Promising Effects of Casearins in Tumor-Bearing Mice and Antinociceptive Action against Oncologic Pain: Molecular Docking and In Vivo Findings

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Autor(es): dc.contributorFederal University of Piauí-
Autor(es): dc.contributorAnimals Veterinary Hospital-
Autor(es): dc.contributorOswaldo Cruz Foundation-
Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.creatorSilva, Jurandy do Nascimento-
Autor(es): dc.creatorBeserra Filho, José Ivo Araújo-
Autor(es): dc.creatorAcha, Boris Timah-
Autor(es): dc.creatorAlmeida, Fernanda Regina de Castro-
Autor(es): dc.creatorBatista, Emanuelle Karine Frota-
Autor(es): dc.creatorSilva, Valdenizia Rodrigues-
Autor(es): dc.creatorBomfim, Larissa Mendes-
Autor(es): dc.creatorSoares, Milena Botelho Pereira-
Autor(es): dc.creatorBezerra, Daniel Pereira-
Autor(es): dc.creatordos Santos, André Gonzaga-
Autor(es): dc.creatorde Andrade, Francisco das Chagas Pereira-
Autor(es): dc.creatorMendes, Anderson Nogueira-
Autor(es): dc.creatorArcanjo, Daniel Dias Rufino-
Autor(es): dc.creatorFerreira, Paulo Michel Pinheiro-
Data de aceite: dc.date.accessioned2025-08-21T20:42:54Z-
Data de disponibilização: dc.date.available2025-08-21T20:42:54Z-
Data de envio: dc.date.issued2025-04-29-
Data de envio: dc.date.issued2024-05-01-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.3390/ph17050633-
Fonte completa do material: dc.identifierhttps://hdl.handle.net/11449/302165-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/302165-
Descrição: dc.descriptionSafer analgesic drugs remain a hard challenge because of cardiovascular and/or gastrointestinal toxicity, mainly. So, this study evaluated in vivo the antiproliferative actions of a fraction with casearins (FC) from Casearia sylvestris leaves against human colorectal carcinomas and antihyperalgesic effects on inflammatory- or opiate-based pain relief and oncologic pain in Sarcoma 180 (S180)-bearing mice. Moreover, docking investigations evaluated the binding among Casearin X and NMDA(N-methyl-D-aspartate)-type glutamate receptors. HCT-116 colorectal carcinoma-xenografted mice were treated with FC for 15 days. Antinociceptive assays included chemically induced algesia and investigated mechanisms by pharmacological blockade. Intraplantar region S180-bearing animals received a single dose of FC and were examined for mechanical allodynia and behavior alterations. AutoDock Vina determined molecular interactions among Cas X and NMDA receptor subunits. FC reduced tumor growth at i.p. (5 and 10 mg/kg) and oral (25 mg/kg/day) doses (31.12–39.27%). FC reduced abdominal pain, as confirmed by formalin and glutamate protocols, whose antinociception activity was blocked by naloxone and L-NAME (neurogenic phase) and naloxone, atropine, and flumazenil (inflammatory phase). Meanwhile, glibenclamide potentiated the FC analgesic effects. FC increased the paw withdrawal threshold without producing changes in exploratory parameters or motor coordination. Cas X generated a more stable complex with active sites of the NMDA receptor GluN2B subunits. FC is a promising antitumor agent against colorectal carcinomas, has peripheral analgesic effects by desensitizing secondary afferent neurons, and inhibits glutamate release from presynaptic neurons and/or their action on cognate receptors. These findings emphasize the use of clerodane diterpenes against cancer-related pain conditions.-
Descrição: dc.descriptionLaboratory of Experimental Cancerology (LabCancer) Department of Biophysics and Physiology Federal University of Piauí-
Descrição: dc.descriptionDepartment of Chemistry Federal University of Piauí-
Descrição: dc.descriptionLaboratory of Functional and Molecular Studies in Physiopharmacology (Lafmol) Department of Biophysics and Physiology Federal University of Piauí-
Descrição: dc.descriptionLaboratory of Pain Pharmacology Department of Biochemistry and Pharmacology Federal University of Piauí-
Descrição: dc.descriptionAnimals Veterinary Hospital-
Descrição: dc.descriptionLaboratory of Tissue Engineering and Immunopharmacology Oswaldo Cruz Foundation-
Descrição: dc.descriptionLaboratory of Pharmacognosy Faculty of Pharmaceutical Sciences State University Júlio de Mesquita Filho-
Descrição: dc.descriptionLaboratory of Innovation in Science and Technology (Lacitec) Department of Biophysics and Physiology Federal University of Piauí-
Descrição: dc.descriptionLaboratory of Pharmacognosy Faculty of Pharmaceutical Sciences State University Júlio de Mesquita Filho-
Idioma: dc.languageen-
Relação: dc.relationPharmaceuticals-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectanticancer action-
Palavras-chave: dc.subjectclerodane diterpenes-
Palavras-chave: dc.subjectcolorectal carcinoma-
Palavras-chave: dc.subjectglutamate receptors-
Palavras-chave: dc.subjectsarcoma 180-
Título: dc.titlePromising Effects of Casearins in Tumor-Bearing Mice and Antinociceptive Action against Oncologic Pain: Molecular Docking and In Vivo Findings-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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