Six new cytotoxic and anti-inflammatory 11,20-epoxy-ent-kaurane diterpenoids from Isodon wikstroemioides  

作　　者：WU Hai-Yan WANG Wei-Guang DU Xue YANG Jin PU Jian-Xin SUN Han-Dong 

机构地区：[1]State Key Laboratory of Phytochemistry and Plant Resources in West China,Kunming Institute of Botany,Chinese Academy of Sciences [2]University of Chinese Academy of Sciences

出　　处：《Chinese Journal of Natural Medicines》2015年第5期383-389,共7页中国天然药物（英文版）

基　　金：supported financially by the National Natural Science Foundation of China(Nos.21322204 and 81172939);the NSFC-Joint Foundation of Yunnan Province(No.U1302223);the reservation-talent project of Yunnan Province(No.2011CI043);the West Light Foundation of the Chinese Academy of Sciences(PU JX)

摘　　要：The present study was designed to determine the chemical constituents of Et OAc extracts of the aerial parts of Isodon wikstroemioides.Compounds 1–8 were isolated and purified by normal-phase silica gel and reversed-phase C18 silica gel column chromatography and HPLC.Their structures were elucidated by extensive spectroscopic methods.Most of them were evaluated for their in vitro cytotoxicity against human cancer HL-60,SMMC-7721,A-549,MCF-7,and SW-480 cells and their inhibitory activity against nitric oxide(NO) production in LPS-activated RAW264.7 macrophages.Among the eight 11,20-epoxy-ent-kauranoids isolated,compounds 1–6(isowikstroemins H–M) were new diterpenoids.Compounds 1,3,and 7 exhibited significant cytotoxicity with IC50 values ranging from(0.84 ± 0.02) to(4.09 ± 0.34) μmol·L-1,while compounds 4 and 5 showed selective cytotoxicity.In addition,compounds 1,3,4,and 7 exhibited inhibitory activity against nitric oxide(NO) production in LPS-activated RAW264.7 macrophages.These results provide a basis for future development of these compounds as anti-cancer and anti-inflammatory agents.The present study was designed to determine the chemical constituents of EtOAc extracts of the aerial parts of Isodon wikstroemioides. Compounds 1-8 were isolated and purified by normal-phase silica gel and reversed-phase C^8 silica gel column chromatography and HPLC. Their structures were elucidated by extensive spectroscopic methods. Most of them were evaluated for their in vitro cytotoxicity against human cancer HL-60, SMMC-7721, A-549, MCF-7, and SW-480 cells and their inhibitory activity against nitric oxide （NO） production in LPS-activated RAW264.7 macrophages. Among the eight 11, 20-epoxy-ent-kauranoids isolated, compounds 1-6 （isowikstroemins H-M） were new diterpenoids. Compounds 1, 3, and 7 exhibited significant cytotoxicity with IC50 values ranging from （0.84 ± 0.02） to （4.09 ±0.34） μmol·L-1, while compounds 4 and 5 showed selective cytotoxicity. In addition, compounds 1, 3, 4, and 7 exhibited inhibitory activity against nitric oxide （NO） production in LPS-aetivated RAW264.7 maerophages. These results provide a basis for future development of these compounds as anti-cancer and anti-inflammatory agents.

关 键 词：Isodon wikstroemioides Isowikstroemins H–M CYTOTOXICITY Anti-inflammatory activity 

分 类 号：R284[医药卫生—中药学]