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综述与进展

蕊木属生物碱arboridinine和arborisidine的全合成研究进展

何卫刚a,b,*, 段明月a, 闫帅a, 叶伟杰a, 徐雪园a, 孙先宇a,*   

  1. a苏州工学院 生物与食品工程学院 江苏常熟 215500;
    b中国药科大学 药学院 江苏南京 210009
  • 收稿日期:2025-07-15 修回日期:2025-09-04
  • 基金资助:
    国家自然科学基金(No. 22401019)资助项目.

Progress in the Total Synthesis of the Kopsia Alkaloids Arboridinine and Arborisidine

He Weiganga,b,*, Duan Mingyuea, Yan Shuaia, Ye Weijiea, Xu Xueyuana, Sun Xianyua,*   

  1. aSchool of Biology and Food Engineering, Suzhou University of Technology, Changshu, Jiangsu 215500;
    bSchool of Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu 210009
  • Received:2025-07-15 Revised:2025-09-04
  • Contact: *E-mail: heweigang@szut.edu.cn; sunxy@cslg.edu.cn
  • Supported by:
    National Natural Science Foundation of China (No. 22401019).

吲哚生物碱分布广泛、结构复杂,并具有丰富的药理活性,是目前天然产物全合成领域的研究热点。生物碱arboridinine和arborisidine是从马来西亚的蕊木属植物中分离得到的,这两个生物碱特殊而高度复杂的笼状结构使其全合成研究极具挑战性,因此得到了广泛关注。本文总结了arboridinine和arborisidine目前的全合成研究进展,以期为相关天然产物的全合成提供参考。

关键词: 生物碱, 全合成, Arboridinine, Arborisidine

Indole alkaloids are widely distributed in nature and have rich pharmacological activities, so many indole alkaloids have emerged as hot targets for the total synthesis of natural products. The alkaloids arboridinine and arborisidine were isolated from a plant of the Kopsia genus found in Malaysia by Kam and co-workers in 2015 and 2016, respectively. These two pentacyclic monoterpenoid indole alkaloids have unique caged skeleton with multiple chiral centers. The highly complex cage structure of these alkaloids has brought great challenges to their total synthesis research. In addition, studies have found that arborisidine exhibits clear anti-gastric cancer activity when combined with pimelautide. The complex and attractive chemical structure and potential pharmacological activity, together with an extremely low natural abundance make their total synthesis research extremely attractive. Soon after the isolation, their total synthesis research has received extensive and sustained attention. Up to now, the total synthesis of arboridinine has be achieved by the research groups of Snyder, Ma, Zhai and Li, and the total synthesis of arborisidine by the groups of Snyder, Ma, Zhu, Jiao, She and Gao. This review summarizes the research progress of total synthesis of arboridinine and arborisidine, in order to provide reference for the total synthesis of the related natural products.

Key words: Alkaloids, Total synthesis, Arboridinine, Arborisidine