Journal
PHYTOCHEMISTRY
Volume 192, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.phytochem.2021.112951
Keywords
Calotropis gigantea; Asclepiadaceae; Cardenolides; Cytotoxicity; Cell cycle
Categories
Funding
- National Natural Science Foundation of China [21778027]
- Supercomputing Center of Lanzhou University, China
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Sixteen cardiac glycosides, including five previously undescribed compounds, were extracted and purified from Calotropis gigantea (L.). These compounds showed potent cytotoxic activities against various human cancer cell lines, with uscharidin and calotropin exhibiting pronounced cytotoxicity at low nanomolar concentrations against A172 and U251 cells, possibly inducing G2/M cell cycle arrest for cell death.
Sixteen cardiac glycosides, including five previously undescribed compounds, were extracted and purified from whole plants of Calotropis gigantea (L.). Spectroscopic data and electronic circular dichroism (ECD) analyses were used to determine their structures. Calogiganin C is the first naturally occurring example of a cardenolide containing a 7-membered lactone in ring A. The cytotoxic activities of these compounds against A172, U251, AGS, PANC-1, HepG2, HCT116 and NCI-H226 cell lines were evaluated. Four of them exhibited the most potent growth inhibitory activity against a panel of human cancer cell lines, including A172, U251, AGS, PANC-1 and HCT116. Notably, uscharidin and calotropin showed pronounced cytotoxicities at low nanomolar concentrations against A172 and U251 cells, and possible cell death mechanism studies manifested that these two compounds induced G2/M cell cycle arrest, which demonstrated promising anticancer potential.
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