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Part Used : รากActivity : CYP3A4 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 : Erythromycin*/ErythrocinDose/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 : รากActivity : CYP3A4 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 : Erythromycin*/ErythrocinDose/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 : รากActivity : CYP3A4 INHIBITIONSolvent/Active Compound : emodin, chrysophanolType of experiment : in silicoType 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 : Result: Emodin could form a strong hydrogen bond with Thr310 (2.4 angstroms) and a relatively weak Pi interaction with Arg212 (6.8 angstroms). No potential interaction existed between chrysophanol and CYP3A4 except Van der Waals. Compared with midazolam, both emodin and chrysophanol were found to be more closely orientated to the center of the heme of CYP3A4.
