Journal: Current topics in medicinal chemistry

Article Title: Therapeutic Potential of the Inhibition of the Retinoic Acid Hydroxylases CYP26A1 and CYP26B1 by Xenobiotics

doi:

Figure Lengend Snippet: Ketoconazole and Liarozole

Article Snippet: A compound similar to ketoconazole, liarozole ( , Liazal™), was developed by Janssen Research Foundation as an inhibitor of cytochrome P450 mediated androgen biosynthesis in testes and adrenals ( ) [ ].

Techniques:

Journal: Current topics in medicinal chemistry

Article Title: Therapeutic Potential of the Inhibition of the Retinoic Acid Hydroxylases CYP26A1 and CYP26B1 by Xenobiotics

doi:

Figure Lengend Snippet: Ketoconazole and Liarozole

Article Snippet: A compound similar to ketoconazole, liarozole ( , Liazal™), was developed by Janssen Research Foundation as an inhibitor of cytochrome P450 mediated androgen biosynthesis in testes and adrenals ( ) [ ].

Techniques:

Journal: Current topics in medicinal chemistry

Article Title: Therapeutic Potential of the Inhibition of the Retinoic Acid Hydroxylases CYP26A1 and CYP26B1 by Xenobiotics

doi:

Figure Lengend Snippet: Effects of RAMBAs on in vivo concentrations on RA. Azole compounds such as ketoconazole inhibit a wide variety of cytochromes P450 in hepatic cells in addition to CYP26 in other cells. RAMBAs such as talarozole tend to be more CYP26-specific which results

Article Snippet: A compound similar to ketoconazole, liarozole ( , Liazal™), was developed by Janssen Research Foundation as an inhibitor of cytochrome P450 mediated androgen biosynthesis in testes and adrenals ( ) [ ].

Techniques: In Vivo

Journal: Current topics in medicinal chemistry

Article Title: Therapeutic Potential of the Inhibition of the Retinoic Acid Hydroxylases CYP26A1 and CYP26B1 by Xenobiotics

doi:

Figure Lengend Snippet: Ketoconazole and Liarozole

Article Snippet: A compound similar to ketoconazole, liarozole ( , Liazal™), was developed by Janssen Research Foundation as an inhibitor of cytochrome P450 mediated androgen biosynthesis in testes and adrenals ( ) [ ].

Techniques:

Journal: Current topics in medicinal chemistry

Article Title: Therapeutic Potential of the Inhibition of the Retinoic Acid Hydroxylases CYP26A1 and CYP26B1 by Xenobiotics

doi:

Figure Lengend Snippet: Ketoconazole and Liarozole

Article Snippet: A compound similar to ketoconazole, liarozole ( , Liazal™), was developed by Janssen Research Foundation as an inhibitor of cytochrome P450 mediated androgen biosynthesis in testes and adrenals ( ) [ ].

Techniques:

Journal: Andrology

Article Title: Humanin protects against chemotherapy-induced stage-specific male germ cell apoptosis in rats

doi: 10.1111/andr.12036

Figure Lengend Snippet: Effect of HN on Leydig cells exposed to ketoconazole (KTZ) for 4 h in vitro. KTZ markedly reduced testosterone levels in cultured Leydig cells. HN did not restore testosterone levels suppressed by KTZ to baseline. We performed eight replicate experiments

Article Snippet: Eight replicate experiments were performed where Leydig cells were incubated, respectively, with vehicle (control), HN (10 mcg/mL), KTZ (10 mcg/mL, Sigma Aldrich, St. Louis, MO, USA), or KTZ + HN at 34 °C for 4 h. After treatment, the culture medium from each well was collected and stored at −20 °C for testosterone measurement.

Techniques: In Vitro, Cell Culture

Journal: Antimicrobial Agents and Chemotherapy

Article Title: Mechanism of Amphotericin B Resistance in Leishmania donovani Promastigotes

doi:

Figure Lengend Snippet: Proposed biosynthetic pathway of ergosterol in L. donovani . Symbols: →, pathway of wild-type promastigotes; ⇒, pathway of AmB-resistant promastigotes; ▪, sites inhibited by ketoconazole; ……→, defective 24-methyltransferase in AmB-resistant promastigotes.

