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

PLoS ONE ◽  
2021 ◽  
Vol 16 (11) ◽  
pp. e0258094
Author(s):  
Maria Alice Miranda Bezerra Medeiros ◽  
Mariana Gama e Silva ◽  
Jackson de Menezes Barbosa ◽  
Érica Martins de Lavor ◽  
Tiago Feitosa Ribeiro ◽  
...  
Keyword(s):  
Acid Metabolism ◽  
General Structure ◽  
Experimental Models ◽  
Arachidonic Acid Metabolism ◽  
Nociceptive Behavior ◽  
Docking Analysis ◽  
Molecular Modification ◽  
Anti Inflammatory ◽  
Acute And Chronic Inflammation ◽  
Inflammatory Effect

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.

Anti-inflammatory Effect of Picrorhiza kurroa in Experimental Models of Inflammation

Planta Medica ◽  
2016 ◽  
Vol 82 (16) ◽  
pp. 1403-1409 ◽  
Author(s):  
Rohit Kumar ◽  
Yogendra Gupta ◽  
Surender Singh ◽  
Arun Raj
Keyword(s):  
Experimental Models ◽  
Picrorhiza Kurroa ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Effects of Tebufelone (NE-11740), a new anti-inflammatory drug, on arachidonic acid metabolism

1994 ◽  
Vol 41 (3-4) ◽  
pp. 156-163 ◽  
Author(s):  
Steven M. Weisman ◽  
Matthew J. Doyle ◽  
Kenneth R. Wehmeyer ◽  
Barbara A. Hynd ◽  
Thomas H. Eichhold ◽  
...  
Keyword(s):  
Arachidonic Acid ◽  
Acid Metabolism ◽  
Arachidonic Acid Metabolism ◽  
Inflammatory Drug ◽  
Anti Inflammatory

scholarly journals Machaerium hirtum (Vell.) Stellfeld Alleviates Acute Pain and Inflammation: Potential Mechanisms of Action

Biomolecules ◽  
2020 ◽  
Vol 10 (4) ◽  
pp. 590 ◽  
Author(s):  
Juliana Agostinho Lopes ◽  
Vinícius Peixoto Rodrigues ◽  
Marcelo Marucci Pereira Tangerina ◽  
Lucia Regina Machado da Rocha ◽  
Catarine Massucato Nishijima ◽  
...  
Keyword(s):  
Transient Receptor Potential ◽  
Antinociceptive Effect ◽  
Folk Medicine ◽  
Receptor Potential ◽  
Experimental Models ◽  
Transient Receptor Potential Channels ◽  
Anti Inflammatory ◽  
Potential Channels ◽  
Inflammatory Effect

Machaerium hirtum (Vell.) Stellfeld (Fabaceae) known in Brazil as “jacaranda de espinho” or “espinheira santa nativa” is a medicinal plant commonly used in folk medicine to treat ulcers, cough and diarrhea. This study aimed to investigate the anti-inflammatory and antinociceptive effects of hydroalcoholic extracts from M. hirtum twig (HEMh) using in vivo experimental models of nociception through the involvement of transient receptor potential channels, acid-sensing ion channel (ASIC), nitrergic, opioidergic, glutamatergic, and supraspinal pathways. Our results revealed an antinociceptive effect of HEMh mediated by the opioidergic, l-arginine-nitric oxide and glutamate systems, as well as by interactions with TRPA1/ASIC channels. The anti-inflammatory effect of HEMh evaluated with a xylene-induced ear edema and by the involvement of arachidonic acid and prostaglandin E2 (PGE2) showed involvement of the COX pathway, based on observed decreases in PGE2 levels. A phytochemical investigation of the HEMh led to the isolation of α-amyrin, β-amyrin, allantoin, apigenin-7-methoxy-6-C-β-d-glucopyranoside, and apigenin-6-C-β-d-glucopyranosyl-8-C-β-d-xylopyranoside. In conclusion, the acute oral administration of HEMh inhibits the nociceptive behavioral response in animals through the nitrergic, opioid, glutamatergic pathways, and by inhibition of the TRPA1 and ASIC channels, without causing locomotor dysfunction. In addition, its anti-inflammatory effect is associated with the COX pathway and decreased PGE2 levels.

scholarly journals Advantages of the use of metformin in patients with impaired uric acid metabolism

2021 ◽  
Vol 93 (5) ◽  
Author(s):  
Maksim S. Eliseev ◽  
Taras S. Panevin ◽  
Olga V. Zhelyabina ◽  
Evgeny L. Nasonov
Keyword(s):  
Type 2 Diabetes ◽  
Uric Acid ◽  
Mechanism Of Action ◽  
Acid Metabolism ◽  
Current Data ◽  
Hypoglycemic Effect ◽  
Anti Inflammatory ◽  
Effective Drugs ◽  
Inflammatory Effect

Metformin is one of the oldest and at the same time relevant and effective drugs for the treatment of type 2 diabetes. At the same time, the mechanism of the hypoglycemic effect was not completely clear until recently. Current data suggest that the mechanism of action of metformin contributes to the development of an anti-inflammatory effect, as well as a decrease in the level of uric acid, and its use can be potentially useful in patients with hyperuricemia and gout.

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