Since long back, several plants species belonging to family Lycopodiaceae or Huperziaceae are being traditionally used in treatment of diseases like Alzheimer’s disease and myasthenia gravis. In 1986, huperzine A, structurally lycodine type of alkaloid was isolated and established as potent acetylcholine esterase inhibitor. Hence, further, in pursuit of similar compounds, several hundreds of different types of lycopodium alkaloids have been isolated from different Lycopodiaceae or Huperziaceae plants species. For few of these recently isolated alkaloids, the possible mechanisms of their biosynthesis have been proposed while few of them were tried for their laboratory total asymmetric synthesis. This review summarized lycodine-type Lycopodium alkaloids, whose isolation, biosynthesis, and total synthesis have been reported after 2000. It also includes structure–activity relationship. More than 40 lycodine-type alkaloids have been isolated and structurally elucidated since 2000. Their biosynthetic pathway suggested that they got biosynthesized from lysine, while structure–activity relationship established the structural requirement of lycodine-type alkaloids to possess potent acetylcholine esterase inhibitory activity.

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最近分离lycodine型石松生物碱及其全合成：回顾

早在很久以前，传统上就使用属于番茄科或石杉科的几种植物来治疗诸如阿尔茨海默氏病和重症肌无力等疾病。1986年，分离出石杉碱甲（一种结构上属于莱考定的生物碱）并将其确立为有效的乙酰胆碱酯酶抑制剂。因此，进一步地，为了追求相似的化合物，已经从不同的番茄科或虎尾草科植物物种中分离了数百种不同类型的番茄科生物碱。对于这些近来分离的生物碱中的几种，已提出了其生物合成的可能机理，而对于其中的实验室完全不对称合成，则进行了尝试。这篇综述总结了lycodine型Lycopodium生物碱，其分离，生物合成和全合成已在2000年后报道。它还包括结构－活动关系。自2000年以来，已经分离并结构阐明了40多种lycodine型生物碱。它们的生物合成途径表明，它们是从赖氨酸中生物合成的，而构效关系确定了lycodine型生物碱具有强大的乙酰胆碱酯酶抑制活性的结构要求。