倍半萜环化机制研究方法进展  

Research advances in methods of cyclezation mechanism of sesquiterpenes

作　　者：邵一珍 里雨桐 巩婷[1] 朱平[1] 庾石山[1] SHAO Yi-zhen;LI Yu-tong;GONG Ting;ZHU Ping;YU Shi-shan(State Key Laboratory of Bioactive Substance and Function of Natural Medicines,Institute of Materia Medica,Chinese Academy of Medical Sciences&Peking Union Medical College,Beijing 100050,China)

机构地区：[1]中国医学科学院,北京协和医学院药物研究所,天然产物活性物质与功能国家重点实验室,北京100050

出　　处：《中国中药杂志》2021年第15期3797-3805,共9页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金重点项目(21732008)。

摘　　要：在天然产物中,萜类化合物数量最多并且包含非常丰富的骨架结构,萜类化合物的环化反应也是自然界中发现的最复杂反应之一。长期以来,结构多样的萜类化合物一直吸引着天然产物化学家去探索其生物合成机制。萜类合酶的酶催化形成了大量的萜类骨架。倍半萜合酶是萜类合酶中的一种,可催化线性的前体法尼基焦磷酸环化成倍半萜骨架。倍半萜合酶可以将单一的法尼基焦磷酸环化成种类丰富的倍半萜骨架。随着倍半萜合酶的不断发现,其环化机制的研究也逐渐深入。近年来,对底物法尼基焦磷酸的同位素标记以及倍半萜合酶的结构解析等方法的发展和完善,使得倍半萜合酶的结构及环化机制研究更为系统和精确。该文分别概述了通过底物同位素标记和蛋白结构研究对倍半萜环化机制的研究方法进展,以及对于倍半萜合酶研究的总结与展望。Terpenes are the largest group of natural products and contain the widest assortment of structural types. Terpene cyclization is also the most complex reaction found in nature. For a long time, terpenoids with diverse structures have attracted natural product chemists to explore their biosynthesis mechanism. Such a large number of terpene skeletons are catalyzed by enzymes called terpene synthase. Sesquiterpene synthase is a kind of terpene synthase, which can catalyze the cyclization of linear precursor farnesyl pyrophosphate(FPP) to sesquiterpene skeletons. Sesquiterpene synthase cyclize a single precursor FPP into many sesquiterpene skeletons. With the continuous discovery of sesquiterpene synthase, the cyclization mechanism of sesquiterpene synthase has been studied deeply. In recent years, with the development and improvement of isotope labeling of substrate FPP and structural analysis of sesquiterpene synthase, the structure and cyclization mechanism of sesquiterpene synthase have been studied more systematically and accurately. In this review, we reviewed the progress of the research methods on the mechanism of sesquiterpene cyclization by substrate isotope labeling and protein structure, as well as the summary and prospect of sesquiterpene synthase research.

关 键 词：倍半萜合酶 蛋白结晶 同位素标记 环化机制 

分 类 号：R284[医药卫生—中药学]