Article Snippet: Ketoconazole was purchased from ICN Biomedicals (Orsay, France).

Techniques:

Journal: Drugs in R & D

Article Title: Pharmacokinetics of the Oral Selective CXCR2 Antagonist AZD5069: A Summary of Eight Phase I Studies in Healthy Volunteers

doi: 10.1007/s40268-018-0236-x

Figure Lengend Snippet: Geometric mean (± SD) plasma concentration versus time profiles of AZD5069 when administered alone on Day 1 and in combination with ketoconazole on Day 3 of a 5-day treatment period with ketoconazole 400 mg daily (DDI study) on a linear scale ( a ) and a log scale ( b )

Article Snippet: The ketoconazole (Nizoral® ) administered in the DDI study was a 200-mg tablet manufactured by Janssen-Cilag, Belgium.

Techniques: Concentration Assay

Journal: British Journal of Pharmacology

Article Title: Human hepatocytes and cytochrome P450‐selective inhibitors predict variability in human drug exposure more accurately than human recombinant P450s) Human hepatocytes and cytochrome P450‐selective inhibitors predict variability in human drug exposure more accurately than human recombinant P450s

doi: 10.1111/bph.14203

Figure Lengend Snippet: Correlation between the average fm CYP3A estimated in hrP450s versus human hepatocytes for 11 CYP3A and/or CYP2D6 substrates. The fm CYP3A was estimated in hepatocytes by comparing the metabolic turnover, following incubation of the compounds in the absence and presence of the selective CYP3A inhibitor ketoconazole. In hrP450s, CL int was estimated in 10 individual hrP450 isoforms and scaled up to an in vivo CL int by applying ISEFs and abundance for each individual P450 enzyme. The fm CYP3A was determined from the fraction of scaled in vivo CL int,CYP3A over Σscaled in vivo CL int,CYPi . Data represent mean values.

Article Snippet: I u = I in , u = I ss × f u + k a × f a × f g × D × f u Q pv (11) Iu = Iin ,u Maximum unbound hepatic inlet concentration of ketoconazole Iss Average systemic plasma concentration of ketoconazole after repeated oral administration fu Human plasma protein binding (3% for ketoconazole, from Simcyp) ka Absorption rate constant (0.032 h−1 for ketoconazole, from Simcyp) fa Fraction absorbed (1 for ketoconazole, from Simcyp) fg Fraction escaping gut metabolism (0.5 for ketoconazole, from Simcyp) D Administered dose of ketoconazole Qpv Portal vein blood flow assumed to be 1148 mL·min−1 (Davies and Morris, )

Techniques: Incubation, In Vivo

Journal: British Journal of Pharmacology

Article Title: Human hepatocytes and cytochrome P450‐selective inhibitors predict variability in human drug exposure more accurately than human recombinant P450s) Human hepatocytes and cytochrome P450‐selective inhibitors predict variability in human drug exposure more accurately than human recombinant P450s

doi: 10.1111/bph.14203

Figure Lengend Snippet: Correlation between predicted and observed AUC‐fold increase in humans for AZD1305 (AZ1), loratadine (LOR) and tolterodine (TOL) following oral co‐administration of the selective CYP3A inhibitor ketoconazole (A). Correlation between predicted and observed AUC‐fold increase in CYP2D6 PMs compared with EMs for metoprolol (MET) and tolterodine (6). Line of unity (solid), twofold deviation (dashed line). The fm CYP3A and fm CYP2D6 values respectively estimated in human hepatocytes were applied for the predictions using a static equation (triangles) and Simcyp (squares).

