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

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dc.contributor.authorMachado, Taisa Maria Mendes Matuiama
dc.contributor.authorAquino, Iara Goncalves
dc.contributor.authorFranchin, Marcelo
dc.contributor.authorZarraga, Miguel O.
dc.contributor.authorBustos, Daniel
dc.contributor.authorSpada, Fernanda Papa
dc.contributor.authorNapimoga, Marcelo Henrique
dc.contributor.authorClemente-Napimoga, Juliana Trindade
dc.contributor.authorAlencar, Severino Matias
dc.contributor.authorBenso, Bruna
dc.contributor.authorAbdalla, Henrique Ballassini
dc.date.accessioned2025-01-20T16:04:30Z
dc.date.available2025-01-20T16:04:30Z
dc.date.issued2024
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.
dc.fuente.origenWOS
dc.identifier.doi10.1016/j.ejphar.2024.177093
dc.identifier.eissn1879-0712
dc.identifier.issn0014-2999
dc.identifier.urihttps://doi.org/10.1016/j.ejphar.2024.177093
dc.identifier.urihttps://repositorio.uc.cl/handle/11534/89781
dc.identifier.wosidWOS:001356076900001
dc.language.isoen
dc.revistaEuropean journal of pharmacology
dc.rightsacceso restringido
dc.subjectApocynin
dc.subjectChalcone
dc.subjectTRPV1
dc.subjectOrofacial pain
dc.subjectTrigeminal ganglion
dc.subjectGalleria mellonella
dc.titleNovel apocynin regulates TRPV1 activity in the trigeminal system and controls pain in a temporomandibular joint neurogenic model
dc.typeartículo
dc.volumen985
sipa.indexWOS
sipa.trazabilidadWOS;2025-01-12
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