The hypolipidemic action of the ACAT inhibitor HL-004 in hamsters fed normal chow.
1. A novel ACAT (acyl-CoA: cholesterol acyltransferase) inhibitor, HL-004, exhibited a strong inhibitory effect on the hepatic and intestinal ACAT, but was less effective on the adrenal ACAT in vitro. 2. HL-004 selectively decreased serum VLDL cholesterol, and inhibited hepatic ACAT activity in hamsters fed normal chow. 3. These results suggest that the cholesterol-lowering effect of HL-004 can be attributed to a decrease in hepatic VLDL secretion via inhibition of ACAT.
Murakami
S
S
Medicinal Research Laboratories, Taisho Pharmaceutical Co., Ltd., Saitama, Japan.
Ohta
Y
Y
Asami
Y
Y
Yamagishi
I
I
Toda
Y
Y
Sato
M
M
Tomisawa
K
K
D000083:Acetanilides / Q000494:pharmacology*; D000813:Anilides / Q000494:pharmacology; D000818:Animals; D000924:Anticholesteremic Agents / Q000494:pharmacology*; D002784:Cholesterol / Q000097:blood; D002788:Cholesterol Esters / Q000097:blood; D006224:Cricetinae; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D066298:In Vitro Techniques; D008074:Lipoproteins / Q000097:blood; D008297:Male; D008647:Mesocricetus; D008862:Microsomes, Liver / Q000201:enzymology / Q000378:metabolism; D017035:Pravastatin / Q000494:pharmacology; D011817:Rabbits; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors*
D000083:Acetanilides; D000813:Anilides; D000924:Anticholesteremic Agents; D002788:Cholesterol Esters; D004791:Enzyme Inhibitors; C092284:HL 004; D008074:Lipoproteins; C069304:PD 128042; D002784:Cholesterol; D002785:Sterol O-Acyltransferase; D017035:Pravastatin