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Part Used : ทั้งต้นActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Aqueous 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 : NegativeRemark : IC50 values for inhibition of CYP3A4 were 838.9 microgram/mL.Note : - Orthosiphon stamineus (OS) components with IC50 values less than 100 microgram/mL (100 micromolar for active constituents) were subsequently determined for Ki (inhibition constant) values and inhibition modes. - In order to determine the modulatory effects of OS components on CYP activities, the enzyme assays were carried out in the presence and absence of OS extracts or active constituents. Metabolite (4-hydroxytolutamide, dextrophan and 6beta-hydroxytestosterone) formations were estimated using HPLC system. For each inhibition study, preliminary experiments were carried out by incubating a single enzyme specific substrate concentration around its Km with a range of OS extract and active constiuent concentrations to determine IC50 values (concentration on inhibitor causing 50% inhibition of enzyme activity).
Part Used : ทั้งต้นActivity : CYP3A4 INHIBITIONSolvent/Active Compound : methanol 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 : NegativeRemark : IC50 values for inhibition of CYP3A4 were 413.1 microgram/mL.Note : - Orthosiphon stamineus (OS) components with IC50 values less than 100 microgram/mL (100 micromolar for active constituents) were subsequently determined for Ki (inhibition constant) values and inhibition modes. - In order to determine the modulatory effects of OS components on CYP activities, the enzyme assays were carried out in the presence and absence of OS extracts or active constituents. Metabolite (4-hydroxytolutamide, dextrophan and 6beta-hydroxytestosterone) formations were estimated using HPLC system. For each inhibition study, preliminary experiments were carried out by incubating a single enzyme specific substrate concentration around its Km with a range of OS extract and active constiuent concentrations to determine IC50 values (concentration on inhibitor causing 50% inhibition of enzyme activity).
Part Used : ทั้งต้นActivity : CYP3A4 INHIBITIONSolvent/Active Compound : dichloromethane 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 : CYP3A4 was moderately inhibited by OS dichloromethane extract in mixed-type mode with an IC50 value of 96.5 and a Ki value of 93.7 microgram/mL.Note : - Orthosiphon stamineus (OS) components with IC50 values less than 100 microgram/mL (100 micromolar for active constituents) were subsequently determined for Ki (inhibition constant) values and inhibition modes. - In order to determine the modulatory effects of OS components on CYP activities, the enzyme assays were carried out in the presence and absence of OS extracts or active constituents. Metabolite (4-hydroxytolutamide, dextrophan and 6beta-hydroxytestosterone) formations were estimated using HPLC system. For each inhibition study, preliminary experiments were carried out by incubating a single enzyme specific substrate concentration around its Km with a range of OS extract and active constiuent concentrations to determine IC50 values (concentration on inhibitor causing 50% inhibition of enzyme activity).
Part Used : ทั้งต้นActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Petroleum ether 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 : CYP3A4 was found to be noncompetitively inhibited by OS petroleum ether extract with IC50 value of 46.3 and Ki value of 44.9 microgram/mL.Note : - Orthosiphon stamineus (OS) components with IC50 values less than 100 microgram/mL (100 micromolar for active constituents) were subsequently determined for Ki (inhibition constant) values and inhibition modes. - In order to determine the modulatory effects of OS components on CYP activities, the enzyme assays were carried out in the presence and absence of OS extracts or active constituents. Metabolite (4-hydroxytolutamide, dextrophan and 6beta-hydroxytestosterone) formations were estimated using HPLC system. For each inhibition study, preliminary experiments were carried out by incubating a single enzyme specific substrate concentration around its Km with a range of OS extract and active constiuent concentrations to determine IC50 values (concentration on inhibitor causing 50% inhibition of enzyme activity).
