Antifungal activity of 25-azalanosterol against Candida species.
The antifungal properties of 25-azalanosterol was investigated. Compared to normal antifungal reagents, fluoconazole, clotrimazole and voriconazole, it exhibited significant anti-Candida activity (the minimum inhibitory concentration [MIC] ranges were 0.125-8, 0.5-8 and 0.5-32 microg/mL against C. albicans, C. krusei and C. glabrata, respectively), but showed little toxicity to mice liver cells at clinical dosage after 24 h of exposure, with the lowest lactate dehydrogenase and the highest ED(50) compared to four other azoles antifungal agents. 25-Azalanosterol inhibited the incorporation of [methyl-(3)H(3)] AdoMet into the C-24 of ergosterol in whole cells of C. albicans. Thus, 25-azalanosterol, as an inhibitor of the growth of C. albicans in vitro, may have considerable potential as a new class of anti-Candida agent that lacks toxic side effects in the mammalian host.
Wang
J
J
College of Life Science and Technology, Shanxi University, Taiyuan, 030006, People's Republic of China. junqingwang@yahoo.com
Wu
J
J
D000818:Animals; D000935:Antifungal Agents / Q000494:pharmacology* / Q000633:toxicity; D002175:Candida / Q000187:drug effects*; D002460:Cell Line; D022781:Hepatocytes / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D007810:Lanosterol / Q000031:analogs & derivatives* / Q000494:pharmacology* / Q000633:toxicity; D051379:Mice; D008826:Microbial Sensitivity Tests; D012436:S-Adenosylmethionine / Q000037:antagonists & inhibitors
D000935:Antifungal Agents; D007810:Lanosterol; D012436:S-Adenosylmethionine