3,4,5-Trimethoxycinnamic acid, one of the constituents of Polygalae Radix exerts anti-seizure effects by modulating GABAAergic systems in mice
3,4,5-Trimethoxycinnamic acid, one of the constituents of Polygalae Radix exerts anti-seizure effects by modulating GABAAergic systems in mice
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DOI：
10.1016/j.jphs.2015.07.021
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发表时间：
2016-05-01
影响因子：
3.5
通讯作者：
Chen, Chang-Rui
中科院分区：
文献类型：
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作者：
Chen, Chang-Yuan;Wei, Xu-Dong;Chen, Chang-Rui
远志是一种重要的药用植物，广泛应用于非洲大部分地区。3，4，5-三甲氧基肉桂酸（TMCA）是远志属植物远志的有效成分之一。TMCA的抗癫痫作用机制目前尚不清楚。我们研究了TMCA的抗癫痫作用。以5、10和20 mg/kg剂量给予TMCA，并通过小鼠最大电休克（MES）和戊四氮（PTZ）模型评价抗癫痫发作作用。以10和20 mg/kg剂量给予TMCA显著降低了MES诱导的强直性后肢伸展（THE）的发生率。在PTZ癫痫发作模型中，与溶剂处理的动物相比，TMCA显著延迟肌阵挛性抽搐（MJ）的发作，并降低癫痫发作的严重程度和死亡率。TMCA 10和20 mg/kg给药组也未检测到全身阵挛性癫痫发作（GCS）。预先给予GABAA/苯二氮卓类（BZ）受体拮抗剂氟马西尼可阻断TMCA的抗癫痫发作作用。这些数据支持TMCA作为GABAA/BZ受体激动剂用于抗癫痫治疗的进一步研究。(C)2015作者制作和主办由爱思唯尔B。V.代表日本药理学会。这是一个在CC BY-NC-ND许可证下的开放获取文章（http：//creativecommons.org/licenses/by-nc-nd/4.0/）。
Polygalae Radix is an important medicinal plant that is widely used in most of Africa. 3,4,5-Trimethoxycinnamic acid (TMCA) is one of the constituents of Polygalae Radix. Until now, the mechanisms involved in the anti-seizure property of TMCA are still unclear. We examined the anti-seizure effect of TMCA. TMCA administered at doses of 5, 10 and 20 mg/kg and evaluated anti-seizure effects by maximal electroshock (MES) and pentylenetetrazol (PTZ) models in mice. TMCA administered at doses of 10 and 20 mg/kg significantly reduced the incidence of MES-induced tonic hindlimb extension (THE). TMCA significantly delayed the onset of myoclonic jerks (MJ), and decreased the seizure severity and mortality compared with the vehicle-treated animals in PTZ seizure model. TMCA 10 and 20 mg/kg treated groups also did not determined generalized clonic seizures (GCS).Pretreatment with a GABAA/benzodiazepine (BZ) receptor antagonist flumazenil blocked the antiseizure effects of TMCA. These data support the further investigation of TMCA as a GABAA/BZ receptor agonist for anti-seizure therapy. (C) 2015 The Authors. Production and hosting by Elsevier B. V. on behalf of Japanese Pharmacological Society. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).