| Texto completo | |
| Autor(es): Mostrar menos - |
Pina, Licia T. S.
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Rabelo, Thallita K.
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Trindade, Gabriela G. G.
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Almeida, Iggo K. S.
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Oliveira, Marlange A.
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dos Santos, Priscila L.
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Souza, Diego Santos
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de Menezes-Filho, Jose E. R.
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Lins de Vasconcelos, Carla Maria
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Santos, Sandra L.
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Scotti, Luciana
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Scotti, Marcus T.
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Araujo, Adriano A. S.
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Quintans, Jullyana S. S.
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Quintans Junior, Lucindo J.
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Guimaraes, Adriana G.
Número total de Autores: 16
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| Tipo de documento: | Artigo Científico |
| Fonte: | Journal of Pharmacy and Pharmacology; v. 74, n. 11, p. 11-pg., 2022-08-17. |
| Resumo | |
Objectives Considering that gamma-terpinene (gamma-TPN) is a monoterpene found in Cannabis oil, with high lipophilicity and limited pharmacokinetics, our objective was to evaluate whether its complexation in beta-cyclodextrin (gamma-TPN/beta-CD) could improve its physicochemical properties and action on cancer pain, as well as verify the mechanisms of action involved. Methods The gamma-TPN/beta-CD was prepared and submitted to physicochemical characterization. Animals with sarcoma 180 were treated (vehicle, gamma-TPN 50 mg/kg, gamma-TPN/beta-CD 5 mg/kg or morphine) and assessed for hyperalgesia, TNF-alpha and IL-1 beta levels, iNOS and c-Fos activity. The effects of gamma-TPN on calcium channels were studied by patch-clamp and molecular docking. Results beta-CD improved the physicochemical properties and prolonged the anti-hyperalgesic effect of gamma-TPN. This compound also reduced the levels of IL-1 beta, TNF-alpha and iNOS in the tumour, and c-Fos protein in the spinal cord. In addition, it reduced Ca2+ current, presenting favourable chemical interactions with different voltage-dependent calcium channels. Conclusion These results indicate that the complexation of gamma-TPN into beta-CD increases its stability and time effect, reducing spinal neuroactivity and inflammation by blocking calcium channels. (AU) | |
| Processo FAPESP: | 19/18918-0 - Participação do óxido nítrico nas arritmias cardíacas durante o Hipotireoidismo |
| Beneficiário: | Diego Santos de Souza |
| Modalidade de apoio: | Bolsas no Brasil - Pós-Doutorado |