Description
Clotrimazole is an imidazole antifungal that also exhibits anti-parasitic, antimalarial, and anticancer chemotherapeutic activities. Clotrimazole inhibits synthesis of ergosterol and other sterols, preventing fungal cell wall formation; it also inhibits the H+/K+ ATPase and the Na+/K+ ATPase. In vivo and in vitro, clotrimazole induces G0/G1 cell cycle arrest, decreases the Bcl-2:Bax ratio, stimulates apoptosis, and inhibits proliferation and tumor growth. Additionally, this compound inhibits degradation of heme, inducing hemolysis and suppressing growth of Plasmodium in vitro.
References
Wang J, Jia L, Kuang Z, et al. The in vitro and in vivo antitumor effects of clotrimazole on oral squamous cell carcinoma. PLoS One. 2014 Jun 3;9(6):e98885. PMID: 24892421.
Witzke A, Lindner K, Munson K, et al. Inhibition of the gastric H,K-ATPase by clotrimazole. Biochemistry. 2010 Jun 1;49(21):4524-32. PMID: 20423050.
Huy NT, Takano R, Hara S, et al. Enhancement of heme-induced membrane damage by the anti-malarial clotrimazole: the role of colloid-osmotic forces. Biol Pharm Bull. 2004 Mar;27(3):361-5. PMID: 14993803.
Plempel M. On the action kinetics of clotrimazole. Chemotherapy. 1982;28 Suppl 1:22-31. PMID: 6761084.
