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Thai / English name |
Part Used : -Activity : CYP3A4 INHIBITIONSolvent/Active Compound : MyricetinType 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 : ใบActivity : CYP3A4 INHIBITIONSolvent/Active Compound : -Type of experiment : in vitroType of animal : otherType of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 25 microgram/mlDuration : 5 minutesType of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : -Result : PositiveRemark : - Details of the standardized Ginkgo extracts: 4.78% Quercetin, 3.73% Kaempferol, 2.13% Isorhamnetin, 12.0% Quercetin glycoside, 9.65% Kaempferol glycoside, 5.19% Isorhamnetin glycoside, 1.61% Bilobalide, 1.41% Ginkgolide A, 0.31% Ginkgolide J, 5.57% Ginkgolide B, 0.38% Ginkgolide C. - Results: The degree of CYP3A4 inhibition of Ginkgo biloba was 45.9% and IC50 values of that inhibit CYP3A4-mediated metabolism of midazolam = 75.1 microgram/ml, 95% Cl: 53.0-106.Note : The effects of complementary and alternative medicine (CAM) on CYP3A4-mediated metabolism of midazolam and docetaxel were determined in human liver microsomes (HLM), using liquid-chromatography coupled to tandem mass spectrometry (LC-MS/MS).
Part Used : ใบActivity : CYP3A4 INHIBITIONSolvent/Active Compound :Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 100 microgram/mlDuration : 30 minutesType of interaction : PharmacokineticsInteraction with drug : Docetaxel*/TaxotereDose/Conc.(drug) : -Result : PositiveRemark : - Details of the standardized Ginkgo extracts: 4.78% Quercetin, 3.73% Kaempferol, 2.13% Isorhamnetin, 12.0% Quercetin glycoside, 9.65% Kaempferol glycoside, 5.19% Isorhamnetin glycoside, 1.61% Bilobalide, 1.41 Ginkgolide A, 0.31% Ginkgolide J, 5.57% Ginkgolide B, 0.38% Ginkgolide C. - Results: The degree of CYP3A4 inhibition of Ginkgo biloba was 45.1% and IC50 values of that inhibit CYP3A4-mediated metabolism of docetaxel = 155 microgram/ml, 95% Cl: 81.3-297.Note : The effects of complementary and alternative medicine (CAM) on CYP3A4-mediated metabolism of midazolam and docetaxel were determined in human liver microsomes (HLM), using liquid-chromatography coupled to tandem mass spectrometry (LC-MS/MS).
Part Used : ไม่ระบุActivity : CYP3A4 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 : CYP3A4 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 CYP3A4 (Ki=155+/-43 microgram/mL.)Note : Data incomplete
Part Used : ไม่ระบุActivity : CYP3A4 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 : CYP3A4 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 : CYP3A4 INHIBITIONSolvent/Active Compound : Ginkgo biloba extraction (GBE)Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 10N(Treatment) : 10Sex : MaleAge : -Route : Oral administrationDose/Conc.(herb) : GBE intake 360 mg/dDuration : 28 daysType of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : -Result : PositiveRemark : - Midazolam 8 mg were orally administered to 10 male healthy volunteers before and after GBE intake. - AUC0-alpha for midazolam was singnificantly (25%) increased by GBE intake and oral clearance was significantly (26%) decreased.Note : - Data incomplete