Article Snippet: I u = I in , u = I ss × f u + k a × f a × f g × D × f u Q pv (11) Iu = Iin ,u Maximum unbound hepatic inlet concentration of ketoconazole Iss Average systemic plasma concentration of ketoconazole after repeated oral administration fu Human plasma protein binding (3% for ketoconazole, from Simcyp) ka Absorption rate constant (0.032 h−1 for ketoconazole, from Simcyp) fa Fraction absorbed (1 for ketoconazole, from Simcyp) fg Fraction escaping gut metabolism (0.5 for ketoconazole, from Simcyp) D Administered dose of ketoconazole Qpv Portal vein blood flow assumed to be 1148 mL·min−1 (Davies and Morris, )

Techniques:

Journal: International Journal of Nanomedicine

Article Title: Size- and shape-dependent clinical and mycological efficacy of silver nanoparticles on dandruff

doi: 10.2147/IJN.S86828

Figure Lengend Snippet: Skin photographs of the dorsal surface of rats. Notes: ( A ) Control group I showing no redness, no inflammation; ( B ) M. furfur diseased group, scales on the skin; ( C ) and ( D ) Groups III and IV treated with itracanozole and ketoconazole, respectively, showing skin with decreased scales as compared to Group II with pinkish color; ( E ) Group V (20 nm spherical Ag NPs) showing complete treatment of M. furfur as compared to Group II; ( F ) and ( G ) Groups VI and VII (50 nm spherical- and rod-shaped Ag NPs) also showed normalization of the skin but less as compared to group V. Abbreviations: M. furfur , Malassezia furfur ; NPs, nanoparticles.

Article Snippet: Antifungal drugs such as itraconazole and ketoconazole were obtained from HiMedia Laboratories Pvt.

Techniques:

Journal: International Journal of Nanomedicine

Article Title: Size- and shape-dependent clinical and mycological efficacy of silver nanoparticles on dandruff

doi: 10.2147/IJN.S86828

Figure Lengend Snippet: Histopathological microphotographs of different groups of studied rats. Notes: ( A ) Control I; ( B ) M. furfur diseased model group II; antifungal agent-treated groups; ( C ) III (itracanozole); ( D ) IV (ketoconazole); ( E ) V (20 nm spherical-shaped Ag NPs); ( F ) VI (50 nm spherical), and ( G ) VII (50 nm rod-shaped Ag NPs). Abbreviations: M. furfur , Malassezia furfur ; NPs, nanoparticles.

Article Snippet: Antifungal drugs such as itraconazole and ketoconazole were obtained from HiMedia Laboratories Pvt.

Techniques:

Journal: Journal of applied toxicology : JAT

Article Title: Prediction of drug-induced liver injury using keratinocytes

doi: 10.1002/jat.3435

Figure Lengend Snippet: Concentration- and time-dependent induction of S100A8, S100A9, NALP3, IL-1β and RAGE in hepatotoxic drug-treated mouse keratinocytes. Primary mouse keratinocytes were pooled ( n = 3) and cultured for 48 h (A). Isolated keratinocytes were treated with 10 and 100 μM diclofenac, ketoconazole and flutamide for 6 and 48 h (B). mRNA levels of NALP3 and IL-1β were measured by quantitative reverse transcription–polymerase chain reaction. Expression was normalized with the cyclophilin mRNA expression. Data are the means ± SD of three independent determinations. * P

Article Snippet: Allopurinol, azathioprine, diclofenac, diphenhydramine, flutamide, ibuprofen, imipramine, indomethacin, isoniazid, kanamycin, ketoconazole, metronidazole, nifedipine, phenobarbital, phenytoin, pioglitazone, sulfamethoxazole, troglitazone and valproic acid were purchased from Wako Pure Chemical (Osaka, Japan).

Techniques: Concentration Assay, Cell Culture, Isolation, Reverse Transcription Polymerase Chain Reaction, Expressing

Journal: Journal of applied toxicology : JAT

Article Title: Prediction of drug-induced liver injury using keratinocytes

doi: 10.1002/jat.3435

Figure Lengend Snippet: Concentration-dependent induction of S100A8, S100A9, NALP3, IL-1β and RAGE in hepatotoxic drug-treated HaCaT cells. HaCaT cells were treated with diclofenac, ketoconazole and flutamide (10 and 100 μM) for 48 h. mRNA expression levels of S100A8, S100A9, NALP3, IL-1β and RAGE were measured by quantitative reverse transcription–polymerase chain reaction. Gene expressions were normalized with the GAPDH expression. Data are the means ± SD of three independent determinations. * P

Article Snippet: Allopurinol, azathioprine, diclofenac, diphenhydramine, flutamide, ibuprofen, imipramine, indomethacin, isoniazid, kanamycin, ketoconazole, metronidazole, nifedipine, phenobarbital, phenytoin, pioglitazone, sulfamethoxazole, troglitazone and valproic acid were purchased from Wako Pure Chemical (Osaka, Japan).

