High throughput screening for glutathione S-transferase inhibitors / 药学学报
Acta Pharmaceutica Sinica
;
(12): 108-112, 2008.
Article
in Chinese
| WPRIM
| ID: wpr-268162
ABSTRACT
To identify the inhibitor of glutathione S-transferase (GST), a high-throughput screening method was established in a 384-well microplate with total 35 microL 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 degrees C , 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 x 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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Substrate Specificity
/
Chemistry
/
Dinitrochlorobenzene
/
Drug Evaluation, Preclinical
/
Enzyme Inhibitors
/
Glutathione
/
Glutathione Transferase
/
Methods
Type of study:
Diagnostic study
/
Screening study
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2008
Type:
Article
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