Synonym |
Thai / English name |
Part Used : ใบActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Ginkgolide AType 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 : NegativeRemark : Results: No effect at the highest concentration tested.Note : 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 : ใบActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Ginkgolide BType 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 : NegativeRemark : Results: No effect at the highest concentration tested.Note : 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 : ใบActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Ginkgolide CType 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 : NegativeRemark : Results: No effect at the highest concentration tested.Note : 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 : ใบActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Ginkgolic acid lType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 156 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) :Result : NegativeRemark : Results: lC50 values (micromolar) of test compounds for CYP1A2 inhibition = 4.81 micromolar lC50 values (micromolar) of test compounds for CYP2C9 inhibition = 2.41 micromolar lC50 values (micromolar) of test compounds for CYP2C19 inhibition = 4.22 micromolar C50 values (micromolar) of test compounds for CYP2D6 inhibition = 10.42 micromolar lC50 values (micromolar) of test compounds for CYP3A4 (BzRes) inhibition = 18.80 micromolar lC50 values (micromolar) of test compounds for CYP3A4 (BFC) inhibition = 6.74 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 : ใบActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Ginkgolic acid llType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 184 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) :Result : PositiveRemark : Results: lC50 values (micromolar) of test compounds for CYP1A2 inhibition = 4.88 micromolar lC50 values (micromolar) of test compounds for CYP2C9 inhibition = 1.94 micromolar lC50 values (micromolar) of test compounds for CYP2C19 inhibition = 4.41 micromolar lC50 values (micromolar) of test compounds for CYP2D6 inhibition = 7.82 micromolar lC50 values (micromolar) of test compounds for CYP3A4 (BzRes) inhibition = 15.60 micromolar lC50 values (micromolar) of test compounds for CYP3A4 (BFC) inhibition = 6.25 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 : ใบActivity : CYP3A4 INHIBITIONSolvent/Active Compound : -Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 12 (M/F=6/6)N(Treatment) : 12 (M/F=6/6)Sex : Both sexAge : 67+/-5.2 yrs.Route : Oral administrationDose/Conc.(herb) : 60 mg four times daily (standardized to 24% flavones glycoside and 6% terpene lactones)Duration : 28 daysType of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : 8 mgResult : NegativeRemark :Note : Twelve healthy volunteers were randomly assigned to receive each botanical supplement for 28 days followed by a 30-day washout period. Probe drug cocktails of midazolam, caffeine, chlorzoxazone and debrisoquine were administered before (days -1, 0) and at the end of supplementation (days 27, 28). Pre- and post-supplementation phenotypic ratios were determined for CYP3A4, CYP1A2, CYP2E1 and CYP2D6 using 1-hydroxymidazolam/midazolam serum ratios (1-hour), paraxanthine/caffeine serum ratios (6-hour), 6-hydroxychlorzoxazone/chlorzoxazone serum ratios (2-hour) and debrisoquine urinary recovery ratios (8-hour), respectively.
Part Used : -Activity : CYP3A4 INHIBITIONSolvent/Active Compound : AmentoflavoneType 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 : -Remark :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 : -Activity : CYP3A4 INHIBITIONSolvent/Active Compound : LuteolinType 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 : KaempferolType 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.