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Part Used : ใบActivity : CYP2C19 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 : CYP2C19 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 : CYP2C19 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 : CYP2C19 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 : CYP2C19 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 : CYP2C19 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 : ไม่ระบุActivity : CYP2C19 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
