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1.
Neurochem Int ; 178: 105796, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38936553

RESUMO

The Ocimum species present active compounds with the potential to develop drugs for treating chronic disease conditions, such as anxiety and seizures. The present study aims to investigate the anticonvulsant and anxiolytic-like effect of the essential oil from O. basilicum Linn (OEFOb) leaves and its major constituent estragole (ES) in vivo on adult zebrafish (aZF) and in silico. The aZF were treated with OEFOb or ES or vehicle and submitted to the tests of toxicity, open-field, anxiety, and convulsion and validated the interactions of the estragole on the involvement of GABAergic and serotonergic receptors by molecular docking assay. The results showed that the oral administration of OEFOb and ES did not have a toxic effect on the aZF and showed anxiolytic-like effects with the involvement of GABAA, 5-HT1, 5-HT2A/2C and 5-HT3A/3B as well on anxiety induced by alcohol withdrawal. The OEFOb and ES showed anticonvulsant potential attenuating the seizures induced by pentylenetetrazole (PTZ) by modulation of the GABAA system. Both anxiolytic and anticonvulsant effects were corroborated by the potential of the interaction of ES by in silico assay. These study samples demonstrate the pharmacological evidence and potential for using these compounds to develop new anxiolytic and anticonvulsant drugs.


Assuntos
Derivados de Alilbenzenos , Anisóis , Ansiolíticos , Anticonvulsivantes , Ocimum basilicum , Óleos Voláteis , Folhas de Planta , Convulsões , Peixe-Zebra , Animais , Ansiolíticos/farmacologia , Ansiolíticos/química , Ansiolíticos/isolamento & purificação , Anticonvulsivantes/farmacologia , Anticonvulsivantes/química , Anticonvulsivantes/isolamento & purificação , Óleos Voláteis/farmacologia , Óleos Voláteis/isolamento & purificação , Óleos Voláteis/química , Folhas de Planta/química , Ocimum basilicum/química , Anisóis/farmacologia , Anisóis/isolamento & purificação , Derivados de Alilbenzenos/farmacologia , Convulsões/tratamento farmacológico , Convulsões/induzido quimicamente , Simulação de Acoplamento Molecular , Ansiedade/tratamento farmacológico , Masculino , Pentilenotetrazol/toxicidade
2.
Biomed Pharmacother ; 153: 113478, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-36076580

RESUMO

Valencene (VLN) is a sesquiterpene found in juices and essential oils of citrus species such as Cyperus rotundus. Considering the evidence that this species has anti-inflammatory effects, the present study aims to evaluate the anti-inflammatory activity of VLN in vivo and in silico. Swiss mice (n = 6) were orally treated according to their treatment groups as follows: VLN (10, 100 or 300 mg/kg), negative control (0.9% saline), and positive controls (indomethacin 25 mg/kg or promethazine 6 mg/kg). The anti-inflammatory activity was evaluated in murine models of acute and chronic inflammation. The inhibition of acute inflammation was evaluated in models of paw edema induced by different inflammatory agents (carrageenan, dextran, histamine, and arachidonic acid (AA)) and carrageenan-induced pleurisy and peritonitis. The modulation of chronic inflammation was evaluated in a granuloma model induced cotton pellets implantation. The interaction with inflammatory targets was evaluated in silico using molecular docking analysis. The administration of VLN to challenged mice significantly inhibited paw edema formation with no significant difference between the administered doses. The compound also reduced albumin extravasation, leukocyte recruitment, and the production of myeloperoxidase (MPO), IL-1ß, and TNF-α in both pleural and peritoneal lavages. According to the mathematical-statistical model observed in silico analysis, this compound has favorable energy to interact with the cyclooxygenase enzyme (COX-2) and the histamine 1 (H1) receptor. Finally, animals treated with the sesquiterpene showed a reduction in both granuloma weight and concentration of total proteins in a chronic inflammation model. Given these findings, it is concluded that NLV presents promising pharmacological activity in murine models of acute and chronic inflammation.


Assuntos
Anti-Inflamatórios não Esteroides , Sesquiterpenos , Animais , Anti-Inflamatórios/uso terapêutico , Anti-Inflamatórios não Esteroides/farmacologia , Carragenina/uso terapêutico , Ciclo-Oxigenase 2 , Edema/induzido quimicamente , Edema/tratamento farmacológico , Granuloma/tratamento farmacológico , Histamina , Inflamação/metabolismo , Camundongos , Simulação de Acoplamento Molecular , Extratos Vegetais/farmacologia , Sesquiterpenos/farmacologia
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