Rosiglitazone stimulates the release and synthesis of insulin by enhancing GLUT-2, glucokinase and BETA2/NeuroD expression.
Peroxisome proliferator-activated receptor (PPAR)-gamma is a member of the nuclear receptor superfamily, and its ligands, the thiazolidinediones, might directly stimulate insulin release and insulin synthesis in pancreatic beta-cells. In the present study, we examined the effects of rosiglitazone (RGZ) on insulin release and synthesis in pancreatic beta-cell (INS-1). Insulin release and synthesis were stimulated by treatment with RGZ for 24h. RGZ upregulated the expressions of GLUT-2 and glucokinase (GCK). Moreover, it was found that RGZ increased the expression of BETA2/NeuroD gene which could regulate insulin gene expression. These results suggest that RGZ could stimulate the release and synthesis of insulin through the upregulation of GLUT-2, GCK, and BETA2/NeuroD gene expression.
Kim
Hyo-Sup
HS
Division of Endocrinology and Metabolism, Samsung Biomedical Research Institute (SBRI), Seoul, Republic of Korea.
Noh
Jung-Hyun
JH
Hong
Seung-Hyun
SH
Hwang
You-Cheol
YC
Yang
Tae-Young
TY
Lee
Myung-Shik
MS
Kim
Kwang-Won
KW
Lee
Moon-Kyu
MK
D000813:Anilides / Q000494:pharmacology; D000818:Animals; D051792:Basic Helix-Loop-Helix Proteins / Q000378:metabolism*; D002478:Cells, Cultured; D005941:Glucokinase / Q000378:metabolism*; D005947:Glucose / Q000493:pharmacokinetics; D051273:Glucose Transporter Type 2 / Q000378:metabolism*; D007004:Hypoglycemic Agents / Q000494:pharmacology; D007328:Insulin / Q000096:biosynthesis* / Q000378:metabolism; D000078790:Insulin Secretion; D050417:Insulin-Secreting Cells / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D007340:Insulinoma; D008297:Male; D009419:Nerve Tissue Proteins / Q000378:metabolism*; D047495:PPAR gamma / Q000187:drug effects; D051381:Rats; D020334:Rats, Inbred OLETF; D000077154:Rosiglitazone; D045162:Thiazolidinediones / Q000494:pharmacology*; D015854:Up-Regulation / Q000187:drug effects
D000813:Anilides; D051792:Basic Helix-Loop-Helix Proteins; D005941:Glucokinase; D005947:Glucose; D051273:Glucose Transporter Type 2; D007004:Hypoglycemic Agents; D007328:Insulin; D009419:Nerve Tissue Proteins; D047495:PPAR gamma; D000077154:Rosiglitazone; D045162:Thiazolidinediones; C457499:2-chloro-5-nitrobenzanilide; C495683:Slc2a2 protein, rat; C093564:Neurogenic differentiation factor 1