Laboratorio de Neurofarmacología de Productos Naturales, Dirección de Investigaciones en Neurociencias, Instituto Nacional de Psiquiatría "Ramón de La Fuente Muñiz", Calz. México-Xochimilco 101, Col. San Lorenzo Huipulco, 14370, Ciudad de México, Mexico.
Laboratorio de Neurofisiología Del Control y La Regulación, Dirección de Investigaciones en Neurociencias, Instituto Nacional de Psiquiatría "Ramón de La Fuente Muñiz", Calz. México-Xochimilco 101, Col. San Lorenzo Huipulco, 14370, Ciudad de México, Mexico.
J Ethnopharmacol. 2021 May 10;271:113866. doi: 10.1016/j.jep.2021.113866. Epub 2021 Jan 21.
Ruta chalepensis L. (Rutaceae) is used in traditional medicine to treat a wide variety of disorders such as rheumatism, fever, mental disorders, dropsy, neuralgia, menstrual problems, anxiety, and epilepsy.
To evaluate and compare the anticonvulsant properties of an aqueous extract and ethyl acetate (AcOEt) fraction of R. chalepensis on pentylenetetrazole (PTZ)-induced seizures and maximal electroshock (MES) test in mice, by analyzing behavior and electroencephalogram (EEG), as well as GABA receptors involvement.
The effect of an acute administration of different dosage of the aqueous extract (300 or 500 mg/kg) or AcOEt fraction (100, 300, 500 or 1000 mg/kg) of R. chalepensis was explored on two different models of acute seizure induction in mice, the PTZ and maximal electroshock (MES) tests. Behavioral and electrographic effects were quantified. Additionally, the possible involvement of the GABA receptors was explored in the presence of picrotoxin (a non-competitive antagonist of the GABA receptor).
AcOEt fraction of R. chalepensis was more efficient than aqueous extract to reduce the incidence of tonic-clonic seizures and mortality in a significant and dose-dependent manner in both the PTZ and MES tests. This anticonvulsant effect was not abolished in the presence of picrotoxin. The EEG spectral power analysis revealed that aqueous extract decreased alpha and beta power, while AcOEt fraction decreased alpha and gamma power confirming previous findings of its depressant effect in the central nervous system. It is important to mention that the highest dosage of the AcOEt (1000 mg/kg) produced a severe suppression or isoelectric EEG activity (EEG flattening), recognized as a comatose state, suggesting a neurotoxic effect at this dosage.
Our data reinforce that depressant and anticonvulsant effects of R. chalepensis depend in part on the presence of constituents from medium polarity. We also found that anticonvulsant effect is not mediated by GABA receptors. In addition, cautious is emphasized when high doses of this natural product are used in traditional medicine since it might produce neurotoxic effects.
山乌龟（卫矛科）在传统医学中被用于治疗多种疾病，如风湿、发热、精神障碍、水肿、神经痛、月经问题、焦虑和癫痫。
通过分析行为和脑电图（EEG）以及 GABA 受体参与情况，评估和比较山乌龟水提物和乙酸乙酯（AcOEt）部分对戊四氮（PTZ）诱导的癫痫发作和最大电休克（MES）试验的抗惊厥特性。
研究了山乌龟水提物（300 或 500mg/kg）或 AcOEt 部分（100、300、500 或 1000mg/kg）的急性给药对两种不同的急性惊厥诱导模型（PTZ 和 MES 试验）在小鼠中的作用。量化了行为和脑电图的影响。此外，在存在苦毒蕈碱（GABA 受体的非竞争性拮抗剂）的情况下，探讨了 GABA 受体的可能参与情况。
AcOEt 部分比水提物更有效地减少强直-阵挛性癫痫发作的发生率和死亡率，在 PTZ 和 MES 试验中均呈显著的剂量依赖性。在存在苦毒蕈碱的情况下，这种抗惊厥作用没有被消除。脑电图谱功率分析显示，水提物降低了α和β功率，而 AcOEt 部分降低了α和γ功率，证实了其对中枢神经系统的抑制作用。重要的是要提到，AcOEt 的最高剂量（1000mg/kg）产生了严重的抑制或等电脑电图活动（脑电图平坦化），被认为是昏迷状态，表明在此剂量下存在神经毒性作用。
我们的数据强化了山乌龟的抑制和抗惊厥作用部分取决于中极性成分的存在。我们还发现，抗惊厥作用不是由 GABA 受体介导的。此外，在传统医学中使用这种天然产物的高剂量时，应谨慎，因为它可能产生神经毒性作用。
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