Loewenthal Dan, Dagan Shai, Drug Eyal
Department of Analytical Chemistry, Israel Institute for Biological Research (IIBR), Ness-Ziona7410001, Israel.
School of Chemistry, Faculty of Exact Sciences, Tel-Aviv University, Tel Aviv6997801, Israel.
Anal Chem. 2023 Feb 7;95(5):2623-2627. doi: 10.1021/acs.analchem.2c04842. Epub 2023 Jan 23.
Analytical chemists are often challenged to screen for bioactive compounds in complex matrices, sometimes without a priori knowledge of the exact compound of interest. Therefore, "flagging" techniques, highlighting common characteristics of bioactive compounds, are highly sought after. In this work, we demonstrate a double flagging method, where unknown organophosphorus acetylcholinesterase inhibitors are "flagged" out of a complex matrix by the presence of organophosphorus-indicative ions as well as their acetylcholinesterase inhibition. This is accomplished by flagging the LC chromatographic retention time of phosphorus-indicative ions using accurate mass high-energy in-source CID products, and the retention time of acetylcholinesterase inhibiting compounds using a parallel microfractionation-based bioassay. We successfully apply this method to screen VX, VM, and RVX nerve agents as well as methomyl, a carbamate pesticide, out of soil and whole blood samples at low μM to sub-μM concentrations. This methodology can be easily extended to diverse chemical families and biological activities of interest.
分析化学家常常面临在复杂基质中筛选生物活性化合物的挑战,有时甚至事先并不清楚具体感兴趣的化合物是什么。因此,能够突出生物活性化合物共同特征的“标记”技术备受青睐。在这项工作中,我们展示了一种双重标记方法,即通过有机磷指示离子的存在及其对乙酰胆碱酯酶的抑制作用,从复杂基质中“标记”出未知的有机磷乙酰胆碱酯酶抑制剂。这是通过使用精确质量的高能源内CID产物标记磷指示离子的液相色谱保留时间,以及使用基于平行微分离的生物测定法标记乙酰胆碱酯酶抑制化合物的保留时间来实现的。我们成功地将该方法应用于从土壤和全血样品中筛选低 microM 至亚 microM 浓度的 VX、VM 和 RVX 神经毒剂以及氨基甲酸酯类农药灭多威。这种方法可以很容易地扩展到各种感兴趣的化学家族和生物活性。