Author | Nascimento, Olívia Azevêdo | |
Author | Santo, Renan Fernandes do Espírito | |
Author | Opretzka, Luíza Carolina França | |
Author | Barbosa Filho, José Maria | |
Author | Gutierrez, Stanley Juan Chavez | |
Author | Villarreal, Cristiane Flora | |
Author | Soares, Milena Botelho Pereira | |
Access date | 2017-03-16T17:14:05Z | |
Available date | 2017-03-16T17:14:05Z | |
Document date | 2016 | |
Citation | NASCIMENTO, O. A. et al. Pharmacological Properties of Riparin IV in Models of Pain and Inflammation. Molecules, v. 21, p. 1757, 2016. | pt_BR |
ISSN | 1420-3049 | pt_BR |
URI | https://www.arca.fiocruz.br/handle/icict/18064 | |
Sponsorship | Fundação de Amparo à Pesquisa do Estado da Bahia (FAPESB), Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) and Fundação Oswaldo Cruz (FIOCRUZ). | pt_BR |
Language | eng | pt_BR |
Publisher | MDPI | pt_BR |
Rights | open access | pt_BR |
Subject in Portuguese | Anti-inflamatórios | pt_BR |
Subject in Portuguese | Antinocicepção | pt_BR |
Subject in Portuguese | PGE2 | pt_BR |
Subject in Portuguese | Citocinas | pt_BR |
Subject in Portuguese | Riparinas | pt_BR |
Title | Pharmacological Properties of Riparin IV in Models of Pain and Inflammation | pt_BR |
Type | Article | pt_BR |
DOI | 10.3390/molecules21121757 | |
Abstract | Riparins, natural alkaloids of the alkamide group, can be synthesized by simple methods, enhancing their potential application in pharmaceutical development. Here, the pharmacological properties of riparins were investigated in in vitro and in vivo assays of pain and inflammation in Swiss mice. Inflammatory mediators were measured by radioimmunoassay and Real-Time PCR. Riparins I, II, III and IV (1.56-100 mg/kg; ip) produced dose-related antinociceptive effects in the formalin test, exhibiting ED50 values of 22.93, 114.2, 31.05 and 6.63 mg/kg, respectively. Taking the greater potency as steering parameter, riparin IV was further investigated. Riparin IV did not produce antinociceptive effect on the tail flick, suggesting that its antinociception is not a centrally-mediated action. In fact, riparin IV (1.56-25 mg/kg) produced dose-related antinociceptive and antiedematogenic effects on the complete Freund's adjuvant (CFA)-induced paw inflammation in mice. During CFA-induced inflammation, riparin IV did not modulate either the production of cytokines, TNF-α and IL-10, or COX-2 mRNA expression. On the other hand, riparin IV decreased the PGE₂ levels in the inflamed paw. In in vitro assays, riparin IV did not exhibit suppressive activities in activated macrophages. These results indicate, for the first time, that riparin IV induces antinociceptive and anti-inflammatory effects, possibly through the inhibition of prostanoid production. | pt_BR |
Affilliation | Universidade Federal da Bahia. Faculdade de Farmácia. Salvador, BA, Brasil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
Affilliation | Universidade Federal da Bahia. Faculdade de Farmácia. Salvador, BA, Brasil | pt_BR |
Affilliation | Universidade Federal da Paraíba. Laboratório de Tecnologia Farmacêutica. João Pessoa, PB, Brasil | pt_BR |
Affilliation | Universidade Federal do Piauí. Departamento de Bioquímica e Farmacologia. Teresina, PI, Brasil | pt_BR |
Affilliation | Universidade Federal da Bahia. Faculdade de Farmácia. Salvador, BA, Brasil / Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil / Hospital São Rafael. Centro de Biotecnologia e Terapia Celular. Salvador, BA, Brasil | pt_BR |
Subject | Anti-inflammatory | pt_BR |
Subject | Antinociception | pt_BR |
Subject | PGE2 | pt_BR |
Subject | Cytokines | pt_BR |
Subject | Riparins | pt_BR |