caa a22 4500 46576682X CHVBK 20180323111916.0 cr unu---uuuuu 170327e19901101xx s 000 0 eng 10.1007/BF02544034 doi (NATIONALLICENCE)springer-10.1007/BF02544034 Comparison of the effect of six compactin-related compounds on cholesterol synthesis in five human cell types [Elektronische Daten] [D. Sviridov, A. Endo, M. Pavlov, V. Repin, V. Smirnov] We have investigated the effect of six compactin-related compounds—mevinolin, compactin, ML-236A, monacolin X, monacolin L and dihydromonacolin L—on cholesterol synthesis in human umbilical vein endothelial cells, human small intestine epithelial cells, human hepatoma cell line HEP G2, normal human skin fibroblasts and in skin fibroblasts from a patient with familial homozygous hypercholesterolemia. The inhibition of cholesterol synthesis was found to depend on both the cell type and the type of compound used. The most effective compounds were mevinolin and compactin. Monacolin X, monacolin L and ML-236A were less effective, and dihydromonacolin L was the least efficacious. Endothelial and epithelial cells were sensitive to very low concentrations of inhibitors (IC50=1.0-30 pg/mL), HEP G2 cells required higher concentrations (IC50=0.01-66 ng/mL) and fibroblasts needed even higher concentrations (IC50=0.1-200 ng/mL). Lactone and acid forms of the inhibitors were equally active. None of the inhibitors had any effect on either protein or fatty acid synthesis in any of the cell types studied. It can be concluded that different compactin-related compounds show a range of potencies as cholesterol synthesis inhibitors and a dose-dependent tissue-selectivity. American Oil Chemists' Society, 1985 Sviridov D. Institute of Experimental Cardiology, National Cardiology Research Center, 3rd Cherepkovskaya st. 15, 121552, Moscow, USSR aut Endo A. Department of Agricultural and Biological Chemistry, Tokyo Noko University, 183, Tokyo, Japan aut Pavlov M. Institute of Experimental Cardiology, National Cardiology Research Center, 3rd Cherepkovskaya st. 15, 121552, Moscow, USSR aut Repin V. Institute of Experimental Cardiology, National Cardiology Research Center, 3rd Cherepkovskaya st. 15, 121552, Moscow, USSR aut Smirnov V. Institute of Experimental Cardiology, National Cardiology Research Center, 3rd Cherepkovskaya st. 15, 121552, Moscow, USSR aut Lipids Springer-Verlag 25/11(1990-11-01), 685-690 0024-4201 25:11<685 1990 25 11745 https://doi.org/10.1007/BF02544034 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF02544034 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Sviridov D. Institute of Experimental Cardiology, National Cardiology Research Center, 3rd Cherepkovskaya st. 15, 121552, Moscow, USSR aut NATIONALLICENCE 700 1- Endo A. Department of Agricultural and Biological Chemistry, Tokyo Noko University, 183, Tokyo, Japan aut NATIONALLICENCE 700 1- Pavlov M. Institute of Experimental Cardiology, National Cardiology Research Center, 3rd Cherepkovskaya st. 15, 121552, Moscow, USSR aut NATIONALLICENCE 700 1- Repin V. Institute of Experimental Cardiology, National Cardiology Research Center, 3rd Cherepkovskaya st. 15, 121552, Moscow, USSR aut NATIONALLICENCE 700 1- Smirnov V. Institute of Experimental Cardiology, National Cardiology Research Center, 3rd Cherepkovskaya st. 15, 121552, Moscow, USSR aut NATIONALLICENCE 773 0- Lipids Springer-Verlag 25/11(1990-11-01), 685-690 0024-4201 25:11<685 1990 25 11745 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer