Two glutathione S-transferase inhibitors from Radix Angelicae sinensis.
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.
Huang
Feng
F
Medical College of Shantou University, Shantou, 515031, China.
Li
Shaojing
S
Lu
Xinhua
X
Liu
Ailin
A
Du
Guanhua
G
Shi
Ganggang
G
D029971:Angelica sinensis / Q000737:chemistry*; D017209:Apoptosis; D001572:Benzofurans / Q000302:isolation & purification / Q000494:pharmacology; D002460:Cell Line; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D005982:Glutathione Transferase / Q000037:antagonists & inhibitors*; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D010936:Plant Extracts / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry
C488006:11-angeloylsenkyunolide F; D001572:Benzofurans; D004791:Enzyme Inhibitors; D010936:Plant Extracts; D005982:Glutathione Transferase