Klochkov Sergey, Neganova Margarita
Institute of Physiologically Active Compounds Russian Academy of Sciences Chernogolovka Russia
RSC Adv. 2021 May 26;11(31):19185-19195. doi: 10.1039/d1ra02558a. eCollection 2021 May 24.
Alkaloids, secondary plant metabolites, are used in traditional medicine in many countries to treat various pathological conditions. Securinine, a unique indolizidine alkaloid combining four cycles, "6-azobicyclo[3.2.1]octane" as a key structure fused with α,β-unsaturated-γ-lactone and piperidine ring, has a broad spectrum of actions including anti-inflammatory, antibacterial, neuroprotective and antitumor, and has been previously used in medical practice. It has several reactive centers, which are double bonds at positions 12-13 and 14-15, and this is a challenging scaffold for the synthesis of biologically active compounds. In this review, works on the production of modified securinine derivatives and their biological activity are addressed. Both monovalent and bivalent derivatives that are most promising in our opinion, and have potential for further research, are considered.
生物碱作为植物次生代谢产物，在许多国家的传统医学中用于治疗各种病理状况。一叶萩碱是一种独特的吲哚里西啶生物碱，它结合了四个环，“6-氮杂双环[3.2.1]辛烷”作为关键结构与α,β-不饱和-γ-内酯和哌啶环稠合，具有广泛的作用，包括抗炎、抗菌、神经保护和抗肿瘤作用，并且此前已应用于医学实践。它有几个反应中心，位于12-13位和14-15位的双键，这对于合成生物活性化合物来说是一个具有挑战性的骨架。在这篇综述中，将探讨修饰一叶萩碱衍生物的制备及其生物活性的相关研究。本文考虑了单价和二价衍生物，我们认为它们最具前景，并且有进一步研究的潜力。
