Germacranolide sesquiterpenes from Carpesium cernuum and their anti-leukemia activity.

Chin J Nat Med

Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academic of Sciences, Guiyang 550014, China; State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, China. Electronic address:

Published: July 2021

AI Article Synopsis

  • The study isolated three new sesquiterpenes (1-3) and six known analogues (4-9) from the plant Carpesium cernuum, determining their structures using advanced NMR and ECD techniques.
  • The anti-leukemia effects of these compounds were tested on three different leukemia cell lines, revealing that compounds 1-3 displayed moderate cytotoxicity.
  • Specifically, compound 2 showed promise as an anti-leukemia agent by inducing apoptosis through the downregulation of the Bcl-2 protein and activating caspase enzymes in K562 cells.

Article Abstract

In this study, three new germacranolide sesquiterpenes (1-3), together with six related known analogues (4-9) were isolated from the whole plant of Carpesium cernuum. Their structures were established by a combination of extensive NMR spectroscopic analysis, HR-ESIMS data, and ECD calculations. The anti-leukemia activities of all compounds towards three cell lines (HEL, KG-1a, and K562) were evaluated in vitro. Compounds 1-3 exhibited moderate cytotoxicity with IC values ranging from 1.59 to 5.47 μmol·L. Mechanistic studies indicated that 2 induced apoptosis by decreasing anti-apoptotic protein Bcl-2 and activating the caspase family in K562 cells. These results suggest that compound 2 is a potential anti-leukemia agent.

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http://dx.doi.org/10.1016/S1875-5364(21)60052-3DOI Listing

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