Studies on Hypolipidemic Agents. V. : Influence of 5-Tridecylpyrazole-3-carboxylic Acid, a New Hypolipidemic Agent, on Intestinal Cholesterol Absorption in Rats
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概要
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In order to clarify the inhibitory mechanism of 5-tridecylpyrazole-3-carboxylic acid (TDPC) on the absorptive process of cholesterol, the effects of this agent on micelle in vitro and intestinal uptake of cholesterol in rats as measured by the ligated-loop method in situ were investigated using β-sitosterol as a reference agent.TDPC did not affect the micellar formation of distribution of micellar size, both of which are important determinants in the process of cholesterol uptake, but β-sitosterol increased the distribution of large-size micelles (>450nm).TDPC significantly decreased the intestinal cholesterol uptake by 27%, 44% and 59% at the dose levels of 0.25,0.50 and 1.0mg, respectively. Similarly, β-sitosterol significantly decreased the cholesterol uptake by 79% at the dose of 1.0mg.It is apparent from the above data that the hypocholesterolemic activity of TDPC and β-sitosterol partly depends on interference with intestinal cholesterol uptake, though there is a difference between the two agents in terms of the effect on micellar size. It can be assumed that both energy-dependent and -independent systems are involved in the process of the intestinal cholesterol uptake, and hte inhibitory effect of TDPC might berelated to the energy-independent system rather than the energy-dependent system.
- 公益社団法人日本薬学会の論文
- 1988-03-25
著者
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渡辺 隆史
東京薬学大学薬学部臨床生化学教室
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渡辺 隆史
Department of Clinical Biochemistry, Tokyo College of Pharmacy
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須賀 哲弥
Department of Clinical Biochemistry, Tokyo College of Pharmacy
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釈 邦夫
Department Of Development Morishita Pharmaceutical Co. Ltd.
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須賀 哲弥
Department Of Clinical Biochemistry Tokyo College Of Pharmacy
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