Techniques: Concentration Assay, Expressing, Reverse Transcription Polymerase Chain Reaction

Journal: Comparative Hepatology

Article Title: Interactions between xenoestrogens and ketoconazole on hepatic CYP1A and CYP3A, in juvenile Atlantic cod (Gadus morhua)

doi: 10.1186/1476-5926-4-2

Figure Lengend Snippet: In vivo CYP3A enzyme activities (A) and in vivo CYP3A protein expression (B) . CYP3A enzyme activities and protein expression in juvenile Atlantic cod exposed in vivo to vehicle (5 ml peanut oil/kg fish), ketoconazole (12 mg/kg fish), nonylphenol (25 mg/kg fish), ethynylestradiol (5 mg/kg fish) and ketoconazole + nonylphenol (12 + 25 mg/kg fish). A) BFCOD activities. B) CYP3A protein levels analyzed using PAb against rainbow trout CYP3A. Each bar represents mean values of eight to nine fish ± SD; a Significantly different from vehicle treated fish; b Significantly different from ketoconazole+nonylphenol treated fish; P

Article Snippet: For comparison, the IC50 values for ketoconazole, nonylphenol and ethynylestradiol were determined in cDNA expressed human CYP3A4 baculovirus supersomes using the CYP3A4 inhibition kit from BD Gentest.

Techniques: In Vivo, Expressing, Fluorescence In Situ Hybridization

Journal: Comparative Hepatology

Article Title: Interactions between xenoestrogens and ketoconazole on hepatic CYP1A and CYP3A, in juvenile Atlantic cod (Gadus morhua)

doi: 10.1186/1476-5926-4-2

Figure Lengend Snippet: CYP3A Western blot (A) and CYP3A 2D-immunoblots (B) . A) Western blot of hepatic microsomal CYP3A proteins in juvenile Atlantic cod treated with vehicle (5 ml peanut oil/kg fish) and ketoconazole (12 mg/kg fish) detected using PAb against rainbow trout CYP3A. B) 2D-gel electrophoresis followed by immunoblotting using PAb against rainbow trout CYP3A. Each blot represent pooled liver microsomes of eight to nine fish for each treatment; vehicle (5 ml peanut oil/kg fish), ketoconazole (12 mg/kg fish), nonylphenol (25 mg/kg fish), ethynylestradiol (5 mg/kg fish), ketoconazole + nonylphenol (12 + 25 mg/kg fish).

Article Snippet: For comparison, the IC50 values for ketoconazole, nonylphenol and ethynylestradiol were determined in cDNA expressed human CYP3A4 baculovirus supersomes using the CYP3A4 inhibition kit from BD Gentest.

Techniques: Western Blot, Fluorescence In Situ Hybridization, Two-Dimensional Gel Electrophoresis, Electrophoresis

Journal: Comparative Hepatology

Article Title: Interactions between xenoestrogens and ketoconazole on hepatic CYP1A and CYP3A, in juvenile Atlantic cod (Gadus morhua)

doi: 10.1186/1476-5926-4-2

Figure Lengend Snippet: Non-competitive inhibition of CYP1A by ketoconazole (A) and non-competitive inhibition of CYP3A by ketoconazole (B) . Dixon plots for ketoconazole on A) EROD activity (diamonds represent 8.2; squares represent 25 and triangles represent 677 pM ethoxyresorufin). B) BFCOD activity (diamonds represent 48; squares represent 84 and triangles represent 200 μM BFC).

Article Snippet: For comparison, the IC50 values for ketoconazole, nonylphenol and ethynylestradiol were determined in cDNA expressed human CYP3A4 baculovirus supersomes using the CYP3A4 inhibition kit from BD Gentest.

