Cytotoxic cardenolides from Calotropis gigantea

Yi-Lin He; Hong-Ying Yang; Pei-Zhi Huang; Wei-Jiao Feng; Kun Gao

doi:10.1016/j.phytochem.2021.112951

Cytotoxic cardenolides from Calotropis gigantea

Phytochemistry. 2021 Dec:192:112951. doi: 10.1016/j.phytochem.2021.112951. Epub 2021 Sep 24.

Authors

Yi-Lin He¹, Hong-Ying Yang², Pei-Zhi Huang², Wei-Jiao Feng², Kun Gao³

Affiliations

¹ State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou, 730000, People's Republic of China; Research Institute, Lanzhou Jiaotong University, Lanzhou, 730070, People's Republic of China.
² State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou, 730000, People's Republic of China.
³ State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou, 730000, People's Republic of China. Electronic address: npchem@lzu.edu.cn.

PMID: 34563976
DOI: 10.1016/j.phytochem.2021.112951

Abstract

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.

Keywords: Asclepiadaceae; Calotropis gigantea; Cardenolides; Cell cycle; Cytotoxicity.

MeSH terms

Antineoplastic Agents*
Antineoplastic Agents, Phytogenic* / pharmacology
Calotropis*
Cardenolides / pharmacology
Cardiac Glycosides*
Cell Line, Tumor

Substances

Antineoplastic Agents
Antineoplastic Agents, Phytogenic
Cardenolides
Cardiac Glycosides