| Synonym |
| Thai / English name |
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : BergaptenType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : For the reversible inhibition study, 22 microliters of cDNA-expressed human CYP3A4 (200 pmol/mL) was preincubated with 10 microliters of freshly prepared NADPH-generating system (yielding final concentrations of 1 mmol/L NADP+, 10 mmol/L of glucose-6-phosphate, and 1 U/mL of glucose-6-phosphate dehydrogenase) and 950 microliters of phosphate buffer (0.1 mol/L or potassium phosphate, 1 mmol/L of ethylenediaminetetraacetic acid, 5 mmol/L magnesium chloride, pH 7.4) at 37 degrees celsius. After 3 minutes, 10 microliters of 0.1, 1, or 10 mol/L bergapten was added, followed by 10 microliters of 0.5 mmol/L saquinavir.Duration : 15 minType of interaction : PharmacokineticsInteraction with drug : SaquinavirDose/Conc.(drug) : 10 microliter of 0.5 mmol/L saquinavirResult : PositiveRemark : Result: Preliminary kinetic studies showed that metabolism of saquinavir to its major metabolite, M-7, were reversibly inhibited by bergapten with a 50% inhibitory concentration that ranged from 10 to 100 micromol/L. Subsequently, bergapten was shown to produce time- and concentration-dependent inhibition of the enzyme.
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : BergaptenType 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, 25 microliters of cDNA-expressed human CYP3A4 (2 mmol/mL) was preincubated with 1.2 microliters of NADPH-generating system and 93 microliters of phosphate buffer. After 3 minutes, 10 microliters of bergapten was added to achieve final concentrations of 0, 0.1, 1, 10, or 100 micromol/L. After 0, 15, and 30 minutes, 10 microliters of reaction mixture was removed and added to 990 microliters of a solution composed of 10 microliters of 0.5 mmol/L of saquinavir, 10 microliters of NADPH-generating system, and 970 microliters of phosphate buffer.Duration : 15 minType of interaction : PharmacokineticsInteraction with drug : SaquinavirDose/Conc.(drug) : 10 microliter of 0.5 mmol/L saquinavirResult : PositiveRemark : Result: Preliminary kinetic studies showed that metabolism of saquinavir to its major metabolite, M-7, were reversibly inhibited by bergapten with a 50% inhibitory concentration that ranged from 10 to 100 micromol/L. Subsequently, bergapten was shown to produce time- and concentration-dependent inhibition of the enzyme.
