4.7 Article

Cytotoxic sesquiterpenoids against hepatic stellate cell line LX2 from Artemisia lavandulaefolia

期刊

BIOORGANIC CHEMISTRY
卷 103, 期 -, 页码 -

出版社

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2020.104107

关键词

Artemisia lavandulaefolia; Sesquiterpenoids; Cytotoxicity; HSC-LX2; Extracellular matrix

资金

  1. Yunnan Wanren Project [YNWRKJLJ-2019-002]
  2. Program of Yunling Scholarship
  3. Reserve Talents of Young and Middle-aged Academic and Technical Leaders in Yunnan Province
  4. Youth Innovation Promotion Association, CAS [Y201756]

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The preliminary assay suggested that the EtOH extract of Artemisia lavandulaefolia had cytotoxicity against hepatic stellate cell line LX2 (HSC-LX2) with an inhibitory ratio of 94.1% at 400 mu g/mL. Bioassay-guided investigation led to eleven new sesquiterpenoids, artemilavanolides C-F (1-4) and artemlavandulolides A-G (5-11), as well as thirteen known compounds (12-24). Their structures were elucidated by extensive spectro-scopic data and X-ray crystallographic analysis. Cytotoxicity evaluation suggested that fourteen compounds exhibited activity against HSC-LX2; compounds 22, 23 and 24 were comparable to the positive control, silybin (IC50, 162.3 mu M); compounds 6, 9 and 16 showed moderate activity with IC50 values of 109.3, 114.0 and 124.2 mu M. Importantly, compounds 14, 15 and 18 displayed significant cytotoxicity against HSC-LX2 with IC50, values of 52.1, 16.5 and 21.3 mu M, and inhibitory activity on the deposition of human collagen type I (Col I) and human laminin (HL) with IC50 values ranging from 7.3 to 71.6 mu M and from 18.6 to 72.9 mu M.

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