Antifungal activity against Cryptococcus neoforman

Class Synthetic, broad-spectrum bis-triazole antifungal agent with activity against Cryptococcus neoformans md Candida species ... 

Garlic has in vitro antifungal effects against Cryptococcus neoformans, Candida spp., Trichophyton, Epidermophyton, Microsporum, Aspergillus spp., and Mucor pusillus (40). When five volunteers consumed 10-25 mL of fresh garlic extract, urine samples had antifungal activity, but susceptibility from serum samples dropped significantly (42). 

Barchiesi F, Schimizzi AM, Caselli F, et al. Activity of the new antifungal triazole, posaconazole, against Cryptococcus neoformans. J Antimicrob Chemother 2001 48 769-773. 

Some fluoroquinolones appear to be active against fni and parasites. For instance, the Mannich derivatives of norfloxacin 132 demonstrate a considerable antifungal activity against Histoplasma capsulatum. One of compounds of this family is more active than clotrimazole towards Microsporum audouinii, while other derivatives surpass clotrimazole in relation to Cryptococcus neoformans or Microsporum gypsum. From all derivatives 132 which have been studied (Scheme 57), compound with R=Br, X=N, R =NH2, Y-Z=CH, A=COMe, R -R3=OMe proved to exhibit the highest antifungal activity (MIC for Cryptococcus neoformans and Microsporum audouinii 0,6 pg/ml) [341],... 

F. Barchiesi, A. M. Schimizzi, F. Caselli, D. Giannini, B. Camiletti, A. Giacometti, L. Falconi Di Francesco and G. Scalise, Activity of the new antifungal triazole, posaconazole, against Cryptococcus neoformans, J. Antimicrob. Chemother., 2001, 48, 769-773. 

Furthermore, angelicin, libanorin, psoralen, and aurapten isolated from extracts of the plant Diplotaenia damavandica have shown antifungal activity against Candida albicans, Cryptococcus neoformans, Cladosporium cucumer-inum, Saccharomyces cerevisiae, and Aspergillus niger [255,256]. 

Amphotericin B is particularly effective against systemic infections caused by C. albicans and Cryptococcus neoformans. It is poorly absorbed from the gastrointestinal tract and is thus usually administered by intravenous injection under strict medical supervision. Amphotericin B methyl ester (Fig. 5.15C) is water-soluble, unlike amphotericin B itself, and can be administered intravenously as a solution. The two forms have equal antifungal activity but higher peak serum levels are obtained with the ester. Although the ester is claimed to be less toxic, neurological effects have been observed. An ascorbate salt has recently been described which is water-soluble, of similar activity and less toxic. 

Berberine chloride was evaluated for in vitro activity against Candida albicans, Cryptococcus neoformans, Mycobacterium intracellularae, Trichophyton mentagrophytes, and Saccharomyces cerevasiae, as well as representative Gram-positive and Gram-negative bacteria. The alkaloid was found to exhibit moderate to good antifungal activity, and the minimum inhibitory concentrations were determined as follows Candida albicans (0.39 pg/ml) ... 

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