银杏内酯类化合物的来源、结构修饰与新剂型研究进展

Research Progress on Sources, Structural Modification and New Dosage Forms of Ginkgolides

  • 摘要: 银杏内酯是从银杏叶、根中分离得到一类萜内酯类化合物,作为强效血小板活化因子(Platelet activating factor,PAF)拮抗剂以及非特异性甘氨酸受体(Glycine receptor,GlyR)和γ-氨基丁酸(γ-Amino-Bu-Tyric acid,GABA)受体拮抗剂,目前广泛用于心脑血管疾病。自发现银杏叶提取物中的内酯成分的PAF拮抗活性后,众多科学家对此类化合物的构效关系、结构修饰、药理药效方面开展了大量研究。作为天然药物银杏内酯有着疗效好、毒副作用小的优势,具有良好的发展趋势,银杏内酯、银杏内酯衍生物及其制剂的研发将会带来更好的经济效益和社会效益,造福人类。本文对银杏内酯的研究及最新进展进行综述,并回顾其开发历程及相关研究,以期为天然药物的开发带来新的思考。

     

    Abstract: Ginkgolide is a kind of azlactone compound isolated from Ginkgo biloba leaves and roots. It acts as a potent platelet activating factor (PAF) antagonist and non-specific Glycine receptor (GlyR) and γ- Γ-Amino-Bu-Tyric acid (GABA) receptor antagonists are widely used in cardiovascular and cerebrovascular diseases. Since the discovery of PAF antagonistic activity of lactone components in Ginkgo biloba extract, many scientists have conducted extensive research on the structure-activity relationship, structural modification, and pharmacological effects of such compounds. As a natural drug, ginkgolides have the advantages of good curative effect and small side effects, and have a good development trend. The research and development of ginkgolides, ginkgolides and their preparations will bring better economic and social benefits. For the benefit of mankind. This article reviews the research and recent progress of ginkgolides, and reviews its development process and related research, with a view to bringing new thinking to the development of natural medicines.

     

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