Effects of KST48 [(2R,5SR)3-(2-chlorobenzoyl)-5-(4-chlorophenoxymethyl)-2(3,4-dichlorophenyl) oxazolidine] on glucose transport in L6 myocytes.
KST48 [(2R,5SR)3-(2-chlorobenzoyl)-5-(4-chlorophenoxymethyl)-2-(3,4-dichlorophenyl)oxazolidine] is an oxazolidine derivative that showed significant stimulating effects on glucose transport in L6 myocytes. The effects of KST48 on glucose uptake were assayed by measuring the transport of 2-deoxyglucose in L6 myocytes. The translocation of glucose transport-4 (GLUT-4) was examined by western blot analysis. KST48 enhanced glucose transport in a concentration dependent manner and the maximum effect was observed at 50 micromol/L. The stimulation of glucose transport was characterized as the increase in Vmax without any significant change of Km value. This enhanced glucose transport was found to be decreased by the treatment with phenylarsine oxide and genistein, but not by the treatment with wortmannin and tyrphostin 25. KST48 was also proved to increase the GLUT-4 translocation. These results suggest that KST48 increases glucose transport in L6 myocytes by stimulating the translocation of GLUT4 to plasma membrane and this action might be mediated by protein tyrosine kinase but not by phosphatidyl inositol 3-kinase.
Lee
Dong-Ook
DO
College of Pharmacy, Seoul National Universitya, Seoul, Korea.
Khil
Lee-Yong
LY
Chang
Tong-Shin
TS
Han
Ho-Kyu
HK
Chae
Sang-Ho
SH
Ahn
Mee-Young
MY
Lee
You-Mie
YM
Lee
Byung-Hoon
BH
Jung
jin-Ho
jH
Kim
Young-Chul
YC
Moon
Chang-Kiu
CK
D000963:Antimetabolites / Q000378:metabolism; D002460:Cell Line; D002470:Cell Survival; D003847:Deoxyglucose / Q000378:metabolism; D004591:Electrophoresis, Polyacrylamide Gel; D005947:Glucose / Q000378:metabolism*; D051275:Glucose Transporter Type 4; D006843:Hydrocarbons, Chlorinated / Q000494:pharmacology*; D007004:Hypoglycemic Agents / Q000494:pharmacology; D015151:Immunoblotting; D007328:Insulin / Q000494:pharmacology; D007700:Kinetics; D008687:Metformin / Q000494:pharmacology; D009004:Monosaccharide Transport Proteins / Q000378:metabolism; D032342:Muscle Cells / Q000187:drug effects / Q000378:metabolism*; D009124:Muscle Proteins / Q000378:metabolism; D032446:Myoblasts / Q000187:drug effects / Q000378:metabolism; D010080:Oxazoles / Q000494:pharmacology*; D021381:Protein Transport / Q000187:drug effects; D011505:Protein-Tyrosine Kinases / Q000378:metabolism; D013347:Subcellular Fractions / Q000187:drug effects / Q000378:metabolism
C496268:(2R,5SR)3-(2-chlorobenzoyl)-5-(4-chlorophenoxymethyl)-2(3,4-dichlorophenyl) oxazolidine; D000963:Antimetabolites; D051275:Glucose Transporter Type 4; D006843:Hydrocarbons, Chlorinated; D007004:Hypoglycemic Agents; D007328:Insulin; D009004:Monosaccharide Transport Proteins; D009124:Muscle Proteins; D010080:Oxazoles; D008687:Metformin; D003847:Deoxyglucose; D011505:Protein-Tyrosine Kinases; D005947:Glucose