title: Betulinic acid has an inhibitory effect on pancreatic lipase and induces adipocyte lipolysis.
abstract: Betulinic acid is a pentacyclic triterpenic acid that exists naturally in many kinds of food and has many biological functions. The present study investigated the antiobesity properties of betulinic acid and possible mechanisms by which betulinic acid functions. To examine the antilipase function of betulinic acid, the ability of betulinic acid to inhibit pancreatic lipase activity in vitro and to prevent the elevation of plasma triacylglycerol levels was tested after oral administration of a lipid emulsion in rats. In addition, the lipolytic effects of betulinic acid were assayed in rat adipose tissues. The activity of cAMP-dependent phosphodiesterase was also measured in vitro. Betulinic acid inhibited pancreatic lipase activity in a dose-dependent manner at concentrations of 1.5-100 µM (IC₅₀ value of 21.10 µM) and prevented the elevation of plasma triacylglycerol levels 2 h after oral administration of the lipid emulsion at a dose of 100 mg/kg. In addition, betulinic acid had a strong lipolytic effect, which was mediated by cAMP-dependent phosphodiesterase inhibition. In conclusion, betulinic acid may exert antiobesity effects by directly inhibiting pancreatic lipase, which would prevent the absorption of lipid from the small intestine. In addition, it was found that betulinic acid may further accelerate fat mobilization by enhancing the levels of lipolysis in adipose tissues.
authors: Diabetic Complications Research Center, Division of Traditional Korean Medicine-TKM Integrated Research, Korea Institute of Oriental Medicine, Daejeon, South Korea.
authors: Junghyun
authors: J
authors: Kim
authors: Young Seub
authors: YS
authors: Lee
authors: Chan-Sik
authors: CS
authors: Kim
authors: Jin Sook
authors: JS
authors: Kim
mesh_terms: D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000378:metabolism; D017667:Adipocytes / Q000187:drug effects*; D000273:Adipose Tissue / Q000187:drug effects; D000818:Animals; D019440:Anti-Obesity Agents / Q000494:pharmacology*; D005990:Glycerol / Q000032:analysis; D008049:Lipase / Q000037:antagonists & inhibitors*; D008066:Lipolysis / Q000187:drug effects*; D008297:Male; D053978:Pentacyclic Triterpenes; D010727:Phosphoric Diester Hydrolases / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D014280:Triglycerides / Q000097:blood; D014315:Triterpenes / Q000494:pharmacology*; D000094062:Betulinic Acid
chemical_list: D019440:Anti-Obesity Agents; D053978:Pentacyclic Triterpenes; D014280:Triglycerides; D014315:Triterpenes; D008049:Lipase; D010727:Phosphoric Diester Hydrolases; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D005990:Glycerol; D000094062:Betulinic Acid