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Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : grapefruit juice serum (aqueous extract)Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : For the mechanism-based inhibition study, 5 pmol of cDNA-expressed CYP3A4 in 35 microL potassium phosphate buffer was incubated, in triplicate, with 1 microL of a 50-fold concentrated solution of serum. The reaction was initiated with NADPH (1-mmol/L final concentration). After 0 and 15 minutes, 15 microL of this primary incubation mixture was diluted (1:40) into 585 microL of secondary reaction mixture containing NADPH (1 mmol/L), BFC (25 micromol/L), bovine serum albumin (40 microg/mL), and magnesium chloride (3 mmol/L) in potassium phosphate buffer.Duration : 15 minType of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Result: Aftera 40-fold dilution, without preincubation (corresponding to a DHB concentration of approximately 1 micromol/L), CYP3A4 activity was inhibited by 40%+/-9% relative to vehicle. After a 15-minute preincubation, activity was inhibited by 88%+/-2%. These results translated into 79%+/-6% mechanism-based inhibition of the enzyme by serum. The 95% Cl for this difference was 1%+/-9%.
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : 6',7'-dihydroxybergamottin (DHB)Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : For the mechanism-based inhibition study, 5 pmol of cDNA-expressed CYP3A4 in 35 microL potassium phosphate buffer was incubated, in triplicate, with 1 microL of a 50-fold concentrated solution of serum. The reaction was initiated with NADPH (1-mmol/L final concentration). After 0 and 15 minutes, 15 microL of this primary incubation mixture was diluted (1:40) into 585 microL of secondary reaction mixture containing NADPH (1 mmol/L), BFC (25 micromol/L), bovine serum albumin (40 microg/mL), and magnesium chloride (3 mmol/L) in potassium phosphate buffer.Duration : 15 minType of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Result: Aftera 40-fold dilution, without preincubation, CYP3A4 activity was inhibited by 35%+/-4% relative to vehicle. After a 15-minute preincubation, activity was inhibited by 86%+/-3%. These results translated into 78%+/-5% mechanism-based inhibition of the enzyme by purified DHB. The 95% Cl for this difference was 1%+/-9%.
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : grapefruit juice serum (aqueous extract)Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : To each set of duplicate or triplicate culture inserts (The Caco-2 cell clone P27.7 was cultured on laminin-coated inserts), 2 mL of differentiation medium containing 2 microL of a 1000-fold concentrated solution of serum was added to the apical compartment, followed by 2.5 mL of plain differentiation medium to the basolateral compartment. The culture inserts were incubated at 37 degress celsius for 0, 2, 4, or 8 hours.Duration : 8 hrs.Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Result: ACYP3A4-expressing Caco-2 cells were incubated with serum (at the concentration used in the clinical study). Compared with vehicle, serum rapidly reduced CYP3A4 protein content in the cells, resulting in losses of 71%, at 8 hours. The time-averaged extents of protein loss by serum was 43% when assessed from the areas under the CYP3A4 protein versus time curves ([AUCvehicle-AUCtreatment]/AUCvehicle).
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : 6',7'-dihydroxybergamottin (DHB)Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : To each set of duplicate or triplicate culture inserts (The Caco-2 cell clone P27.7 was cultured on laminin-coated inserts), 2 mL of differentiation medium containing DHB (30 micromol/L) was added to the apical compartment, followed 2.5 mL of plain differentiation medium to the basolateral compartment. The culture inserts were incubated at 37 degress celsius for 0, 2, 4, or 8 hours.Duration : 8 hrs.Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Result: ACYP3A4-expressing Caco-2 cells were incubated with purified DHB. (Under our cell culture conditions [0.1% ethanol], the limit of solubility of DHB was 30 micromol/L; therefore 30 micromol/L was tested [rather than 38 micromol/L]). Compared with vehicle, purified DHB rapidly reduced CYP3A4 protein content in the cells, resulting in losses of 66%, at 8 hours. The time-averaged extents of protein loss by purified DHB was 43% when assessed from the areas under the CYP3A4 protein content versus time curves ([AUCvehicle-AUCtreatment]/AUCvehicle).
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: Grapefruit juice reduced enterocyte concentrations of CYP3A4, inhibition of P-glycoprotein ativity by other compounds, 6',7'-Dihydroxybergamottin not.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 : grapefruit juice (GFJ)Type of experiment : in vitroType of animal : -Type of study : Cross-sectionN(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : TacrolimusDose/Conc.(drug) : -Result : PositiveRemark : Result: GFJ significantly inhibited 6beta-hydroxylation of testosterone in human liver microsomes by 83.9%.Note : In conclusion, pomelo constituents inhibit the activity of CYP3A4 and may thereby produce an increase in the blood level of tacrolimus. Data incomplete
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Crude extract was prepared from squeezed juice of grapefruitType 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: Grapefruit juice crude extract exhibited IC50 values of 76.96 +/- 12.28 microgram/mLNote : Data incomplete
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : bergaptolType 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 : Bergaptol was found to be potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 micromolar.Note : Data incomplete
Part Used : เปลือกผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : bergaptolType 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 : Bergaptol was found to be potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 micromolar.Note : Data incomplete
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : geranylcoumarinType 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 : Geranylcoumarin was found to be potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 42.93 micromolar.Note : Data incomplete
