Pedro Henrique de Azambuja Carvalho1, Auri Rocha Duval2, Fabio Renato Manzolli Leite3, Fernanda Nedel4,5, Wilson Cunico2, Rafael Guerra Lund6. 1. a Oral Microbiology Laboratory , Pelotas Dental School, Federal University of Pelotas , Pelotas , RS , Brazil . 2. b LaQuiABio - Laboratory of Bioactive Applied Chemistry , Center of Chemical, Pharmaceutical and Food Sciences (CCQFA), Federal University of Pelotas , Pelotas , RS , Brazil . 3. c Clinics and Semiology Department , Pelotas Dental School, Federal University of Pelotas , Pelotas , RS , Brazil . 4. d Cell and Tissue Biology Nucleus (NCTBio), Post-Graduate Program in Dentistry, Pelotas Dental School, Federal University of Pelotas , Pelotas , RS , Brazil . 5. e Post-Graduate Program in Health and Behavior, Catholic University of Pelotas , Pelotas , RS , Brazil , and. 6. f Post-Graduate Program in Dentistry, Pelotas Dental School, Federal University of Pelotas , Rio Grande do Sul , Brazil.
Abstract
OBJECTIVE: This work describes the anti-enzymatic activity of (7-chloroquinolin-4-yl)arylhydrazones against Candida albicans and examines their cytotoxicity. MATERIAL AND METHODS: 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. RESULTS: 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. CONCLUSION: These results revealed that select (7-chloroquinolin-4-yl)arylhydrazones may be potential antifungal agents for the control of C. albicans infections.
OBJECTIVE: This work describes the anti-enzymatic activity of (7-chloroquinolin-4-yl)arylhydrazones against Candida albicans and examines their cytotoxicity. MATERIAL AND METHODS: 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. RESULTS: 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. CONCLUSION: These results revealed that select (7-chloroquinolin-4-yl)arylhydrazones may be potential antifungal agents for the control of C. albicans infections.
Authors: Ulviye Acar Cevik; Begum Nurpelin Saglik; Yusuf Ozkay; Zerrin Canturk; Juan Bueno; Fatih Demirci; Ali Savas Koparal Journal: Curr Pharm Des Date: 2017 Impact factor: 3.116
Authors: Lais Cavalcanti Dos Santos Velasco de Souza; Lucas Martins Alcântara; Pãmella Antunes de Macêdo-Sales; Nathália Faria Reis; Débora Sena de Oliveira; Ricardo Luiz Dantas Machado; Reinaldo Barros Geraldo; André Luis Souza Dos Santos; Vítor Francisco Ferreira; Daniel Tadeu Gomes Gonzaga; Fernando de Carvalho da Silva; Helena Carla Castro; Andréa Regina de Souza Baptista Journal: Pharmaceuticals (Basel) Date: 2022-01-01