Triacylglycerols based on 2-(N-tert-butoxycarbonylamino)-oleic acid are potent inhibitors of pancreatic lipase

摘要

Human pancreatic(HPL)and gastric(HGL)lipases are essential enzymes for efficient fat digestion.The hydrolysis of dietary triacylglycerols by these enzymes to form monoacylglycerols and free fatty acids is a necessary step for fat absorption by the enterocytes.Therefore,potent and specific inhibitors of digestive lipases are of interest,because they may find applications as anti-obesity agents.Here,we present the synthesis of a novel class of potent human pancreatic lipase(HPL)inhibitors,based on the non-natural amino acid 2-(N-tert-butoxycarbonylamino)-oleic acid,which was esterified with glycerol and 2-methyl-glycerol.