中文摘要：

谷胱甘肽转移酶（glutathione S-transferase，GST）是一组具有多种生理功能的同工酶家族，广泛分布于动植物体内，作为机体的Ⅱ相解毒酶，参与机体的解毒作用。研究表明，GST的酶活性水平与肿瘤的耐药性密切相关。因此，GST可能是治疗耐药肿瘤的潜在药物作用靶点。

英文摘要：

To identify the inhibitor of glutathione S-transferase （GST） , a high-throughput screening method was established in a 384-well microplate with total 35μL 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 IC50 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.