Factor Xa inhibitor of microbial origin of F02 2172.docVIP

 PAGE \* MERGEFORMAT 16 Factor Xa inhibitor of microbial origin of F02 2172 Author: Lu Xinhua, the wisdom of Ma Ying Zheng quartz DONG Yue-sheng Ren Mu Dong Hua He Jiangong Abstract Using a center set up by the factor Xa inhibitor, high-throughput in vitro screening model, a large number of fungal strains from the library and its sources of metabolites can be screened to generate a positive active compounds strains F02ZA  2172, the strain The fermentation broth by organic solvent extraction, silica gel column chromatography, ODS column chromatography, Sephadex LH  20 column chromatography and HPLC preparation of separation, to be F02  2172A, B, and C three active compounds. By UV, MS, NMR and other physical and chemical data analysis to determine the three compounds were known compounds, 6  epi  ophiobolin K, ophiobolin K and ophiobolin G the structure of the same, but this kind of compounds on the inhibitory activity of factor Xa has not been reported. Keywords: factor Xa inhibitor of microbial twice sesquiterpenes F02  2172, factor Xa inhibitors from metabolites of microorganisms ABSTRACT A high throughput screening model was established for screening factor Xa inhibitors from thousands of strains of fungi, as a result, a strain, F02ZA  2172 with potent suppression activity was isolated. The culture broth of it was processed by solvent extraction, silica column chromatography, Sephadex LH  20 column chromatography and ODS HPLC preparation to obtain three pure active compounds named F02  2172A, B and C. Their chemical structures were elucidated as the compounds named 6  epi  ophiobolin K, ophiobolin K and ophiobolin G by physicochemical properties and spectral data of UV, MS, 1H  NMR and 13C  NMR respectively. The compounds are reported as factor Xa inhibitors for the first time. KEY WORDS Microorganisms; Factor Xa inhibitor; Sesterterpenes Thrombosis are cardiovascular diseases (such as myocardi