4.7 Article

Screening of Monoamine Oxidase Inhibitors from Seeds of Nigella glandulifera Freyn et Sint. by Ligand Fishing and Their Neuroprotective Activity

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PLANTS-BASEL
卷 12, 期 4, 页码 -

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MDPI
DOI: 10.3390/plants12040882

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Nigella glandulifera; ligand fishing; neuroprotection; monoamine oxidase-B inhibitor; Parkinson's disease

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This study found that the seeds of Nigella glandulifera contain Tauroside E and thymoquinone, which can inhibit monoamine oxidase B (MAO-B) and have therapeutic effects on Parkinson's disease.
Nigella glandulifera 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 N. glandulifera seeds for rapid screening of MAO-B inhibitors coupled with HPLC-MS. Tauroside E and thymoquinone were found to inhibit the enzyme with IC50 values of 35.85 mu M and 25.54 mu M, 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.

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