Enterostatin reduces serum cholesterol levels by way of a CCK(1) receptor-dependent mechanism.
Enterostatin (APGPR), an anorectic pentapeptide derived from the amino terminus of procolipase, significantly reduced serum cholesterol levels after oral administration at a dose of 100 mg/kg for 3 days in mice fed a high-cholesterol-cholic acid diet. The hypocholesterolemic effect of APGPR was inhibited by pretreatment with lorglumide, an antagonist for cholecystokinin 1 (CCK(1)) receptor, even though APGPR does not have any affinity for CCK(1) receptors. Similarly, the hypocholesterolemic activity of VPDPR, an APGPR analogue, was blocked by lorglumide. These results suggest that the hypocholesterolemic effects of APGPR and VPDPR are mediated by a CCK(1) receptor-dependent mechanism.
Takenaka
Yasuyuki
Y
Division of Food Science and Biotechnology, Graduate School of Agriculture, Kyoto University, Gokasho Uji, Kyoto 611-0011, Japan.
Shimano
Tomoko
T
Mori
Takaaki
T
Hou
I-Ching
IC
Ohinata
Kousaku
K
Yoshikawa
Masaaki
M
D000818:Animals; D019742:Chemokines, CC; D002784:Cholesterol / Q000097:blood*; D003089:Colipases / Q000494:pharmacology*; D004792:Enzyme Precursors / Q000494:pharmacology*; D008297:Male; D051379:Mice; D009842:Oligopeptides / Q000494:pharmacology; D010446:Peptide Fragments / Q000494:pharmacology*; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors / Q000378:metabolism*
C511142:Ccl28 protein, mouse; D019742:Chemokines, CC; D003089:Colipases; D004792:Enzyme Precursors; D009842:Oligopeptides; D010446:Peptide Fragments; D011949:Receptors, Cholecystokinin; C107385:valyl-prolyl-aspartyl-prolyl-arginine; C037107:procolipase; D002784:Cholesterol