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Six new cytotoxic and anti-inflammatory 11, 20-epoxy-entkaurane diterpenoids from Isodon wikstroemioides
  • ISSN号:2095-6975
  • 期刊名称:《中国天然药物:英文版》
  • 时间:0
  • 分类:R284[医药卫生—中药学;医药卫生—中医学]
  • 作者机构:[1]State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy ofSciences, Kunming 650201, China, [2]University of Chinese Academy of Sciences, Beijing 100049, China
  • 相关基金:This work was 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), and the West Light Foundation of the Chinese Academy of Sciences (PU JX).
中文摘要:

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.

英文摘要:

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.

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期刊信息
  • 《中国天然药物:英文版》
  • 北大核心期刊(2008版)
  • 主管单位:中华人民共和国教育部
  • 主办单位:中国药科大学 中国药学会
  • 主编:吴晓明
  • 地址:南京童家巷24号中国药科大学2号信箱
  • 邮编:210009
  • 邮箱:cpucjnm@163.com
  • 电话:025-83271565 83271568
  • 国际标准刊号:ISSN:2095-6975
  • 国内统一刊号:ISSN:32-1845/R
  • 邮发代号:28-306
  • 获奖情况:
  • 国内外数据库收录:
  • 美国国际药学文摘,美国化学文摘(网络版),波兰哥白尼索引,美国生物医学检索系统,美国科学引文索引(扩展库),美国生物科学数据库,中国中国科技核心期刊,中国北大核心期刊(2008版)
  • 被引量:6564