Effect of ER ligands on ACAT activity measured in rat peritoneal macrophages stimulated with acLDLs
Rat peritoneal macrophages were preincubated with compounds and then allowed to convert into foam cells by 15-h incubation with 100 μg/ml acLDL. Cellular lipids and cholesteryl ester amounts were determined by following the incorporation of 14C-labeled oleic acid into cholesteryl esters as described under Materials and Methods. Values are the average of three experiments ± S.E.M., each carried out in duplicate.
Compound | Percentage of ACAT Inhibition in Rat Peritoneal Macrophage Stimulated with acLDLs (at the Indicated Concentration of Compound) | ||
|---|---|---|---|
| 5 μM | 10 μM | ||
| Sah 58-035 | 31.5 ± 2.7 | 64.1 ± 4.6 | |
| Tamoxifen | 42.6 ± 3.5 | 92.3 ± 6.4 | |
| CI-628 | 48.3 ± 2.7 | 84.8 ± 4.1 | |
| ICI 164,384 | 21.3 ± 4.8 | 34.2 ± 7.8 | |
| OH-Tamoxifen | 6.4 ± 4.8 | 22.2 ± 5.4 | |
| Raloxifene | 8.4 ± 7.5 | 26.8 ± 4.3 | |