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Part Used : ไม่ระบุActivity : DRUG INTERACTIONSolvent/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 : DRUG INTERACTIONSolvent/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 : DRUG INTERACTIONSolvent/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 : DRUG INTERACTIONSolvent/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 : DRUG INTERACTIONSolvent/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 : DRUG INTERACTIONSolvent/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.
Part Used : ต้นอ่อนActivity : DRUG INTERACTIONSolvent/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) : 100 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) 100 mg/kg/day SFN, and (d) 10 mg/kg/day rifampicin and 100 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. Result: The SFN dose rate was then increased to 100 mg/kg/day for 3 days to see if higher doses might effectively antagonize rifampicin induction. Again, rifampicin administration led to a large but highly variable (and thus not significant) increase in Cyp3a11 mRNA that was not abrogated by co-administration of SFN. In fact, in these mice, the 100 mg dose of SFN led to an higher levels of cyp3A11 mRNA induction relative to rifampicin alone; i.e., 3.53+/-0.76 to 12.9+/-7.3 fold.
Part Used : ต้นอ่อนActivity : DRUG INTERACTIONSolvent/Active Compound : Sulforaphane (SFN)Type of experiment : in vivoType of animal : mouseType of study : -N(Total) :N(Treatment) :Sex : -Age :Route : IntraperitonealDose/Conc.(herb) : 25 mg/kg/, 3 times per dayDuration : 3 daysType of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : NegativeRemark : Type of experiment: Loss of righting Reflex (LORR) assay. - For the third arm, mice were dosed with rifampicin (40 mg/kg once per day, at a volume of 5 ml/kg) and SFN (50 mg/kg, 3 times per day via IP at a volume of 5 ml/kg) for a further three days. Result: Consistent with the induction of Cyp3a11 mRNA following rifampicin, mice administered 40 mg/kg/d of rifampicin had a significantly reduced LORR time following a dose of 2,2,2-tribromoethanol. Co-administration of SFN at 25 mg/kg dose had no effect on the ability of rifampicin to induce Cyp3a11, as indicated by LORR times.
Part Used : ต้นอ่อนActivity : DRUG INTERACTIONSolvent/Active Compound : Sulforaphane (SFN)Type of experiment : in vivoType of animal : mouseType of study : -N(Total) :N(Treatment) :Sex : -Age :Route : IntraperitonealDose/Conc.(herb) : 50 mg/kg/, 3 times per dayDuration : 3 daysType of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : NegativeRemark : Type of experiment: Loss of righting Reflex (LORR) assay. - Mice were dosed with rifampicin (40 mg/kg once per day, at a volume of 5 ml/kg) and SFN (50 mg/kg, 3 times per day via IP at a volume of 5 ml/kg) for a further three days. Result: Consistent with the induction of Cyp3a11 mRNA following rifampicin, mice administered 40 mg/kg/d of rifampicin had a significantly reduced LORR time following a dose of 2,2,2-tribromoethanol. Co-administration of SFN at 50 mg/kg dose had no effect on the ability of rifampicin to induce Cyp3a11, as indicated by LORR times.
Part Used : ไม่ระบุActivity : DRUG INTERACTIONSolvent/Active Compound : L-sulforaphane (SFN)Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 5 micromolars/LDuration : 72 hoursType of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Type of experiment: Breast cancer cell lines MCF7.
