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Novel apocynin regulates TRPV1 activity in the trigeminal system and controls pain in a temporomandibular joint neurogenic model

dc.contributor.authorMendes Matuiama Machado, Taisa Maria
dc.contributor.authorGonçalves Aquino, Iara
dc.contributor.authorFranchin, Marcelo
dc.contributor.authorZarraga, Miguel O.
dc.contributor.authorBustos, Daniel
dc.contributor.authorPapa Spada, Fernanda
dc.contributor.authorHenrique Napimoga, Marcelo
dc.contributor.authorClemente-Napimoga, Juliana Trindade
dc.contributor.authorAlencar, Severino Matias
dc.contributor.authorBenso, Bruna
dc.contributor.authorBallassini Abdalla, Henrique
dc.date.accessioned2025-03-26T12:35:46Z
dc.date.available2025-03-26T12:35:46Z
dc.date.issued2024
dc.identifier.urihttp://repositorio.ucm.cl/handle/ucm/5874
dc.description.abstractObjective Herein, we investigate the potential analgesic effect of a newly synthesized chalcone-derived apocynin in a neurogenic pain model. Methods Molecular docking was used to foretell the apocynin binding features and dynamics with the TRPV1 channel, and the activity was tested in vitro, using transfected HEK 293T cells with the rat TRPV1 receptor. The analgesic effect of apocynin was investigated using a capsaicin-induced pain model. The expression of TRPV1, TRPA1, TRPM8, and MAPKs was assessed by electrophoresis, and immunosorbent assays were performed to quantify the neurotransmitters Substance P, Glutamate, and CGRP. A survival assay using Galleria mellonella was carried out to determine the toxicity. Results We observed that apocynin exhibits greater thermodynamic stability. Upon apocynin ligand binding, it changes the electrostatic potential for a predominantly electronegative state in the interior and neutral in its external vanilloid pocket. Treatment of apocynin induces antinociceptive effects against the noxious challenge of capsaicin. Histologically, apocynin decreased the number of TRPV1+ immunopositive cells. Electrophoresis showed reduced phosphorylation of p44/42 (ERK1/2) and decreased protein levels of substance P, and CGRP. In the survival assay, apocynin showed low toxicity. Conclusions In conclusion, we provide proof-of-principles that the newly synthesized apocynin compound effectively prevented nociception in a neurogenic model of orofacial pain.es_CL
dc.language.isoenes_CL
dc.rightsAtribución-NoComercial-SinDerivadas 3.0 Chile*
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/3.0/cl/*
dc.sourceEuropean Journal of Pharmacology, 985, 177093es_CL
dc.subjectApocynines_CL
dc.subjectChalconees_CL
dc.subjectTRPV1es_CL
dc.subjectOrofacial paines_CL
dc.subjectTrigeminal gangliones_CL
dc.subjectGalleria mellonellaes_CL
dc.titleNovel apocynin regulates TRPV1 activity in the trigeminal system and controls pain in a temporomandibular joint neurogenic modeles_CL
dc.typeArticlees_CL
dc.ucm.facultadFacultad de Medicinaes_CL
dc.ucm.indexacionScopuses_CL
dc.ucm.indexacionIsies_CL
dc.ucm.urisciencedirect.ucm.elogim.com/science/article/pii/S0014299924007830?via%3Dihubes_CL
dc.ucm.doidoi.org/10.1016/j.ejphar.2024.177093es_CL


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Atribución-NoComercial-SinDerivadas 3.0 Chile
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