药用植物中木脂素生物合成DIR基因研究进展  

Research progress in DIR gene of lignan biosynthesis in medicinal plants

作　　者：陈煜 刘久石 穆新路 董雨青 魏雪苹 李斌 齐耀东[1] 刘海涛[1] 张本刚[1] 肖培根[1] CHEN Yu;LIU Jiu-shi;MU Xin-lu;DONG Yu-qing;WEI Xue-ping;LI Bin;QI Yao-dong;LIU Hai-tao;ZHANG Ben-gang;XIAO Pei-gen(Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine,Ministry of Education,Institute of Medicinal Plant Development,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100193,China)

机构地区：[1]中国医学科学院,北京协和医学院药用植物研究所,中草药物质基础与资源利用教育部重点实验室,北京100193

出　　处：《中国中药杂志》2022年第11期2890-2898,共9页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(81872965)。

摘　　要：药用活性成分多来源于药用植物的次生代谢产物,是药用植物发挥药效的物质基础。木脂素是一类分布广泛,存在高效生物活性的植物次生代谢产物,在临床实践中,发现木脂素类化合物具有抗病毒、抗肿瘤、抗菌和抗氧化等活性。木脂素的化学结构多样,一般含有多个手性中心,且多具有旋光性,其生物合成要依赖植物体内的氧化偶合反应,该反应常常存在位置选择和立体选择,使合成的木脂素难以形成外消旋体,而主要以一种立体构型存在。Dirigent(DIR)是一类指导木脂素生物合成的蛋白,这种蛋白在指导木脂素合成的位置选择和立体选择上发挥着重要作用。关于木脂素类化合物生物合成的植物体外研究显示,缺少DIR蛋白参与时得到外消旋的终产物;DIR蛋白参与反应时,则可得到以一种立体构型存在的产物,表明DIR蛋白在植物次生代谢产物生物合成过程中起不对称诱导作用。该研究系统综述了DIR蛋白的生物学意义,DIR基因的克隆情况、基因结构、催化机制以及在菘蓝、杜仲、连翘、丹参、三七和五味子等药用植物中的研究进展,为DIR基因的后续研究工作提供参考。The active components, mainly derived from secondary metabolites of medicinal plants, are the material basis for the efficacy of medicinal plants. Lignans, the secondary metabolites in plants with high bioactivity, are widely distributed in a variety of plant species, and their antiviral, antitumor, antibacterial, and antioxidant activities have been proved in clinical practice. Generally, lignans are diverse in structures with many chiral centers, and most of them are optically active. The biosynthesis of lignans depends on the oxidative coupling reaction through site selection and stereo selection, which impedes synthesized lignans to form racemates, but makes them in a three-dimensional configuration. Dirigent protein(DIR) plays an important role in guiding location selection and stereo selection of lignans in biosynthesis. In vitro studies on lignan biosynthesis have shown that racemic end products are obtained in the absence of DIR proteins, while the products in a three-dimensional configuration can be yielded in the presence of DIR proteins, indicating that DIR proteins play an asymmetric role in the biosynthesis of plant secondary metabolites. The present study reviewed the biolo-gical significance of DIR protein, the cloning of DIR gene, gene structure, catalytic mechanism, and the research progress in Isatis indigotica, Eucommia ulmoides, Forsythia suspensa, Salvia miltiorrhiza, Panax pseudoginseng var. notoginseng, and Schisandra chinensis, which provides a reference for the follow-up research of DIR gene.

关 键 词：DIR 木脂素 立体构型 氧化偶合 生物合成 

分 类 号：R284.1[医药卫生—中药学]