Techniques: Inhibition, Activity Assay

Journal: Comparative Hepatology

Article Title: Interactions between xenoestrogens and ketoconazole on hepatic CYP1A and CYP3A, in juvenile Atlantic cod (Gadus morhua)

doi: 10.1186/1476-5926-4-2

Figure Lengend Snippet: CYP3A Western blot after in vivo incubation . Western blot of CYP3A proteins in pooled liver microsomes from Atlantic cod detected using PAb against rainbow trout CYP3A. The blot illustrates representative samples after in vitro incubation with 1.0 μM ketoconazole and 50 μM ethynylestradiol for 30 or 60 min.

Article Snippet: For comparison, the IC50 values for ketoconazole, nonylphenol and ethynylestradiol were determined in cDNA expressed human CYP3A4 baculovirus supersomes using the CYP3A4 inhibition kit from BD Gentest.

Techniques: Western Blot, In Vivo, Incubation, In Vitro

Journal: Comparative Hepatology

Article Title: Interactions between xenoestrogens and ketoconazole on hepatic CYP1A and CYP3A, in juvenile Atlantic cod (Gadus morhua)

doi: 10.1186/1476-5926-4-2

Figure Lengend Snippet: A) In vivo CYP1A enzyme activities (A) and in vivo CYP1A protein expression (B) . CYP1A enzyme activities and protein expression in juvenile Atlantic cod exposed in vivo to vehicle (5 ml peanut oil/kg fish), ketoconazole (12 mg/kg fish), nonylphenol (25 mg/kg fish), ethynylestradiol (5 mg/kg fish) and ketoconazole + nonylphenol (12 + 25 mg/kg fish). A) EROD activities. B) CYP1A protein levels analyzed using PAb against rainbow trout CYP1A. Each bar represents mean values of eight to nine fish ± SD; a Significantly different from vehicle treated fish; b Significantly different from ketoconazole+nonylphenol treated fish; P

Article Snippet: For comparison, the IC50 values for ketoconazole, nonylphenol and ethynylestradiol were determined in cDNA expressed human CYP3A4 baculovirus supersomes using the CYP3A4 inhibition kit from BD Gentest.

Techniques: In Vivo, Expressing, Fluorescence In Situ Hybridization

Journal: The Journal of Pharmacology and Experimental Therapeutics

Article Title: Camptothecin Attenuates Cytochrome P450 3A4 Induction by Blocking the Activation of Human Pregnane X Receptor S⃞

doi: 10.1124/jpet.110.168294

Figure Lengend Snippet: Recruitment of coactivator SRC-1 to hPXR. A, analyses of the recruitment of SRC-1 to hPXR by a mammalian two-hybrid system. Rifampicin treatment and ketoconazole treatment were used as controls. The luciferase activity was measured and normalized for transfection efficiency with β-galactosidase activity. The interaction potentials are indicated as luciferase induction folds compared with vehicle control group (0.1% DMSO). Columns, mean induction folds determined in triplicate independent experiments. Bars are S.D. *, P

Article Snippet: Rifampicin, SR12813, and ketoconazole were from BIOMOL Research Laboratories (Plymouth Meeting, PA).

Techniques: Luciferase, Activity Assay, Transfection

Journal: BMC Biotechnology

Article Title: Development of Caco-2 cells expressing four CYPs via a mammalian artificial chromosome

doi: 10.1186/s12896-020-00637-8

Figure Lengend Snippet: Activity of each CYP in the Caco-2 4CYPs-MAC cells. a The metabolic activity of each CYP in Caco-2 4CYPs-MAC cells. The relative activity for each CYP was measured by comparing the parental Caco-2 cells and the Caco-2 4CYPs-MAC #2 (mean ± S.E., n = 3). b Permeability test using MDZ. The permeability test was performed 23 d after seeding Caco-2 cells and Caco-2 4CYPs-MAC #2, whereby 3 μM MDZ was added to the apical side, and after 30 min, the apical, intracellular, and basal supernatants were collected. The 1′-OH MDZ in the supernatant was measured through LC-MS/MS. c CYP3A4 inhibition test. Ketoconazole, an inhibitor of CYP3A4, was added to the Caco-2 4CYPs-MAC #2 and incubated for 1 h. A luminescent substrate was measured to detect CYP3A4 activity with different concentrations of ketoconazole

Article Snippet: Cells were seeded in a 48-well collagen-coated plate at 2.5 × 104 cells/well, and the medium was changed after 2 d. The next day, the medium was collected, cells were washed twice with PBS, and then 100 μL of TM (pH 6.5) containing ketoconazole (Tokyo Chemical Industry) at 0, 0.01, 0.1, 1.0, 10, and 100 μM was added to each set of three wells.

