RT Journal Article
SR Electronic
A1 Figueroa-Valverde, Lauro
A1 Diaz-Cedillo, Francisco
A1 Lopez-Ramos, Maria
A1 Garcia-Cervera, Elodia
A1 Pool-Gomez, Eduardo
A1 Cardena-Arredondo, Carlos
A1 Ancona-Leon, Graciela
T1 Glibenclamide-pregnenolone derivative has greater hypoglycemic effects and biodistribution than glibenclamide-OH in alloxan-rats
JF Biomedical papers
YR 2012
VO 156
IS 2
SP 122
OP 127
DO 10.5507/bp.2012.028
UL https://biomed.papers.upol.cz/artkey/bio-201202-0006.php
AB Aim: The present study was designed to investigate the activity of two glibenclamide derivatives on glucose concentration. An additional aim 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.