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Part Used : หัวActivity : CYP2C9 INHIBITIONSolvent/Active Compound : allicinType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 98 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) :Result : PositiveRemark : Results: lC50 values (micromolar) of test compounds for CYP1A2 inhibition = 44.22 micromolar lC50 values (micromolar) of test compounds for CYP2C9 inhibition = 5.14 micromolar lC50 values (micromolar) of test compounds for CYP2C19 inhibition = 3.52 micromolar lC50 values (micromolar) of test compounds for CYP2D6 inhibition = 47.10 micromolar lC50 values (micromolar) of test compounds for CYP3A4 (BzRes) inhibition = 60.10 micromolar lC50 values (micromolar) of test compounds for CYP3A4 (BFC) inhibition = 43.73 micromolarNote : Evaluated the effects of 25 purified components of commonly used herbal products on the catalytic activity of cDNA-expressed cytochrome P450 isoforms in in vitro experiments. Increasing concentrations of the compounds were incubated with a panel of recombinant human CYP isoforms (CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4) and their effects on the conversion of specific surrogate substrates measured fluorometrically in a 96-well plate format.
Part Used : หัวActivity : CYP2C9 INHIBITIONSolvent/Active Compound : dihydromethysticinType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 180 micromolarDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) :Result : PositiveRemark : Results: lC50 values (micromolar) of test compounds for CYP1A2 inhibition = 14.8 micromolar lC50 values (micromolar) of test compounds for CYP2C9 inhibition = 13.35 micromolar lC50 values (micromolar) of test compounds for CYP2C19 inhibition = 0.43 micromolar C50 values (micromolar) of test compounds for CYP2D6 inhibition = 37.03 micromolar lC50 values (micromolar) of test compounds for CYP3A4 (BzRes) inhibition = 11.4 micromolar lC50 values (micromolar) of test compounds for CYP3A4 (BFC) inhibition = 2.49 micromolarNote : Evaluated the effects of 25 purified components of commonly used herbal products on the catalytic activity of cDNA-expressed cytochrome P450 isoforms in in vitro experiments. Increasing concentrations of the compounds were incubated with a panel of recombinant human CYP isoforms (CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4) and their effects on the conversion of specific surrogate substrates measured fluorometrically in a 96-well plate format.
Part Used : -Activity : CYP2C9 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 : CYP2C9 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 : CYP2C9 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 : หัวActivity : CYP2C9 INHIBITIONSolvent/Active Compound : -Type 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 : Garlic constituents have been shown to modulate the activity of various CYP isozymes in vitro. These constituents exhibit and inhibitory effect on CYP2C9* 1, CYP2C19, CYP3A4, CYP3A5, and CYP3A7 metabolism, whereas no effect on CYP2D6 was observed.Note : Data incomplete, data from review article
Part Used : หัวActivity : CYP2C9 INHIBITIONSolvent/Active Compound : fresh and aged garlic extractType 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 : Garlic extracts, both fresh and aged, were responsible for the inhibition of CYP3A4 in human liver microsomes, and complementary DNA (cDNA) - expressed CYP2C9, CYP2C19, CYP3A4, CYP3A5, and CYP3A7 activities.Note : Data incomplete, data from review article
