肉苁蓉总苷的神经保护作用评估及新型脑靶向天然 MAO-B 抑制剂的研究

IF 4.1 3区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
ACS Chemical Neuroscience Pub Date : 2024-12-18 Epub Date: 2024-11-23 DOI:10.1021/acschemneuro.4c00608
Xinyuan Zhai, Wenyu Xie, Muhammad Danish Yaqoob, Feng Zhao, Hong Zhe Zhu, Shang Shen Yang, Kai Wang, Xumei Wang, Hai Chao Wang, Xiaoming Wang
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引用次数: 0

摘要

在这项研究中,我们研究了肉苁蓉总苷(TC)在 MPTP 诱导的神经元损伤中的作用。此外,我们还筛选了单胺氧化酶 B(MAO-B)的潜在抑制成分。研究结果表明,TC可通过抑制MAO-B的活性来改善运动障碍和多巴胺(DA)神经元的凋亡,同时减少神经胶质细胞的数量,调整单胺神经递质的代谢水平,降低炎症和氧化应激水平。随后,我们进一步构建了含药脑组织的快速筛选方法,筛选出了5种能透过血脑屏障与MAO-B结合的候选成分,并提交进行生物活性评价和抑制机制研究。综上所述,我们在TC中发现了2'-乙酰乳糖苷是一种很有前景的可逆性混合天然MAO-B抑制剂,并建立了一种快速筛选方法,用于筛选具有血脑屏障通透性特征的中枢神经系统药物,为神经退行性疾病的治疗提供了潜在的候选药物和有效的筛选策略。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Evaluation of the Neuroprotective Effect of Total Glycosides of Cistanche deserticola and Investigation of Novel Brain-Targeting Natural MAO-B Inhibitors.

In this study, we investigated the role of total glycosides of Cistanche deserticola (TC) in MPTP-induced neuronal injury. Further, we screened potential inhibitory components of monoamine oxidase B (MAO-B). The study results indicate that TC may improve movement disorders and apoptosis of dopamine (DA) neurons by inhibiting MAO-B activity while reducing the number of glial cells, adjusting the metabolism level of monoamine neurotransmitters, and lowering inflammation and oxidative stress levels. Subsequently, a rapid screening method for drug-containing brain tissue was further constructed, and five candidate components that can cross the blood-brain barrier and bind to MAO-B were screened and submitted for biological activity evaluation and inhibition mechanism research. In summary, we discovered 2'-acetylacteoside as a promising and reversible mixed natural MAO-B inhibitor in TC and developed a rapid screening method for screening central nervous system drugs with blood-brain barrier permeability characteristics, providing potential candidates and an effective screening strategy for neurodegenerative diseases.

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来源期刊
ACS Chemical Neuroscience
ACS Chemical Neuroscience BIOCHEMISTRY & MOLECULAR BIOLOGY-CHEMISTRY, MEDICINAL
CiteScore
9.20
自引率
4.00%
发文量
323
审稿时长
1 months
期刊介绍: ACS Chemical Neuroscience publishes high-quality research articles and reviews that showcase chemical, quantitative biological, biophysical and bioengineering approaches to the understanding of the nervous system and to the development of new treatments for neurological disorders. Research in the journal focuses on aspects of chemical neurobiology and bio-neurochemistry such as the following: Neurotransmitters and receptors Neuropharmaceuticals and therapeutics Neural development—Plasticity, and degeneration Chemical, physical, and computational methods in neuroscience Neuronal diseases—basis, detection, and treatment Mechanism of aging, learning, memory and behavior Pain and sensory processing Neurotoxins Neuroscience-inspired bioengineering Development of methods in chemical neurobiology Neuroimaging agents and technologies Animal models for central nervous system diseases Behavioral research
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