| Synonym |
| Thai / English name |
Part Used : -Activity : CYP3A4 INHIBITIONSolvent/Active Compound : bergamottinType 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 : NaringeninType 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 : ผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : -Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 2-6 mg/mlDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : NegativeRemark : The effect of the single Chinese herbal preparation on CYP3A4 activity in human liver microsome in 3 different concentrations, 2 mg/ml 4 mg/ml and 6 mg/ml.
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Methanol elutes of ethyl acetate extracts of orange juiceType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : The reaction mixture, consisting of 1.3 mM NADP, 3.3 mM glucose 6-phsophate, 0.4 U/ml of glucose-6-phosphate dehydrogenase, 3.3 mM magnesium chloride, and 0.2 mM testosterone in 100 mM potassium phosphate buffer (pH 7.4), was preincubated for 5 min at 37 degrees celsius in the presence of ethyl acetate extracts of orange juice. The reaction was started by the addition of 1.25 pmol of P450, in the case of human CYP3A4, and 0.05 mg of protein, in the case of human liver microsomes. After incubation for 15 min at 37 degrees celsius, the reaction was stopped by the addition of methylene chloride.Duration : 15 min.Type of interaction : PharmacokineticsInteraction with drug : TestosteroneDose/Conc.(drug) : 0.2 nM testosteroneResult : NegativeRemark : Result: No significant inhibitory effect on testosterone 6beta-hydroxylation (endogenous substrate of cytochrome P450 3A4) was observed in any of the methanol eluates (0 - 100% methanol eluates).
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : 3,3',4',5,6,7,8-heptamethoxyflavone (HMF)Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : The reaction mixture, consisting of 1.3 mM NADP, 3.3 mM glucose 6-phosphate, 0.4 U/ml of glucose-6-phosphate dehydrogenase, 3.3 mM magnesium chloride, and 0.2 mM testosterone in 100 mM potassium phosphate buffer (pH 7.4), was preincubated for 5 min at 37 degrees celsius in the presence of HMF 0.1, 1, 10, 100 microM. The reaction was started by the addition of 1.25 pmol of P450, in the case of human CYP3A4, and 0.05 mg of protein, in the case of human liver microsomes. After incubation for 15 min at 37 degrees celsius, the reaction was stopped by the addition of methylene chloride.Duration : 15 min.Type of interaction : PharmacokineticsInteraction with drug : TestosteroneDose/Conc.(drug) : 0.2 mM testosteroneResult : NegativeRemark : Result: Neither compound markedly inhibited 6beta-hydroxylation of testosterone by human liver microsomes or recombinant human CYP3A4.
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : tangeretinType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : The reaction mixture, consisting of 1.3 mM NADP, 3.3 mM glucose 6-phosphate, 0.4 U/ml of glucose-6-phosphate dehydrogenase, 3.3 mM magnesium chloride, and 0.2 mM testosterone in 100 mM potassium phosphate buffer (pH 7.4), was preincubated for 5 min at 37 degrees celsius in the presence of tangeretin 0.1, 1, 10, 100 microM. The reaction was started by the addition of 1.25 pmol of P450, in the case of human CYP3A4, and 0.05 mg of protein, in the case of human liver microsomes. After incubation for 15 min at 37 degrees celsius, the reaction was stopped by the addition of methylene chloride.Duration : 15 min.Type of interaction : PharmacokineticsInteraction with drug : TestosteroneDose/Conc.(drug) : 0.2 mM testosteroneResult : NegativeRemark : Result: Neither compound markedly inhibited 6beta-hydroxylation of testosterone by human liver microsomes or recombinant human CYP3A4.
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : nobiletinType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : The reaction mixture, consisting of 1.3 mM NADP, 3.3 mM glucose 6-phosphate, 0.4 U/ml of glucose-6-phosphate dehydrogenase, 3.3 mM magnesium chloride, and 0.2 mM testosterone in 100 mM potassium phosphate buffer (pH 7.4), was preincubated for 5 min at 37 degrees celsius in the presence of nobiletin 0.1, 1, 10, 100 microM. The reaction was started by the addition of 1.25 pmol of P450, in the case of human CYP3A4, and 0.05 mg of protein, in the case of human liver microsomes. After incubation for 15 min at 37 degrees celsius, the reaction was stopped by the addition of methylene chloride.Duration : 15 min.Type of interaction : PharmacokineticsInteraction with drug : TestosteroneDose/Conc.(drug) : 0.2 mM testosteroneResult : NegativeRemark : Result: Neither compound markedly inhibited 6beta-hydroxylation of testosterone by human liver microsomes or recombinant human CYP3A4.
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : 6',7'-DihydroxybergamottinType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 6',7'-Dihydroxybergamottin 0 to 50 micromol/L.Duration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Result: Seville orange juice reduced enterocyte concentrations of CYP3A4 an average of 40%.Note : Conclusions: 6'7'-Dihydroxybergamottin is not responsible for the effects of grapefruit juice on cyclosporine. Because the interaction did not occur with Seville orange juice despite reduced enterocyte concentrations of CYP3A4, inhibition of P-glycoprotein activity by other compounds in grapefruit juice may be responsible. Reduced enterocyte CYP3A4 by 6',7'-dihydroxybergamottin could be important for other drugs whose bioavailability is less dependent on P-glycoprotein. Data incomplete.
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Crude extract was prepared from squeezed juice of Citrus sinensisType 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 : Result: Crude extract prepared from juice of Citrus sinensis exhibited IC50 values of 153.20 +/- 43.83 microgram/mL, compared with that of grapefruit juice crude extract at 76.96 +/- 12.28 microgram/mL. The preincubation of citrus crude extract with cytochrome P450 3A4 in the presence of NADPH led to the enhancement of cytochrome P450 3A4 inhibition. Percent inhibition at the preincubation period of 15 minutes demonstrated 57.86 +/- 6.90% compared with 45.12 +/- 3.01% at 0 minute preincubation period for Citrus sinensis.Note : Data incomplete
