Yan Huan, Ba Ming-Yu, Li Xu-Hong, Guo Jia-Mei, Qin Xu-Jie, He Li, Zhang Zhong-Quan, Guo Ying, Liu Hai-Yang
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China; Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China.
Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Fitoterapia. 2016 Dec;115:64-68. doi: 10.1016/j.fitote.2016.09.023. Epub 2016 Oct 2.
Phytochemical investigation on the whole plant of Chloranthus japonicus (Chloranthaceae) led to the isolation and identification of three new lindenane-type sesquiterpenoid dimers, chlorajaponilides F-H (1-3), along with seven known ones (4-10). Their chemical structures were established by extensive spectral evidence. Compounds 1 and 2 are both dimeric sesquiterpenoids featuring a rare hydroperoxy group at C-5. All compounds were tested for their activities on wild type HIV-1 replication and compounds 1, 2, 5, and 9 were effective with EC values from 3.08 to 17.16μM. All these four compounds showed the same inhibitory effects on the two NNRTI-resistant HIV strains as on wild-type HIV-1 with EC change folds from 0.61 to 1.6μM. Furthermore, compounds 1, 5, and 9 exhibited inhibitory activities on HCV replication with the similar potency as their activities on HIV-1. Our finding may provide a clue to address the problem of HIV-1 and HCV co-infection.
对日本金粟兰（金粟兰科）全株进行的植物化学研究，导致分离并鉴定出三种新的椴烷型倍半萜二聚体，即日本金粟兰内酯F - H（1 - 3），以及七种已知化合物（4 - 10）。它们的化学结构通过广泛的光谱证据得以确定。化合物1和2均为二聚倍半萜，在C - 5位具有罕见的氢过氧基。对所有化合物进行了针对野生型HIV - 1复制活性的测试，化合物1、2、5和9具有活性，EC值为3.08至17.16μM。这四种化合物对两种耐非核苷类逆转录酶抑制剂（NNRTI）的HIV毒株显示出与对野生型HIV - 1相同的抑制作用，EC变化倍数为0.61至1.6μM。此外，化合物1、5和9对丙型肝炎病毒（HCV）复制表现出抑制活性，其效力与其对HIV - 1的活性相似。我们的发现可能为解决HIV - 1和HCV合并感染问题提供线索。
