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《Acta Pharmaceutica Sinica》 2008-01
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High throughput screening for glutathione S-transferase inhibitors

ZHANG Dan-shen~(1,2),ZHANG Tian-tai~1,LI Shao-jing~1, DU Guan-hua~(1)(1.Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China;2.Department of Pharmacy,Hebei North University,Zhangjiakou 075000,China)  
To identify the inhibitor of glutathione S-transferase(GST),a high-throughput screening method was established in a 384-well microplate with total 35 μL volume,and the absorbance at 340 nm is detected.The concentrations of substrates,CDNB and GST were determined by chromatometry.The optimal enzyme kinetics reaction time and temperature are 2 h and 30 ℃,respectively.The established model was evaluated by NaOCl,a known GST inhibitor,and the parameter Z′ was 0.77,which showed a high feasibility and stability of the assay.A total of 31 098 compounds were screened,of which 4 compounds were shown to inhibit GST activity,high inhibiting activity for their IC_(50) of GST inhibition was 3.94,4.05,74.85,and 77.41 mg·L~(-1),separately.The results indicated that the colorimetric method by using CDNB and GSH as substrate is stable,sensitive,reproducible and also suitable for high throughput screening.
【Fund】: 国家自然科学基金重点资助项目(30630073).
【CateGory Index】: R965.1
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