Encapsulation of 16-Hydroxycleroda-3,13-Dine-16,15-Olide in Mesoporous Silica Nanoparticles as a Natural Dipeptidyl Peptidase-4 Inhibitor Potentiated Hypoglycemia in Diabetic Mice.

摘要: Natural supplements comprise good efficacy with less adverse effects as against diabetic therapy, but their advancement anti-diabetic agents is unsatisfactory regard to the delivery system. Dipeptidyl peptidase-4 (DPP4)/CD26) can degrade glucagon-like pepetide-1 (GLP-1) which renders a decrease of blood glucose levels. 16-hydroxycleroda-3,13-dine-16,15-olide (HCD) extracted from Polyalthia longifolia, exhibits numerous medicinal potentials including hypoglycemic potential. On consideration HCD application, bioavailability affected by low solubility. Extended experiments confirmed biocompatible mesoporous silica nanoparticles (MSNs) encapsulation resulted in sustained release property delivering for inhibition DPP4 via activity and protein levels analysis. In enzymatic assay, MSN-HCD directly changed activity. Moreover, were treated Caco-2 cells determined within cells. The results revealed that caused reduction time- dose-dependent fashion. Orally administered diet-induced mice alleviated an oral tolerance test. addition, administration five weeks biochemical cues such pyruvate transaminase (GPT), glutamate oxaloacetate (GOT), triglycerides (TG), cholesterol (CHO), glycated hemoglobin (HbA1c) commendable further confirmation down-regulation hyperglycemia. Furthermore, this formulation effectively controlled significantly decreased body weight mice, suggesting exerts natural inhibitor potential clinical drug treatment diabetes.