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Development of an online UPLC-PDA-ESI-Q-TOF-MS-LOX-FLD system for rapid screening of anti-inflammatory compounds in Polygala tenuifolia Willd
Journal of Pharmaceutical and Biomedical Analysis ( IF 3.4 ) Pub Date : 2023-03-22 , DOI: 10.1016/j.jpba.2023.115353
Mimi Sun 1 , Mengmeng Yuan 1 , Hong Wang 2 , Runxin Yin 2 , Chenjia Yan 2 , Meihua Yin 1 , Zenghu Su 1 , Xinyu Lei 2 , Xiangyu Fu 2 , Senfeng Sun 2 , Yazhuo Huang 2 , Hongbo Xu 1 , Shizhong Chen 2
Affiliation  

In this study, the first ultra-high performance liquid chromatography-photo-diode array-electrospray ionization-quadrupole-time-of-flight-mass spectrometry-lipoxygenase-fluorescence detector (UPLC-PDA-ESI-Q-TOF-MS-LOX-FLD) online system was developed for the identification and evaluation of anti-inflammatory active ingredients in Polygala tenuifolia Willd. Using this system, the UPLC fingerprints, mass fragments and LOX-binding peak profiles in the samples were rapidly and simultaneously obtained. A total of 101 compounds were isolated and identified and 38 compounds (11 oligosaccharide esters, nine xanthones, 17 saponins, and one glycosyloxyflavone) showed strong LOX-binding activity. Six compounds were selected to study their LOX-binding ability, and the results indicated that the content of the six compounds had a good linear relationship with the LOX-binding ability, and it was found that the substitution position, the type of substituent and the number of glycosyl groups all had a certain influence on the LOX-binding ability of the compounds. The LOX-binding activities of 10 compounds were verified by the surface plasmon resonance (SPR) technique and the activity results were consistent with the online system. After validation, we identified 7 active compounds that combined with LOX to exert anti-inflammatory effects for the first time. All the results fully demonstrate the efficiency, stability and reliability of the online system and this work provides an exemplary and useful method for the rapid screening of potential anti-inflammatory active compounds in P. tenuifolia and other traditional Chinese medicines. At the same time, it provides a new direction for screening small molecule inhibitors of enzymes like LOX.



中文翻译:

开发用于快速筛选远志中抗炎化合物的在线 UPLC-PDA-ESI-Q-TOF-MS-LOX-FLD 系统

在这项研究中,第一个超高效液相色谱-光电二极管阵列-电喷雾电离-四极杆-飞行时间-质谱-脂氧合酶-荧光检测器(UPLC-PDA-ESI-Q-TOF-MS-LOX -FLD)开发了远志抗炎活性成分鉴定评价在线系统威尔德。使用该系统,可以快速同时获得样品中的 UPLC 指纹图谱、质量碎片和 LOX 结合峰图谱。共分离和鉴定了 101 种化合物,其中 38 种化合物(11 种低聚糖酯、9 种氧杂蒽酮、17 种皂苷和 1 种糖基氧基黄酮)显示出很强的 LOX 结合活性。选取6种化合物对其LOX结合能力进行了研究,结果表明6种化合物的含量与LOX结合能力具有良好的线性关系,发现取代位置、取代基类型和糖基基团的数量均对化合物的LOX结合能力有一定的影响。通过表面等离子共振(SPR)技术验证了10个化合物的LOX结合活性,活性结果与在线系统一致。经过验证,我们首次鉴定出 7 种与 LOX 结合发挥抗炎作用的活性化合物。所有结果充分证明了在线系统的效率、稳定性和可靠性,该工作为快速筛选潜在的抗炎活性化合物提供了一种示范和有用的方法。P. tenuifolia等中药。同时,为筛选LOX等酶的小分子抑制剂提供了新的方向。

更新日期:2023-03-23
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