Antidiabetic activity of some pentacyclic acid triterpenoids, role of PTP-1B: In vitro, in silico, and in vivo approaches
Por:
Ramírez-Espinosa J.J., Rios M.Y., López-Martínez S., López-Vallejo F., Medina-Franco J.L., Paoli P., Camici G., Navarrete-Vázquez G., Ortiz-Andrade R., Estrada-Soto S.
Publicada:
1 jun 2011
Resumen:
The aim of the current study was to investigate the oral antidiabetic activity of four structurally-related triterpenic acids: ursolic (RE-01), oleanolic (RE-02), moronic (RE-03) and morolic (RE-04) acids. STZ-nicotinamide diabetic rats were treated with these triterpenes (50 mg/kg) and the antidiabetic effects in acute experiment were determined. All compounds showed significant antidiabetic activity in comparison with control group (p < 0.05). The in vitro inhibitory activity of compounds against protein tyrosine phosphatase 1B (PIP-1B) was also evaluated. At 50 mu M, the enzymatic activity was almost completely inhibited. All compounds were docked with a crystal structure of PTP-1B. Docking results suggested the potential binding of the triterpenic acids in a binding pocket next to the catalytic site. An extensive hydrogen bond network with the carboxyl group and Van der Waals interactions stabilize the protein-ligand complexes. (C) 2011 Elsevier Masson SAS. All rights reserved.
Filiaciones:
Ramírez-Espinosa J.J.:
Facultad de Farmacia, Universidad Autónoma Del Estado de Morelos, Avenida Universidad 1001, Col. Chamilpa, Cuernavaca, Morelos 62209, Mexico
Rios M.Y.:
Centro de Investigaciones Químicas, Universidad Autónoma Del Estado de Morelos, Avenida Universidad 1001, Col. Chamilpa, Cuernavaca, Morelos 62209, Mexico
López-Martínez S.:
Centro de Investigaciones Químicas, Universidad Autónoma Del Estado de Morelos, Avenida Universidad 1001, Col. Chamilpa, Cuernavaca, Morelos 62209, Mexico
López-Vallejo F.:
Torrey Pines Institute for Molecular Studies, Port St. Lucie, FL 34987, United States
Medina-Franco J.L.:
Torrey Pines Institute for Molecular Studies, Port St. Lucie, FL 34987, United States
Paoli P.:
Dipartimento di Scienze Biochimiche, Universitá degli Studi di Firenze, Viale Morgani 50, 50134 Firenze, Italy
Camici G.:
Dipartimento di Scienze Biochimiche, Universitá degli Studi di Firenze, Viale Morgani 50, 50134 Firenze, Italy
Navarrete-Vázquez G.:
Facultad de Farmacia, Universidad Autónoma Del Estado de Morelos, Avenida Universidad 1001, Col. Chamilpa, Cuernavaca, Morelos 62209, Mexico
Ortiz-Andrade R.:
Facultad de Química, Universidad Autónoma de Yucatán, Mérida, Calle 421 No. 41 X 26 Y 28 Col. Industrial, C.P. 97150 Mérida Yucatán 97150, Mexico
Estrada-Soto S.:
Facultad de Farmacia, Universidad Autónoma Del Estado de Morelos, Avenida Universidad 1001, Col. Chamilpa, Cuernavaca, Morelos 62209, Mexico
All Open Access; Green
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