Highly efficient synthesis and antitumor activity of monosaccharide saponins mimicking components of Chinese folk medicine Cordyceps sinensis

Abstract

Ergosterol 3-O-β-d-glucopyranoside (1a) and ergosterol 3-O-β-d-galactopyranoside (1b) were highly efficiently synthesized and evaluated for their inhibitory activities against two tumor cell lines. The structures of these compounds were extensively confirmed by ¹H, ¹³C NMR, IR, and HRMS. Compounds 1a and 1b exhibited interesting cytotoxic profiles. The antitumor activity of compound 1a was higher than that of 1b.

Keywords:

• ergosterol
• saponins
• glycosylation
• Cordyceps sinensis

Acknowledgments

This work was financially supported by Program for Changjiang Scholars and Innovative Research Team in University (IRT1166), National Agricultural Innovation Project (No. 2011GB2A100009), Natural Science Foundation of Tianjin City (No. 09JCZDJC21800), the Foundation of Tianjin Educational Committee (No. 20090604), the Scientific and Technical Supporting Programs of Science and Technology Commission Foundation of Tianjin (No. 08ZCGHHZ00800), National Natural Science Foundation of China (NSFC, No. 31000279), and Recruited faculty research start-up foundation in Tianjin University of Science and Technology (No. 0200060).