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Part Used : ใบActivity : CYP2E1 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 : ChlorzoxazoneDose/Conc.(drug) : 500 mgResult : NegativeRemark : Long-term administration of G. biloba had no modulatary effect on CYP2E1.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 : CYP2E1 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 : CYP2E1 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 CYP2E1 (Ki=127+/-42 microgram/mL.)Note : Data incomplete
Part Used : ไม่ระบุActivity : CYP2E1 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
Part Used : ไม่ระบุActivity : CYP2E1 INHIBITIONSolvent/Active Compound : Flavonoidic fraction of EGb761Type 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 flavonoidic fraction of EGB761 showed high inhibition of CYP2C9, CYP1A2, CYP2E1, and CYP3A4 (ki's between 4.9 and 55 microgram/mL)Note : Data incomplete
Part Used : ใบActivity : CYP2E1 INHIBITIONSolvent/Active Compound : ginkgo biloba ext. (GBE)Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : Cells (E47 cells) of Ginkgo biloba ext. (GBE) and alc. group were cultured by 150 g/L GBE for 3 h, and then by alc. for 24 h.Duration : 3 h.Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Result: Compared with those of the alc. and fish oil groups, the expression and activity of CYP2E1 in E47 cells of fish oil and GBE group as well as alc. and GBE group were lower. GBE can inhibit the expression and activity of CYP2E1.Note : The expression of cytochrome P 450 2E1 (CYP2E1) protein in E47 cells was detected using Western blot, the CYP2E1 activity was measured using p-nitrophenol (PNP) probe. Cell cultured by Dulbecco's Modified Eagle's Medium (DMEM) were the controls. Data incomplete.
Part Used : ใบActivity : CYP2E1 INHIBITIONSolvent/Active Compound : ginkgo biloba ext. (GBE)Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : Cells of fish oil and GBE group were cultured by 150 g/L GBE for 3h, and then by fish oil for 24 h.Duration : 3 h.Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Result: Compared with those of the alc. and fish oil groups, the expression and activity of CYP2E1 in E47 cells of fish oil and GBE group as well as alc. and GBE group were lower. GBE can inhibit the expression and activity of CYP2E1.Note : The expression of cytochrome P 450 2E1 (CYP2E1) protein in E47 cells was detected using Western blot, the CYP2E1 activity was measured using p-nitrophenol (PNP) probe. Cell cultured by Dulbecco's Modified Eagle's Medium (DMEM) were the controls. Data incomplete.
