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-1-¹⁴CのCholesterolへの取込みにおよぼす影響

抄録

The effects of several benzoquinone and naphthoquinone derivatives on the incorporation of acetate-1-¹⁴C into cholesterol have been examined in rat liver homogenates. Within the test compounds, vitamin K₃, 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^-3M) 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-1-¹⁴C into cholesterol as well as mechanisms of the inhibition are discussed.