Part Used : ทั้งต้นActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Rosmarinic acidType 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 : CYP3A4 was moderate inhibited by rosmarinic acid in uncompetitive inhibition mode with an IC50 value of 86.9 microgram/mL (241.2 micromolar) and a Ki of 118.3 microgram/mL (328.3 micromolar).Note : - Orthosiphon stamineus (OS) components with IC50 values less than 100 microgram/mL (100 micromolar for active constituents) were subsequently determined for Ki (inhibition constant) values and inhibition modes. - In order to determine the modulatory effects of OS components on CYP activities, the enzyme assays were carried out in the presence and absence of OS extracts or active constituents. Metabolite (4-hydroxytolutamide, dextrophan and 6beta-hydroxytestosterone) formations were estimated using HPLC system. For each inhibition study, preliminary experiments were carried out by incubating a single enzyme specific substrate concentration around its Km with a range of OS extract and active constiuent concentrations to determine IC50 values (concentration on inhibitor causing 50% inhibition of enzyme activity).
Part Used : ทั้งต้นActivity : CYP3A4 INHIBITIONSolvent/Active Compound : sinensetinType 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 : NegativeRemark : IC50 values for inhibition of CYP3A4 were >200 microgram/mL (>537.1 micromolar).Note : - Orthosiphon stamineus (OS) components with IC50 values less than 100 microgram/mL (100 micromolar for active constituents) were subsequently determined for Ki (inhibition constant) values and inhibition modes. - In order to determine the modulatory effects of OS components on CYP activities, the enzyme assays were carried out in the presence and absence of OS extracts or active constituents. Metabolite (4-hydroxytolutamide, dextrophan and 6beta-hydroxytestosterone) formations were estimated using HPLC system. For each inhibition study, preliminary experiments were carried out by incubating a single enzyme specific substrate concentration around its Km with a range of OS extract and active constiuent concentrations to determine IC50 values (concentration on inhibitor causing 50% inhibition of enzyme activity).
Part Used : ทั้งต้นActivity : CYP3A4 INHIBITIONSolvent/Active Compound : eupatorinType 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 : CYP3A4 was found to be noncompetitively inhibited by OS petroleum ether extract with IC50 value of 5.0 microgram/mL (14.5 micromolar) and Ki value of 3.2 microgram/mL (9.3 micromolar).Note : - Orthosiphon stamineus (OS) components with IC50 values less than 100 microgram/mL (100 micromolar for active constituents) were subsequently determined for Ki (inhibition constant) values and inhibition modes. - In order to determine the modulatory effects of OS components on CYP activities, the enzyme assays were carried out in the presence and absence of OS extracts or active constituents. Metabolite (4-hydroxytolutamide, dextrophan and 6beta-hydroxytestosterone) formations were estimated using HPLC system. For each inhibition study, preliminary experiments were carried out by incubating a single enzyme specific substrate concentration around its Km with a range of OS extract and active constiuent concentrations to determine IC50 values (concentration on inhibitor causing 50% inhibition of enzyme activity).
Part Used : ไม่ระบุActivity : CYP3A4 INHIBITIONSolvent/Active Compound : -Type of experiment : humanType of animal : -Type of study : Cross-sectionN(Total) : 56 (M/F = 24/32)N(Treatment) : 1Sex : Both sexAge : 68.7 +/- 7.7 yrsRoute : Oral administrationDose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : Amlodipine*/AmlopineDose/Conc.(drug) : -Result : PositiveRemark : หญ้าหนวดแมวมีฤทธิ์ยับยั้งเอนไซม์ CYP3A4 ทำให้ยาเมตาบอไลซ์ผ่าน CYP3A4 ถูกแปรสภาพลดลง ทำให้ระดับยาในเลือดสูงขึ้นNote : Data incomplete, data from review article
Part Used : ไม่ระบุActivity : CYP3A4 INHIBITIONSolvent/Active Compound : ethanolType 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 : The ethanolic extract of Orthosiphon aristatus inhibited CYP3A4 activity with IC50 value 40+/-8.7 microgram/ml.Note : Testosterone 6beta-hydroxylase and dextromethorphan O-demethylase were used as maker of CYP3A4 and CYP2D6 activity, respectively.
Part Used : ไม่ระบุActivity : CYP3A4 INHIBITIONSolvent/Active Compound : aqueousType 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 : The aqueous extract of Orthosiphon aristatus inhibited CYP3A4 activity with IC50 value 286.7+/-65.1 microgram/ml.Note : Testosterone 6beta-hydroxylase and dextromethorphan O-demethylase were used as maker of CYP3A4 and CYP2D6 activity, respectively.
