Comprehensive Insights into Arecoline Hydrobromide: Pharmacology, Toxicity, and Pharmacokinetics

Arecoline hydrobromide (AH) is an active alkaloid found in betel nut. AH was first extensively employed for treatment of tapeworm infection in dogs in Australia. In the last 2 decades, AH has gained increasing attention due to its multiple and notable pharmacological activities in various diseases, including: acaricidal activity against cattle ticks; anticataract activity; therapeutic and alleviating effects against diabetes complications, including male reproductive damage and cataract; treatment of rheumatoid arthritis (RA); and protection against gastric ulcer. In addition, AH may have potassium channel inhibitory activity, regulate of CYP2B (Cytochrome P450 2B) expression, and regulate mRNA expression of hepatorenal transporters. In terms of toxicity, the data showed that AH may have sub-chronic, long-term and acute toxicities, and teratogenic effects. Additionally, in pharmacokinetic studies, rapid LC-MS/MS methods have been applied to determine AH or arecoline quantitatively. In summary, the above studies suggested that AH may have considerable application prospects and great potential value in clinical practice in the future, but limitations of current studies and new challenges in AH were also be discussed, and future development directions were suggested in toxicities and pharmacokinetics. This article aims to review the pharmacological activity, pharmacokinetics, and toxicity of the natural alkaloid, arecoline hydrobromide.