Techniques: Activity Assay, Permeability, Liquid Chromatography with Mass Spectroscopy, Inhibition, Incubation

Journal: Journal of Pharmaceutical Health Care and Sciences

Article Title: Effect of health foods on cytochrome P450-mediated drug metabolism

doi: 10.1186/s40780-017-0083-x

Figure Lengend Snippet: Effect of representative inhibitors on P450-mediated metabolism in Ad-P450 cells. Ad-P450 cells were incubated in culture medium containing P450 substrate cocktail and each typical P450 inhibitor (furafylline [0.05–30 μM], sulfaphenazole [0.01–10 μM], ticlopidine [0.3–300 μM], quinidine [0.01–10 μM], or ketoconazole [0.01–10 μM]) for 5 h. These media were collected and metabolites were analyzed by LC-MS/MS. The activity levels are shown as means ± SD ( n = 3)

Article Snippet: Ketoconazole was purchased from LKT Laboratories (St. Paul, MN, USA).

Techniques: Incubation, Liquid Chromatography with Mass Spectroscopy, Mass Spectrometry, Activity Assay

Journal: Comparative Hepatology

Article Title: Interactions between xenoestrogens and ketoconazole on hepatic CYP1A and CYP3A, in juvenile Atlantic cod (Gadus morhua)

doi: 10.1186/1476-5926-4-2

Figure Lengend Snippet: In vivo CYP3A enzyme activities (A) and in vivo CYP3A protein expression (B) . CYP3A enzyme activities and protein expression in juvenile Atlantic cod exposed in vivo to vehicle (5 ml peanut oil/kg fish), ketoconazole (12 mg/kg fish), nonylphenol (25 mg/kg fish), ethynylestradiol (5 mg/kg fish) and ketoconazole + nonylphenol (12 + 25 mg/kg fish). A) BFCOD activities. B) CYP3A protein levels analyzed using PAb against rainbow trout CYP3A. Each bar represents mean values of eight to nine fish ± SD; a Significantly different from vehicle treated fish; b Significantly different from ketoconazole+nonylphenol treated fish; P

Article Snippet: Hence, ketoconazole, nonylphenol, and ethynylestradiol interact with CYP1A enzymes, indicating a possible site for interaction of these different classes of xenobiotics.

Techniques: In Vivo, Expressing, Fluorescence In Situ Hybridization

Journal: Comparative Hepatology

Article Title: Interactions between xenoestrogens and ketoconazole on hepatic CYP1A and CYP3A, in juvenile Atlantic cod (Gadus morhua)

doi: 10.1186/1476-5926-4-2

Figure Lengend Snippet: CYP3A Western blot (A) and CYP3A 2D-immunoblots (B) . A) Western blot of hepatic microsomal CYP3A proteins in juvenile Atlantic cod treated with vehicle (5 ml peanut oil/kg fish) and ketoconazole (12 mg/kg fish) detected using PAb against rainbow trout CYP3A. B) 2D-gel electrophoresis followed by immunoblotting using PAb against rainbow trout CYP3A. Each blot represent pooled liver microsomes of eight to nine fish for each treatment; vehicle (5 ml peanut oil/kg fish), ketoconazole (12 mg/kg fish), nonylphenol (25 mg/kg fish), ethynylestradiol (5 mg/kg fish), ketoconazole + nonylphenol (12 + 25 mg/kg fish).

Article Snippet: Hence, ketoconazole, nonylphenol, and ethynylestradiol interact with CYP1A enzymes, indicating a possible site for interaction of these different classes of xenobiotics.

