Medicinal and Process Chemistry Division, Central Drug Research Institute (CSIR), Chattar Manzil Palace, M.G. Marg, Lucknow 226001, India.
Eur J Med Chem. 2011 Oct;46(10):5206-11. doi: 10.1016/j.ejmech.2011.08.012. Epub 2011 Aug 12.
Bioassay guided fractionation of the ethanolic extract of Polyalthia longifolia var. pendula, led to the discovery of the clerodane diterpene, 16α-hydroxycleroda-3, 13 (14) Z-dien-15, 16-olide (1), as a new structural class of HMG-CoA reductase inhibitor. Importantly, the in vivo effects of 1 corroborated well with its molecular docking analysis and also with its hamster plasma pharmacokinetics.
生物测定指导下对聚叶槌果藤变种pendula 的乙醇提取物进行分段分离,发现了新结构类型的 HMG-CoA 还原酶抑制剂,即 clerodane 二萜 16α-羟基克来若内酯(1)。重要的是,1 的体内作用与其分子对接分析以及仓鼠血浆药代动力学非常吻合。