Sadeghnia Hamid R, Cortez Miguel A, Liu Dick, Hosseinzadeh Hossein, Snead O Carter
Department of Pharmacology, Mashhad University of Medical Sciences, Mashhad, Iran.
J Pharm Pharm Sci. 2008;11(3):1-14. doi: 10.18433/j38g6j.
We examined the effect of safranal, a constituent of Crocus sativus, in acute experimental animal models of generalized absence seizures.
the effect of acute systemic administration of safranal on latency to seizure onset as well as spike and wave discharches (SWD) duration following pharmacologically-induced absence seizures was investigated in wildtype mice. We further characterized its effects on the GABAergic system through the regional modification of [3H] flunitrazepam, a benzodiazepine agonist binding site and [3H] CGP54626A, a GABAB receptor antagonist binding site in mouse brain.
The systemic administration of safranal resulted in a significant and dose-dependent attenuation in experimental absence seizures elicited by either gamma-butyrolactone (GBL), baclofen (BAC) or low doses of GABAA receptor antagonists; pentylenetetrazole (PTZ), picrotoxin (PTX) and bicuculline (BMC). After a single intraperitoneal administration of safranal (291 mg/kg), no changes in baseline electrocorticographic (ECoG) recording were observed, however, a significant decrease in [3H] flunitrazepam binding was seen in the cortex (33.16%, p<0.001), hippocampus (27.36%, p<0.01) and thalamus (29.91%, p<0.01) of mouse brain, while the [3H] CGP54626A binding did not show any modification in the same brain regions.
These data indicate that there is an antiabsence seizure property in safranal and its effect may be due to modifications on the benzodiazepine binding sites of the GABAA receptor complex.
我们研究了藏红花的成分藏红花醛在全身性失神发作急性实验动物模型中的作用。
在野生型小鼠中，研究了藏红花醛急性全身给药对药理学诱导的失神发作后癫痫发作起始潜伏期以及棘波和慢波放电（SWD）持续时间的影响。我们通过对[3H]氟硝西泮（一种苯二氮䓬激动剂结合位点）和[3H] CGP54626A（一种GABAB受体拮抗剂结合位点）在小鼠脑中的区域修饰，进一步表征了其对GABA能系统的影响。
藏红花醛的全身给药导致由γ-丁内酯（GBL）、巴氯芬（BAC）或低剂量GABAA受体拮抗剂；戊四氮（PTZ）、印防己毒素（PTX）和荷包牡丹碱（BMC）诱发的实验性失神发作显著且剂量依赖性地减轻。单次腹腔注射藏红花醛（291 mg/kg）后，未观察到基线脑电图（ECoG）记录有变化，然而，在小鼠脑的皮质（33.16%，p<0.001）、海马体（27.36%，p<0.01）和丘脑（29.91%，p<0.01）中，[3H]氟硝西泮结合显著降低，而在相同脑区中[3H] CGP54626A结合未显示任何改变。
这些数据表明藏红花醛具有抗失神发作特性，其作用可能归因于对GABAA受体复合物苯二氮䓬结合位点的修饰。
