J (6.1mg...

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Abstract

The invention relates to the technical field of medicines, in particular to 16 cytospolides A-P which are separated from a plant endophytic fungus cytospora sp. fermentation product and have anti-tumor and antibacterial activity. The in-vitro anti-tumor test proves that the cytospolides A-P have the effect of obviously inhibiting HCT116 (human colon cancer cells), A549 (human lung cancer cells), QGY-7703 (human liver cancer cells), A375 (human melanoma cells), and U937 (human leukemia cells) tumor cell strains; and the in-vitro antibacterial test proves that the cytospolides A-P have the effect of obviously inhibiting microbotryum violaceum, septoria tritici, Escherichia coli and bacillus megaterium. Therefore, the cytospolides A-P can be used for preparing anti-tumor or antibacterial medicines, are novel lead compounds for developing the anti-tumor and antibacterial medicines, and have great significance for developing and utilizing plant endophyte resources.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a class of 16 ten-membered ring lactone compounds Cytospolides A~P with antitumor and antibacterial activities isolated from the fermented product of endophytic fungus Cytospora sp. Background technique [0002] Endophytic fungus is a class of fungi that exist in the stems and leaves of healthy plants and form insignificant infections. As the main microbial species, endophytic fungi have a large variety and quantity, and they distribute a wide range of host plants. The diversity of the micro-ecological system in which they live, coupled with the diversity of the ecological environment in which the host plants themselves live, so their secondary metabolites It also has rich diversity and can provide rich potential resources for the research of natural medicines. The endophytic fungus Cytospora sp. belongs to Deuteromycotina, Coelomycetes, Sphaeropsidales and Cytospora fungi. Cyto...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D313/00C07D493/08A61K31/365A61P35/00A61P35/02A61P31/04A61P31/10
CPCY02A50/30
Inventor 张文李玲卢山易杨华孙鹏汤华刘宝姝
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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