mesaconitine

Mesaconitine is a highly potent C19-diterpenoid alkaloid primarily derived from plants of the *Aconitum* genus, such as *Aconitum carmichaelii* (Fuzi). It is recognized as one of the major active and toxic constituents of these plants, which are traditionally used in East Asian medicine for the treatment of rheumatoid arthritis, joint pain, and inflammation. Mesaconitine exerts its biological effects by acting as a potent activator of voltage-gated sodium channels; it binds to site 2 of the channel's alpha subunit, preventing inactivation and leading to persistent membrane depolarization. This mechanism accounts for its analgesic properties as well as its severe cardiotoxicity and neurotoxicity. The compound is primarily metabolized by the cytochrome P450 enzyme CYP3A4 and is a substrate for the efflux transporter P-glycoprotein (P-gp). Its pharmacokinetics can be significantly altered by inflammatory conditions, such as rheumatoid arthritis, which may suppress the expression and function of these metabolic and transport pathways.

Other names

MA