AIM: The present study was designed to investigate the activity of two glibenclamide derivatives on glucose concentration. An additionalAIM was to identify the biodistribution of glibenclamide derivatives in different organs in a diabetic animal model. METHODS: The effects of two glibenclamide derivatives on glucose concentration were evaluated in a diabetic animal model. In addition, glibenclamide derivatives were bound to Tc-99m using radioimmunoassay methods. To evaluate the pharmacokinetics of the glibenclamide derivatives over time (15, 30, 45 and 60 min) the Tc-99m-glibenclamide conjugates were used. RESULTS: The results showed that glibenclamide-pregnenolone had greater hypoglycemic activity than glibenclamide or glibenclamide-OH. The data also showed that the biodistribution of Tc-99m-glibenclamide-OH in all organs was less than that of the Tc-99m-glibenclamide-pregnenolone derivative. CONCLUSIONS: The glibenclamide-pregnenolone derivative had greater hypoglycemic effects and its biodistribution was wider than glibenclamide-OH. The data suggest that the steroid nucleus may be important to the hypoglycemic activity of the glibenclamide-pregnenolone derivative and this could be related to the degree of lipophilicity induced by the steroid nucleus in the chemical structure of glibenclamide-pregnenolone.

Centro Estatal de Oncologia Campeche Cam Mexico

Escuela Nacional de Ciencias Biologicas del Instituto Politecnico Nacional Prol Carpio y Plan de Ayala s n Col Santo Tomas D F C P 11340 Mexico

Laboratorio de Investigacion en Ciencias Biologicas y Farmacoqimica Facultad de Ciencias Quimico Biologicas Universidad Autonoma de Campeche Av Agustin Melgar Col Buenavista C P 24039 Campeche Cam Mexico

References provided by Crossref.org