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Part Used : หัวActivity : CYP3A4 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 : CYP3A4 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 : น้ำมันActivity : CYP3A4 INHIBITIONSolvent/Active Compound :Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 12 (M/F=6/6)N(Treatment) : 12 (M/F=6/6)Sex : Both sexAge : 67+/-5.2 yrs.Route : Oral administrationDose/Conc.(herb) : 500 mg three times dailyDuration : 28 daysType of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : 8 mgResult : NegativeRemark :Note : Twelve healthy volunteers were randomly assigned to receive each botanical supplement for 28 days followed by a 30-day washout period. Probe drug cocktails of midazolam, caffeine, chlorzoxazone and debrisoquine were administered before (days -1, 0) and at the end of supplementation (days 27, 28). Pre- and post-supplementation phenotypic ratios were determined for CYP3A4, CYP1A2, CYP2E1 and CYP2D6 using 1-hydroxymidazolam/midazolam serum ratios (1-hour), paraxanthine/caffeine serum ratios (6-hour), 6-hydroxychlorzoxazone/chlorzoxazone serum ratios (2-hour) and debrisoquine urinary recovery ratios (8-hour), respectively.
Part Used : -Activity : CYP3A4 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 : Ketoconazole*/Nizoral/Levoketoconazole/Panfungol/Ketoisdin/Orifungal M/Ketozole/Normocort/Ketoderm/Fungarest/Fungoral/Extina/Ketoconazolum/Brizoral/Kuric/Ketoconazol/Xolegel/Onofin K/Teryzolin/TerzolinDose/Conc.(drug) : -Result : NegativeRemark : The IC50/IC25 ratios for the inhibiting herbal remedies ranged from 2.15 to 2.67, indicating similar inhibition profiles of the herbal inhibitors of CYP3A4. Garlic and Natto K2 were classified as non-inhibitors. Although Agaricus, noni juice, mistletoe and green tea inhibited CYP3A4 metabolism in vitro, clinically relevant systemic or intestinal interactions with CYP3A4 were considered unlikely, except for a probable inhibition of intestinal CYP3A4 by the green tea product.Note : Testosterone was used as a substrate and ketoconazole as a positive quantitative inhibition control.
Part Used : -Activity : CYP3A4 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 : CYP3A4 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 : CYP3A4 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 : CYP3A4 INHIBITIONSolvent/Active Compound : -Type of experiment : humanType of animal : -Type of study : Cross overN(Total) : 18N(Treatment) : 18Sex : MaleAge : -Route : Oral administrationDose/Conc.(herb) : allicin capsule 180 mg once dailyDuration : 14 daysType of interaction : PharmacokineticsInteraction with drug : OmeprazoleDose/Conc.(drug) : -Result : NegativeRemark : The results of this study demonstrate that allicin reduces the metabolism of omeprazole by inhibiting CYP2C19 activity in healthy Chinese male subjects with the genotype CYP2C19*1/CYP2C19*1 or CYP2C19*1/CYP2C19*2 or*3 but not CYP2C19*2/CYP2C19*2. Allicin did not significantly affect the activity of CYP3A4 in all subjects after 14 days of exposure.Note : - Eighteen subjects (six CYP2C19*1/CYP2C19*1, four CYP2C19*1/CYP2C19*2, two CYP2C19*1/CYP2C19*3, and six CYP2C19*2/CYP2C19*2) - On the 15th day, all subjects were given a single oral dose of omeprazole (20 mg capsule) with 250 ml of warm water after an overnight fast.
Part Used : เหง้าActivity : CYP3A4 INHIBITIONSolvent/Active Compound : -Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 25 microgram/mlDuration : 5 minutesType of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : -Result : PositiveRemark : - Details of the standardized Garlic extracts: Garlic extract 100:1 (m/m), Allicin scordinin alliin.Note : The effects of complementary and alternative medicine (CAM) on CYP3A4-mediated metabolism of midazolam and docetaxel were determined in human liver microsomes (HLM), using liquid-chromatography coupled to tandem mass spectrometry (LC-MS/MS).
Part Used : เหง้าActivity : CYP3A4 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 : 30 minutesType of interaction : PharmacokineticsInteraction with drug : Docetaxel*/TaxotereDose/Conc.(drug) : -Result : PositiveRemark : - Details of the standardized Garlic extracts: Garlic extract 100:1 (m/m), Allicin scordinin alliin.Note : The effects of complementary and alternative medicine (CAM) on CYP3A4-mediated metabolism of midazolam and docetaxel were determined in human liver microsomes (HLM), using liquid-chromatography coupled to tandem mass spectrometry (LC-MS/MS).
