de Azambuja Carvalho Pedro Henrique, Duval Auri Rocha, Manzolli Leite Fabio Renato, Nedel Fernanda, Cunico Wilson, Lund Rafael Guerra
a Oral Microbiology Laboratory , Pelotas Dental School, Federal University of Pelotas , Pelotas , RS , Brazil .
b LaQuiABio - Laboratory of Bioactive Applied Chemistry , Center of Chemical, Pharmaceutical and Food Sciences (CCQFA), Federal University of Pelotas , Pelotas , RS , Brazil .
J Enzyme Inhib Med Chem. 2016;31(1):126-31. doi: 10.3109/14756366.2015.1010527. Epub 2015 Mar 25.
This work describes the anti-enzymatic activity of (7-chloroquinolin-4-yl)arylhydrazones against Candida albicans and examines their cytotoxicity.
Ten C. albicans strains [nine isolates and one azole-resistant standard strain (ATCC 62342)] were used to assess the anti-enzymatic activity. Fifteen compounds at sub-antifungal concentrations ranging from 12.5 to 100 µg/ml were assessed after a 30-min exposure. The strains were seeded onto petri dishes with selective agar media for aspartyl proteases (Saps) and phospholipases (PLs). Enzymatic inhibition was measured by the reduction of the precipitation zone (Pz) against untreated strains (positive control). A colorimetric MTT assay was used with 3T3/NIH mouse fibroblasts to evaluate cytotoxicity. Cells were exposed to 15 compounds in concentrations from 6.25 to 100 µg/ml for 24 and 48 h.
Four hydrazones showed enzymatic repression values over 40% to Pl and three over 20% to Saps. The cell viability was over 50% at hydrazone concentrations of 25-100 µg/ml.
These results revealed that select (7-chloroquinolin-4-yl)arylhydrazones may be potential antifungal agents for the control of C. albicans infections.
本研究描述了（7-氯喹啉-4-基）芳基腙对白色念珠菌的抗酶活性，并检测了它们的细胞毒性。
使用10株白色念珠菌菌株[9株分离株和1株唑类耐药标准菌株（ATCC 62342）]评估抗酶活性。在30分钟暴露后，评估15种浓度范围为12.5至100μg/ml的亚抗真菌浓度的化合物。将菌株接种到含有天冬氨酸蛋白酶（Saps）和磷脂酶（PLs）的选择性琼脂培养基的培养皿上。通过测量相对于未处理菌株（阳性对照）沉淀区（Pz）的减少来测定酶抑制作用。使用比色MTT法对3T3/NIH小鼠成纤维细胞进行细胞毒性评估。将细胞暴露于浓度为6.25至100μg/ml的15种化合物中24小时和48小时。
四种腙对PL的酶抑制值超过40%，三种对Saps的酶抑制值超过20%。在腙浓度为25-100μg/ml时，细胞活力超过50%。
这些结果表明，某些（7-氯喹啉-4-基）芳基腙可能是控制白色念珠菌感染的潜在抗真菌剂。
