PT  - JOURNAL ARTICLE
AU  - Figueroa-Valverde, Lauro
AU  - Diaz-Cedillo, Francisco
AU  - Lopez-Ramos, Maria
AU  - Garcia-Cervera, Elodia
AU  - Pool-Gomez, Eduardo
AU  - Cardena-Arredondo, Carlos
AU  - Ancona-Leon, Graciela
TI  - Glibenclamide-pregnenolone derivative has greater hypoglycemic effects and biodistribution than glibenclamide-OH in alloxan-rats
DP  - 2012 Jun 1
TA  - Biomedical papers
PG  - 122--127
VI  - 156
IP  - 2
AID - 10.5507/bp.2012.028
IS  - 12138118
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.