Ayeni Emmanuel Ayodeji, Ma Chao, Hu Yikao, Bai Xiaolin, Zhang Yongmei, Liao Xun
Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, China.
University of Chinese Academy of Sciences, Beijing 100049, China.
Plants (Basel). 2023 Feb 15;12(4):882. doi: 10.3390/plants12040882.
is a traditional medicinal plant used to treat seizures, insomnia, and mental disorders among the Tibetan and Xinjiang people of China. Recent pharmacological research indicates that the seeds of this plant have a neuroprotective effect; however, the chemical components responsible for this effect are unknown. Monoamine oxidase B (MAO-B) has been recognized as a target for developing anti-Parkinson's disease drugs. In this work, MAO-B functionalized magnetic nanoparticles were used to enrich the enzyme's ligands in extracts of seeds for rapid screening of MAO-B inhibitors coupled with HPLC-MS. Tauroside E and thymoquinone were found to inhibit the enzyme with IC values of 35.85 μM and 25.54 μM, respectively. Both compounds exhibited neuroprotective effects on 6-OHDA-induced PC-12 cells by increasing the cell viability to 52% and 58%, respectively, compared to 50% of the injured cells. Finally, molecular docking indicated strong interactions of both inhibitors with the enzyme. This work shows that MAO-B functionalized magnetic nanoparticles are effective for rapid screening of anti-PD inhibitors from complex herbal mixtures and, at the same time, shows the promising potential of this plant's seeds in developing anti-PD drugs.
是一种传统药用植物，在中国藏族和新疆地区的人们中用于治疗癫痫、失眠和精神障碍。最近的药理学研究表明，这种植物的种子具有神经保护作用；然而，产生这种作用的化学成分尚不清楚。单胺氧化酶B（MAO-B）已被公认为开发抗帕金森病药物的靶点。在这项工作中，MAO-B功能化磁性纳米颗粒用于富集该植物种子提取物中的酶配体，以便与HPLC-MS联用快速筛选MAO-B抑制剂。发现牛磺胆酸E和百里醌对该酶具有抑制作用，IC值分别为35.85 μM和25.54 μM。与50%的受损细胞相比，这两种化合物对6-OHDA诱导的PC-12细胞均表现出神经保护作用，细胞活力分别提高到52%和58%。最后，分子对接表明这两种抑制剂与该酶都有强烈的相互作用。这项工作表明，MAO-B功能化磁性纳米颗粒可有效从复杂的草药混合物中快速筛选抗帕金森病抑制剂，同时也显示了这种植物种子在开发抗帕金森病药物方面的潜在前景。
