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In vitro cytotoxic and anti-inflammatory activities of sesquiterpene lactones from Centaurea papposa (Coss.) Greuter by Maria-Eleni Grafakou; Christina Barda; Joerg Heilmann; Helen Skaltsa is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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In the pursuit of highly active specialized metabolites from endemic plants, Centaurea papposa (Coss.) Greuter, an endemic plant in Algeria and Tunisia, was investigated and afforded eleven sesquiterpene lactones (1-11). Cytotoxic evaluation of these compounds using the in vitro MTT assay on three human cancerous cell lines (HeLa, SK-MEL-28 and HepG2), revealed that isolates 4, 8 and 9 (IC 50 10 lM) could be potential anti-cancer drugs for cervical cancer according to the National Cancer Institute. Further evaluation of the in vitro anti-inflammatory activity showed that compounds 1 and 4 inhibited the TNF-a induced ICAM-1 expression in HMEC-1 endothelial cells at a maximum of 21% and 2% of the control (IC 50 values 21.9 and 5.7 lM, respectively). The Michael reactions of the a-methylene-c-lactone ring seem to be responsible for the strong activity, while no toxicity was observed in the HMEC-1 cells in all the range of tested concentrations (6.25-50.0 mM).

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Author

Maria-Eleni Grafakou; Christina Barda; Joerg Heilmann; Helen Skaltsa

Publisher

Informa UK Limited

Published

2022

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)