LAQV, REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Porto, Portugal.
Dipartimento di Chimica e Chimica Industriale, Università di Pisa, Pisa, Italy.
J Enzyme Inhib Med Chem. 2022 Dec;37(1):1527-1536. doi: 10.1080/14756366.2022.2073443.
A novel automated method based on sequential injection analysis (SIA), a non-segmented flow injection technique, was developed to evaluate glutathione S-transferase P1-1 (GST P1-1) activity in the presence of organometallic complexes with putative anticancer activity. The assay is based on the reaction of L-glutathione (GSH) and 1-chloro-2,4-dinitrobenzene (CDNB) in the presence of GST P1-1 to afford the GS-DNB conjugate and the reaction may be monitored by an increase in absorbance at 340 nm. A series of ruthenium, iron, osmium and iridium complexes were evaluated as GST P1-1 inhibitors by evaluating their half-maximal inhibitory concentration (IC). An iridium compound displays the lowest IC value of 6.7 ± 0.7 µM and an iron compound displays the highest IC value of 275 ± 9 µM. The SIA method is simple to use, robust, reliable, and efficient and uses fewer reagents than batch methods and each analysis takes only 5 minutes.
一种基于顺序注射分析（SIA）的新型自动化方法，是一种非分段流动注射技术，已被开发用于评估具有潜在抗癌活性的有机金属配合物存在下谷胱甘肽 S-转移酶 P1-1（GST P1-1）的活性。该测定基于 GST P1-1 存在下 L-谷胱甘肽（GSH）和 1-氯-2,4-二硝基苯（CDNB）的反应，以提供 GS-DNB 缀合物，并且可以通过在 340nm 处吸光度的增加来监测反应。一系列钌、铁、锇和铱配合物被评估为 GST P1-1 抑制剂，通过评估它们的半最大抑制浓度（IC）来评估。一种铱化合物显示出最低的 IC 值为 6.7±0.7μM，而一种铁化合物显示出最高的 IC 值为 275±9μM。SIA 方法简单易用、稳健、可靠且高效，与批量方法相比，它使用的试剂更少，每次分析仅需 5 分钟。
