ABSTRACT
Objective:To investigate the effect of extract of mung bean seed coat ( MBSC) on the activity of CYP3A4 in vitro. Methods:Midazolam was used as the probe drug, and an HPLC method for determining the metabolite of midazolam ( l-hydroxyl mid-azolam) in rat liver microsome incubation system was established. Three important parameters including the incubation time, concen-tration of rat microsome and probe concentration were optimized for rat liver microsome incubation system, and then the optimal incuba-tion system was applied to study the effect of MBSC extract on CYP3A4 activity and the potential mechanism. Results: The results showed MBSC crude extract could inhibit CYP3A4 activity to 38. 14% as that in the control group(P<0. 05) with IC50 value of 489. 7μg·ml-1 . The mechanism might be related to competition-noncompetition inhibition. Conclusion: MBSC extract exhibits inhibitive potency to CYP3A4 in in-vitro model. Further studies should be conducted to check the influence of MBSC on CYP3A4 in vivo.
ABSTRACT
Objective:To investigate the effect of extract of mung bean seed coat ( MBSC) on the activity of CYP3A4 in vitro. Methods:Midazolam was used as the probe drug, and an HPLC method for determining the metabolite of midazolam ( l-hydroxyl mid-azolam) in rat liver microsome incubation system was established. Three important parameters including the incubation time, concen-tration of rat microsome and probe concentration were optimized for rat liver microsome incubation system, and then the optimal incuba-tion system was applied to study the effect of MBSC extract on CYP3A4 activity and the potential mechanism. Results: The results showed MBSC crude extract could inhibit CYP3A4 activity to 38. 14% as that in the control group(P<0. 05) with IC50 value of 489. 7μg·ml-1 . The mechanism might be related to competition-noncompetition inhibition. Conclusion: MBSC extract exhibits inhibitive potency to CYP3A4 in in-vitro model. Further studies should be conducted to check the influence of MBSC on CYP3A4 in vivo.