da Rosa Monte Machado Gabriella, Diedrich Denise, Ruaro Thaís Carine, Zimmer Aline Rigon, Lettieri Teixeira Mário, de Oliveira Luís Flávio, Jean Mickael, Van de Weghe Pierre, de Andrade Saulo Fernandes, Baggio Gnoatto Simone Cristina, Fuentefria Alexandre Meneghello
Postgraduate Program in Agricultural Microbiology and Environment, Federal University of Rio Grande do Sul, Sarmento Leite n° 500, Farroupilha, Porto Alegre, RS, 90050-170, Brazil.
Laboratory of Applied Mycology - Faculty of Pharmacy, Federal University of Rio Grande do Sul, Porto Alegre, Brazil.
Braz J Microbiol. 2020 Dec;51(4):1691-1701. doi: 10.1007/s42770-020-00348-4. Epub 2020 Jul 31.
Fungal infections have emerged as a current serious global public health problem. The main problem involving these infections is the expansion of multidrug resistance. Therefore, the prospection of new compounds with efficacy antifungal becomes necessary. Thus, this study evaluated the antifungal profile and toxicological parameters of quinolines derivatives against Candida spp. and dermatophyte strains. As a result, a selective anti-dermatophytic action was demonstrated by compound 5 (geometric means (GM = 19.14 μg ml)). However, compounds 2 (GM = 50 μg ml) and 3 (GM = 47.19 μg ml) have presented only anti-Candida action. Compounds 3 and 5 did not present cytotoxic action. Compound 5 did not produce dermal and mucosal toxicity. In addition, this compound showed the absence of genotoxic potential, suggesting safety for topical and systemic use. Quinolines demonstrated a potent anti-dermatophytic and anti-yeast action. Moreover, compound 5 presented an excellent toxicological profile, acting as a strong candidate for the development of a new effective and safe compound against dermatophytosis of difficult treatment.
真菌感染已成为当前严重的全球公共卫生问题。这些感染涉及的主要问题是多重耐药性的扩大。因此，寻找具有抗真菌功效的新化合物变得必要。因此，本研究评估了喹啉衍生物对念珠菌属和皮肤癣菌菌株的抗真菌谱和毒理学参数。结果，化合物5表现出选择性抗皮肤癣菌作用（几何均值（GM = 19.14 μg/ml））。然而，化合物2（GM = 50 μg/ml）和3（GM = 47.19 μg/ml）仅表现出抗念珠菌作用。化合物3和5没有细胞毒性作用。化合物5没有产生皮肤和粘膜毒性。此外，该化合物显示没有遗传毒性潜力，表明其局部和全身使用的安全性。喹啉表现出强大的抗皮肤癣菌和抗酵母作用。此外，化合物5具有优异的毒理学特性，是开发一种针对难治性皮肤癣菌病的新型有效且安全化合物的有力候选者。
