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Isoorientin is a potent inhibitor of COX-2 with an IC50 value of 39 μM.

Isoorientin is a Selective Inhibitor of Cyclooxygenase-2 (COX-2) from the Tubers of Pueraria tuberosa[1]. PANC-1 and PATU-8988 cells are grown for 24 hours in the presence of Isoorientin (0, 20, 40, 80, and 160 μM), and a CCK8 solution is added. The cell viability decreases significantly at the concentrations of 20, 40, 80, and 160 μM. After the cells are cultured with Isoorientin (0, 20, 40, 80, and 160 μM for PANC-1; 0, 20, 40, 80, 160, and 320 μM for PATU-8988) for 24 hours, the expression of p-AMPK and AMPK is assessed by Western blotting. After the Isoorientin treatment, the p-AMPK expression is increased. Then, in the shRNA group, the concentration of 80 μM is used to detect the effects of Isoorientin. The expression levels of AMPK and p-AMPK are much lower in the shRNA group than in the wild-type PC cells (WT) and the group that is transfected with a negative control lentivirus (NC)[2].

Animals treated with Isoorientin at 10 mg/kg and 20 mg/kg body weight have a statistically significant reduction in paw edema, with a mean peak thickness of 1.19±0.05 mm and 1.08±0.04 mm, respectively. This indicated that Isoorientin significantly attenuates paw edema compared with the control group[3].

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