We present the inhibitory properties of the R. pompana anthocyanin fraction (RPAF) and its major constituents on alpha-glucosidase (AG), pancreatic lipase (PL), HMG-CoA reductase, and ornithine decarboxylase (ODC). The effect of RPAF was also evaluated in ICR male mice subjected to oral glucose tolerance test (OGTT) and hypercaloric/atherogenic diet for 30 days. RP-HPLC/MS profiling revealed that RPAF contained five major anthocyanins and induced slight inhibition on PL and HMG-CoA reductase (IC50 , 245-338 μg mL-1 ) whereas strong activity on AG and ODC (IC50 , 130-133 μg mL-1 ) was observed. Kinetic studies and molecular docking with pelargonidin-3-O-rutinoside (P3R) on ODC, revealed changes in Km (0.9514-0.9746 mM) and Vmax (1.96-2.32 μmol mg-1 min-1 ) suggesting mixed inhibition and molecular interaction with two active sites of ODC. P3R showed antiproliferative activity (IC50, 46.5 μM) and decreased polyamine accumulation in DLD-1 cells. The results of OGTT confirmed that RPAF regulates postprandial glucose levels in diabetic animals which experienced a significant glucose depletion (30 %; p<0.001) from 30 to 120 min post-treatment. Prolonged supplementation of RPAF caused significant decrease (p<0.001) in plasma glucose, total cholesterol, LDL-c and triglycerides as well as significant increase (p<0.001) of HDL-c compared with normoglycemic untreated animals.
Keywords: Rhamnus pompana; anthocyanins; antiproliferative; hypoglycaemic; hypolipidemic.
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