Two glutathione S‐transferase inhibitors from Radix Angelicae sinensis
Copyright policy )Two glutathione S‐transferase inhibitors from Radix Angelicae sinensis
AbstractChemotherapy for malignant tumors fails because of multidrug resistance (MDR). The overexpression of glutathione S‐transferase (GST) with MDR is considered one of the major obstacles to successful cancer chemotherapy. High‐throughput screening was performed to search for inhibitors of GST from natural products. Two compounds isolated from Radix Angelicae sinensis had an inhibitory effect on GST, with 50% inhibitory concentration (IC50) values of 16.80 and 7.30μm. Kinetic analyses showed that the two compounds acted as reversible noncompetitive inhibitors of GST. They also increased apoptosis of B‐MD‐C1 (ADR+/+) cells induced by adriamycin with low cytotoxic activity. Radix Angelicae sinensis may be a potential source of GST inhibition for pharmaceutical use. Copyright © 2010 John Wiley & Sons, Ltd.
- Institute of Chinese Materia Medica China (People's Republic of)
- Chinese Academy of Medical Sciences & Peking Union Medical College China (People's Republic of)
- China Academy of Chinese Medical Sciences China (People's Republic of)
- North China Pharmaceutical Group Corp China (People's Republic of)
- PEKING UNION MEDICAL COLLEGE China (People's Republic of)
Models, Molecular, Plant Extracts, Angelica sinensis, Apoptosis, Plant Roots, Cell Line, Inhibitory Concentration 50, Humans, Enzyme Inhibitors, Benzofurans, Glutathione Transferase
Models, Molecular, Plant Extracts, Angelica sinensis, Apoptosis, Plant Roots, Cell Line, Inhibitory Concentration 50, Humans, Enzyme Inhibitors, Benzofurans, Glutathione Transferase
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