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埃博霉素(epothilones)是黏细菌纤维堆囊菌(Sorangium cellulosum)产生的一类聚酮次级代谢产物,与临床上广泛应用的抗肿瘤化疗药物紫杉醇具有相同的稳定微管活性,且对紫杉醇耐药的肿瘤细胞亦具有活性。目前多个埃博霉素药物在进行临床试验。其中发酵产量成为该药研发的重点。文中综述埃博霉素在生物合成方面的相关研究进展,主要介绍近年来通过遗传和生化等途径对埃博霉素基因簇结构特征以及合成酶特性方面的相关研究和前景。
Epothilones, a class of polyketide secondary metabolites produced by Sorangium cellulosum, have the same stable microtubule activity as Paclitaxel, a widely used anticancer chemotherapeutic drug in clinic. Taxol-resistant tumor cells are also active. Several epothilone drugs are currently undergoing clinical trials. Among them, the fermentation yield has become the focus of the drug research and development. This review summarizes the progress of research on the biosynthesis of epothilone, and mainly introduces the related research and prospects of the epothilones gene cluster structure and the characteristics of the synthase in recent years through genetic and biochemical methods.