(7-Chloroquinolin-4-yl)arylhydrazones: Candida albicansenzymatic repression and cytotoxicity evaluation, Part 2
| Autor: | Pedro Henrique de Azambuja Carvalho, Rafael Guerra Lund, Auri R. Duval, Fábio Renato Manzolli Leite, Wilson Cunico, Fernanda Nedel |
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| Rok vydání: | 2015 |
| Předmět: |
0301 basic medicine
Antifungal Agents Aspartic Acid Proteases food.ingredient 030106 microbiology Biology 01 natural sciences Microbiology Mice Structure-Activity Relationship 03 medical and health sciences food Candida albicans Drug Discovery Animals Agar MTT assay Viability assay Enzyme Inhibitors Cytotoxicity Cells Cultured Cell Proliferation Pharmacology chemistry.chemical_classification Dose-Response Relationship Drug Molecular Structure Cell growth Hydrazones General Medicine Fibroblasts biology.organism_classification Corpus albicans 0104 chemical sciences 010404 medicinal & biomolecular chemistry Enzyme chemistry Phospholipases NIH 3T3 Cells Quinolines Colorimetry |
| Zdroj: | Journal of Enzyme Inhibition and Medicinal Chemistry. 31:126-131 |
| ISSN: | 1475-6374 1475-6366 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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