Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: EC:6.2.1.1 (ACS)
 78,556 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Small molecular weight aliphatic dicarboxylic acids, i.e. dimethylmalonic acid, diethylmalonic acid and maleic acid, afford greater than 35% reduction in serum cholesterol and triglycerides levels in CF1 mice at 20 mg/kg/day, i.p. Furthermore, these agents lowered greater than 40% serum cholesterol levels in rat after oral administration at 20 mg/kg/day. Dimethylmalonic and diethylmalonic acids lowered rat serum triglyceride levels by at least 23%. Rat tissue lipids, e.g. liver, small intestinal mucosa and aorta wall, were reduced in concentration and fecal lipids were elevated by dimethyl- and diethylmalonic acids. Rat serum lipoproteins after 14 days of treatment demonstrated reduction of VLDL and LDL cholesterol levels with elevated HDL cholesterol levels by dimethylmalonic and maleic acids. The agents also inhibited de novo hepatic enzyme activities, specifically mitochondrial citrate exchange, acetyl-CoA synthetase, ATP-dependent citrate lyase, acyl-CoA:cholesterol acyltransferase, cholesterol-7 alpha-hydroxyase, sn-glycerol-3-phosphate acyltransferase and phosphatidate phosphohydrolase, which would result in the reduction of de novo synthesis of fatty acids, cholesterol and triglycerides.
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PMID:Hypolipidemic activity of aliphatic dicarboxylic acids in rodents. 179 8

Significant hypolipidemic activity was demonstrated by 6-ethoxycarbonyl-1-3-phenyl-1,3,5-triazabicyclo[3.1.0]hexane-2,4-dione, 2-ethoxycarbonyl-5-phenyl-1,3,5-triazine-4,6(1H,5H)-dione and 2-ethoxycarbonyl-5-(4-chlorophenyl)-1,3,5-triazine-4,6(1H,5H)-dione in rodents at 20 mg/kg/day. These agents lowered serum cholesterol and triglyceride levels by approximately 40% in mice after 16 d. Tissue lipids in rat liver, small intestinal mucosa, aortic wall and feces were reduced by treatment with the agents. Very low density lipoprotein (VLDL) and low density lipoprotein (LDL) cholesterol levels were reduced in the rat; high density lipoprotein (HDL) cholesterol levels were elevated after 14 d of treatment. The activities of regulatory enzymes, e.g., acetyl-CoA synthetase, acyl-CoA:cholesterol acyltransferase, cholesterol 7 alpha-hydroxylase, sn-glycerol-3-phosphate acyltransferase, phosphatidylate phosphohydrolase and heparin-induced lipoprotein lipase, involved in de novo synthesis of hepatic lipids were affected by the agents. The new compounds may represent another class of potentially useful hypolipidemic agents for the treatment of atherosclerosis since HDL cholesterol levels were increased and VLDL and LDL cholesterol levels were lowered by some of the agents.
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PMID:Hypolipidemic activity of 6-alkoxycarbonyl-3-aryl-1,3,5- triazabicyclo[3.1.0]hexane-2,4-diones and 2-alkoxycarbonyl-5-aryl-1,3,5-triazine-4,6(1H,5H)-diones in rodents. 846 53

Adipose tissue fatty acid storage varies according to sex, adipose tissue depot and degree of fat gain. However, the mechanism(s) for these variations is not completely understood. We recently published findings based on the glycerol 3-phosphate acyltransferase (GPAT) enzyme activity assay we optimized for use with human adipose tissue. These findings include a decrease in total GPAT and GPAT1 as a function of adipocyte size in both omental and subcutaneous adipose tissue and a strong, positive correlations between ACS, GPAT, and DGAT activities for both sexes and depots and between these storage factors and palmitate storage rates into TAG. The aim of this commentary is to expand upon the data from our recent publication. We describe here additional details on the optimization of the GPAT enzyme activity assay, a correlation between DGAT and percentage palmitate in the diacylglycerol fraction, and sex differences in fatty acid storage factors and storage rates into TAG at high palmitate concentrations.
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PMID:More insights into a human adipose tissue GPAT activity assay. 2714 1