TABLE 3

IC50 of ZJP, berberine, and coptisine toward VEN metabolism in microsomes and rhCYP2D6

InhibitorsIC50 value
ODVNDVNODV
RLMZJP (μg/ml)129.9 ± 2.6>57542.8 ± 8.0
Berberine (μM)64.5 ± 11.5>100059.5 ± 18.6
Coptisine (μM)27.0 ± 6.2>20016.9 ± 0.1
HLMZJP (μg/ml)30.5 ± 5.5>28811.5 ± 10.2
Berberine (μM)30.5 ± 9.6>500>500
Coptisine (μM)2.3 ± 1.3>100>100
rhCYP2D6*1/*1ZJP (μg/ml)15.4 ± 4.5N/AN/A
Berberine (μM)2.5 ± 0.9
Coptisine (μM)0.7 ± 0.2
rhCYP2D6*10/*10ZJP (μg/ml)2.3 ± 1.0N/AN/A
Berberine (μM)1.5 ± 0.2
Coptisine (μM)2.2 ± 0.2
  • N/A, not applicable.