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.