Alexidine dihydrochloride 对多种真菌病原体具有抗真菌和抗生物膜活性。它是一种抗癌剂，可靶向哺乳动物细胞中的线粒体酪氨酸磷酸酶 PTPMT1，并导致线粒体凋亡。

Alexidine dihydrochloride has antifungal and antibiofilm activity against a diverse range of fungal pathogens. Alexidine dihydrochloride is an anticancer agent that targets a mitochondrial tyrosine phosphatase, PTPMT1, in mammalian cells and causes mitochondrial apoptosis. Thus, Alexidine dihydrochloride has the potential to be developed as a pan-antifungal, antibiofilm drug.

Alexidine dihydrochloride can decimate at low concentrations (1.5 to 6 μg/mL) mature biofilms of Candida, Cryptococcus, and Aspergillus spp. that are known to be resistant to almost all classes of antifungal drugs. Alexidine dihydrochloride displays activity against most Candida spp.; MIC values of ≤1.5 μg/mL are observed for all isolates tested under planktonic conditions, with the exception of Candida parapsilosis and Candida krusei and it also displays striking activity against clinically relevant fluconazole-resistant Candida isolates: C. albicans (CA2, CA6, and CA10), C. glabrata (CG2 and CG5), C. parapsilosis (CP5), and C. auris (CAU-09 and CAU-03)[1]. Inhibition of planktonic growth by Alexidine dihydrochloride reveals a complete inhibition of filamentation or proliferation of the imaged fungi. Alexidine dihydrochloride results in 50% killing of HUVECs and lung epithelial cells, at concentrations 5- to 10-fold higher than the MIC required to kill planktonically growing fungal pathogens[1]. In fact, at 10-fold-lower concentrations (150 ng/mL) of planktonic MICs, Alexidine dihydrochloride could inhibit lateral yeast formation and biofilm dispersal in C. albicans[1].

Biofilm formation by C. Albicans is chosen to focus on because a murine biofilm model has been well established in this fungus and used for testing the effects of established and new antifungal agents. In fact, fungal CFU determination reveals that Alexidine dihydrochloride inhibits 67% of fungal biofilm growth and viability, compared to the control untreated biofilms[1]. The effect of the drugs on the 24-h-old biofilms growing in the jugular vein catheters of mice is visualized microscopically, which reveals significantly lower density of the biofilms in catheters treated with Alexidine dihydrochloride.

1715-30-6

C26H57ClN10

545.25

Alexidine dihydrochloride

DMSO:250 mg/mL (429.77 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years