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Part Used : เปลือกต้นActivity : CYP2D6 INHIBITIONSolvent/Active Compound : methanolType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 1.65 mg/ml of water extract powderDuration : -Type of interaction : PharmacokineticsInteraction with drug : Dextromethorphan*/Dextromethorfan/DextromorphanDose/Conc.(drug) : -Result : PositiveRemark : Among the MeOH-soluble fractions, Piper nigrum leaf showed the highest inhibitory activity against CYP3A4 (91.7%) and Punica granatum against CYP2D6 (98.1%). The water extract MeOH-soluble fraction showed inhibitory activity more than 70% were fractionated with EtOAc. The most potent inhibitory activity against CYP3A4 (IC50 avlue of 25 mg/ml) was found for the extract of Pi. nigrum leaf, while that of Catharanthus roseus showed the most potent inhibitory effect against CYP2D6 (IC50 value of 11 mg/ml).Note : Ketoconazole and quinidine (1 micromolar) were used as the positive control for CYP3A4 and CYP2D6, respectively.
Part Used : เปลือกต้นActivity : CYP2D6 INHIBITIONSolvent/Active Compound : ethylacetateType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 1.65 mg/ml of water extract powderDuration : -Type of interaction : PharmacokineticsInteraction with drug : Dextromethorphan*/Dextromethorfan/DextromorphanDose/Conc.(drug) : -Result : PositiveRemark : Among the MeOH-soluble fractions, Piper nigrum leaf showed the highest inhibitory activity against CYP3A4 (91.7%) and Punica granatum against CYP2D6 (98.1%). The water extract MeOH-soluble fraction showed inhibitory activity more than 70% were fractionated with EtOAc. The most potent inhibitory activity against CYP3A4 (IC50 avlue of 25 mg/ml) was found for the extract of Pi. nigrum leaf, while that of Catharanthus roseus showed the most potent inhibitory effect against CYP2D6 (IC50 value of 11 mg/ml).Note : Ketoconazole and quinidine (1 micromolar) were used as the positive control for CYP3A4 and CYP2D6, respectively.
Part Used : ใบActivity : CYP2D6 INHIBITIONSolvent/Active Compound : 100% methanolType 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 : - Dried, plant samples (~10 g) were extracted in 100 mL of 100% methanol (MeOH) evernight. - Plant extracts were screened for the ability to induce CYP1A2 and CYP3A4. 1A2DRE (human XRECYP1A2-luciferase promoter) and DPX2 (human PXRCYP3A4-luciferase promoter) in hepatoma cell lines. Criteria for "positive" plant samples was set at ~40% of the response seen for the prototype inducers, i.e., > 40-fold in luciferase activity for CYP1A2 and > 3.5-fold increase for CYP3A4. - Plant extracts were screened for inhibitiory activity towards CYP1A2, CYP3A4, and CYP2D6 using enzyme-selective model substrates in human liver microsomes. Methoxyresorufin (MR) was used to assess CYP1A2 activity, 7-benzyloxyquinoline (7-BQ) was used to assess CYP3A4 activity and 7-methoxy-4-(aminomethyl)-coumarin (MAMC) was used to assess CYP2D6 activity. Extracts showing >50% inhibition at half-saturating and/or saturating substrate concentrations were deemed inhibitory.
