RESUMO

This present study was to evaluate the protein tyrosine phosphatase 1B (PTP1B) inhibitory activity of nine diterpenes isolated from seeds of Phalaris canariensis, as well as their effect on streptozotocin-nicotinamide-induced type 2 diabetic mice. Their structures were established by spectroscopic analyses. Diterpenes, 1, 4, and 2 exhibited the strongest inhibitory activity on PTP1B with IC50 values of 6.9, 7.3, and 6.5 µM, respectively, The administration of 1-9 showed significant effect on hyperglycemia, among them 1, 4, and 2 reduced fasting glucose levels (55.65%, 54.27%, and 51.22%, respectively). Results revealed that diterpenes performed potential antidiabetic activity via inhibition of PTP1B.[Formula: see text].

Assuntos

Diabetes Mellitus Experimental , Diterpenos , Phalaris , Animais , Hipoglicemiantes , Camundongos , Estrutura Molecular , Proteína Tirosina Fosfatase não Receptora Tipo 1 , Sementes , Estreptozocina