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Molecules 2016, 21(12), 1757; doi:10.3390/molecules21121757

Pharmacological Properties of Riparin IV in Models of Pain and Inflammation

1
Faculdade de Farmácia, Universidade Federal da Bahia, 40170-290 Salvador, BA, Brazil
2
Centro de Pesquisas Gonçalo Moniz, FIOCRUZ, 40296-710 Salvador, BA, Brazil
3
Laboratório de Tecnologia Farmacêutica, Universidade Federal da Paraíba, 58051-900 João Pessoa, PB, Brazil
4
Departamento de Bioquímica e Farmacologia, Universidade Federal do Piauí, 64049-550 Teresina, PI, Brazil
5
Centro de Biotecnologia e Terapia Celular, Hospital São Rafael, 41253-190 Salvador, BA, Brazil
*
Author to whom correspondence should be addressed.
Academic Editor: David J. Newman
Received: 11 November 2016 / Revised: 7 December 2016 / Accepted: 17 December 2016 / Published: 21 December 2016
(This article belongs to the Special Issue Natural Product: A Continuing Source of Novel Drug Leads)
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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. View Full-Text
Keywords: anti-inflammatory; antinociception; PGE2; cytokines; riparins anti-inflammatory; antinociception; PGE2; cytokines; riparins
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MDPI and ACS Style

Nascimento, O.A.; Espírito-Santo, R.F.; Opretzka, L.C.F.; Barbosa-Filho, J.M.; Gutierrez, S.J.C.; Villarreal, C.F.; Soares, M.B.P. Pharmacological Properties of Riparin IV in Models of Pain and Inflammation. Molecules 2016, 21, 1757.

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