Tang Junhao, Ma Ying, Zhao Yujun, Ma Xiaohui, Wang Jian
College of Traditional Chinese Medicine, Yunnan University of Chinese Medicine, Kunming 650500, China.
State Key Laboratory for Quality Ensurance and Sustainable Use of Dao-di Herbs, National Resource Center for Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
Molecules. 2025 May 18;30(10):2208. doi: 10.3390/molecules30102208.
Terpenoids have significant biological activity and good clinical efficacy and are important for defence and physiological regulation in plants. Andrographolide and similar labdane-related diterpenoids have been isolated and characterized as the main medicinal constituents of drugs from . To better study the diversity of terpenoids of , a total of 39 were screened, and 27 full-length genes encoding ApTPSs were obtained. The results showed that ApTPS4 could convert GGPP to -CPP and that ApTPS5 could convert -CPP to kaurene. This study first identified six sesquiterpene synthases with biological activity and also indicated the presence of sesquiterpenes with multiple skeletons in . The increase in the number of -copalyl diphosphate synthases and the loss of biological function by most sesquiterpene synthases and monoterpene synthases may explain why diterpenoids are the main specific metabolites in compared with the metabolites produced by AtTPSs found in the genome. As revealed by site-directed mutagenesis, 533Val of ApTPS16 is an important site for maintaining the single main product capability, and 534Tyr of ApTPS17 may also be more important. The ApTPS17 Y534V mutation caused it to lose its main biological function. This study characterized a novel -copalyl diphosphate synthase and six sesquiterpene synthases. This provided evidence for the existence of other terpenoids and revealed the diversity of chemical components, providing a reference for future pharmacological research for .
萜类化合物具有显著的生物活性和良好的临床疗效,对植物的防御和生理调节具有重要作用。穿心莲内酯和类似的与半日花烷相关的二萜类化合物已被分离并鉴定为穿心莲药物的主要药用成分。为了更好地研究穿心莲萜类化合物的多样性,共筛选了39个基因,获得了27个编码穿心莲萜类合酶(ApTPSs)的全长基因。结果表明,ApTPS4可以将牻牛儿基牻牛儿基焦磷酸(GGPP)转化为 - 古巴焦磷酸(-CPP),ApTPS5可以将 -CPP转化为贝壳杉烯。本研究首次鉴定出6种具有生物活性的倍半萜合酶,也表明穿心莲中存在具有多种骨架的倍半萜。与拟南芥基因组中AtTPSs产生的代谢产物相比,- 柯巴基二磷酸合酶数量的增加以及大多数倍半萜合酶和单萜合酶生物功能的丧失,可能解释了为什么二萜类化合物是穿心莲中的主要特异性代谢产物。定点诱变结果表明,ApTPS16的533Val是维持单一主要产物能力的重要位点,ApTPS17的534Tyr可能也更重要。ApTPS17的Y534V突变导致其失去主要生物功能。本研究对一种新型的 - 柯巴基二磷酸合酶和6种倍半萜合酶进行了表征。这为其他萜类化合物的存在提供了证据,揭示了化学成分的多样性,为穿心莲未来的药理研究提供了参考。