Chindo Ben A, Schröder Helmut, Becker Axel
Department of Pharmacology and Toxicology, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna, Nigeria; Institute of Pharmacology and Toxicology, Faculty of Medicine, Otto-von-Guericke University, Leipziger Str. 44, 39120 Magdeburg, Germany; Department of Pharmacology and Toxicology, National Institute for Pharmaceutical Research and Development, P. M. B. 21, Abuja, Nigeria.
Institute of Pharmacology and Toxicology, Faculty of Medicine, Otto-von-Guericke University, Leipziger Str. 44, 39120 Magdeburg, Germany.
Phytomedicine. 2015 Jan 15;22(1):86-93. doi: 10.1016/j.phymed.2014.10.005. Epub 2014 Oct 25.
Decoctions of Ficus plathyphylla are used in Nigeria's folk medicine to manage epilepsy for many years and their efficacies are widely acclaimed among the rural communities of Northern Nigeria. In this study, we examined the ameliorative effects of the standardized methanol extract of Ficus platyphylla (FP) stem bark on seizure severity, cognitive deficit and neuronal cell loss in pentylenetetrazole-kindled mice. The (35)S-GTPγS, glutamate and γ-aminobutyric acid receptors binding properties of the extract were also evaluated. Male CD-1 mice were kindled with an initial subeffective dose of pentylenetetrazole (PTZ, 37.5mg/kg, i.p.) for a total of 13 convulsant injections and the treatment groups concurrently received FP (100 and 200mg/kg). Control animals received the same number of saline injections. Twenty-four h after kindling completion the animals' learning performance was tested in a two-way shuttle-box. The animals were challenged with another subeffective dose of PTZ (32.5mg/kg, i.p.) on day 7 after kindling completion. Animals were sacrificed a day after the challenged experiment and the brains were processed for histological investigation. FP ameliorates seizure severity, cognitive deficits and neuronal cell loss in PTZ kindled mice. Components of the extract showed affinity for GABAergic and glutamatergic receptors. Glutamate release was diminished and the (35)S-GTPγS binding assay revealed no intrinsic activity at glutamatergic receptors. Our results revealed that FP contains psychoactive secondary metabolites with anticonvulsant properties, thus supporting the isolation and development of the biologically active components of this medicinal plant as antiepileptic agents.
多年来,在尼日利亚民间医学中,阔叶榕煎剂一直被用于治疗癫痫,其疗效在尼日利亚北部农村社区广受赞誉。在本研究中,我们研究了阔叶榕(FP)茎皮的标准化甲醇提取物对戊四氮点燃小鼠癫痫严重程度、认知缺陷和神经元细胞损失的改善作用。还评估了该提取物的(35)S-GTPγS、谷氨酸和γ-氨基丁酸受体结合特性。雄性CD-1小鼠先用亚有效剂量的戊四氮(PTZ,37.5mg/kg,腹腔注射)点燃,共进行13次惊厥注射,治疗组同时接受FP(100和200mg/kg)。对照动物接受相同次数的生理盐水注射。点燃完成后24小时,在双向穿梭箱中测试动物的学习性能。在点燃完成后第7天,用另一个亚有效剂量的PTZ(32.5mg/kg,腹腔注射)对动物进行激发。激发实验后一天处死动物,对大脑进行组织学研究。FP可改善PTZ点燃小鼠的癫痫严重程度、认知缺陷和神经元细胞损失。提取物的成分对GABA能和谷氨酸能受体显示出亲和力。谷氨酸释放减少,(35)S-GTPγS结合试验显示在谷氨酸能受体上无内在活性。我们的结果表明,FP含有具有抗惊厥特性的精神活性次生代谢物,从而支持将这种药用植物的生物活性成分分离和开发为抗癫痫药物。