J Pharm Pharmacogn Res 3(suppl. 1): S2, 2015
Proceedings of the 4th International Symposium on Pharmacology of Natural Products FAPRONATURA 2015 September 21st-25th, 2015; Cuban Society of Pharmacology. Topes de Collantes, Sancti Spiritus, Cuba.
L-02: PREDICTIVE STRATEGY TO SCREENING NATURAL CANDIDATES FOR TYPE 2 DIABETES BASED ON PTP-1B AND DPP-IV INHIBITORY ACTIVITY AND in vitro GLUCOSE UPTAKE
Marrero E1, Sánchez J1, Young L2, Harvey A2.
Introduction: The present study is aimed to determine the underlying mechanism of the antidiabetic potentiality of seven Cuban plants based on relevant therapeutic target of type 2 diabetes: Allophylus cominia (L.) Sw., Ocimum tenuiflorum, Persea americana, Sechium edule, Momordica charantia and Jatropha aethiopica. Methods: Leaves aqueous extracts and its fractions were evaluated on protein tyrosine phosphatase 1B (PTP1B) and dipeptidyl peptidase-IV (DPPIV) enzymatic activities and the glucose uptake to identify candidates as phytopharmaceuticals in treating diabetes. In PTP1B assay (DiFMUP) was used as substrate and (TFMS) as standard inhibitor; in DPPIV assay (Gly-pro-AMC) was used as substrate and as standard inhibitor (P32/98); in both assays, the enzymatic activity inhibition was calculated by fluorescence using excitation wavelength of 360 nm and emission wavelength of 460 nm. Glucose uptake studies were performed on fully differentiated 3T3-L1 adipocyte using 2-deoxy-D-[3H] glucose and insulin as positive control, radioactivity into the cells was measured with a microplate scintillation counter. Results: The extracts from A. cominia, O. tenuiflorum and P. americana inhibited the enzymatic activity of PTP1B in a concentration dependent manner, resulting more actives the polar fractions from A. cominia and P americana. All the extracts and fractions showed inhibition of enzymatic activity of DPPIV, at higher concentrations. A. cominia inhibited enzymatic activity of this protease in an extract concentration dependent manner. A. cominia, O. tenuiflorum and P. americana extracts exhibited enhance of glucose uptake in 3T3-L1 adipocytes. Conclusions: The aqueous extracts from A. cominia, P. americana and O. tenuiflorum and some of its fractions could be promising antidiabetic candidates. Further A. cominia studies based on bio-guided estructure-activity assays of the aqueous extracts and fractions revealed quercitrin and mearnsetrin flavonoids as the key components in that activity.
Citation Format: Marrero E, Sánchez J, Young L, Harvey A (2015) Predictive strategy to screening natural candidates for type 2 diabetes based on PTP-1b and DPP-iv inhibitory activity and in vitro glucose uptake. [Abstract]. In: Proceedings of the FAPRONATURA 2015; 2015 Sep 21-25; Topes de Collantes, Sancti Spiritus: CSF. J Pharm Pharmacogn Res 3(Suppl. 1): S2. Abstract nr L-02.