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Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : bergamottinType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 200 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) :Result : PositiveRemark : Results: lC50 values (micromolar) of test compounds for CYP1A2 inhibition = 0.48 micromolar lC50 values (micromolar) of test compounds for CYP2C9 inhibition = 0.33 micromolar lC50 values (micromolar) of test compounds for CYP2C19 inhibition = 0.19 micromolar lC50 values (micromolar) of test compounds for CYP2D6 inhibition = 0.35 micromolar lC50 values (micromolar) of test compounds for CYP3A4 (BFC) inhibition = 1.47 micromolarNote : Evaluated the effects of 25 purified components of commonly used herbal products on the catalytic activity of cDNA-expressed cytochrome P450 isoforms in in vitro experiments. Increasing concentrations of the compounds were incubated with a panel of recombinant human CYP isoforms (CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4) and their effects on the conversion of specific surrogate substrates measured fluorometrically in a 96-well plate format.
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : 6,7-dihydroxybergamottinType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 217 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) :Result : PositiveRemark : Results: lC50 values (micromolar) of test compounds for CYP1A2 inhibition = 10.23 micromolar lC50 values (micromolar) of test compounds for CYP2C9 inhibition = 1.17 micromolar lC50 values (micromolar) of test compounds for CYP2C19 inhibition = 0.097 micromolar lC50 values (micromolar) of test compounds for CYP2D6 inhibition = 1.19 micromolar lC50 values (micromolar) of test compounds for CYP3A4 (BFC) inhibition = 1.66 micromolarNote : Evaluated the effects of 25 purified components of commonly used herbal products on the catalytic activity of cDNA-expressed cytochrome P450 isoforms in in vitro experiments. Increasing concentrations of the compounds were incubated with a panel of recombinant human CYP isoforms (CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4) and their effects on the conversion of specific surrogate substrates measured fluorometrically in a 96-well plate format.
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : naringeninType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 200 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) :Result : PositiveRemark : Results: lC50 values (micromolar) of test compounds for CYP1A2 inhibition = 83.09 micromolar lC50 values (micromolar) of test compounds for CYP2C9 inhibition = 2.57 micromolar lC50 values (micromolar) of test compounds for CYP2C19 inhibition = 3.48 micromolar lC50 values (micromolar) of test compounds for CYP2D6 inhibition = 159.12 micromolar lC50 values (micromolar) of test compounds for CYP3A4 (BzRes) inhibition = 11.90 micromolar lC50 values (micromolar) of test compounds for CYP3A4 (BFC) inhibition = 20.46 micromolarNote : Evaluated the effects of 25 purified components of commonly used herbal products on the catalytic activity of cDNA-expressed cytochrome P450 isoforms in in vitro experiments. Increasing concentrations of the compounds were incubated with a panel of recombinant human CYP isoforms (CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4) and their effects on the conversion of specific surrogate substrates measured fluorometrically in a 96-well plate format.
Part Used : -Activity : CYP3A4 INHIBITIONSolvent/Active Compound : bergamottinType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark :Note : Three coumarins and 12 flavonoids significantly suppressed CYP3A4 or CYP2C9 activities. Lineweaver-Burk plot analysis indicated that apigenin and its dimer amentoflavone and imperatorin displayed a mixed type of inhibition on CYP3A4 or CYP2C9. Among the inhibitors, amentoflavone was the most potent inhibitor of CYP3A4 and CYP2C9 activities with IC50 values of 0.07 and 0.03 micromolar, respectively. The Ki value of amentoflavone was significantly lower than that of the CYP2C9 inhibition positive control sulfaphenazole.
Part Used : -Activity : CYP3A4 INHIBITIONSolvent/Active Compound : NaringeninType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark :Note : Three coumarins and 12 flavonoids significantly suppressed CYP3A4 or CYP2C9 activities. Lineweaver-Burk plot analysis indicated that apigenin and its dimer amentoflavone and imperatorin displayed a mixed type of inhibition on CYP3A4 or CYP2C9. Among the inhibitors, amentoflavone was the most potent inhibitor of CYP3A4 and CYP2C9 activities with IC50 values of 0.07 and 0.03 micromolar, respectively. The Ki value of amentoflavone was significantly lower than that of the CYP2C9 inhibition positive control sulfaphenazole.
