Cancer: Lung
Action: Multi-drug resistance reversal
MDR
Glutathione S-transferase (GST) is a key enzyme in the development of multi-drug resistance (MDR) in tumors. Inhibition of the expression, or activity, of GST has emerged as a promising therapeutic strategy for the reversal of MDR.
Coniferyl ferulate (CF), isolated from the root of Radix Angelica sinensis (RAS), showed strong inhibition of human placental GST. Using the high-throughput screening model, CF's 50% inhibition concentration (IC50) was 0.3 µM, which was greater than the established GSTP1-1 inhibitor, ethacrynic acid (EA).
Moreover, CF showed strong apoptotic activity and could markedly decrease the overexpression of P-gp. The results demonstrated that CF could inhibit GST activity in a concentration-dependent manner and showed a potential MDR reversal effect for anti-tumor adjuvant therapy.
CF demonstrates strong GST inhibitory activity and may serve as a prospective MDR reversal agent in the treatment of cancer. In addition, CF could potentially be used as a promising chemo-sensitizer capable of indirectly regulating P-gp expression via modulation of GST activity, and with fewer adverse effects. Further investigation of CF in anti-tumor adjuvant therapy is warranted (Chen et al., 2013).
Ferulic acid (FA) is widely considered as a biologically active component in Angelica sinensis, and used as one of the marker compounds for the quality control of Angelica sinensis. However, in A. sinensis, FA mainly exists as its ester, coniferyl ferulate (CF). The potency of CF is much higher than that of FA, and the IC50 values for AA, ADP and THR were 7.1 ± 0.3, 276.4 ± 53.4 and 77.5 ± 23.1 µg/ml, respectively (Yu et al., 2009).
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