Wittebolle Veerle, Lemriss Sanaâ, La Morella Gracia, Errante Jaccomo, Boiron Patrick, Barret Roland, Sarciron Marie Elisabeth
Department of Parasitology and Medical Mycology, Claude Bernard University, Lyon cedex, France.
Mycoses. 2006 May;49(3):169-75. doi: 10.1111/j.1439-0507.2006.01233.x.
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 microg 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.
合成了2-苯亚磺酰基-(1,4)-萘醌及其14种衍生物，并用于评估它们对人骨髓单核细胞系的细胞毒性以及对两种酵母（白色念珠菌和热带念珠菌）、两种丝状真菌（黑曲霉和尖孢镰刀菌）和一种皮肤癣菌（断发毛癣菌）的抗真菌活性。与作为参考药物的两性霉素B相比，研究了其细胞毒性和抗真菌活性。在0.2微克/毫升时，没有化合物的毒性比两性霉素B显著更高。在热带念珠菌、尖孢镰刀菌和断发毛癣菌上，GFL 10、GFL 13和GFL 30的抗真菌活性取得了最佳结果。对于白色念珠菌和黑曲霉，两性霉素B与其他分子之间没有差异。对这三种化合物进行了甾醇定量和时间-杀菌曲线研究，以确认它们在麦角甾醇合成中的作用。时间-杀菌曲线显示出抑菌活性。对于热带念珠菌，GFL 10、GFL 13和GFL 30比两性霉素B更好地延长了生长延迟，而对于尖孢镰刀菌则相反。至于断发毛癣菌，GFL10和GFL13产生了延迟，但GFL 30的效果稍不明显。
