Studies on Hypolipidemic Agents. IV. Influence of a New Hypolipidemic Agent, 5-Tridecylpyrazole-3-carboxylic Acid, on Cholesterol Metabolism in Rats

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The comparative effects of 5-tridecylpyrazole-3-carboxylic acid (TDPC) and clofibrate or β-sitosterol on cholesterol (CH) metabolism were investigated in normal and hyperlipidemic rats. The present study demonstrated that TDPC possesses a potent hypocholesterolemic activity in both types of rats, and also improves the α/β-lipoprotein ratio and anti-atherogenic index in hyperlipidemic rats. Although TDPC at 0.3% caused an increase of liver weight in both types of rats, the adverse effect of TDPC was less than that of clofibrate in normal rats. TDPC, like clofibrate, remarkably suppressed sterol biosynthesis from [^<14>C] acetate. Dual-isotope experiments suggested that TDPC (300 mg/kg) and β-sitosterol (100 mg/kg) inhibit the intestinal absorption of CH, though the effect was not statistically significant. It is apparent from the data presented that TDPC, unlike clofibrate, exerts its hypocholesterolemic effect by multiple modes of action, including the inhibition of both synthesis and absorption of CH.
社団法人日本薬学会の論文
1985-11-25