Ya'u J, Yaro A H, Malami S, Musa M A, Abubakar A, Yahaya S M, Chindo B A, Anuka J A, Hussaini I M
Department of Pharmacology and Therapeutics, Ahmadu Bello University , Zaria , Nigeria .
Pharm Biol. 2015;53(9):1329-38. doi: 10.3109/13880209.2014.981280. Epub 2015 Apr 9.
Carissa edulis Vahl (Apocynaceae) is used in Nigerian folk medicine to manage a plethora of diseases including epilepsy, cancer, and inflammation; its efficacy is widely acclaimed among communities of northern Nigeria.
This study establishes anticonvulsant activities of aqueous fraction of ethanol root bark extract of Carissa edulis (RAF) and sub-fractions (S1 and S2) in animal models.
We evaluated the acute toxicity of the RAF, S1 and S2, and the anticonvulsant activity using pentylenetetrazole (PTZ), picrotoxin, strychnine, N-methyl-d-aspartate (NMDA), isoniazid (INH), and aminophylline-induced seizures in mice. Their effects on maximal electroshock (MES) and kindling-induced seizures were studied in chicks and in rats, respectively, and in the electrophysiological study. The doses used for RAF were 150, 300, and 600 mg/kg while S1 and S2 were 250, 500, and 1000 mg/kg. Both RAF and sub-fractions were administered once during the experiment.
The intraperitoneal LD50 of the RAF was estimated to be 2222.61 mg/kg and that of the S1 and S2 were above 5000 mg/kg. RAF protected the mice by 50% while sub-fractions by 16.67% against PTZ-induced seizures. RAF offered 33.33 and 16.67% protection against strychnine and NMDA models, respectively. However, RAF offered 66.67-33.33% protections against aminophylline-induced seizures at doses of 150 and 600 mg/kg, but RAF, S1, and S2 had no effect on MES-induced seizures.
Our results validate the use of the plant traditionally in the management of epilepsy, thus supporting the appraisal of biologically active components of this plant as antiepileptic agents.
假虎刺(夹竹桃科)在尼日利亚民间医学中用于治疗多种疾病,包括癫痫、癌症和炎症;其疗效在尼日利亚北部社区广受赞誉。
本研究在动物模型中确定假虎刺乙醇根皮提取物的水相部分(RAF)及其亚组分(S1和S2)的抗惊厥活性。
我们评估了RAF、S1和S2的急性毒性,并使用戊四氮(PTZ)、印防己毒素、士的宁、N-甲基-D-天冬氨酸(NMDA)、异烟肼(INH)和氨茶碱诱导小鼠癫痫发作来评估其抗惊厥活性。分别在雏鸡和大鼠中研究了它们对最大电休克(MES)和点燃诱导癫痫发作的影响,并进行了电生理研究。RAF的使用剂量为150、300和600mg/kg,而S1和S2为250、500和1000mg/kg。在实验过程中,RAF和亚组分均给药一次。
RAF的腹腔注射半数致死量估计为2222.61mg/kg,S1和S2的腹腔注射半数致死量高于5000mg/kg。RAF使小鼠对PTZ诱导的癫痫发作的保护率为50%,而亚组分的保护率为16.67%。RAF分别对士的宁和NMDA模型提供33.33%和16.67%的保护。然而,在150和600mg/kg剂量下,RAF对氨茶碱诱导的癫痫发作提供66.67%-33.33%的保护,但RAF、S1和S2对MES诱导的癫痫发作没有影响。
我们的结果证实了该植物在传统上用于治疗癫痫的用途,从而支持将该植物的生物活性成分评估为抗癫痫药物。