title: Polyphenolic Compounds as Pancreatic Lipase Inhibitors.
abstract: Obesity and its associated diseases such as diabetes mellitus and coronary heart diseases are a major challenge for our society. An important target for the treatment of obesity includes the development of inhibitors of nutrient digestion and absorption. Inhibition of pancreatic lipase and the associated reduction of lipid absorption is an attractive approach for the discovery of potent agents. Currently, the only clinically approved pharmacologic agent as pancreatic lipase inhibitor is Orlistat. However, its usage is compromised by unpleasant gastrointestinal adverse reactions (oily stools, oily spotting, flatulence). The use of botanical materials as a potential source of new drugs is of increasing importance and application. Natural products that are interesting for obesity treatment are generally considered to have less toxic and side effects than totally synthetic drugs. One of the most important sources of potential pancreatic lipase inhibitors represents the class of polyphenols. This article summarizes most studied subclasses of polyphenols including flavonoids, hydroxycinnamic acids, hydroxybenzoic acids and lignans with pancreatic lipase inhibitory effects. A structural comparison of potent inhibitors shows an increased inhibitory effect depending on number and position of phenolic hydroxyl groups, degree of polymerization and elimination of glycosylation during digestion.
authors.affiliation: Institute of Pharmacy, Freie Universität Berlin, Berlin, Germany.
authors.forename: Tina
authors.initials: T
authors.lastname: Buchholz
authors.affiliation: Institute of Pharmacy, Freie Universität Berlin, Berlin, Germany.
authors.forename: Matthias F
authors.initials: MF
authors.lastname: Melzig
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005419:Flavonoids / Q000494:pharmacology; D006801:Humans; D007783:Lactones / Q000009:adverse effects / Q000627:therapeutic use; D017705:Lignans / Q000494:pharmacology; D008049:Lipase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D050356:Lipid Metabolism; D009765:Obesity / Q000188:drug therapy*; D000077403:Orlistat; D010179:Pancreas / Q000201:enzymology; D059808:Polyphenols / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D019440:Anti-Obesity Agents; D004791:Enzyme Inhibitors; D005419:Flavonoids; D007783:Lactones; D017705:Lignans; D059808:Polyphenols; D000077403:Orlistat; D008049:Lipase