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Antinociceptive and anti-inflammatory effects of hydrazone derivatives and their possible mechanism of action in mice.

ABSTRACT: Pain and inflammation are unpleasant experiences that usually occur as a result of tissue damage. Despite the number of existing analgesic drugs, side effects limit their use, stimulating the search for new therapeutic agents. In this sense, five hydrazone derivatives (H1, H2, H3, H4, and H5), with general structure R1R2C = NNR3R4, were synthesized with molecular modification strategies. In this paper, we describe the ability of hydrazone derivatives to attenuate nociceptive behavior and the inflammatory response in mice. Antinociceptive activity was evaluated through acetic acid-induced writhing and formalin-induced nociception tests. In both experimental models, the hydrazone with the greatest potency (H5) significantly (p < 0.05) reduced nociceptive behavior. Additionally, methods of acute and chronic inflammation induced by different chemicals (carrageenan and histamine) were performed to evaluate the anti-inflammatory effect of H5. Moreover, molecular docking analysis revealed that H5 can block the COX-2 enzyme, reducing arachidonic acid metabolism and consequently decreasing the production of prostaglandins, which are important inflammatory mediators. H5 also changes locomotor activity. In summary, H5 exhibited relevant antinociceptive and anti-inflammatory potential and acted on several targets, making it a candidate for a new multi-target oral anti-inflammatory drug.

SUBMITTER: Medeiros MAMB

PROVIDER: S-EPMC8612535 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature

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Antinociceptive and anti-inflammatory effects of hydrazone derivatives and their possible mechanism of action in mice.

Medeiros Maria Alice Miranda Bezerra MAMB Gama E Silva Mariana M de Menezes Barbosa Jackson J Martins de Lavor Érica É Ribeiro Tiago Feitosa TF Macedo Cícero André Ferreira CAF de Souza Duarte-Filho Luiz Antonio Miranda LAM Feitosa Thiala Alves TA de Jesus Silva Jussara J Fokoue Harold Hilarion HH Araújo Cleônia Roberta Melo CRM de Assis Gonsalves Arlan A Augusto de Araújo Ribeiro Luciano L Almeida Jackson Roberto Guedes da Silva JRGDS

PloS one 20211124 11

Pain and inflammation are unpleasant experiences that usually occur as a result of tissue damage. Despite the number of existing analgesic drugs, side effects limit their use, stimulating the search for new therapeutic agents. In this sense, five hydrazone derivatives (H1, H2, H3, H4, and H5), with general structure R1R2C = NNR3R4, were synthesized with molecular modification strategies. In this paper, we describe the ability of hydrazone derivatives to attenuate nociceptive behavior and the inf ...[more]

PMID: 34818331

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Project description:Prunus cerasus (P. cerasus) is an alternative-medicine used traditionally for amelioration of chronic-ailments marked by elevation in oxidative-stress like neuropathy. The oxidative-stress control was reported to ameliorate the inflammatory-process. This study aimed to phytochemically-investigate P. cerasus most-active phytochemicals utilizing in-vivo biological models to explore their gastroprotective, anti-inflammatory, and antinociceptive potentials and their possible mechanisms of action. Sonication with EtAc was used to extract P. cerasus fruit (Scf), and seed (Scs). The phytochemical-investigation of Scf was performed by RP-HPLC, while that of Scs was explored utilizing GC-FID. A bio-guided-fraction and isolation method was done utilizing column-chromatography, and have shown that cyanidin-3-glucoside (Cy3G) was the most-active constituent in Scf, while linoleic-acid (LA) was the most-active constituent in Scs. Scf, Scs, Cy3G, and LA significantly (p ? 0.05) protected the gastric-mucosa against HCl/EtOH-induced gastric-lesions. Scs (200?mg/kg) has shown the most gastroprotective-potentials, and had comparable-results to ranitidine (50?mg/kg). Scf, Scs, Cy3G, and LA have shown significant anti-inflammatory and antinociceptive potentials against carrageenan induced-edema and nociceptive-pain, respectively, where Scs (200?mg/kg) has shown the most anti-inflammatory and antinociceptive potentials, and had comparable results to ibuprofen (100?mg/kg). Scf, Scs, Cy3G, and LA have counter-acted carrageenan-induced oxidative-stress markers, with increased serum-catalase and reduced-glutathione levels, and decreased lipid-peroxidation. Histopathological-studies demonstrated gastroprotective potentials, regeneration and improvement of the spleen-structural architecture when treated with highest doses of Scs and Scf. The reduction of the pro-inflammatory TNF-alpha and IL-6, and elevation the anti-inflammatory factor IL-10 levels, spleen regenerative-capacity and oxidative-stress amelioration might be the main-mechanism responsible for P. cerasus anti-inflammatory potentials. P. cerasus appears to aid in ameliorating the inflammatory process, and reducing pain-thresholds while preserving the stomach.

Dataset Information

Antinociceptive and anti-inflammatory effects of hydrazone derivatives and their possible mechanism of action in mice.

Publications

Antinociceptive and anti-inflammatory effects of hydrazone derivatives and their possible mechanism of action in mice.

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