The crude drug, Chotoko (Uncariae Uncis cam Ramlus), the hooks of Uncaria spp. (Rubiaceae), has been claimed to possess sedative and anti-spasmodic actions, and is contained in a Chinese traditional preparation, Choto-san, as a main crude drug. Examinations were made on the anti-convulsion effects of Choto-san and Chotoko against some animal models of epilepsy conducted by the stimulation of drugs or electricity. Oral administration of the Choto-san extract to mice at the doses of 1.0 g/kg and 3.0 g/kg tended to inhibit the glutamate-induced convulsion in a dose-dependent manner, and the effect of the Chotoko extract at a 3.0 g/kg dose was significant, while both the extracts showed no activity against the picrotoxine-induced, strychinine-induced, and electroshock convulsions. The Choto-san preparation without Chotoko was inactive, and the activity of the Chotoko extract was more potent than that of the every crude drug comprising Choto-san, suggesting that Chotoko plays the most important role in the Choto-san prescription and contains some active compounds. Bioassay-guided fractionation of the Chotoko extract led to the location of the active components in the less polar alkaloids-containing fraction, from which three indole alkaloids, geissoschizine methylether (1), hirsuteine (2) and hirsutine (3), and an oxyindole alkaloid, isocorynoxeine (4) were isolated and identified. Oral administration of 1 and 2 to mice at the doses of 50, 100, and 200 mg/kg inhibited the glutamate-induced convulsion in a dose-dependent manner. The effect of 3, the dihydro derivative of 2, was less potent than those of 1 and 2. Compound 4 showed no activity at a 100 mg/kg dose compared with control. The above results support the Chinese herbal description of the anti-spasmodic action of Chotoko, and show that 1 and 2 contained in Chotoko must be mainly contributed to the activity. It is also suggested that Choto-san may be clinically available for treatment of epilepsy.

译文

粗药,chootoko (Uncariae Uncis cam Ramlus),钩藤属的钩。(茜草科),据称具有镇静和抗痉挛作用,并作为主要生药包含在中国传统制剂Choto-san中。检查了Choto-san和Chotoko对通过药物或电刺激进行的某些癫痫动物模型的抗惊厥作用。以1.0g/kg和3.0g/kg的剂量对小鼠口服Choto-san提取物倾向于以剂量依赖性方式抑制谷氨酸引起的惊厥,并且以3.0g/kg的剂量对Chotoko提取物的作用是显着的,尽管两种提取物均对苦豆碱诱导的,马冬氨酸诱导的和电击惊厥均无活性。不含Chotoko的Choto-san制剂无活性,并且Chotoko提取物的活性比包含Choto-san的每种粗制药物的活性更有效,这表明Chotoko在Choto-san处方中起着最重要的作用,并且包含一些活性化合物。生物测定指导的Chotoko提取物的分馏导致活性成分在极性较小的含生物碱部分中的位置,其中三种吲哚生物碱,geissoschizine methylether (1),hirsuteine (2) 和hirsutine (3),以及一种氧吲哚生物碱,分离并鉴定了异糖苷 (4)。以50、100和200 mg/kg的剂量对小鼠口服1和2以剂量依赖性方式抑制谷氨酸诱导的惊厥。2的二氢衍生物3的作用不如1和2的作用。与对照相比,化合物4在100 mg/kg剂量下无活性。以上结果支持了中草药对Chotoko的抗痉挛作用的描述,并表明Chotoko中所含的1和2必须主要有助于该活性。还建议Choto-san在临床上可用于治疗癫痫。

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