Hypolipidemic activity of tetrakis-mu-(trimethylamine-boranecarboxylato)-bis(trimethylamin e- carboxyborane)-dicopper(II) in rodents and its effect on lipid metabolism.

A binuclear copper(II) complex was shown to have potent hypolipidemic activity in rats and mice at low doses, i.e., 2.5-10 mg/kg/d. The agent moderately lowered liver ATP-dependent citrate lyase, acetyl CoA synthetase, and phosphatidate phosphohydrolase activities in vivo. The appetite of the animal was reduced by drug treatment, and orally administered cholesterol absorption from the intestine was markedly lowered. Higher lipid levels were found in the chyme and the feces, indicating accelerated excretion of lipids by the drug, probably via the biliary route. Organs, e.g., liver and small intestine, as well as serum lipoprotein levels, demonstrated lower lipid content after drug administration. Thus, this chemical class of agents may have potential as a hypolipidemic agent in humans.

[1]  I. Hall,et al.  Antihyperlipidemic activity of saccharin analogues in rodents. , 1983, Journal of pharmaceutical sciences.

[2]  I. Hall,et al.  Antihyperlipidemic activity of phthalimide analogues in rodents. , 1983, Journal of pharmaceutical sciences.

[3]  A. McPhail,et al.  Antihyperlipidemic activity of amine cyanoboranes, amine carboxyboranes, and related compounds. , 1981, Journal of pharmaceutical sciences.

[4]  I. Hall,et al.  Boron betaine analogs: antitumor activity and effects on Ehrlich ascites tumor cell metabolism. , 1979, Journal of pharmaceutical sciences.

[5]  C. Rozé,et al.  Action of tiadenol and clofibrate on biliary excretions of cholesterol and bile salts in rats. , 1979, Digestion.

[6]  C. Shively,et al.  A sensitive gas-chromatographic assay using a nitrogen-phosphorus detector for determination of antipyrine and aminopyrine in biological fluids. , 1979, Pharmacology.

[7]  R. Mavis,et al.  Pulmonary surfactant synthesis. A highly active microsomal phosphatidate phosphohydrolase in the lung. , 1978, Journal of lipid research.

[8]  O. Wieland,et al.  Measurement of ATP citrate-lyase and acetyl-CoA synthetase activity using arylamine acetyltransferase. , 1978, Analytical biochemistry.

[9]  C. Piantadosi,et al.  Hypolipidemic activity of in vitro inhibitors of hepatic and intestinal sn-glycerol-3-phosphate acyltransferase and phosphatidate phosphohydrolase. , 1977, Atherosclerosis.

[10]  D. Kritchevsky,et al.  The influence of 1,1-bis(4'-(1"-carboxy-1"-methylpropoxy)-phenyl)cyclohexane (a new aryloxy compound, S-8527) on cholesterol metabolism in rats. , 1973, Atherosclerosis.

[11]  G. R. Williams,et al.  The sensitivity of dicarboxylate anion exchange reactions o transport inhibitors in rat-liver mitochondria. , 1970, Biochimica et biophysica acta.

[12]  G. R. Williams,et al.  The effects of 2-ethylcitrate and tricarballylate on citrate transport in rat liver mitochondria and fatty acid synthesis in rat white adipose tissue. , 1970, European journal of biochemistry.

[13]  J. Lowenstein,et al.  Effects of magnesium ions, adenosine triphosphate, palmitoylcarnitine, and palmitoyl coenzyme A on acetyl coenzyme A carboxylase. , 1968, The Journal of biological chemistry.

[14]  A. C. Peacock,et al.  EVALUATION OF A RECENTLY REPORTED STABLE LIEBERMANN-BURCHARD REAGENT AND ITS USE FOR THE DIRECT DETERMINATION OF SERUM TOTAL CHOLESTEROL. , 1964, Clinica chimica acta; international journal of clinical chemistry.

[15]  J. Thorp,et al.  Modification of Metabolism and Distribution of Lipids by Ethyl Chlorophenoxyisobutyrate , 1962, Nature.

[16]  R. Brady,et al.  Biosynthesis of Fatty Acids I. STUDIES WITH ENZYMES OBTAINED FROM LIVER , 1960 .

[17]  J. Folch,et al.  A simple method for the isolation and purification of total lipides from animal tissues. , 1957, The Journal of biological chemistry.

[18]  R. Havel,et al.  The distribution and chemical composition of ultracentrifugally separated lipoproteins in human serum. , 1955, The Journal of clinical investigation.

[19]  O. H. Lowry,et al.  Protein measurement with the Folin phenol reagent. , 1951, The Journal of biological chemistry.

[20]  J. H. Bragdon Colorimetric determination of blood lipides. , 1951, The Journal of biological chemistry.

[21]  F. Wilcoxon,et al.  A simplified method of evaluating dose-effect experiments. , 1948, The Journal of pharmacology and experimental therapeutics.

[22]  E. Hendry,et al.  The phospholipins of blood. , 1935, The Biochemical journal.