Suciu Felicia, Mihai Dragos Paul, Ungurianu Anca, Andrei Corina, Pușcașu Ciprian, Chițescu Carmen Lidia, Ancuceanu Robert Viorel, Gird Cerasela Elena, Stefanescu Emil, Blebea Nicoleta Mirela, Popovici Violeta, Rosca Adrian Cosmin, Ghiță Cristina Isabel Viorica, Negres Simona
Faculty of Pharmacy, "Ovidius" University of Constanta, 900470 Constanta, Romania.
Faculty of Pharmacy, "Carol Davila" University of Medicine and Pharmacy, 020956 Bucharest, Romania.
Int J Mol Sci. 2025 Jul 3;26(13):6426. doi: 10.3390/ijms26136426.
The current study evaluated the anticonvulsant properties of ethanolic extracts from , , and using integrated phytochemical, in vivo, biochemical, and computational approaches. Phytochemical analysis by UHPLC-HRMS/MS revealed the presence of various bioactive compounds, notably flavonoids such as isorhamnetin, quercetin, and kaempferol. In an electroshock-induced seizure model, extract (MAE, 100 mg/kg) demonstrated significant anticonvulsant effects, reducing both seizure duration and incidence, likely mediated by flavonoid interactions with GABA-A and 5-HT3A receptors, as suggested by target prediction and molecular docking analyses. The extracts of (AAE, 100 mg/kg) and (PIE, 50 mg/kg) exhibited moderate, non-significant anticonvulsant activities. At the same time, (VOE, 50 mg/kg) displayed considerable antioxidant and anti-inflammatory properties but limited seizure protection. All extracts significantly reduced brain inflammation markers (TNF-α) and enhanced antioxidant defenses, as indicated by total thiols. Molecular docking further supported the interaction of key phytochemicals, including naringenin and chlorogenic acid, with human and mouse 5-HT3A receptors. Overall, extract exhibited promising therapeutic potential for epilepsy management, warranting further investigation into chronic seizure models and optimized dosing strategies.
本研究采用综合植物化学、体内、生化和计算方法,评估了[植物名称1]、[植物名称2]和[植物名称3]乙醇提取物的抗惊厥特性。通过超高效液相色谱-高分辨质谱/质谱进行的植物化学分析表明,存在多种生物活性化合物,特别是黄酮类化合物,如异鼠李素、槲皮素和山奈酚。在电休克诱导的癫痫模型中,[植物名称1]提取物(MAE,100毫克/千克)表现出显著的抗惊厥作用,缩短了癫痫发作持续时间并降低了发作发生率,靶点预测和分子对接分析表明,这可能是黄酮类化合物与GABA-A和5-HT3A受体相互作用介导的。[植物名称2]提取物(AAE,100毫克/千克)和[植物名称3]提取物(PIE,50毫克/千克)表现出中等程度的、不显著的抗惊厥活性。同时,[植物名称4]提取物(VOE,50毫克/千克)表现出相当的抗氧化和抗炎特性,但癫痫保护作用有限。所有提取物均显著降低了脑炎症标志物(TNF-α),并增强了抗氧化防御能力,总硫醇含量表明了这一点。分子对接进一步支持了关键植物化学物质,包括柚皮苷和绿原酸,与人及小鼠5-HT3A受体的相互作用。总体而言,[植物名称1]提取物在癫痫治疗方面显示出有前景的治疗潜力,值得对慢性癫痫模型和优化给药策略进行进一步研究。