Hirsutine induces apoptosis and is a potent Dengue virus inhibitor exhibiting low cytotoxicity.Hirsutine has anticancer, cardioprotective, anti-hypertensive and anti-arrhythmic activities, it also has vasodilatation activity, the mechanism is related to blockade of Ca2+ influx through L-type Ca2+ channels and inhibition of intracellular Ca2+ release may have no relationship with K+ channels.

The clinical utility of Hirsutine against human breast cancer. Among six distinct human breast cancer cell lines, Hirsutine showed strong cytotoxicity against HER2-positive/p53-mutated MDA-MB-453 and BT474 cell lines. Conversely, HER2-negative/p53 wild-type MCF-7 and ZR-75-1 cell lines showed resistance against Hirsutine-induced cytotoxicity. Hirsutine induced apoptotic cell death in the MDA-MB-453 cells, but not in the MCF-7 cells, through activation of caspases. Furthermore, Hirsutine induced the DNA damage response in the MDA-MB-453 cells, but not in the MCF-7 cells, as highlighted by the upregulation of γH2AX expression. Along with the induction of the DNA damage response, the suppression of HER2, NF-κB and Akt pathways and the activation of the p38 MAPK pathway in the MDA-MB-453 cells were observed[1]