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Part Used : ใบActivity : CYP1A2 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 : CYP1A2 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 : CYP1A2 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 : CYP1A2 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 : CYP1A2 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 : CYP1A2 INHIBITIONSolvent/Active Compound : IsorhemnetinType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 100 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) :Result : PositiveRemark : Results: lC50 values (micromolar) of test compounds for CYP1A2 inhibition = 41.90 micromolar lC50 values (micromolar) of test compounds for CYP2C19 inhibition = 49.81 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 : CYP1A2 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 : CaffeineDose/Conc.(drug) : 100 mgResult : PositiveRemark :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 : ไม่ระบุActivity : CYP1A2 INHIBITIONSolvent/Active Compound : ginkgolidesType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 0.1 - 10 micrograms/mLDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : NegativeRemark : Within 0.1 to 10 micrograms/mL, the hydrolyzed ginkgolides showed direct inhibition against CYP1A2, 2B6,2C8,2C9,2C19,2D6,2E1,3A4m (midazolam as substrate) and 3A4t (testosterone as sustrate), with IC50 values determined to be 410 micrograms/mL (concentrations expressed as the sum of equivalent concentrations of ginkgolideA, B and K). For the metabolism-dependent inhibition studies, the preincubation of 30 min did not substantially alter the IC50 values when compared with the corresponding values in the direct inhibition studies. The activities and mRNA expression levels for CYP1A2 and 2B6 with in each drug-treated group (0.1, 1 and 10 micrograms/mL) were not affected after the 48-h incubation. For CYP3A4, the activity and mRNA expression level were not altered when incubated with 0.1 and 1 micrograms/mL of hydrolyzed ginkgolides. When incubated with hydrolyzed ginkgolides at 10 micrograms/mL, the relative activity and relative mRNA expression level of CYP3A4 remarkably increased to 4.59+/-3.67 and 17.2+/-9.16-fold of corresponding vehicle control values, respectively. The hydrolyzed ginkbolides is not likely to cause DDI via inhibition of the major human CYPs.Note : DDI = drug-drug interaction
Part Used : ไม่ระบุActivity : CYP1A2 INHIBITIONSolvent/Active Compound : Ginkgo biloba ext. (EGb761)Type of experiment : non specifiedType 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 : The full ext. was found to a lesser inhibit CYP1A2 (Ki=106+/-24 microgram/mL.)Note : Data incomplete
Part Used : ไม่ระบุActivity : CYP1A2 INHIBITIONSolvent/Active Compound : The terpenoidic fractionType of experiment : non specifiedType 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 : NegativeRemark : The terpenoidic fraction inhibited only CYP2C9 (Ki=15+/-6 microgram/mL.)Note : Data incomplete
