Tolbutamide hydroxylation by human liver microsomes: Kinetic characterisation and relationship to other cytochrome P-450 dependent xenobiotic oxidations
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Cited by (214)
Inhibitory effects of cytochrome P450 enzymes CYP2C8, CYP2C9, CYP2C19 and CYP3A4 by Labisia pumila extracts
2012, Journal of EthnopharmacologyCitation Excerpt :All the extracts were kept at 4 °C until further use. High-performance liquid chromatography (HPLC) method was employed to establish enzyme assays, namely tolbutamide 4-methyhydroxylase, S-mephenytoin 4-hydroxylase and testosterone 6β-hydroxylase assays (activity markers of CYP2C9, CYP2C19 and CYP3A4, respectively) in accordance to reported methods (Miners et al., 1988; Wang et al., 1997; Wrighton et al., 1993). The details of all the three HPLC methods have been described in our earlier published papers (Pan et al., 2010, 2011).
1,1-Diarylalkenes as anticancer agents: Dual inhibitors of tubulin polymerization and phosphodiesterase 4
2011, Bioorganic and Medicinal ChemistryDiscovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancer
2011, Bioorganic and Medicinal ChemistryCitation Excerpt :The concentration of the substrate was referenced from the data sheet from GENTEST Corp. (7-ethoxyresorufin O-deethylation for CYP1A2, coumarin 7-hydroxylation for CYP2A6, S-(+)-mephenytoin 4′-hydroxylation for CYP2C19, (±)-bufuralol 1′-hydroxylation for CYP2D6, 4-nitrophenol hydroxylation for CYP2E1 and testosterone 6β-hydroxylation activity for CYP3A4) or the published reports (ethoxycoumarin O-deethylation for CYP2B6 and tolbutamide hydroxylation for CYP2C8 and 2C9) 62,63 with slight modifications. The marker reactions specific for CYP isoforms other than CYP3A4 were measured according to published analytical methods62,64–68 with slight modifications. Testosterone 6β-hydroxylation activity for CYP3A4 was analyzed using the following HPLC conditions: column, Inertsil ODS-2 (150 × 4.6 mm I.D.; GL Science, Tokyo, Japan); detection wavelength, 254 nm; flow rate, 1.0 mL/min; column temperature, 50 °C; mobile phase, 10 mmol/L acetate buffer (pH 4.3)/acetonitrile = 7/3.
In vitro effects of active constituents and extracts of Orthosiphon stamineus on the activities of three major human cDNA-expressed cytochrome P450 enzymes
2011, Chemico-Biological InteractionsCitation Excerpt :Tolbutamide 4-methyhydroxylation [14], dextromethorphan O-demethylation [15] and testosterone 6β-hydroxylation assays [16], which served as activity markers for CYP2C9, CYP2D6 and CYP3A4 respectively, were established and performed in accordance to published procedures. Incubation was performed in accordance to the published procedures [14] with some modifications. Incubations were carried out in volumes of 0.5 mL for 1.5 h.
17,20-Lyase inhibitors. Part 4: Design, synthesis and structure-activity relationships of naphthylmethylimidazole derivatives as novel 17,20-lyase inhibitors
2011, Bioorganic and Medicinal ChemistryCitation Excerpt :The concentration of the substrates was referenced from the data sheet from GENTEST Corp. [(±)-bufuralol 1′-hydroxylation for CYP2D6 and testosterone 6β-hydroxylation activity for CYP3A4] or published reports (tolbutamide hydroxylation for CYP2C8 and 2C9)60,61 with slight modifications. The marker reactions specific for CYP isoforms except for CYP3A4, were measured by published analytical methods60,62–66 with slight modifications. Testosterone 6β-hydroxylation activity for CYP3A4 was analyzed under the following HPLC conditions: Inertsil ODS-2 column (150 × 4.6 mm I.D.; GL Science, Tokyo, Japan), detection wavelength 254 nm, flow rate 1.0 mL/min, column temperature 50 °C, and mobile phase 10 mmol/L acetate buffer (pH4.3)/acetonitrile = 7/3.