Cytotoxic sesquiterpenoids against hepatic stellate cell line LX2 from Artemisia lavandulaefolia

Abstract

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 μg/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 spectroscopic 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 μM); compounds 6, 9 and 16 showed moderate activity with IC₅₀ values of 109.3, 114.0 and 124.2 μM. Importantly, compounds 14, 15 and 18 displayed significant cytotoxicity against HSC-LX2 with IC₅₀ values of 52.1, 16.5 and 21.3 μM, 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 μM and from 18.6 to 72.9 μM.

Keywords: Artemisia lavandulaefolia; Cytotoxicity; Extracellular matrix; HSC-LX2; Sesquiterpenoids.