Design and oral hypoglycemic activity of novel oral hypoglycemic peptide ODA / 中国药科大学学报
Journal of China Pharmaceutical University
;
(6): 511-518, 2023.
Artigo
em Chinês
| WPRIM
| ID: wpr-987673
ABSTRACT
@#Incretin promotes insulin secretion through a glucose-dependent mechanism, involving glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). Therefore, their correspondingly specific receptors GLP-1R and GIPR are suitable targets for the treatment of type 2 diabetes. Based on the oral hypoglycemic peptide OHP2 designed by our team, we further designed a new oral hypoglycemic peptide, ODA to reduce glucose. Compared with OHP2, ODA exhibited better lipophilicity as well as the enhanced endocytosis and transcytosis in Caco-2 cells. In addition, ODA remained the ability to activate GLP-1R and enhanced the binding ability to GIPR. The hypoglycemic efficacy of the low-dose ODA (0.53 mg/kg) is comparable to that of OHP2 (1.06 mg/kg). These results indicated that ODA could be a new oral drug with potential for the treatment of type 2 diabetes.
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Índice:
WPRIM (Pacífico Ocidental)
Idioma:
Chinês
Revista:
Journal of China Pharmaceutical University
Ano de publicação:
2023
Tipo de documento:
Artigo
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