Relative induction of mRNA for HMG CoA reductase and LDL receptor by five different HMG-CoA reductase inhibitors in cultured human cells.
Relative induction of mRNA for HMG CoA reductase and LDL receptor by five different HMG-CoA reductase inhibitors in cultured human cells.
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在培养的人类细胞中，五种不同的 HMG-CoA 还原酶抑制剂对 HMG CoA 还原酶和 LDL 受体 mRNA 的相对诱导。
DOI：
10.5551/jat1994.7.138
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发表时间：
2000
影响因子：
4.4
通讯作者：
Y. Saito
中科院分区：
文献类型：
--
作者：
S. Morikawa;M. Umetani;S. Nakagawa;H. Yamazaki;H. Suganami;K. Inoue;M. Kitahara;T. Hamakubo;T. Kodama;Y. Saito
用核糖核酸酶保护试验定量测定了不同的3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶抑制剂对培养的人肝癌细胞系Hep G2中HMG-CoA还原酶和低密度脂蛋白（LDL）受体mRNA的诱导作用。包括美伐他汀、辛伐他汀、阿托伐他汀和NK-104在内的亲脂性抑制剂能够增加HMG-CoA还原酶和LDL受体的mRNA水平，但亲水性抑制剂普伐他汀在Hep G2细胞中无效，如先前报道的。在亲脂性抑制剂中，NK-104在0.1至10 μ M之间最有效地诱导LDL受体mRNA，而这些抑制剂对HMG-CoA还原酶mRNA的诱导程度彼此没有显著差异。当细胞用每种抑制剂的IC 50浓度的200倍过量处理时，NK-104能够最有效地诱导LDL受体mRNA。这些结果表明，HMG-CoA还原酶抑制剂对还原酶和LDL受体的mRNA上调的作用彼此不同，并且在这些亲脂性抑制剂之间不同。NK-104对Hep G2细胞LDL受体mRNA的诱导作用最强。
The effect of various 3-hydroxy-3 methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors on the induction of HMG-CoA reductase and low density lipoprotein (LDL) receptor mRNA were quantitatively determined in the cultured human hepatoma cell line Hep G2 by means of a ribonuclease protection assay. Lipophilic inhibitors including mevastatin, simvastatin, atorvastatin and NK-104 were able to increase the levels of mRNAs for HMG-CoA reductase and the LDL receptor, but the hydrophilic inhibitor pravastatin was not effective in Hep G2 cells as had previously been reported. The LDL receptor mRNA was induced by NK-104 most effectively between 0.1 to 10 microM among the lipophilic inhibitors, whereas the degrees of induction of HMG-CoA reductase mRNA by these inhibitors did not differ significantly from each other. When cells were treated with a 200-fold excess of the IC50 concentration of each inhibitor, NK-104 was able to induce LDL receptor mRNA most effectively. These results indicate that the effect of HMG-CoA reductase inhibitors on the upregulation of mRNA for reductase and LDL receptor are different from each other and among these lipophilic inhibitors. NK-104 is most effective in inducing LDL receptor mRNA in Hep G2 cells.
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影响因子：
10.5
作者：
Kim, JB;Spiegelman, BM
通讯作者：
Spiegelman, BM
影响因子：
--
作者：
J. Goldstein;S. Basu;Michael S. Brown
通讯作者：
J. Goldstein;S. Basu;Michael S. Brown
DOI：
10.1073/pnas.95.11.5987
发表时间：
1998-05-26
影响因子：
11.1
作者：
Horton, JD;Bashmakov, Y;Shimano, H
通讯作者：
Shimano, H
影响因子：
56.9
作者：
BROWN, MS;GOLDSTEIN, JL
通讯作者：
GOLDSTEIN, JL
影响因子：
15.9
作者：
Horton, JD;Shimomura, I;Shimano, H
通讯作者：
Shimano, H