Cephaeline

Cephaeline is an alkaloid originally isolated from C. ipecacuanha with diverse biological activities. It inhibits the cytochrome P450 (CYP) isoforms CYP2D6 and CYP3A4 in vitro (Kis = 54 and 355 μM, respectively). Cephaeline reduces Zika virus (ZIKV) NS1 protein expression in HEK293 cells (IC50 = 26.4 nM) and reduces viral titer in ZIKV-infected SNB-19 cells (IC50 = 3.11 nM). In vivo, cephaeline (2 mg/kg, i.p.) reduces serum viral load in ZIKV-infected Ifnar1-/- mice. It induces emesis in ferrets when administered at a dose of 0.5 mg/kg, an effect that is prevented by the serotonin (5-HT) receptor subtype 5-HT3 antagonist ondansetron. Cephaeline (1 mg/kg) also increases output of respiratory tract fluid in rabbits.