Synthesis, Characterization and Biological Activity of Chemically Modified Insulin Derivative with Alpha Lipoic Acid

A novel chemically-modified insulin, ε-NB29-lipoyl insulin, was selectively prepared by the covalent linkage of α-lipoic acid (LA) to the ε-amino group of LysB29 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.