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Part Used : ไม่ระบุActivity : CYP2D6 INHIBITIONSolvent/Active Compound : ginsenoside F1Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 10-100 micromolars of F1Duration : 10 min incubationType of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Result: F1 exhibited a weaker inhibition of the activity of CYP2D6Note : Type of experiment: Human livers were obtained from three Chinese autopsy sample (males, ages 27, 29 and 42 years). Conclusion: The degradation of ginsenosides in the gastrointestinal tract may play an important role in the ginseng-associated drug-drug interactions, but the effects might be not due to Rh1 and F1.
Part Used : ไม่ระบุActivity : CYP2D6 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) : 500 mg three times daily (standardized to 5% ginsenosides)Duration : 28 daysType of interaction : PharmacokineticsInteraction with drug : Debrisoquin*/Debrisoquine/Debrisochinum/IsocaramidineDose/Conc.(drug) : 5 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 : -Activity : CYP2D6 INHIBITIONSolvent/Active Compound : BST204Type 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 : The inhibitory potency of BST204 and its bioactive ginsenosides, R-Rg3, S-Rg3, R-Rh2 and S-Rh2, was determined using a nine - CYP isozyme cocktail assay in pooled human liver microsomes. Combining nine specific substrates for each CYP in cocktails is particularly useful because it is possible to measure multiple CYP activities in the same microsomal incubation. In brief, the 90-microlitre incubation mixture, including pooled human liver microsomes (final concentration 0.25 mg/mL), 0.1 M phosphate buffer, each P450-selective substrate cocktail set, and test compounds (0-5 micromolars) was pre-incubated for 5 min at 37 degrees celsius.
Part Used : -Activity : CYP2D6 INHIBITIONSolvent/Active Compound : Ginsenoside S-Rg3Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 0-50 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : EquivocalRemark : The inhibitory potency of BST204 and its bioactive ginsenosides, R-Rg3, S-Rg3, R-Rh2 and S-Rh2, was determined using a nine-CYP isozyme cocktail assay in pooled human liver microsomes and IC50 values of ginsenoside S-Rg3 in reversible inhibition CYP450 (CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4/5) was > 50 micromolar.
Part Used : -Activity : CYP2D6 INHIBITIONSolvent/Active Compound : Ginsenoside R-Rg3Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 0-50 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : EquivocalRemark : The inhibitory potency of BST204 and its bioactive ginsenosides, R-Rg3, S-Rg3, R-Rh2 and S-Rh2, was determined using a nine-CYP isozyme cocktail assay in pooled human liver microsomes and IC50 values of ginsenoside S-Rg3 in reversible inhibition CYP450 (CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4/5) was > 50 micromolar.
Part Used : -Activity : CYP2D6 INHIBITIONSolvent/Active Compound : Ginsenoside R-Rh2Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 0-50 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : EquivocalRemark : The inhibitory potency of BST204 and its bioactive ginsenosides, R-Rg3, S-Rg3, R-Rh2 and S-Rh2, was determined using a nine-CYP isozyme cocktail assay in pooled human liver microsomes and IC50 values of ginsenoside S-Rg3 in reversible inhibition CYP450 (CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4/5) was > 50 micromolar.
Part Used : -Activity : CYP2D6 INHIBITIONSolvent/Active Compound : Ginsenoside S-Rh2Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 0-50 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : EquivocalRemark : The inhibitory potency of BST204 and its bioactive ginsenosides, R-Rg3, S-Rg3, R-Rh2 and S-Rh2, was determined using a nine-CYP isozyme cocktail assay in pooled human liver microsomes and IC50 values of ginsenoside S-Rg3 in reversible inhibition CYP450 (CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4/5) was > 50 micromolar.
Part Used : -Activity : CYP2D6 INHIBITIONSolvent/Active Compound : BST204 (a purified dry extract of ginseng)Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 0-50 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : The inhibition potency of BST204 and its bioactive ginsenosides, R-Rg3, S-Rg3, R-Rh2 and S-Rh2, was determined using a nine-CYP isozyme cocktail assay in pooled human liver microsomes and BST204 slightly inhibited CYP2C8, CYP2D6, CYP2C9, and CYP2B6 activities with IC50 values of 17.4, 26.8, 31.5, and 49.7 microgram/mL, respectively.