Back to Search
Start Over
Artemicapillasins A–N, cytotoxic coumaric acid analogues against hepatic stellate cell LX2 from Artemisia capillaris (Yin-Chen).
- Source :
-
Bioorganic Chemistry . Dec2021, Vol. 117, pN.PAG-N.PAG. 1p. - Publication Year :
- 2021
-
Abstract
- [Display omitted] • Fourteen new coumaric acid analogues were isolated from Artemisia capillaris. • Twelve compounds exhibited cytotoxicity against HSC-LX2. • Compound 2 displayed potent inhibitory activity on the deposition of Col Ⅰ, HL and HA. • This study provides more evidence for the traditional use of Artemisia capillaris against hepatic fibrosis. 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 μg/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 μM. The most active artemicapillasin B (2) gave an IC 50 value of 24.5 μM, which was about 7 times more toxic than the positive drug silybin (IC 50 , 162.3 μM). 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 IC 50 values of 11.0, 14.4 and 13.8 μM, 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. [ABSTRACT FROM AUTHOR]
- Subjects :
- *LIVER cells
*ARTEMISIA
*HEPATIC fibrosis
*HYALURONIC acid
*ACIDS
Subjects
Details
- Language :
- English
- ISSN :
- 00452068
- Volume :
- 117
- Database :
- Academic Search Index
- Journal :
- Bioorganic Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 153681192
- Full Text :
- https://doi.org/10.1016/j.bioorg.2021.105441