天然产物曲地酸及其类似物研究进展

Progress in the studies on natural product asterric acid and its analogues

曲地酸(asterric acid)及其类似物是从一些曲霉和青霉等真菌的发酵液中提取分离得到的一类含二苯醚结构的化合物,具有抗菌、抗肿瘤等医药活性以及杀菌、杀线虫及抑制水芹种子萌芽等农药活性,其中曲地酸作为血管内皮生长因子(VEGF)抑制剂和抗生素已被制成为商品化的生物试剂,应用于生物和医学相关领域的研究。对曲地酸及其类似物的来源、结构及物理性质、生物合成及代谢机理,以及其医用和农用活性方面的研究进展进行了综述,对其化学合成及结构改造的前景进行了展望。

Asterric acid and its derivatives, possessing a diphenyl ether structure, were isolated from a number of AspergiUus and Penicillium species＇ culture. They exhibited good or excellent medicinal activity and pesticide activity such as antifungal, antibacterial, cytototoxic activity, fungicidal activity, nematicidal activity and seed germination inhibition of water dropwort and so on. In particularly, asterric acid as an inhibitor of vascular endothelial growth factor （VEGF） has commercialized as biochemical reagent and was applied to the studies on biology and medicine. The advances in the isolation, structures and biological activity of asterric acid and its derivatives have been reviewed. Their biosynthetic and metabolic mechanism, total synthesis and structure modification have been also introduced.