D'Hooge R, Pei Y Q, Raes A, Lebrun P, van Bogaert P P, de Deyn P P
Laboratory of Neurochemistry and Behaviour, Born-Bunge Foundation, University of Antwerp, Belgium.
Arzneimittelforschung. 1996 Jun;46(6):557-60.
In traditional Chinese medicine, a mixture of radish and pepper is used to treat epilepsy. The presumptive effectiveness of this prescription might be due to the anticonvulsant actions of the principal component of pepper, the alkaloid piperine (CAS 94-62-2). The effects of piperine on convulsions induced in mice by agonists at different excitatory amino acid receptor subtypes were studied. Piperine was shown to significantly block convulsions induced by intracerebroventricular injection of threshold doses of kainate, but to have no or only slight effects on convulsions induced by L-glutamate, N-methyl-D-aspartate or guanidinosuccinate. Piperine suspensions, injected intraperitoneally, 1 h before injection of the threshold intracerebroventricular dose of kainate for the induction of clonic convulsions (1 nmol), blocked these convulsions with an ED50 (and 95% confidence interval) of 46 (25-86) mg/kg. Although piperine did block convulsions, induced by kainate, the compound does not appear to act as a kainate receptor antagonist. Whole-cell currents induced by the application of kainate to spinal cord cells in primary dissociated cultures were not affected by co-application of piperine.
在传统中医中，萝卜和胡椒的混合物被用于治疗癫痫。该方剂的假定疗效可能归因于胡椒的主要成分——生物碱胡椒碱（化学物质登记号94-62-2）的抗惊厥作用。研究了胡椒碱对不同兴奋性氨基酸受体亚型激动剂诱导的小鼠惊厥的影响。结果表明，胡椒碱能显著阻断脑室内注射阈剂量的海藻酸所诱导的惊厥，但对L-谷氨酸、N-甲基-D-天冬氨酸或胍基琥珀酸诱导的惊厥无作用或仅有轻微作用。在脑室内注射阈剂量的海藻酸（1 nmol）诱导阵挛性惊厥前1小时，腹腔注射胡椒碱悬浮液，可阻断这些惊厥，其半数有效剂量（ED50）（及95%置信区间）为46（25 - 86）mg/kg。尽管胡椒碱确实能阻断海藻酸诱导的惊厥，但该化合物似乎并非作为海藻酸受体拮抗剂起作用。在原代解离培养的脊髓细胞中，应用胡椒碱与海藻酸共同作用时，海藻酸诱导的全细胞电流不受影响。
