| Author | Andrade Neto, Valter Viana | |
| Author | Guedes, Herbert Leonel de Matos | |
| Author | Gomes, Daniel Cláudio de Oliveira | |
| Author | Cavalheiro, Marilene Marcuzzo do Canto | |
| Author | Bergmann, Bartira Rossi | |
| Author | Santos, Eduardo Caio Torres | |
| Access date | 2017-05-30T13:23:16Z | |
| Available date | 2017-05-30T13:23:16Z | |
| Document date | 2012 | |
| Citation | ANDRADE NETO, Valter Viana; et al. The stepwise selection for ketoconazole resistance induces upregulation of C14-demethylase (CYP51) in Leishmania amazonensis. Mem Inst Oswaldo Cruz, v..107, n.3, p.416-419. May 2012. | pt_BR |
| ISSN | 0074-0276 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/19059 | |
| Language | eng | pt_BR |
| Publisher | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz | pt_BR |
| Rights | open access | |
| Subject in Portuguese | Resistência a medicamentos | pt_BR |
| Subject in Portuguese | Azóis | pt_BR |
| Subject in Portuguese | Ergosterol | pt_BR |
| Subject in Portuguese | Biossíntese | pt_BR |
| Subject in Portuguese | Leishmania | pt_BR |
| Title | The stepwise selection for ketoconazole resistance induces upregulation of C14-demethylase (CYP51) in Leishmania amazonensis | pt_BR |
| Type | Article | |
| Abstract | Ketoconazole is a clinically safe antifungal agent that also inhibits the growth of Leishmania spp. A study was undertaken to determine whether Leishmania parasites are prone to becoming resistant to ketoconazole by upregulating C14-demethylase after stepwise pharmacological pressure. Leishmania amazonensis promastigotes [inhibitory concentration (IC)50 = 2 μM] were subjected to stepwise selection with ketoconazole and two resistant lines were obtained, La8 (IC50 = 8 μM) and La10 (IC50 = 10 μM). As a result, we found that the resistance level was directly proportional to the C14-demethylase mRNA expression level; we also observed that expression levels were six and 12 times higher in La8 and La10, respectively. This is the first demonstration that L. amazonensis can up-regulate C14-demethylase in response to drug pressure and this report contributes to the understanding of the mechanisms of parasite resistance. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Tripanosomatídeos. Rio de Janeiro, RJ. Brasil. | pt_BR |
| Affilliation | Universidade Federal do Rio de Janeiro. Instituto de Biofísica Carlos Chagas Filho. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Universidade Federal do Rio de Janeiro. Instituto de Biofísica Carlos Chagas Filho. Rio de Janeiro, RJ, Brasil / Universidade Federal do Espírito Santo. Departamento de Patologia. Núcleo de Doenças Infecciosas. Vitória, ES, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Tripanosomatídeos. Rio de Janeiro, RJ. Brasil. | pt_BR |
| Affilliation | Universidade Federal do Rio de Janeiro. Instituto de Biofísica Carlos Chagas Filho. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Tripanosomatídeos. Rio de Janeiro, RJ. Brasil. | pt_BR |
| Subject | drug resistance | pt_BR |
| Subject | azoles | pt_BR |
| Subject | ergosterol biosynthesis | pt_BR |
| Subject | Leishmania amazonensis | pt_BR |
| e-ISSN | 1678-8060 | |
| xmlui.metadata.dc.subject.ods | 03 Saúde e Bem-Estar | |
