| Synonym |
| Thai / English name |
Part Used : -Activity : CYP3A4 INHIBITIONSolvent/Active Compound : bergamottinType 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 : ImperatoninType 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 : -Remark :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 : NaringeninType 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 : กิ่งActivity : CYP3A4 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.
Part Used : เปลือกผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Furanocoumarins (FCs) (bergamottin (BG) and 6,7-dihydroxybergamottin (DHBG)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 : Result: CYP3A inhibitory activities of crystd. grapefruit peel, grapefruit marmalade, lemon peel and bitter orange slice were close to that of 100% grapefruit juice.Note : The max, BG content was 5.6 microgram/g in lemon peel. The max. DHBG content was 7.2 microgram/g in crystd. grapefruit peel, about 1/30 that of raw peel. Grapefruit marmalade and crystd.grapefruit peel contained similar amts. of FCs to 100% grapefruit juice, but FCs were not detected in pomelo (buntan) marmalade or crystd. iyokan peel. Good correlation (r = 0.78) was obsd. between the FC contents of these peel products and those CYP3A inhibitory activities. Prepn. of homemade grapefruit marmalade and crystd. peel revealed that considerably lower DHBG content in these products and lower CYP3A inhibitory activity than anticipated were attributable to outflow of DHBG to broth during boiling of the raw peel. Data incomplete
