Rapid Screening α-Glucosidase Inhibitors from Natural Products by At-Line Nanofractionation with Parallel Mass Spectrometry and Bioactivity Assessment
Rapid Screening α-Glucosidase Inhibitors from Natural Products by At-Line Nanofractionation with Parallel Mass Spectrometry and Bioactivity Assessment
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DOI：
10.1016/j.chroma.2020.461740
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发表时间：
2021-01-04
影响因子：
4.1
通讯作者：
Zhang, Tingting
中科院分区：
文献类型：
--
作者：
Liu, Ruijie;Kool, Jeroen;Zhang, Tingting
本研究成功建立了一种新型的在线纳米分级筛选平台，用于从天然产物中快速筛选和鉴定α-葡萄糖苷酶抑制剂。基于高密度孔板的时程生物测定与高分辨率质谱（MS）平行进行，提供了一种直接和快速的程序，同时获得活性化合物的化学和生物信息。通过在同一孔板上进行多次纳米分级，并比较亲水作用液相色谱（HILIC）和反相液相色谱（RPLC）的正交分离结果，可以准确地从共洗脱液中鉴定α-葡萄糖苷酶抑制剂。对该筛选平台进行了综合评价和验证，并应用于绿色茶多酚和银杏叶黄酮的筛选。通过生物活性色谱图与质谱图的峰形和保留时间的准确匹配，成功筛选并鉴定了10种α-葡萄糖苷酶抑制剂。该筛选方法快速、有效，避免了对低丰度/活性抑制剂的忽视。(C)2020爱思唯尔B. V.保留所有权利。
In this study, a novel at-line nanofractionation screening platform was successfully developed for the rapid screening and identification of alpha-glucosidase inhibitors from natural products. A time-course bioassay based on high density well-plates was performed in parallel with high resolution mass spectrometry (MS), providing a straightforward and rapid procedure to simultaneously obtain chemical and biological information of active compounds. Through multiple nanofractionations into the same well-plate and comparisons of the orthogonal separation results of hydrophilic interaction liquid chromatography (HILIC) and reversed-phase liquid chromatography (RPLC), the alpha-glucosidase inhibitors can be accurately identified from co-eluates. The screening platform was comprehensively evaluated and validated, and was applied to the screenings of green tea polyphenols and Ginkgo folium flavonoids. After accurate peak shape and retention time matching between the bioactivity chromatograms and MS chromatograms, ten alpha-glucosidase inhibitors were successfully screened out and identified. The proposed screening method is rapid, effective and can avoid ignoring low abundant/active inhibitors. (C) 2020 Elsevier B.V. All rights reserved.