Author | Moreira, Fernanda de Lima | |
Author | Riul, Thalita Bachelli | |
Author | Moreira, Marcela de Lima | |
Author | Pilon, Alan Cesar | |
Author | Dias-Baruffi, Marcelo | |
Author | Araújo, Márcio Sobreira Silva | |
Author | Lopes, Norberto Peporine | |
Author | Oliveira, Anderson R M de | |
Access date | 2022-10-03T15:37:09Z | |
Available date | 2022-10-03T15:37:09Z | |
Document date | 2018 | |
Citation | MOREIRA, Fernanda de Lima et al. Leishmanicidal Effects of Piperlongumine (Piplartine) and Its Putative Metabolites. Planta Med., v. 84, n. 15, p. 1141-1148, 2018. doi: 10.1055/a-0614-2680. DOI: 10.1055/a-0614-2680 | en_US |
ISSN | 0032-0943 | en_US |
URI | https://www.arca.fiocruz.br/handle/icict/54974 | |
Language | eng | en_US |
Publisher | George Thieme | en_US |
Rights | restricted access | en_US |
Title | Leishmanicidal Effects of Piperlongumine (Piplartine) and Its Putative Metabolites | en_US |
Type | Article | en_US |
DOI | 10.1055/a-0614-2680 | |
Abstract | Piperlongumine is an amide alkaloid found in Piperaceae species that shows a broad spectrum of biological properties, including antitumor and antiparasitic activities. Herein, the leishmanicidal effect of piperlongumine and its derivatives produced by a biomimetic model using metalloporphyrins was investigated. The results showed that IC (50) values of piperlongumine in promastigote forms of Leishmania infantum and Leishmania amazonensis were 7.9 and 3.3 mu M, respectively. The IC (50) value of piperlongumine in the intracellular amastigote form of L.amazonensis was 0.4 mu M, with a selectivity index of 25. The piperlongumine biomimetic derivatives, Ma and Mb, also showed leishmanicidal effects. We also carried out an in vitro metabolic degradation study showing that Ma is the most stable piperlongumine derivative in rat liver microsome incubations. The results presented here indicate that piperlongumine is a potential leishmanicidal candidate and support the biomimetic approach for development of new antileishmanial derivatives. | en_US |
Affilliation | Universidade de São Paulo. Faculdade de Ciências Farmacêuticas de Ribeirão Preto. Ribeirão Preto, SP, Brazil. | en_US |
Affilliation | Universidade de São Paulo. Faculdade de Ciências Farmacêuticas de Ribeirão Preto. Departamento de Análises Clínicas, Toxicológicas e Bromatológicas. Ribeirão Preto, SP, Brazil. | en_US |
Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brazil. | en_US |
Affilliation | Universidade de São Paulo. Faculdade de Ciências Farmacêuticas de Ribeirão Preto. Núcleo de Pesquisa em Produtos Naturais e Sintéticos. Ribeirão Preto, SP, Brazil. | en_US |
Affilliation | Universidade de São Paulo. Faculdade de Ciências Farmacêuticas de Ribeirão Preto. Departamento de Análises Clínicas, Toxicológicas e Bromatológicas. Ribeirão Preto, SP, Brazil. | en_US |
Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brazil. | en_US |
Affilliation | Universidade de São Paulo. Faculdade de Ciências Farmacêuticas de Ribeirão Preto. Núcleo de Pesquisa em Produtos Naturais e Sintéticos. Ribeirão Preto, SP, Brazil. | en_US |
Affilliation | Universidade de São Paulo. Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto. Departamento de Química. Ribeirão Preto, SP, Brazil. | en_US |
Subject | Cyclic amides | en_US |
Subject | Piplartine | en_US |
Subject | Metalloporphyrin | en_US |
Subject | Leishmaniasis | en_US |
Subject | Selectivity index | en_US |
Subject | Piperlongumine | en_US |
Subject | Piperaceae | en_US |
Subject | Analogues | en_US |