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目的筛选细胞凋亡相关疾病中重要靶点——卡斯帕酶-3抑制剂。方法利用自建的快速、高效、高通量的卡斯帕酶-3抑制剂的筛选方法,从数千株菌株中筛选阳性菌株。阳性菌株的发酵产物进行分离纯化获得活性化合物,再通过对活性化合物的紫外、质谱、核磁等理化数据的分析进行结构鉴定。结果筛选得到一个活性化合物F03ZA-673A。该化合物对卡斯帕酶-3有较强的抑制活性,IC50=21.1μmol.L-1,它与L-671,776结构相同。结论F03ZA-673 A为一个活性较强的微生物来源卡斯帕酶-3特异性的抑制剂,该化合物对卡斯帕酶-3的抑制活性未见国内外报道。
Objective To screen Caspase-3 inhibitor, an important target of apoptosis-related diseases. Methods A rapid, efficient and high-throughput screening method of Caspase-3 inhibitor was used to screen positive strains from thousands of strains. The active compounds were isolated and purified from the fermentation products of the positive strains. The structures of the active compounds were identified by the analysis of physico-chemical data such as UV, MS and NMR. As a result, an active compound F03ZA-673A was screened. This compound has a strong inhibitory activity against caspase-3, IC50 = 21.1 μmol.L-1, which has the same structure as L-671,776. Conclusion F03ZA-673 A is a specific inhibitor of caspase-3, a strong active microbial source. The inhibitory activity of this compound on caspase-3 has not been reported in China and abroad.