IC50 values and minimum inhibitory concentration (MIC) for the inhibition of human liver cytosolic lithocholic acid (LCA) sulfonation by selective estrogen receptor modulator (SERMs)
Data are expressed as mean ± S.E.M. of three to four independent experiments conducted in duplicate.
| Chemical Class | Chemical | IC50 (µM) | IC50 (µM) | IC50 (µM) | MIC (µM) | MIC (µM) | MIC (µM) |
|---|---|---|---|---|---|---|---|
| LCA Sulfonation | GLCA Sulfonation | TLCA Sulfonation | LCA Sulfonation | GLCA Sulfonation | TLCA Sulfonation | ||
| Triphenylethylene | Clomifene | 3.2 ± 0.5 | 3.6 ± 0.3 | 1.5 ± 0.2 | 3 | 1 | 0.3 |
| Triphenylethylene | Tamoxifen | 16.3 ± 5.3 | 13.7 ± 1.6 | 10.1 ± 0.8 | 10 | 30 | 30 |
| Triphenylethylene | Toremifene | 9.2 ± 5.3 | 11.0 ± 1.2 | 3.2 ± 1.1 | 10 | 3 | 3 |
| Triphenylethylene | Ospemifene | 3.0 ± 0.2 | 2.55 ± 0.02 | 2.3 ± 0.4 | 10 | 3 | <0.1 |
| Triphenylethylene | Droloxifene | 1.5 ± 0.2 | 1.5 ± 0.1 | 0.75 ± 0.01 | 1 | 1 | 0.1 |
| Benzothiophene | Raloxifene | 0.28 ± 0.04 | 0.41 ± 0.03 | 0.18 ± 0.02 | 0.1 | 0.3 | 0.1 |
| Benzothiophene | Arzoxifene | 0.29 ± 0.04 | 0.20 ± 0.01 | 0.08 ± 0.01 | 0.3 | 0.1 | 0.01 |
| Tetrahydronaphthale | Lasofoxifene | 1.0 ± 0.1 | 0.50 ± 0.01 | 0.25 ± 0.01 | 0.3 | 0.1 | <0.01 |
| Tetrahydronaphthale | Nafoxidine | 12.2 ± 2.1a | 6.6 ± 5.2a | 1.4 ± 0.7a | 100 | >100 | 10 |
| Indole | Bazedoxifene | 0.21 ± 0.03 | 0.29 ± 0.01 | 0.13 ± 0.02 | 0.03 | 0.1 | 0.3 |
| Benzopyran | Acolbifene | 12.9 ± 3.2 | 10.1 ± 0.7 | 7.0 ± 0.3 | 10 | 10 | 3 |
GLCA, glycolithocholic acid; TLCA, taurolithocholic acid.
↵a Complete inhibition was not reached (Figs. 5–7).