SXR binding constants for tocopherols and tocotrienols
Ki and ± 95% confidence interval (95% CI) values were determined by nonlinear regression using the Cheng-Prussoff equation from eight-point curves performed in triplicate; for competitive ligands, the Ki = Kd. Assays were performed at constant 3H-SR12813 concentration [50 nM; Kd = 40 nM (Jones et al., 2000)]. Total specific binding was determined as the counts displaced by 10 μM clotrimazole.
Compound | Ki | 95% CI | |
---|---|---|---|
μM | |||
α-Tocopherol | NB | NB | |
β-Tocopherol | NB | NB | |
γ-Tocopherol | NB | NB | |
δ-Tocopherol | NB | NB | |
α-Tocotrienol | 8.0 | 5.2-12.0 | |
β-Tocotrienol | 6.4 | 4.6-9.0 | |
γ-Tocotrienol | 7.1 | 3.9-13.0 | |
δ-Tocotrienol | 4.9 | 2.5-9.6 | |
Clotrimazole | 0.79 | 0.62-1.0 |
NB, no specific binding.