Cholesterol生合成の阻害物質に関する研究(第2報) : BenzoquinoneならびにNaphthoquinone誘導体のラット肝無細胞系におけるAcetate-1-^<14>CのCholesterolへの取込みにおよぼす影響

概要

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The effects of several benzoquinone and naphthoquinone derivatives on the incorporation of acetate-1-^<14>C into cholesterol have been examined in rat liver homogenates. Within the test compounds, vitamin K_3,tauranin, acetylmaesaquinone, 2-methyl-3,6-dibromo- 1,4-benzoquinone, ubiquinone-0 (UQ-0) showed potent inhibitory action. Furthermore, the inhibition by 2-methyl-3,6-dibromo-1,4-benzoquinone was not affected in the presence of cysteine (5×10^<-5>-5×10^<-3>M) or ATP (10^<-4>-10<-3>M). In the case of ubiquinone-0 (UQ-0), the inhibition was not affected by ATP addition, but it was restored considerably by cysteine. On the basis of the present experiments, structure activity relationship between quinone derivatives and their effects on the incorporation of acetate-1-^<14>C into cholesterol as well as mechanisms of the inhibition are discussed.
公益社団法人日本薬学会の論文
1970-04-25