Lipases and lipolysis in the human digestive tract: where do we stand?
OBJECTIVE
The review evaluates current knowledge of the different lipases catalyzing triglyceride lipolysis in the human digestive tract, focusing on their mode of action - information useful for developing strategies to regulate the bioavailability of fatty acid.


RESULTS
Optimal levels of digestive lipases promote efficient triglyceride lipolysis in healthy humans. Management of fatty acid bioavailability during pancreatic insufficiencies, however, requires enzyme replacement therapy. Such therapy entails gastro-protected porcine pancreatic powder, associated with antacid treatment when duodenal pH is too acidic; recently, enteric-coated high-buffered pancrelipase or recombinant gastric lipase have been used. Another promising strategy is to focus on lipid substrate to optimize lipid-water interface properties. Research on obesity treatment focuses on inhibitors. Orlistat is the first inhibitor to be used extensively. Others treatments are in development, including human pancreatic lipase C-terminal, polyphenols, specific proteins and peptides; however, their relevance has not yet been tested in humans.


CONCLUSIONS
A better knowledge of lipase structure and mode of action will help the development of new natural inhibitors with fewer secondary effects. More intensive research in protein engineering for recombinant lipase production and in clinical nutrition, together with careful evaluation of patients' individual needs is necessary.
Armand
Martine
M
INSERM, U476 'Nutrition Humaine et Lipides', INRA, UMR1260, Université Méditerranée Aix-Marseille 2, Faculté de Médecine, IPHM-IFR 125, Marseille, France. martine.armand@medecine.univ-mrs.fr
D000818:Animals; D001682:Biological Availability; D004064:Digestive System / Q000201:enzymology*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D007783:Lactones / Q000494:pharmacology; D008049:Lipase / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism*; D008066:Lipolysis / Q000187:drug effects / Q000502:physiology; D000077403:Orlistat; D014280:Triglycerides / Q000378:metabolism* / Q000493:pharmacokinetics
D004791:Enzyme Inhibitors; D007783:Lactones; D014280:Triglycerides; D000077403:Orlistat; D008049:Lipase