Francisco Lucas A. Batista , Sandra Maria B. de Araújo , Daniela Braga de Sousa , Francisco Bastos C. Sobrinho , Maria Gabriely de Lima Silva , Maria Rayane C. de Oliveira , Roger Henrique S. da Costa , Lindaiane Bezerra Rodrigues , Franciglauber Silva Bezerra , Djane Ventura de Azevedo , Antônio Eufrásio Vieira-Neto , Francisco Ernani A. Magalhães , Irwin Rose Alencar de Menezes
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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 GABA<sub>A</sub>, 5-HT<sub>1</sub>, 5-HT<sub>2A/2C</sub> and 5-HT<sub>3A/3B</sub> 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 GABA<sub>A</sub> system. Both anxiolytic and anticonvulsant effects were corroborated by the potential of the interaction of ES by <em>in silico</em> assay. 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引用次数: 0
摘要
欧鼠李属植物的活性化合物具有开发治疗慢性疾病(如焦虑症和癫痫发作)药物的潜力。本研究旨在调查欧芹叶精油(OEFOb)及其主要成分雌甾醇(ES)对成年斑马鱼(aZF)的抗惊厥和抗焦虑作用。用 OEFOb 或 ES 或载体处理成年斑马鱼,并对其进行毒性、开放场、焦虑和惊厥测试,通过分子对接试验验证了雌甾醇与 GABA 能受体和血清素能受体的相互作用。结果表明,口服 OEFOb 和 ES 不会对 aZF 产生毒性作用,并且在 GABAA、5-HT1、5-HT2A/2C 和 5-HT3A/3B 受体的参与下,对酒精戒断引起的焦虑表现出类似抗焦虑的作用。通过调节 GABAA 系统,OEFOb 和 ES 显示出抗惊厥潜力,可减轻戊四唑(PTZ)诱发的癫痫发作。ES 的相互作用潜能也证实了这两种抗焦虑和抗惊厥作用。这些研究样本证明了使用这些化合物开发抗焦虑和抗惊厥新药的药理证据和潜力。
Anticonvulsant and anxiolytic-like potential of the essential oil from the Ocimum basilicum Linn leaves and its major constituent estragole on adult zebrafish (Danio rerio)
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.
期刊介绍:
Neurochemistry International is devoted to the rapid publication of outstanding original articles and timely reviews in neurochemistry. Manuscripts on a broad range of topics will be considered, including molecular and cellular neurochemistry, neuropharmacology and genetic aspects of CNS function, neuroimmunology, metabolism as well as the neurochemistry of neurological and psychiatric disorders of the CNS.