Muto Nilton Akio, Hamoy Moisés, da Silva Ferreira Chryslen Brenda, Hamoy Akira Otake, Lucas David Cristian Rodrigues, de Mello Vanessa Jóia, Rogez Hervé
Centre for Valorization of Amazonian Bioactive Compounds (CVACBA), Federal University of Pará (UFPA), Belém, Brazil.
Laboratory of Pharmacology and Toxicology of Natural Products, Institute of Biological Sciences of Federal University of Pará (ICB-UFPA), Belém, Brazil.
Front Cell Neurosci. 2022 May 11;16:872743. doi: 10.3389/fncel.2022.872743. eCollection 2022.
Epilepsy is one of the most common neurological diseases globally, resulting from a disorder in brain activity. This condition can be triggered by birth trauma, traumatic brain injury (TBI), infections of the brain and stroke. More than 70 million people suffer seizures caused by neurological abnormalities. Approximately 80% of all epileptic patients reside in low-income conditions or in developing countries, and over 75% of patients do not receive proper treatment. Our previous study found an anticonvulsant property of an extract of stone (EEOS) that caused myorelaxation, sedation, and cardiac and respiratory depression after intraperitoneal administration. The present study investigated through electroencephalographic (EEG) profiling the anticonvulsant protective properties of EEOS in induced convulsing rats. Male Wistar rats were treated with EEOS (300 mg/kg), diazepam (DZP) (5 mg/kg), pentylenetetrazol (PTZ) (60 mg/kg) and flumazenil (FMZ) (0.1 mg/kg) by intraperitoneal (i.p.). Electrodes implanted on the dura mater provided EEG data in which EEOS suppressed seizure deflagration caused by PTZ. In addition, EEOS presented no significant difference in comparison to DZP, which has the same mechanism of action. After FMZ injection, a GABAA receptor antagonist blocked the anticonvulsive effect in both the DZP and EEOS groups, suggesting that EEOS exerts it action on the GABAA receptor at the benzodiazepine (BDZ) subunit.
癫痫是全球最常见的神经系统疾病之一，由大脑活动紊乱引起。这种病症可由出生创伤、创伤性脑损伤（TBI）、脑部感染和中风引发。超过7000万人患有由神经异常引起的癫痫发作。所有癫痫患者中约80%生活在低收入环境或发展中国家，超过75%的患者未得到适当治疗。我们之前的研究发现，一种石提取物（EEOS）具有抗惊厥特性，腹腔注射后会引起肌肉松弛、镇静以及心脏和呼吸抑制。本研究通过脑电图（EEG）分析，研究了EEOS对诱导惊厥大鼠的抗惊厥保护特性。雄性Wistar大鼠通过腹腔注射（i.p.）接受EEOS（300mg/kg）、地西泮（DZP）（5mg/kg）、戊四氮（PTZ）（60mg/kg）和氟马西尼（FMZ）（0.1mg/kg）治疗。植入硬脑膜的电极提供了EEG数据，其中EEOS抑制了PTZ引起的癫痫发作爆燃。此外，与具有相同作用机制的DZP相比，EEOS没有显著差异。注射FMZ后，一种GABAA受体拮抗剂阻断了DZP组和EEOS组的抗惊厥作用，表明EEOS在苯二氮䓬（BDZ）亚基上对GABAA受体发挥作用。
