Mendes Josiane Lima, da Silva Luiz Everson, do Amaral Wanderlei, Confortin Camila, Amâncio Ferreira Maria Kueirislene, Marinho Márcia Machado, da Silva Mendes Francisco Rogênio, Marinho Emmanuel Silva, Romão Ivana Carneiro, Magalhães Emanuel Paula, de Menezes Ramon Róseo Paula Pessoa Bezerra, de Menezes Jane Eire Silva Alencar, Dos Santos Hélcio Silva
State University of Ceará, Postgraduate Program in Biotechnology- Northeast Biotechnology Network (RENORBIO), Fortaleza, Ceará, Brazil.
Federal University of Paraná, Matinhos, Paraná, Brazil.
Chem Biodivers. 2025 Jul;22(7):e202403357. doi: 10.1002/cbdv.202403357. Epub 2025 Mar 27.
Benzodiazepines are medications used to treat anxiety and epilepsy disorders. However, because of the existing adverse effects, new and safer medications are being sought. Therefore, this study aims to evaluate the chemical composition and the anxiolytic and anticonvulsant actions of the essential oil of Marlierea eugeniopsoides and its majority constituents α-pinene and β-pinene. The toxicity was analyzed, and the anxiolytic behavior of fish treated with the oil was assessed in light/dark tests and open field tests (n = 6 animals/group). In the test to evaluate the anticonvulsant effect of the sample, pentylenetetrazole (PTZ) was used to induce seizures through immersion. Subsequently, the mechanism of action was investigated with the γ-aminobutyric acid (GABA) antagonist, and molecular docking and ADMET study was conducted. The study revealed that M. eugeniopsoides oil (spring and summer) was nontoxic and influenced zebrafish locomotion at all doses. Spring oil had anxiolytic effects at all doses, while summer oil showed this only at the highest dose. Both oils affected GABA, with spring oil displaying anticonvulsant properties, unlike summer oil, suggesting a seasonal influence on oil behavior. Molecular docking indicated that inhibitors and ligands interacted beneficially, with α-pinene demonstrating superior inhibition and cellular permeability.
苯二氮䓬类药物是用于治疗焦虑症和癫痫症的药物。然而,由于存在不良反应,人们正在寻找新的更安全的药物。因此,本研究旨在评估 Eugeniopsoides 马利雷亚(Marlierea eugeniopsoides)精油及其主要成分α-蒎烯和β-蒎烯的化学成分、抗焦虑和抗惊厥作用。分析了其毒性,并通过明暗试验和旷场试验(每组6只动物)评估了用该精油处理的鱼类的抗焦虑行为。在评估样品抗惊厥作用的试验中,戊四氮(PTZ)通过浸泡诱导癫痫发作。随后,用γ-氨基丁酸(GABA)拮抗剂研究其作用机制,并进行分子对接和药物代谢动力学(ADMET)研究。研究表明,Eugeniopsoides 马利雷亚精油(春季和夏季)无毒,且在所有剂量下均影响斑马鱼的运动。春季精油在所有剂量下均具有抗焦虑作用,而夏季精油仅在最高剂量下才显示出这种作用。两种精油均影响GABA,春季精油具有抗惊厥特性,而夏季精油则不然,这表明季节对精油行为有影响。分子对接表明抑制剂和配体之间存在有益的相互作用,α-蒎烯表现出更强的抑制作用和细胞通透性。