新型抗肿瘤抗生素布雷菲德菌素A的研究进展

Advance in the Antitumor Drug Development of Brefeldin A

布雷菲德菌素A是一种天然存在的大环内酯类抗生素,能有效抑制蛋白质由内质网向高尔基体的转运过程,是一种广泛应用于哺乳动物信号传导研究的分子工具;布雷菲德菌素A具有抗真菌、抗病毒、抗有丝分裂、抗肿瘤等生物学活性,布雷菲德菌素A及其衍生物是重要的抗肿瘤候选药。本文综述了布雷菲德菌素A的理化性质、作用机制、生物学活性、生产方法及其结构修饰等方面的研究进展。

Brefeldin A,a hydrophobic macrolide antibiotic produced by a number of fungi,displays strong inhibition activity against the transport of proteins from the endoplasmic reticulum to the Golgi complex, resulting in its wide use as a molecular tool in the studies signal transduction pathways in mammalian cells. Moreover,it has diverse biological activi- ties including antifungal, antiviral,cytostatic,antimitotic and antitumor effects, making brefeldin A and its derivatives an- titumor drug candidates. This article reviewed the recent progress in brefeldin A research,focusing on its physicochemical properties, molecular mechanism of action, biological activities, production, and structural modification.