Affiliation: | 1. Centro de Investigación y de Estudios Avanzados del IPN, Unidad Irapuato, Km 9.6 Carretera, C.P. 36824 Irapuato-León, Gto, Mexico Universidad Politécnica Metropolitana de Puebla, Popocatépetl s/n Reserva Territorial Atlixcáyotl, Tres Cerritos, CP 72480 Puebla, CP, Mexico;2. Centro de Investigación y de Estudios Avanzados del IPN, Unidad Irapuato, Km 9.6 Carretera, C.P. 36824 Irapuato-León, Gto, Mexico;3. Universidad Politécnica Metropolitana de Puebla, Popocatépetl s/n Reserva Territorial Atlixcáyotl, Tres Cerritos, CP 72480 Puebla, CP, Mexico;4. Dirección de Innovación y Transferencia de Conocimiento, Benemérita Universidad Autónoma de Puebla, Prolongación de la 24 Sur y Av. San Claudio, Cd. Universitaria, CP 72570 Puebla, CP, Mexico;5. CONAHCyT-Centro Universitario de Vinculación y Transferencia de Tecnología, Benemérita Universidad Autónoma de Puebla, Prolongación de la 24 Sur y Av. San Claudio, Cd. Universitaria, CP 72570 Puebla, CP, Mexico |
Abstract: | 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. |