Benzethonium (chloride)

Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and α4β2 neurons in Xenopus laevis oocytes, which has antibacterial, anticancer, antisepsis and disinfection activity. Benzethonium chloride induced Apoptosis and activated caspases in cancer cell lines. Benzethonium chloride ablates the tumor-forming ability of FaDu cells, delays the growth of xenograft tumors in vivo^[1][2][3]. In Vitro:Benzethonium chloride (0.1 g/L, 10 s) results in only a 50% reduction in bacterial number against S. mutans MT8148 and Streptococcus sobrinus^[1].
Benzethonium chloride (0.1-100 μM, 48 h) reduces cell viability against FaDu and C666-1 (both human cancer) cell lines with EC₅₀ values of 3.8 and 5.3 μM, respectively^[2].
Benzethonium chloride (9 μM, 24-48 h) induces apoptosis and caspase activation in FaDu cells^[2].
Benzethonium chloride (0.1 and 5 mg/L, 24-72 h) shows great acute toxicity to C. elegans, induces an inhibition on hatching and increases mortality in zebrafish embryos^[3].
In Vivo:Benzethonium chloride (5 mg/kg, i.p., daily for 5 days) results in elimination of tumor formation and growth delay in established xenograft tumors^[2].