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一种多功能和自动的在线查方法:基于层状流量配置的毛细血管电泳的横向扩散,用于探索天然产品中的PTP1B抑制剂

Juan Gao¹, Erwin Adams¹, Zhengjin Jiang²

¹KU Leuven - University of Leuven, Pharmaceutical Analysis, Department of Pharmaceutical and Pharmacological Sciences, O&N2, PB 923, Herestraat 49 3000 Leuven, Belgium.

Journal of chromatography. A

|December 21, 2024

概括

一种新的毛细电泳 (CE) 方法选蛋白质氨酸酸酶1B (PTP1B) 的天然产品抑制剂. 这种自动化技术提供了快速分析,并确定了协同效应,有助于药物发现.

科学领域:

生物化学生物化学
分析化学分析化学
药理学药理学是指药理学的学科.

背景情况:

由于其多样化的生物活性,天然产品在药物发现中至关重要.
蛋白氨酸酸酶1B (PTP1B) 是代谢疾病的关键标.
查PTP1B抑制剂对于开发新疗法至关重要.

研究的目的:

开发和验证自动在线毛细管电泳 (CE) 方法,用于从天然产品中选PTP1B抑制剂.
研究天然产品组合的潜在协同抑制效应.
用分子对接来阐明抑制的机制.

主要方法:

开发和优化在线CE方法,利用层状流程配置文件的横向扩散 (TDLFP) 进行酶反应.
验证CE方法用于动力常数的确定和抑制剂选.
分子对接的应用,以了解自然化合物与PTP1B的结合相互作用.

主要成果:

开发的CE方法表现出良好的重复性和3分钟的快速分析时间.
精确确定了动力参数 (Km = 3.66 ± 0.97 mM) 和抑制功率 (Na3VO4 的IC50 = 98.50 ± 24.82 μM).
对于 Morus alba L. 与奎尔丁/咖啡酸的联合提取物,观察到对 PTP1B 的协同抑制作用.

结论:

成功建立了一种通用,自动化的在线CE方法,用于高效的PTP1B抑制剂查.
该方法的自动化和低样本消耗使其适合选其他脱酶.
分子对接表明,来自Morus alba L.的化合物通过与其催化和基质识别站点相互作用来抑制PTP1B.

关键词:

毛细管电泳可以通过毛细管电泳进行.分子对接是分子对接.自然产品是天然产品.蛋白质氨酸酸酶是一种蛋白质氨酸酸酶.横向扩散层状流量配置文件的横向扩散.

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