Pharmacological Effects of Cinobufagin

Abstract

Cinobufagin (CBF) is a bufadienolide, which is a major active ingredient of toad venom. In recent years, CBF has attracted increasing attention due to its highly potent and multiple pharmacological activities. To better understand the status of research on CBF, we collated recent studies on CBF to provide a valuable reference for clinical researchers and practitioners. According to reports, CBF exhibits extensive pharmacological properties, including antitumor, analgesic, cardioprotection, immunomodulatory, antifibrotic, antiviral, and antiprotozoal effects. Studies on the pharmacological activity of CBF have mainly focused on its anticancer activity. It has been demonstrated that CBF has a therapeutic effect on liver cancer, osteosarcoma, melanoma, colorectal cancer, acute promyelocytic leukemia, nasopharyngeal carcinoma, multiple myeloma, gastric cancer, and breast cancer. However, the direct molecular targets of CBF are currently unknown. In addition, there are few reports on toxicological and pharmacokinetic of CBF. Subsequent studies focusing on these aspects will help promote the development and application of CBF in clinical practice.

Synthesis of Bufadienolide Cinobufagin via Late-Stage Singlet Oxygen Oxidation/Rearrangement Approach

“…Figure B). Since its isolation in 1932 by Jensen, numerous studies have explored its medicinal properties and demonstrated its clinical significance . In addition to inhibiting Na + ,K + -ATPase, cinobufagin has been shown to regulate secretion of aldosterone and cortisol and StAR gene expression as well as induce cell cycle arrest and apoptosis in tumor cells.…”