Synthesis and in vitro anticancer activities of biotinylated derivatives of glaucocalyxin A and oridonin

Abstract

Fourteen glaucocalyxin A biotinylated derivatives, one glaucocalyxin C biotinylated derivative, and two oridonin biotinylated derivatives were designed and synthesized. Their structures were confirmed from ¹H NMR, ¹³C NMR and HRMS data. The derivatives were evaluated for cytotoxic activities against lung (A549), cervical cancer cell line HeLa derivative (KB), multidrug-resistant KB subline (KB-VIN), triple-negative breast (MDA-MB-231), and estrogen receptor-positive breast (MCF-7) cancer cell lines.

Graphical Abstract

Keywords:

• Glaucocalyxin A
• oridonin
• glaucocalyxin C
• biotin
• anticancer activity

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

This study was funded by the National Natural Science Foundation of China (grant number 81202882); the Social Development Project in Jiangsu Province of China (grant number BE2018322); the Priority Academic Program Development of the Jiangsu Higher Education Institutes, China (PAPD). Partial support was received from National Institutes of Health, NIH (grant number CA177584) awarded to Kuo-Hsiung Lee.