Department of Natural Products Chemistry, Medical University of Lublin, 20-093 Lublin, Poland.
Biothermodynamics, TUM School of Life Sciences, Technical University of Munich, 85354 Freising, Germany.
Int J Mol Sci. 2023 Jan 30;24(3):2598. doi: 10.3390/ijms24032598.
Epilepsy is a neurological disease that burdens over 50 million people worldwide. Despite the considerable number of available antiseizure medications, it is estimated that around 30% of patients still do not respond to available treatment. Herbal medicines represent a promising source of new antiseizure drugs. This study aimed to identify new drug lead candidates with antiseizure activity from endemic plants of New Caledonia. The crude methanolic leaf extract of Guillaumin (Rutaceae) significantly decreased (75 μg/mL and 100 μg/mL) seizure-like behaviour compared to sodium valproate in a zebrafish pentylenetetrazole (PTZ)-induced acute seizure model. The main coumarin compound, halfordin, was subsequently isolated by liquid-liquid chromatography and subjected to locomotor, local field potential (LFP), and gene expression assays. Halfordin (20 μM) significantly decreased convulsive-like behaviour in the locomotor and LFP analysis (by 41.4% and 60%, respectively) and significantly modulated , and gene expression.
癫痫是一种神经系统疾病，全球有超过 5000 万人受到其困扰。尽管有相当数量的抗癫痫药物可供使用，但据估计，仍有约 30%的患者对现有治疗方法没有反应。草药代表了一种有前途的新型抗癫痫药物来源。本研究旨在从新喀里多尼亚的特有植物中鉴定具有抗癫痫活性的新药先导候选物。与丙戊酸钠相比，Guillaumin（芸香科）的粗甲醇叶提取物在斑马鱼戊四氮（PTZ）诱导的急性惊厥模型中显著降低（75μg/mL 和 100μg/mL）惊厥样行为。随后通过液-液色谱法分离出主要香豆素化合物半蒽，并进行了运动、局部场电位（LFP）和基因表达分析。哈尔福德（20μM）在运动和 LFP 分析中显著降低了惊厥样行为（分别降低 41.4%和 60%），并显著调节 基因表达。