Techniques: Western Blot, Fluorescence In Situ Hybridization, Two-Dimensional Gel Electrophoresis, Electrophoresis

Journal: Comparative Hepatology

Article Title: Interactions between xenoestrogens and ketoconazole on hepatic CYP1A and CYP3A, in juvenile Atlantic cod (Gadus morhua)

doi: 10.1186/1476-5926-4-2

Figure Lengend Snippet: Non-competitive inhibition of CYP1A by ketoconazole (A) and non-competitive inhibition of CYP3A by ketoconazole (B) . Dixon plots for ketoconazole on A) EROD activity (diamonds represent 8.2; squares represent 25 and triangles represent 677 pM ethoxyresorufin). B) BFCOD activity (diamonds represent 48; squares represent 84 and triangles represent 200 μM BFC).

Article Snippet: Hence, ketoconazole, nonylphenol, and ethynylestradiol interact with CYP1A enzymes, indicating a possible site for interaction of these different classes of xenobiotics.

Techniques: Inhibition, Activity Assay

Journal: Comparative Hepatology

Article Title: Interactions between xenoestrogens and ketoconazole on hepatic CYP1A and CYP3A, in juvenile Atlantic cod (Gadus morhua)

doi: 10.1186/1476-5926-4-2

Figure Lengend Snippet: CYP3A Western blot after in vivo incubation . Western blot of CYP3A proteins in pooled liver microsomes from Atlantic cod detected using PAb against rainbow trout CYP3A. The blot illustrates representative samples after in vitro incubation with 1.0 μM ketoconazole and 50 μM ethynylestradiol for 30 or 60 min.

Article Snippet: Hence, ketoconazole, nonylphenol, and ethynylestradiol interact with CYP1A enzymes, indicating a possible site for interaction of these different classes of xenobiotics.

Techniques: Western Blot, In Vivo, Incubation, In Vitro

Journal: Comparative Hepatology

Article Title: Interactions between xenoestrogens and ketoconazole on hepatic CYP1A and CYP3A, in juvenile Atlantic cod (Gadus morhua)

doi: 10.1186/1476-5926-4-2

Figure Lengend Snippet: A) In vivo CYP1A enzyme activities (A) and in vivo CYP1A protein expression (B) . CYP1A enzyme activities and protein expression in juvenile Atlantic cod exposed in vivo to vehicle (5 ml peanut oil/kg fish), ketoconazole (12 mg/kg fish), nonylphenol (25 mg/kg fish), ethynylestradiol (5 mg/kg fish) and ketoconazole + nonylphenol (12 + 25 mg/kg fish). A) EROD activities. B) CYP1A protein levels analyzed using PAb against rainbow trout CYP1A. Each bar represents mean values of eight to nine fish ± SD; a Significantly different from vehicle treated fish; b Significantly different from ketoconazole+nonylphenol treated fish; P

Article Snippet: Hence, ketoconazole, nonylphenol, and ethynylestradiol interact with CYP1A enzymes, indicating a possible site for interaction of these different classes of xenobiotics.

Techniques: In Vivo, Expressing, Fluorescence In Situ Hybridization

Journal: Indian Journal of Pharmacology

Article Title: Interaction potential of Trigonella foenum graceum through cytochrome P450 mediated inhibition

doi: 10.4103/0253-7613.165179

Figure Lengend Snippet: Fluorescence assay. Percentage inhibitory effect of Trigonella foenum graecum extract, trigonelline and positive controls on drug metabolizing enzymes cytochrome P3A4 and cytochrome P2D6 (values are mean ± standard error of the mean; n = 3). Ketoconazole dimethyl sulphoxide = ketoconazole dissolved in dimethyl sulphoxide, ketoconazole ethanol = ketoconazole dissolved in ethanol, TFG DMSO = Trigonella foenum graecum dissolved in dimethyl sulphoxide, TFG ethanol = Trigonella foenum graecum dissolved in ethanol, trigonelline DMSO = trigonelline dissolved in dimethyl sulphoxide, trigonelline ethanol = trigonelline dissolved in ethanol, quinidine DMSO = quinidine dissolved in dimethyl sulphoxide, quinidine ethanol = quinidine dissolved in ethanol

Article Snippet: Ketoconazole and quinidine were obtained from Merck (Mumbai, India).

Techniques: Fluorescence