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Part Used : ใบActivity : CYP3A4 INDUCTIONSolvent/Active Compound : tamarixetin (Tam)Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : Tam 10 mcg/mlDuration : HepG2 cells transfected with hCAR or hPXR expression vector were exposed to Tam for 24 h.Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : NegativeRemark : Result: EGb 761, Que and Kae induced CYP3A4 mRNA expression in human constitutive androstane receptor (hCAR)- and human pregnane X receptor (hPXR)- trasfected HepG2 cells through activation of these receptors.Note : Abbreviations: AhR = Arylhydrocarbon receptor GA = Ginkgolide A, GB = Ginkgolide B, CAR = Constitutive androstane receptor, BB = Bilobalide, Que = Quercetin, Kae = Kaempferol, Tam = Tamarexetin
Part Used : ใบActivity : CYP3A4 INDUCTIONSolvent/Active Compound : Ethanol / ginkgolide A, Ginkolide C, bilobalide, quercetin, kaempferolType 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 : Rifampicin*/RifampinDose/Conc.(drug) : -Result : PositiveRemark : 22 ethanol extracts and 8 compounds could activate human PXR and induce CYP3A4 reporter construct in HepG2 cells. Among them, Ginkgo biloba, Ligusticum chuanxiong, Chinese angelica, prepared Rehmannia root, Epimedium brevicornum, Atractylodes macrocephala, Schisandra chinensis, Paeonia lactifora, Ophiopogon japonicus, Polygonum multiflorum, Coptis chinensis, Artemisia scoparia, Trichosanthes kirilowii, Silybum marianum, Gardenia fruit and Lycium chinense could strongly trans-activate PXR. Moreover, ligustilide, schisantherin A, berberine hydrochloride and trans-resveratrol were identified for the first time as efficacious PXR agonists.Note : PXR = pregnane X receptor
Part Used : ไม่ระบุActivity : CYP3A4 INDUCTIONSolvent/Active Compound : Ginkgo biloba extract*Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 100 microgram/mlDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Gingko biloba extract did not alter hCAR or hPXR mRNA expression. Whereas the extract (100 mg/ml) increased CYP2B6 mRNA and CYP2B6-mediated bupropion hydroxylation, the increase was not attenuated by the co-treatment with a hGR antagonist. The same pattern of response was also obtained for CYP3A4 mRNA and CYP3A-mediated testosterone 6b-hydroxylation. Therefore, Ginkgo biloba extract induces CYP2B6 (a hCAR target gene) and CYP3A4 (a hPXR target gene) by a hGR-independent mechanism.Note : *Solvent/active compound: Ginkgo extract (Lot A) 200 micrgram/mL consist ginkogolide A, B, C, J and bilobalide as 2.2, 0.6, 2.8, 1.2 and 5.6 microgram/mL, respectively.
Part Used : ไม่ระบุActivity : CYP3A4 INDUCTIONSolvent/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 INDUCTIONSolvent/Active Compound :Type of experiment : humanType of animal : -Type of study : non specifiedN(Total) : -N(Treatment) : -Sex : -Age : -Route : Non-specifiedDose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : RitonavirDose/Conc.(drug) : -Result : NegativeRemark : Most reports unconfirmed. No effect on CYP1A2, CYP3A4, CYP2E1, CYP2D6 activity in humans, but moderate inducer of CYP2C19. Interaction reported with omeprazole in Chinese patients and fatal seizures in a patient on antieplilepsy medication. Caution if taken with warfarin, antiplatelet dugs, alprazolam, donezepil, trazodone, anticancer drugs.Note : Data from review, data incomplete.
Part Used : ไม่ระบุActivity : CYP3A4 INDUCTIONSolvent/Active Compound : bilobalideType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 2.5-40 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : NegativeRemark : The CYP3A4 reporter gene construct was mildly transactivated by praeruptorin E, emodin, chrysophanol, epifriedelanol, mulberroside A, physcion, salvianolic acid B, and tanshinone llA, although they didn't show significant difference as compared to control group. The CYP3A4 reporter gene construct was no transactivated by other herbal compounds.Note : Type of experiment: LS174T cells
Part Used : ไม่ระบุActivity : CYP3A4 INDUCTIONSolvent/Active Compound : Ginkgolide AType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 2.5-40 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : NegativeRemark : The CYP3A4 reporter gene construct was mildly transactivated by praeruptorin E, emodin, chrysophanol, epifriedelanol, mulberroside A, physcion, salvianolic acid B, and tanshinone llA, although they didn't show significant difference as compared to control group. The CYP3A4 reporter gene construct was no transactivated by other herbal compounds.Note : Type of experiment: LS174T cells
Part Used : ไม่ระบุActivity : CYP3A4 INDUCTIONSolvent/Active Compound : Ginkgolide BType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 2.5-40 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : NegativeRemark : The CYP3A4 reporter gene construct was mildly transactivated by praeruptorin E, emodin, chrysophanol, epifriedelanol, mulberroside A, physcion, salvianolic acid B, and tanshinone llA, although they didn't show significant difference as compared to control group. The CYP3A4 reporter gene construct was no transactivated by other herbal compounds.Note : Type of experiment: LS174T cells
Part Used : ใบActivity : CYP3A4 INDUCTIONSolvent/Active Compound : Ginkgo biloba leaf ext. (GBE)Type 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 : ItraconazoleDose/Conc.(drug) : -Result : NegativeRemark : The metabolism pathways involved for GBE were identified by preincubation of cryopreserved human primary hepatocytes (HPHs) with selective inhibitors of CYP3A4 (itraconazole).Note : Result: GBE showed the inhibition of PAF-induced platelet aggregation with IC50 of 33 mg/L-1, 30% enhancement over the control. These effects of GBE were reduced significantly by selectively inhibiting CYP1A2 but CYP2B6, 2C19, 2E1 and 3A4. The inhibitive effects of GBE on PAF induced platelet aggregation are regulated by CYP1A2. Data incomplete.
Part Used : ไม่ระบุActivity : CYP3A4 INDUCTIONSolvent/Active Compound : G. biloba extractType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 200 mg/mLDuration : 72 hType of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : G. biloba ext. at 200, 400m and 800 mg/mL increased CYP3A4 mRNA expression by 1.7-, 2.4-, and 2.5-fold, resp. The same concentration of the ext. increased CYP3A5 (1.3-3.6-fold) and P- glycoprotein (ABCB) 1 (2.7-6.4-fold) mRNA expression. L-sulforaphane (an hPXR antagonist) decreased CYP3A4, CYP3A5, and ABCB1 gene expression in cells treated with G. biloba ext.Note : Data incomplete
