Breslow J L, Lothrop D A, Spaulding D R, Kandutsch A A
Biochim Biophys Acta. 1975 Jul 22;398(1):10-7. doi: 10.1016/0005-2760(75)90165-4.
In human fibroblasts two oxidized derivatives of cholesterol, 7-ketocholesterol and 25-hydroxycholesterol, but not cholesterol itself, are potent inhibitors of 3-hydroxy-3-methylglutaryl co-enzyme A reductase (mevalonate: NADP+ oxidoreductase (Co-enzyme A acylating), (EC 1.1.1.34), the rate-limiting enzyme in sterol biosynthesis. In addition, these derivatives of cholesterol are effective regulators in cells from homozygous familial hypercholesterolemic individuals. The differences in the inhibitory potencies of the sterols cannot be explained in terms of the amount of uptake into the cell.
在人成纤维细胞中，胆固醇的两种氧化衍生物，7-酮胆固醇和25-羟基胆固醇，而非胆固醇本身，是3-羟基-3-甲基戊二酰辅酶A还原酶（甲羟戊酸：NADP+氧化还原酶（辅酶A酰化），（EC 1.1.1.34），固醇生物合成中的限速酶）的有效抑制剂。此外，这些胆固醇衍生物在纯合子家族性高胆固醇血症个体的细胞中是有效的调节剂。这些固醇抑制效力的差异不能用细胞摄取量来解释。
