Coompo Research Chemicals

The IC50 (50% inhibitory concentration) values for trilobatin of lipid peroxidation in rat liver homogenate was 88 μm. Trilobatin increased superoxide dismutase (SOD) activity with EC50 (50% effective concentration) values of 128 μm, and glutathione peroxidase (GSH-Px) activity with EC50 values of 129 μm, and showed only weak DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging activity.

The inhibitory activities of trilobatin against α-glucosidase and α-amylase were evaluated, and the inhibition mechanism was analysed with Lineweaver–Burk plots. Also the antioxidant activity evaluation of trilobatin was conducted by DPPH radical scavenging assay. Comparing with acarbose, trilobatin showed a strong inhibitory activity against α-glucosidase and a moderate inhibitory activity against α-amylase. The Lineweaver–Burk plots analysis elucidated that trilobatin inhibited the enzyme non-competitively. DPPH scavenging activity of trilobatin (IC50 = 0.57 mg/ml) was higher than rutin (IC50 = 0.72 mg/ml), which indicated that trilobatin had a moderate antioxidant potential. These results suggest that trilobatin is a potential effective α-glucosidase inhibitor for management of postprandial hyperglycemia with less side effect, and provide strong rationale for further animal and clinical studies.