Tapinanthus globiferus is often referred to as an all-purpose herb for the treatment of stroke and epilepsy. The present study investigates the anticonvulsant effect of methanolic leaf extract, active fractions, and lupeol (isolate) of Tapinanthus globiferus in mice as well as the underlying mechanisms. Following phytochemical studies of T. globiferus, preliminary assays were performed to evaluate MLE-induced toxic effect and behavioral changes. The pentylenetetrazol (70 mg/kg, i. p.)-induced seizure was evaluated in mice that were pretreated orally with vehicle 10 mL/kg, MLE (4, 20, or 100 mg/kg), fractions (F1 to F6), lupeol 10 mg/kg or diazepam (3 mg/kg). Methanolic leaf extract preserved neuron viability as well as the relative organ weight, and hematological and biochemical parameters. The behavioral endpoints, neuromuscular coordination, and sensory response parameters revealed a dose-dependent effect of methanolic leaf extract. This extract, active fractions, lupeol, and diazepam potentiated the hypno-sedative effect of the barbiturate and attenuated PTZ-induced acute seizure. This antiseizure effect was completely reversed by flumazenil 2 mg/kg (benzodiazepine site antagonist). Altogether, the benzodiazepine site-mediated anticonvulsant effects of methanolic leaf extract, active fractions, and lupeol corroborate traditional application of T. globiferus against epilepsy.

中文翻译：

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苯二氮卓位点参与蒺藜抗戊四唑致小鼠癫痫发作的抗惊厥活性

Tapinanthus globiferus 通常被称为治疗中风和癫痫的通用草药。本研究调查了枞树的甲醇叶提取物、活性成分和羽扇豆醇（分离物）对小鼠的抗惊厥作用及其潜在机制。在对 T. globiferus 进行植物化学研究后，进行了初步分析以评估 MLE 诱导的毒性作用和行为变化。在用载体 10 mL/kg、MLE（4、20 或 100 mg/kg）、级分（F1 至 F6）、羽扇豆醇 10 口服预处理的小鼠中评估戊四唑（70 mg/kg，ip）诱导的癫痫发作mg/kg 或地西泮 (3 mg/kg)。甲醇叶提取物保留了神经元活力以及相对器官重量以及血液学和生化参数。行为终点、神经肌肉协调、和感官反应参数揭示了甲醇叶提取物的剂量依赖性作用。这种提取物、活性成分、羽扇豆醇和地西泮增强了巴比妥类药物的催眠镇静作用，并减轻了 PTZ 诱导的急性癫痫发作。这种抗癫痫作用被氟马西尼 2 mg/kg（苯二氮卓位点拮抗剂）完全逆转。总而言之，甲醇叶提取物、活性成分和羽扇豆醇的苯二氮卓部位介导的抗惊厥作用证实了 T. globiferus 抗癫痫的传统应用。这种抗癫痫作用被氟马西尼 2 mg/kg（苯二氮卓位点拮抗剂）完全逆转。总而言之，甲醇叶提取物、活性成分和羽扇豆醇的苯二氮卓位点介导的抗惊厥作用证实了 T. globiferus 抗癫痫的传统应用。这种抗癫痫作用被氟马西尼 2 mg/kg（苯二氮卓位点拮抗剂）完全逆转。总而言之，甲醇叶提取物、活性成分和羽扇豆醇的苯二氮卓位点介导的抗惊厥作用证实了 T. globiferus 抗癫痫的传统应用。