(1S)-(-)-马鞭草烯酮的抗惊厥作用涉及 BDNF、COX-2 和 c-fos 的 RNA 表达。
Anticonvulsive activity of (1S)-(-)-verbenone involving RNA expression of BDNF, COX-2, and c-fos.
机构信息
Institute of Research in Drugs and Medicines, Federal University of Paraíba, CP 5009, João Pessoa, PB, 58051-900, Brazil.
Department of Cell and Molecular Biology, Federal University of Paraíba, CP 5009, João Pessoa, PB, 58051-900, Brazil.
出版信息
Naunyn Schmiedebergs Arch Pharmacol. 2017 Sep;390(9):863-869. doi: 10.1007/s00210-017-1388-x. Epub 2017 Jun 2.
(1S)-(-)-verbenone (VRB) is a monoterpene present in the essential oils of many plants which has shown therapeutic effect; however, its anticonvulsant activity has not yet been evaluated. The present work sought to investigate the anticonvulsant activity of VRB using pilocarpine and pentylenetetrazole-induced seizure testing; seeking also probable mechanisms of action. VRB caused no significant changes in motor coordination. Also, no significant data was observed in the pilocarpine-induced seizure tests. In the PTZ-induced seizures test, VRB showed anticonvulsant activity at doses of 200 mg/kg i.p. (733 ± 109.4 s) and 250 mg/kg i.p. (648.8 ± 124.5 s) significantly increasing the latency to onset of first seizure as compared with the vehicle group (51.8 ± 2.84 s). Pretreatment with flumazenil (FLU) did not reverse the anticonvulsive effect of VRB; however, it was able to upregulate BDNF and COX-2 genes and downregulate c-fos. The findings suggest that the anticonvulsant effects of VRB may be related to RNA expression modulations of COX-2, BDNF, and c-fos.
(1S)-(-)-马鞭草烯酮（VRB）是许多植物精油中的一种单萜烯，具有治疗作用；然而，其抗惊厥活性尚未得到评估。本工作旨在使用匹罗卡品和戊四氮诱导的癫痫发作试验来研究 VRB 的抗惊厥活性；并寻找可能的作用机制。VRB 对运动协调没有明显的影响。在匹罗卡品诱导的癫痫发作试验中，也没有观察到显著的数据。在 PTZ 诱导的癫痫发作试验中，VRB 在 200mg/kg ip 剂量（733±109.4s）和 250mg/kg ip 剂量（648.8±124.5s）下表现出抗惊厥活性，与载体组相比，首次发作的潜伏期明显延长（51.8±2.84s）。氟马西尼（FLU）预处理不能逆转 VRB 的抗惊厥作用；然而，它能够上调 BDNF 和 COX-2 基因，并下调 c-fos。这些发现表明，VRB 的抗惊厥作用可能与 COX-2、BDNF 和 c-fos 的 RNA 表达调控有关。
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