Synthesis, characterization and biological activity of chemically modified insulin derivative with alpha lipoic acid.
A novel chemically-modified insulin, epsilon-N(B29)-lipoyl insulin, was selectively prepared by the covalent linkage of alpha-lipoic acid (LA) to the epsilon-amino group of Lys(B29) of insulin without any protecting agent and analyzed by PAGE, HPLC, MALDI-TOF-MS. Monolipoyl- insulin maintained the glucose-lowering effect as well as native insulin and showed a longer duration of action than native insulin and an inhibitory effect towards trypsin degradation.
Huang
Tao
T
Department of Chemistry, Huazhong University of Science and Technology, Wuhan 430074, P.R. China.
Huang
Kaixun
K
D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D007328:Insulin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D015394:Molecular Structure; D012996:Solutions; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; D013379:Substrate Specificity; D013552:Swine; D008063:Thioctic Acid / Q000737:chemistry*; D014357:Trypsin / Q000378:metabolism
D001786:Blood Glucose; D007328:Insulin; D012996:Solutions; D008063:Thioctic Acid; D014357:Trypsin