Artemicapillasins A-N, cytotoxic coumaric acid analogues against hepatic stellate cell LX2 from Artemisia capillaris (Yin-Chen)

doi:10.1016/j.bioorg.2021.105441

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	Artemicapillasins A-N, cytotoxic coumaric acid analogues against hepatic stellate cell LX2 from Artemisia capillaris (Yin-Chen)
	Gao,Zhen ; Huang,Xiao-Yan ; Geng,Chang-An ; Li,Tian-Ze ; Chen,Ji-Jun
	2021
发表期刊	BIOORGANIC CHEMISTRY
ISSN	0045-2068
卷号	117 页码:105441
摘要	Under the guidance of bioassay against HSC-LX2, the EtOH extract and the EtOAc fraction of Artemisia capillaris (Yin-Chen) exhibited cytotoxic activity against HSC-LX2 with inhibitory ratios of 39.7% and 68.7% at the concentration of 400.0 mu g/mL. Bioassay-guided investigation of Fr. D (the active fraction) yielded 14 new coumaric acid analogues, artemicapillasins A-N (1-14). The structures of the isolates were elucidated by spectroscopic analyses involving UV, IR, MS, 1D and 2D NMR spectra and ECD calculations. Cytotoxic activity against HSC-LX2 cells of these isolates was performed to reveal that 12 compounds demonstrated cytotoxicity with inhibitory ratios more than 50% at 400 mu M. The most active artemicapillasin B (2) gave an IC50 value of 24.5 mu M, which was about 7 times more toxic than the positive drug silybin (IC50, 162.3 mu M). Importantly, artemicapillasin B (2) showed significant inhibition on the deposition of human collagen type I (Col I), human laminin (HL) and human hyaluronic acid (HA) with IC50 values of 11.0, 14.4 and 13.8 mu M, which was about 7, 11 and 5 times more active than silybin. Artemicapillasin B (2) as an interesting antihepatic fibrosis candidate is worth in-depth study.
关键词	Artemisia capillaris Coumaric acid analogues Antihepatic fibrosis effects HSC-LX2 Extracellular matrix TRADITIONAL CHINESE HERB ACTIVE CONSTITUENTS LIVER FIBROSIS
DOI	10.1016/j.bioorg.2021.105441
WOS记录号	WOS:000729835300001
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/73753
专题	中国科学院昆明植物研究所
作者单位	1.[Gao, Zhen 2.Huang, Xiao-Yan 3.Geng, Chang-An 4.Li, Tian-Ze 5.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Yunnan Key Lab Nat Med Chem, Kunming 650201, Yunnan, Peoples R China 6.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
推荐引用方式 GB/T 7714	Gao,Zhen,Huang,Xiao-Yan,Geng,Chang-An,et al. Artemicapillasins A-N, cytotoxic coumaric acid analogues against hepatic stellate cell LX2 from Artemisia capillaris (Yin-Chen)[J]. BIOORGANIC CHEMISTRY,2021,117:105441.
APA	Gao,Zhen,Huang,Xiao-Yan,Geng,Chang-An,Li,Tian-Ze,&Chen,Ji-Jun.(2021).Artemicapillasins A-N, cytotoxic coumaric acid analogues against hepatic stellate cell LX2 from Artemisia capillaris (Yin-Chen).BIOORGANIC CHEMISTRY,117,105441.
MLA	Gao,Zhen,et al."Artemicapillasins A-N, cytotoxic coumaric acid analogues against hepatic stellate cell LX2 from Artemisia capillaris (Yin-Chen)".BIOORGANIC CHEMISTRY 117(2021):105441.

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