Riparin B, a Synthetic Compound Analogue of Riparin, Inhibits the Systemic Inflammatory Response and Oxidative Stress in Mice

Abstract

The aim of our study was to evaluate the anti-inflammatory, anti-nociceptive, and anti-oxidant action of Riparin B in vivo. We performed experiments in which we induced paw edema by carrageenan and other mediators, carrageenan-induced peritonitis and the level of myeloperoxidase (MPO) activity, pro-inflammatory cytokines (TNF-α and IL-1β), malondialdehyde (MDA) acid, and glutathione (GSH) from the peritoneal fluid. We also performed behavior tests such as acetic acid-induced writhing, formalin-induced linking, and the hot plate test. Among the doses tested of the Riparin B (1, 3, and 10 mg/kg), the dose of 10 mg/kg showed the strongest effect, and this dose was able to reduce the paw edema induced by carrageenan, dextran, histamine serotonin, bradykinin, 48/80, and PGE2. Similarly, the Riparin B in the same dose reduced cell migration and significantly decreased the nociception induced by formalin and acetic acid and reversed the parameters of the oxidative stress. Thus, we can infer that Riparin B exhibits anti-inflammatory, anti-nociceptive, and anti-oxidant actions in vivo.

Methyl-β-cyclodextrin Inclusion Complex with β-Caryophyllene: Preparation, Characterization, and Improvement of Pharmacological Activities

“…The second phase (24 h after induction of edema) is characterized by the intense accumulation of cells such as macrophages, eosinophils, and lymphocytes. 54 , 55 …”

Potencial bioativo dos análogos sintéticos das riparinas: uma revisão sistemática

“…A Rip-B, apresentou propriedades antibacterianas por efeito modulador, antiinflamatórias, antinociceptivo, antioxidante e antiparasitária (Costa et al, 2016;Mafud et al, 2018;Nunes et al, 2014;Santiago et al, 2015). As riparinas C e D mostraram atividade antibacteriana intrínseca e moduladora, antioxidante e antitumoral (Costa et al, 2016;Nunes et al, 2014).…”

“…O efeito antioxidante foi demonstrado utilizando outras metodologias, como analisado pela medição de glutationa (GSH) e malondialdeído (MDA), o GSH é um antioxidante endógeno enzimático e o MDA é gerado por processos lipoperoxidativos, os resultados demonstram que a Rip-B, é capazes de aumentar os níveis de GSH e diminuir a concentração de MDA (Santiago et al, 2015).…”

“…Em estudos in vivo, as Rip-A e Rip-B mostraram propriedades anti-inflamatórias e antinociceptiva, a inflamação está ligada a efeitos danosos vasculares e celulares, encontrados em um ambiente de intenso estresse oxidativo. Os modelos experimentais com roedores indicaram que as substâncias inibiram o dano vascular, a produção de citocinas pró-inflamatórias (Fator de Necrose Tumoral alfa -TNF-α e Interleucina 1 beta -IL-1β) nos locais afetados, modulando o processo de recrutamento de leucócitos e adesão de células endoteliais (Santiago et al, 2015;Silva et al, 2015).…”

In-silico studies of Riparin B in the design of drugs: Physicochemical, pharmacokinetic and pharmacodynamic parameters

“…Synthetic riparin analogues have already demonstrated antioxidant, including analysis of isolated mitochondria of the brain of mice [6,7] , antimicrobial [8] , antiparasitic [9] , as well as leishmanicide [10] , vasodilator [7] and anti-inflammatory [11] activities. Among the properties of synthetic riparins, their action in the Central Nervous System (CNS), such anxiolytic effects [12] in anxiety models, without affecting the locomotion of the animals used in the experiment [7] , which make them target molecules of new studies aimed at obtaining therapeutic alternatives, and can be used in the treatment of AD.…”