Alexidine 2HCl (dihydrochloride) is an anticancer agent that targets a mitochondrial tyrosine phosphatase, PTPMT1, in mammalian cells and causes mitochondrial apoptosis. Alexidine 2HCl (AXD) as a drug with the highest antifungal and antibiofilm activity against a diverse range of fungal pathogens. AXD significantly potentiated the efficacy of fluconazole against biofilms, displayed low mammalian cell toxicity, and eradicated biofilms growing in mouse central venous catheters in vivo, highlighting its potential as a pan-antifungal drug. AXD has pronounced antifungal activity, including against preformed biofilms, at concentrations lower than mammalian cell toxicity. AXD potentiated the activity of fluconazole and amphotericin B against Candida biofilms in vitro and prevented biofilm growth in vivo[1]. Alexidine was effective in killing the trophozoites at a concentration of 10 mg/mL. However, a higher concentration of Alexidine (100 mg/mL) is required to kill Acanthamoeba cysts and the cytotoxic activities of Alexidine are comparable with chlorhexidine. both Alexidine and chlorhexidine at 100 mg/mL induced significant cytopathic effect on the corneal epithelial cells in vitro[2]. lexidine dihydrochloride (AD) is a bisbiguanide compound commonly used as an oral disinfectant and in contact lens solutions. It possesses antimicrobial, anti-inflammatory and anticancer properties. AD inhibits OC formation and bone resorption in vitro and exert prophylatic protection against LPS-induced osteolysis in vivo[3]. Alexidine dihydrochloride did not interfere with the activities of cisplatin, 5-fluorouracil, or radiation, and interacted in a less-than-additive manner. FaDu ((human hypopharyngeal squamous cancer)) cell clonogenic survival was reduced to < 5% with 1 mM alexidine dihydrochloride, and, correspondingly, this compound decreased the in vivo tumor-forming potential of FaDu cells[4].
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