银杏内酯衍生物和类似物的合成及PAFR和GlyR拮抗活性研究进展

Progress in Synthesis and Antagonistic Activities towards PAFR and GlyR of Ginkgolide Derivatives and Analogs

银杏内酯是从银杏树中分离的二萜内酯成分,它的结构是由6个五元环形成的笼状骨架并嵌有一个独特的叔丁基.研究已证实银杏内酯是血小板活化因子受体(PAFR)和甘氨酸受体(GlyR)的强有力拮抗剂,它的结构变化将引起生物活性的改变.因此,为了寻找更优的PAFR和GlyR拮抗剂,人们合成了许多银杏内酯衍生物及类似物.重点综述了近年来银杏内酯类化合物的构效关系研究.

Ginkgolides are diterpene trilactones with a cage-like skeleton consisting of six five-membered rings and a unique t-Bu group from Ginkgo biloba tree. Many studies have demonstrated that they are highly potent and selective antagonists of platelet activating factor receptor （PAFR） and glycine receptor （GlyR）. Ginkgolide skeleton modifications may conduce to physiological activities variation. Therefore, many ginkgolide derivatives and analogs have been synthesized for the optimal antagonistic activities towards PAFR or GlyR. This review covers the structure-activity relationship studies of ginkgolide derivatives and analogs.