Antifungal effects of aminosulphoxide and disulphide derivatives

Summary 2‐Benzenesulphinyl‐(1,4)‐naphtoquinone and 14 derivatives were synthesised and were used to evaluate their cytotoxicity against a human myelomonocyte cell line and their antifungal activity against two yeast, i.e. Candida albicans and C. tropicalis and against two filamentous fungi such as A...

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Bibliographic Details
Published in:	Mycoses Vol. 49; no. 3; pp. 169 - 175
Main Authors:	Wittebolle, Veerle, Lemriss, Sanaâ, Morella, Gracia La, Errante, Jaccomo, Boiron, Patrick, Barret, Roland, Sarciron, Marie Elisabeth
Format:	Journal Article
Language:	English
Published:	Oxford, UK Blackwell Publishing Ltd 01-05-2006 Wiley
Subjects:	aminosulphoxide derivatives Amphotericin B - pharmacology Antifungal Agents - chemical synthesis Antifungal Agents - chemistry Antifungal Agents - pharmacology Antifungal Agents - toxicity antifungal susceptibility Aspergillus niger Candida albicans Cell Line Disulfides - chemical synthesis Disulfides - chemistry Disulfides - pharmacology disulphide derivatives Ecology, environment Ecosystems Fungi - classification Fungi - drug effects Fusarium oxysporum Humans Life Sciences Microbial Sensitivity Tests Microbiology and Parasitology Monocytes Mycology Naphthoquinones - chemical synthesis Naphthoquinones - chemistry Naphthoquinones - pharmacology Pharmaceutical sciences Pharmacology Trichophyton tonsurans
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Summary:	Summary 2‐Benzenesulphinyl‐(1,4)‐naphtoquinone and 14 derivatives were synthesised and were used to evaluate their cytotoxicity against a human myelomonocyte cell line and their antifungal activity against two yeast, i.e. Candida albicans and C. tropicalis and against two filamentous fungi such as Aspergillus niger and Fusarium oxysporum and against one dermatophyte, namely Trichophyton tonsurans. The cytotoxicity and antifungal activities were investigated in comparison with amphotericin B as reference drug. No compound was significantly more toxic than amphotericin B at 0.2 μg ml−1. The best results of antifungal activity were obtained with GFL 10, GFL 13 and GFL 30 on C. tropicalis, F. oxysporum and T. tonsurans. For C. albicans and A. niger, there was no difference between amphotericin B and the other molecules. The sterol quantitation, the time‐kill curves were carried out for these three compounds in order to confirm their action in ergosterol synthesis. Time‐kill curves showed a fungistatic activity. For C. tropicalis GFL 10, GFL 13 and GFL 30 increased the growth delay better than amphotericin B, in contrast to F. oxysporum. As for T. tonsurans, GFL10 and GFL13 gave a delay, but the effect of GFL 30 was a bit less marked.
Bibliography:	istex:2AC9C1E15607A2AC00AB9D6DE43AEF8D91AF39BC ArticleID:MYC1233 ark:/67375/WNG-3K7456HT-2 ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0933-7407 1439-0507
DOI:	10.1111/j.1439-0507.2006.01233.x