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美维诺林:萝卜植物微粒体3-羟基-3-甲基戊二酰辅酶A还原酶的一种高度特异性抑制剂。

Mevinolin: a highly specific inhibitor of microsomal 3-hydroxy-3-methylglutaryl-coenzyme A reductase of radish plants.

作者信息

Bach T J, Lichtenthaler H K

出版信息

Z Naturforsch C Biosci. 1982 Jan-Feb;37(1-2):46-50. doi: 10.1515/znc-1982-1-209.

DOI:10.1515/znc-1982-1-209
PMID:6917646
Abstract

The fungal metabolite mevinolin, known to be a potent hypocholesterolemic agent, exerts in vitro a strong inhibitory effect on microsomal HMG-CoA reductase from etiolated radish seedlings at a concentration of about three magnitudes lower than the Km towards the natural substrate (S)-HMG-CoA (I50 = 2.5 x 10(-9)M). Beside this, mevinolin significantly inhibits the root elongation of radish as well as of wheat seedlings already at low concentrations of 10 to 100 ppb (= 2.5 x 10(-8) to 2.5 x 10(-7)M).

摘要

真菌代谢产物美伐他汀是一种有效的降胆固醇药物,在体外,它对黄化萝卜幼苗微粒体HMG-CoA还原酶具有很强的抑制作用,其浓度比天然底物(S)-HMG-CoA的Km低约三个数量级(I50 = 2.5×10^(-9)M)。除此之外,美伐他汀在10至100 ppb(= 2.5×10^(-8)至2.5×10^(-7)M)的低浓度下就能显著抑制萝卜和小麦幼苗的根伸长。

相似文献

1
Mevinolin: a highly specific inhibitor of microsomal 3-hydroxy-3-methylglutaryl-coenzyme A reductase of radish plants.美维诺林:萝卜植物微粒体3-羟基-3-甲基戊二酰辅酶A还原酶的一种高度特异性抑制剂。
Z Naturforsch C Biosci. 1982 Jan-Feb;37(1-2):46-50. doi: 10.1515/znc-1982-1-209.
2
Mechanisms of inhibition by mevinolin (MK 803) of microsome-bound radish and of partially purified yeast HMG-CoA reductase (EC.1.1.1.34).美伐他汀(MK 803)对微粒体结合的萝卜和部分纯化的酵母HMG-CoA还原酶(EC.1.1.1.34)的抑制机制。
Z Naturforsch C Biosci. 1983 Mar-Apr;38(3-4):212-9. doi: 10.1515/znc-1983-3-410.
3
Mevinolin: a highly potent competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase and a cholesterol-lowering agent.美伐他汀:一种高效的羟甲基戊二酰辅酶A还原酶竞争性抑制剂及降胆固醇药物。
Proc Natl Acad Sci U S A. 1980 Jul;77(7):3957-61. doi: 10.1073/pnas.77.7.3957.
4
The effect of cholestyramine and Mevinolin on the diurnal cycle of rat hepatic 3-hydroxy-3-methylglutaryl coenzyme A reductase.消胆胺和洛伐他汀对大鼠肝脏3-羟基-3-甲基戊二酰辅酶A还原酶昼夜周期的影响。
J Lipid Res. 1982 Sep;23(7):1026-31.
5
Monacolin K, a new hypocholesterolemic agent that specifically inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase.莫纳可林K,一种新型降胆固醇药物,它能特异性抑制3-羟基-3-甲基戊二酰辅酶A还原酶。
J Antibiot (Tokyo). 1980 Mar;33(3):334-6. doi: 10.7164/antibiotics.33.334.
6
Rapid and substantial lowering of human serum cholesterol by mevinolin (MK-803), an inhibitor of hydroxymethylglutaryl-coenzyme A reductase.
Atherosclerosis. 1982 Jan;41(1):61-5. doi: 10.1016/0021-9150(82)90070-3.
7
Hydroxymethylglutaryl-coenzyme A reductase-containing hepatocytes are distributed periportally in normal and mevinolin-treated rat livers.
Proc Natl Acad Sci U S A. 1984 Sep;81(17):5556-60. doi: 10.1073/pnas.81.17.5556.
8
Suppression of murine neuroblastoma growth in vivo by mevinolin, a competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase.洛伐他汀(一种3-羟基-3-甲基戊二酰辅酶A还原酶的竞争性抑制剂)对小鼠神经母细胞瘤体内生长的抑制作用
J Clin Invest. 1985 Nov;76(5):1748-54. doi: 10.1172/JCI112165.
9
Inhibition of degradation of 3-hydroxy-3-methylglutaryl coenzyme A reductase by mevinolin.
J Biol Chem. 1983 Jul 25;258(14):8547-9.
10
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 4. Side chain ester derivatives of mevinolin.
J Med Chem. 1986 May;29(5):849-52. doi: 10.1021/jm00155a040.

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