微生物来源的Xa因子抑制剂F02-2172的研究

利用一种由本中心建立的Xa因子抑制剂高通量体外筛选模型，从大量真菌菌库及其来源的代谢产物中筛选到了一株可产生阳性活性化合物的菌株F02ZA-2172，该菌株的发酵液经有机溶剂提取、硅胶柱色谱、ODS柱色谱、Sephadex LH-20柱色谱及HPLC制备分离，得到F02-2172A、B和C三个活性化合物。经紫外、质谱、核磁等理化数据分析，确定这三个化合物分别与已知化合物6-epi-ophiobolinK、ophiobolin K和ophiobolin G的结构相同，但该类化合物对Xa因子的抑制活性至今未见报道。

F02-2172, factor Xa inhibitors from metabolites of microorganisms

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.