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Two glutathione S‐transferase inhibitors from Radix Angelicae sinensis
Author(s) -
Huang Feng,
Li Shaojing,
Lu Xinhua,
Liu Ailin,
Du Guanhua,
Shi Ganggang
Publication year - 2011
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.3197
Subject(s) - radix (gastropod) , glutathione , pharmacology , multiple drug resistance , chemistry , chemotherapy , enzyme , glutathione s transferase , glutathione transferase , traditional medicine , biochemistry , biology , medicine , botany , genetics , antibiotics
Chemotherapy 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 (IC 50 ) 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.