Part Used : -Activity : CYP3A4 INHIBITIONSolvent/Active Compound : ApigeninType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark :Note : Three coumarins and 12 flavonoids significantly suppressed CYP3A4 or CYP2C9 activities. Lineweaver-Burk plot analysis indicated that apigenin and its dimer amentoflavone and imperatorin displayed a mixed type of inhibition on CYP3A4 or CYP2C9. Among the inhibitors, amentoflavone was the most potent inhibitor of CYP3A4 and CYP2C9 activities with IC50 values of 0.07 and 0.03 micromolar, respectively. The Ki value of amentoflavone was significantly lower than that of the CYP2C9 inhibition positive control sulfaphenazole.
Part Used : ไม่ระบุActivity : CYP3A4 INHIBITIONSolvent/Active Compound : -Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 100 microgram/mlDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark :
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : grapefruit juice (GFJ)Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 7N(Treatment) : 7Sex : MaleAge : 21-24 yrs.Route : Oral administrationDose/Conc.(herb) : *Duration : 7 daysType of interaction : PharmacokineticsInteraction with drug : CeliprololDose/Conc.(drug) : -Result : PositiveRemark : *Dose: They were orally administered celiprolol (100 mg) with water on the control day. Three days later, they ingested GFJ (200 mL) 3 times a day for 3 d. On day 1, the same drugs were administered with GFJ. On days 3 and 7, the same drugs were administered with water. Pharmacokinetics of drug was evaluated on each trial day. Result: The peak plasma concentration (Cmax) and the area under the plasma concentration-time curve from 0 to 8 h (AUC0-8) of celiprolol significantly decreased on day 1, and the mean ratios of these values and the corresponding control-day values were 0.18 and 0.25, respectively. The Cmax and AUC0-8 returned to the control levels on days 3 and 7.Note : Conclusion: The OATP inhibition caused by GFJ dissipated faster than GFJ- mediated alterations in CYP3A4 activity, which were sustained for at least 48 h. Celiprolol and midazolam are substrated of OATP and CYP3A4.
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : grapefruit juice (GFJ)Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 7N(Treatment) : 7Sex : MaleAge : 21-24 yrs.Route : Oral administrationDose/Conc.(herb) : *Duration : 7 daysType of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : -Result : PositiveRemark : *Dose: They were orally administered celiprolol (100 mg) with water on the control day. Three days later, they ingested GFJ (200 mL) 3 times a day for 3 d. On day 1, the same drugs were administered with GFJ. On days 3 and 7, the same drugs were administered with water. Pharmacokinetics of drug was evaluated on each trial day. Result: (AUC0-8) of midazolam was higher on days 1 and 3 than on the control day (mean ratio, 2.12 and 1.47, respectively). The AUC0-8 returned to the control level on day 7.Note : Conclusion: The OATP inhibition caused by GFJ dissipated faster than GFJ- mediated alterations in CYP3A4 activity, which were sustained for at least 48 h. Celiprolol and midazolam are substrated of OATP and CYP3A4.
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : grapefruit juice (GFJ)Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 21*N(Treatment) : 21Sex : MaleAge : -Route : Oral administrationDose/Conc.(herb) : 200 ml GFJDuration : For development of the pharmacokinetic model of felodipine-GFJ interaction in this study, they utilized pharmacokinetic data obtained from two clinical trials. In the first, nine healthy male volunteers were given 10 mg felodipine ER orally together with either 200 ml tap water or GFJ at 0, 1, 4, 10 or 24 h before administration of felodipine. In the second, 12 healthy male volunteers received 10 mg felodipine ER after daily intake of either 200 ml of tap water of GFJ for 1 day or 14 days.Type of interaction : PharmacokineticsInteraction with drug : FelodipineDose/Conc.(drug) : 10 mg felodipine ER (extended release formulation)Result : PositiveRemark : Result: The model gave a turnover rate of CYP3A4 of 0.0849 h-1, corresponding to a half-life of 8.16 h. Conclusions: GFJ-felodipine interaction increases with increasing frequency and amount of GFJ ingestion, and that an interval of 2-3 days between GFJ intake and felodipine administration is necessary if GFJ-felodipine interaction is to be avoided.
