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姜黄倍半萜烯类化合物毕枯醇在斑马鱼和小鼠癫痫模型中的抗惊厥活性。

Anticonvulsant activity of bisabolene sesquiterpenoids of Curcuma longa in zebrafish and mouse seizure models.

机构信息

Laboratory for Molecular Biodiscovery, Department of Pharmaceutical & Pharmacological Sciences, University of Leuven, Leuven, Belgium.

出版信息

Epilepsy Behav. 2012 May;24(1):14-22. doi: 10.1016/j.yebeh.2012.02.020. Epub 2012 Apr 5.

DOI:10.1016/j.yebeh.2012.02.020
PMID:22483646
Abstract

Turmeric, obtained from the rhizomes of Curcuma longa, is used in South Asia as a traditional medicine for the treatment of epilepsy. To date, in vivo studies on the anticonvulsant activity of turmeric have focused on its principal curcuminoid, curcumin. However, poor absorption and rapid metabolism have limited the therapeutic application of curcumin in humans. To explore the therapeutic potential of turmeric for epilepsy further, we analyzed its anticonvulsant activity in a larval zebrafish seizure assay. Initial experiments revealed that the anticonvulsant activity of turmeric in zebrafish larvae cannot be explained solely by the effects of curcumin. Zebrafish bioassay-guided fractionation of turmeric identified bisabolene sesquiterpenoids as additional anticonvulsants that inhibit PTZ-induced seizures in both zebrafish and mice. Here, we present the first report of the anticonvulsant properties of bisabolene sesquiterpenoids and provide evidence which warrants further investigation toward the mechanistic understanding of their neuromodulatory activity.

摘要

姜黄,从姜黄的根茎中提取,在南亚被用作治疗癫痫的传统药物。迄今为止,姜黄抗惊厥活性的体内研究主要集中在其主要的姜黄素上。然而,吸收不良和快速代谢限制了姜黄素在人类中的治疗应用。为了进一步探索姜黄治疗癫痫的潜力,我们在幼虫斑马鱼惊厥试验中分析了姜黄的抗惊厥活性。初步实验表明,姜黄在斑马鱼幼虫中的抗惊厥活性不能仅用姜黄素的作用来解释。基于斑马鱼生物测定的姜黄分段分离,鉴定出倍半萜类化合物作为另外的抗惊厥剂,可抑制 PTZ 诱导的斑马鱼和小鼠惊厥。在这里,我们首次报道了倍半萜类化合物的抗惊厥特性,并提供了证据,证明有必要进一步研究它们的神经调节活性的机制。

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