咖啡酸衍生物酯的合成、抗真菌活性及其与氟康唑和制霉菌素对念珠菌属的协同作用
Synthesis, antifungal activity of caffeic acid derivative esters, and their synergism with fluconazole and nystatin against Candida spp.
作者信息
Sardi Janaína de Cássia Orlandi, Gullo Fernanda Patrícia, Freires Irlan Almeida, Pitangui Nayla de Souza, Segalla Maicon Petrônio, Fusco-Almeida Ana Marisa, Rosalen Pedro Luiz, Regasini Luís Octávio, Mendes-Giannini Maria José Soares
机构信息
Department of Clinical Analysis, Laboratory of Clinical Mycology, Faculty of Pharmaceutical Sciences, UNESP-Univ Estadual Paulista, Araraquara, SP14801-902, Brazil; Department of Physiological Sciences, Piracicaba Dental School, University of Campinas, Piracicaba, SP13414-90, Brazil.
Department of Clinical Analysis, Laboratory of Clinical Mycology, Faculty of Pharmaceutical Sciences, UNESP-Univ Estadual Paulista, Araraquara, SP14801-902, Brazil.
出版信息
Diagn Microbiol Infect Dis. 2016 Dec;86(4):387-391. doi: 10.1016/j.diagmicrobio.2016.08.002. Epub 2016 Aug 8.
We tested the antifungal potential of caffeic acid and 8 of its derivative esters against Candidaalbicans ATCC 90028 and 9 clinical isolatesand carried out a synergism assay with fluconazole and nystatin. Propyl caffeate (C3) showed the best antifungal activity against the tested strains. When in combination, C3 markedly reduced the MIC of fluconazole and nystatin with synergistic effect up to 64-fold. Finally, C3 showed a high IC value and selective indexagainst oral keratinocytes, demonstrating low toxicity against this cell type and selectivity for yeast cells. Further research should confirm its antifungal potential for development of combined therapy to treat C. albicans infections.
我们测试了咖啡酸及其8种衍生物酯对白色念珠菌ATCC 90028和9株临床分离株的抗真菌潜力，并与氟康唑和制霉菌素进行了协同试验。咖啡酸丙酯（C3）对受试菌株表现出最佳的抗真菌活性。联合使用时，C3显著降低了氟康唑和制霉菌素的最低抑菌浓度，协同效应高达64倍。最后，C3对口腔角质形成细胞显示出高IC值和选择性指数，表明对这种细胞类型毒性低且对酵母细胞具有选择性。进一步的研究应证实其在开发联合疗法治疗白色念珠菌感染方面的抗真菌潜力。
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