Glibenclamide-pregnenolone derivative has greater hypoglycemic effects and biodistribution than glibenclamide-OH in alloxan-rats

Lauro Figueroa-Valverde, Francisco Diaz-Cedillo, Maria Lopez-Ramos, Elodia Garcia-Cervera, Eduardo Pool-Gomez, Carlos Cardena-Arredondo, Graciela Ancona-Leon

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Abstract

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.
Original languageAmerican English
Pages (from-to)122-127
Number of pages6
JournalBiomedical Papers
DOIs
StatePublished - 24 Jul 2012

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Pregnenolone
Alloxan
Glyburide
Hypoglycemic Agents
Rats
Derivatives
Animals
Animal Models
Steroids
Glucose
Pharmacokinetics

Cite this

Figueroa-Valverde, L., Diaz-Cedillo, F., Lopez-Ramos, M., Garcia-Cervera, E., Pool-Gomez, E., Cardena-Arredondo, C., & Ancona-Leon, G. (2012). Glibenclamide-pregnenolone derivative has greater hypoglycemic effects and biodistribution than glibenclamide-OH in alloxan-rats. Biomedical Papers, 122-127. https://doi.org/10.5507/bp.2012.028
Figueroa-Valverde, Lauro ; Diaz-Cedillo, Francisco ; Lopez-Ramos, Maria ; Garcia-Cervera, Elodia ; Pool-Gomez, Eduardo ; Cardena-Arredondo, Carlos ; Ancona-Leon, Graciela. / Glibenclamide-pregnenolone derivative has greater hypoglycemic effects and biodistribution than glibenclamide-OH in alloxan-rats. In: Biomedical Papers. 2012 ; pp. 122-127.
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title = "Glibenclamide-pregnenolone derivative has greater hypoglycemic effects and biodistribution than glibenclamide-OH in alloxan-rats",
abstract = "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.",
author = "Lauro Figueroa-Valverde and Francisco Diaz-Cedillo and Maria Lopez-Ramos and Elodia Garcia-Cervera and Eduardo Pool-Gomez and Carlos Cardena-Arredondo and Graciela Ancona-Leon",
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language = "American English",
pages = "122--127",
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Figueroa-Valverde, L, Diaz-Cedillo, F, Lopez-Ramos, M, Garcia-Cervera, E, Pool-Gomez, E, Cardena-Arredondo, C & Ancona-Leon, G 2012, 'Glibenclamide-pregnenolone derivative has greater hypoglycemic effects and biodistribution than glibenclamide-OH in alloxan-rats', Biomedical Papers, pp. 122-127. https://doi.org/10.5507/bp.2012.028

Glibenclamide-pregnenolone derivative has greater hypoglycemic effects and biodistribution than glibenclamide-OH in alloxan-rats. / Figueroa-Valverde, Lauro; Diaz-Cedillo, Francisco; Lopez-Ramos, Maria; Garcia-Cervera, Elodia; Pool-Gomez, Eduardo; Cardena-Arredondo, Carlos; Ancona-Leon, Graciela.

In: Biomedical Papers, 24.07.2012, p. 122-127.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Glibenclamide-pregnenolone derivative has greater hypoglycemic effects and biodistribution than glibenclamide-OH in alloxan-rats

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

PY - 2012/7/24

Y1 - 2012/7/24

N2 - 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.

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.

U2 - 10.5507/bp.2012.028

DO - 10.5507/bp.2012.028

M3 - Article

SP - 122

EP - 127

JO - Biomedical Papers

JF - Biomedical Papers

SN - 1213-8118

ER -