Department of Neuroscience and Rehabilitation, University of Ferrara, via Fossato di Mortara 70, 44121, Ferrara, Italy.
University Vita-Salute San Raffaele, via Olgettina 58, 20132, Milan, Italy.
Neurotherapeutics. 2022 Oct;19(6):1951-1965. doi: 10.1007/s13311-022-01299-4. Epub 2022 Sep 30.
Temporal lobe epilepsy often manifests months or even years after an initial epileptogenic insult (e.g., stroke, trauma, status epilepticus) and, therefore, may be preventable. However, no such preventive treatment is currently available. Aim of this study was to test an antioxidant agent, 7,8-dihydroxyflavone (7,8-DHF), that is well tolerated and effective in preclinical models of many neurological disorders, as an anti-epileptogenic drug. However, 7,8-DHF also acts as a TrkB receptor agonist and, based on the literature, this effect may imply an anti- or a pro-epileptogenic effect. We found that low- (5 mg/kg), but not high-dose 7,8-DHF (10 mg/kg) can exert strong anti-epileptogenic effects in the lithium-pilocarpine model (i.e., highly significant reduction in the frequency of spontaneous seizures and in the time to first seizure after status epilepticus). The mechanism of these different dose-related effects remains to be elucidated. Nonetheless, considering its excellent safety profile and antioxidant properties, as well as its putative effects on TrkB receptors, 7,8-DHF represents an interesting template for the development of effective and well-tolerated anti-epileptogenic drugs.
颞叶癫痫常发生在初始致痫性损伤(如中风、创伤、癫痫持续状态)后数月甚至数年,因此可能是可预防的。然而,目前尚无此类预防治疗方法。本研究旨在测试一种抗氧化剂 7,8-二羟基黄酮(7,8-DHF),该药物在多种神经疾病的临床前模型中具有良好的耐受性和疗效,可作为一种抗癫痫发生药物。然而,7,8-DHF 也作为 TrkB 受体激动剂发挥作用,根据文献,这种作用可能意味着抗癫痫发生或促癫痫发生的作用。我们发现,低剂量(5mg/kg)而非高剂量 7,8-DHF(10mg/kg)可在锂-匹罗卡品模型中发挥强烈的抗癫痫发生作用(即自发性癫痫发作频率显著降低,癫痫持续状态后首次癫痫发作时间显著延长)。这些不同剂量相关作用的机制仍有待阐明。尽管如此,考虑到其出色的安全性和抗氧化特性,以及其对 TrkB 受体的潜在作用,7,8-DHF 为开发有效且耐受性良好的抗癫痫发生药物提供了一个有趣的模板。