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Part Used : -Activity : CYP3A4 INHIBITIONSolvent/Active Compound : ApigeninType 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 : -Activity : CYP3A4 INHIBITIONSolvent/Active Compound : LuteolinType 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 : -Activity : CYP3A4 INHIBITIONSolvent/Active Compound : 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 : -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 : -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 : ไม่ระบุActivity : 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 : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark :
Part Used : ต้นอ่อนActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Sulforaphane (SFN)Type of experiment : humanType of animal : -Type of study : Cross overN(Total) : 23 (M/F = 12/11)N(Treatment) : 23 (M/F = 12/11)Sex : Both sexAge : average age of 23.7 years (range 20-34)Route : Oral administrationDose/Conc.(herb) : 450 micromolarDuration : The three armed randomized, crossover trial consisted of : the potent pregnane and xenobiotic r eceptor (PXR) ligand - rifampicin 300 mg/d was given alone for 7 days in arm 1; or in daily combination with 450 micromolar SFN (Broccoli Sprout extract) in arm 2; SFN was given alone in arm 3. Midazolam as an in vivo phenotype marker of CYP3A was administered before and after each treatment arm.Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : NegativeRemark : Result: Rifampicin alone decreased midazolam AUC by 70%, indicative of the expected increase in CYP3A4 activity. Co-treatment with SFN did not reduce CYP3A4 induction. Treatment with SFN alone also did not affect CYP3A4 activity in the cohort as a whole. - SFN in the broccoli-sprout power was not able to effectively antagonize rifampicin mediated activaton of PXR, as reflected in the increase in intestinal and/or hepatic CYP3A activity (i. e., increased clearance of orally administered midazolam)
Part Used : ต้นอ่อนActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Sulforaphane (SFN)Type of experiment : humanType of animal : -Type of study : Cross overN(Total) : 23 (M/F = 12/11)N(Treatment) : 23 (M/F = 12/11)Sex : Both sexAge : average age of 23.7 years (range 20-34)Route : Oral administrationDose/Conc.(herb) : 450 micromolarDuration : The three armed randomized, crossover trial consisted of : the potent pregnane and xenobiotic r eceptor (PXR) ligand - rifampicin 300 mg/d was given alone for 7 days in arm 1; or in daily combination with 450 micromolar SFN (Broccoli Sprout extract) in arm 2; SFN was given alone in arm 3. Midazolam as an in vivo phenotype marker of CYP3A was administered before and after each treatment arm.Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Subject (N) treatment: The midazolam AUC data were divided into quartiles and the lower three quartiles from subjects with the higher CYP3A4 activity were examined. Result: - 7 days of SFN treatment caused a 20% decrease in CYP3A4 activity, as reflected by both an increase in midazolam AUC or a decrease in MDZ oral clearance (P<0.001). The mean peak plasma concentration increased from 3.6+/-1.2 ng/ml on day 1 to 4.4+/-1.0 ng/ml on day 8 (P=0.03). - SFN present in the broccoli sprout extract decreased intestinal and hepatic CYP3A4 activity in those members of the population with higher 'basal' CYP3A4 activity, consistent with the hypothesis that SFN is able to at least partially antagonize endogenous ligand mediated activation of PXR, even though it was not able to effectively antagonize the potent exogenous ligand, rifampicin.
Part Used : ต้นอ่อนActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Sulforaphane (SFN)Type of experiment : in vivoType of animal : mouseType of study : -N(Total) :N(Treatment) :Sex : -Age :Route : Oral administrationDose/Conc.(herb) :Duration :Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Type of experiment: Humanized PXR breeder mice were treated with vehicle, rifampicin (10 mg/kg-d), or rifampicin+SFN for 3 days, rifampicin treatment at this dose has been shown to substantially increase hepatic Cyp3a11 mRNA (~12x) and protein (~2.5x) levels in these mice. All treatments were administered by gavage in a volume of 5 ml/kg (2 mg rifampicin/ml). Eight hours after the last dose of SFN and/or rifampin, animals were euthanized and liver tissue was collected for Cyp3a11 (mouse homolog to human CYP3A4) activity analysis. Result: Treatment of male humanized PXR mouse hepatocytes with rifampicin substantially, but variably, induced Cyp3a11 mRNA, and the induction was completely blocked by the addition of SFN in all tested hepatocytes.
Part Used : ต้นอ่อนActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Sulforaphane (SFN)Type of experiment : in vivoType of animal : mouseType of study : -N(Total) :N(Treatment) :Sex : -Age :Route : Oral administrationDose/Conc.(herb) :Duration :Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Type of experiment: Humanized PXR breeder mice were treated with vehicle, rifampicin (10 mg/kg-d), or rifampicin+SFN for 3 days, rifampicin treatment at this dose has been shown to substantially increase hepatic Cyp3a11 mRNA (~12x) and protein (~2.5x) levels in these mice. All treatments were administered by gavage in a volume of 5 ml/kg (2 mg rifampicin/ml). Eight hours after the last dose of SFN and/or rifampin, animals were euthanized and liver tissue was collected for Cyp3a11 (mouse homolog to human CYP3A4) activity analysis. Result: Treatment of female humanized PXR mouse hepatocytes with rifampicin substantially, but variably, induced Cyp3a11 mRNA, and the induction was completely blocked by the addition of SFN in all tested hepatocytes.
Part Used : ต้นอ่อนActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Sulforaphane (SFN)Type of experiment : in vivoType of animal : mouseType of study : -N(Total) :N(Treatment) :Sex : -Age :Route : Oral administrationDose/Conc.(herb) : 50 mg/kg/dayDuration : 3 daysType of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : NegativeRemark : Type of experiment: Female mice were split into four groups: (a) received vehicle, (b) 10 mg/kg/day rifampicin, (c) 50 mg/kg/day SFN, and (d) 10 mg/kg/day rifampicin and 50 mg/kg/day SFN. Mice were administered SFN and/or rifampicin by gavage daily for 3 days and sacrificed 8 h after the final dose. Liver tissue were analyzed for mRNA. Result: Cyp3a11 levels were significantly elevated in the two rifampicin treatment groups, although the magnitude of induction was highly variable. When administered at 50 mg/kg-day for 3 days, SFN treatment had no effect on basal expression of Cyp3a11, and co-administration with rifampicin had no significant effect on the magnitude of rifampicin induction.
