The Hypolipidemic Activity of Furoic Acid and Furylacrylic Acid Derivatives in Rodents |
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Authors: | Hall Iris H. Williams Jr Wallace L. Rhyne Kathryn A. Knowles Margaret |
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Affiliation: | (1) Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill, N.C, 27514 |
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Abstract: | 2-Furoic acid, 3-furoic acid, 3,4-furan dicarboxylic acid and furyl-acrylic acid were evaluated for hypolipidemic activity in mice and rats. 2-Furoic acid was the most potent agent of the four tested, lowering serum cholesterol levels 41 % and serum triglyceride levels 56 % at 20 mg/kg/day in mice and serum cholesterol 50 % and serum triglyceride levels 42 % in rats. 2-Furoic acid effectively suppressed liver mitochondrial citrate exchange, ATP dependent citrate lyase, acetyl CoA synthetase, acyl CoA cholesterol acyl transferase, sn-glycerol-3-phosphate acyl transferase, phosphatidate phosphohydrolase and hepatic lipoprotein lipase enzymatic activities. Lipid levels after 16 days in mice were reduced in the liver. In the rat cholesterol content of the HDL fraction was elevated and lowered in the chylomicron fraction. 2-Furoic acid administration for 14 days resulted in a large portion of 3H-cholesterol being excreted by the biliary route. The furoic acid derivatives appear to have promise as hypolipidemic agents and further studies on their ability to lower lipids are warranted. |
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