| Author | Bezerra, Rômulo José Soares | |
| Author | Silva, Edson F. da | |
| Author | Echevarria, Aurea | |
| Author | Silva, Liliane Gomes da | |
| Author | Finkelstein, Léa Cysne | |
| Author | Monteiro, Fabiane Pereira | |
| Author | Leon, Leonor L. | |
| Author | Genestra, Marcelo | |
| Access date | 2019-04-11T10:45:58Z | |
| Available date | 2019-04-11T10:45:58Z | |
| Document date | 2008 | |
| Citation | BEZERRA, Rômulo José Soares et al. Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2- phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis. Journal of Enzyme Inhibition and Medicinal Chemistry, v. 23, n. 3, p. 328–333, June 2008. | pt_BR |
| ISSN | 1475-6366 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/32444 | |
| Language | eng | pt_BR |
| Publisher | Taylor & Francis | pt_BR |
| Rights | open access | |
| Subject in Portuguese | Leishmania amazonensis | pt_BR |
| Subject in Portuguese | Óxido Nítrico | pt_BR |
| Title | Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis | pt_BR |
| Type | Article | |
| DOI | 10.1080/14756360701585619 | |
| Abstract | L-arginine is involved in the production of both nitric oxide (NO), mediated by nitric oxide synthase (NOS) and L-ornithine, by arginase activity. It is generally accepted that NO regulation occurs mainly at the transcriptional level of NOS. In a previous work we purported that there is evidence that Leishmania sp. can produce NO from L-arginine. An arginase activity in its gene sequence has also been reported in Leishmania parasites. In a search for intracellular targets as potential antileishmanicidal agents, such as the L-arginine metabolism, we used 1,3,4-thiadiazolium mesoionic compounds, that have been demonstrated to be cytotoxic to the Leishmania amazonensis, when compared to Pentamidine isethionate as a reference drug. Parasites were assayed in absence/presence of 4'- and 3'-methoxy mesoionic derivatives in order to verify the effect on NO production and arginase activity in L. amazonensis. The results indicated that the drugs reduce from 70 to 90% of the NO production by the parasite and act on a soluble nitric oxide synthase purified from L. amazonensis promastigotes and axenic amastigotes. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ. Brasil. | pt_BR |
| Affilliation | Universidade Federal Rural do Rio de Janeiro. Departamento de Química. Seropédica, RJ, Brasil. | pt_BR |
| Affilliation | Universidade Federal Rural do Rio de Janeiro. Departamento de Química. Seropédica, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ. Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ. Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ. Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ. Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ. Brasil. | pt_BR |
| Subject | Leishmania amazonensis | pt_BR |
| Subject | Mesionic compounds | pt_BR |
| Subject | Phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine | pt_BR |
| Subject | Nitric oxide | pt_BR |
| Subject | Nitric oxide synthase | pt_BR |
| Subject | Arginase | pt_BR |
| DeCS | Óxido Nítrico Sintase | pt_BR |
| DeCS | Arginase | pt_BR |
| e-ISSN | 1475-6374 | |
