Table 1

Glucuronidation of entacapone and tolcapone (500 μM) by different UGT sources at 50 μM and 2 mM UDP-glucuronic acid

UGT SourceEntacapone ActivityTolcapone ActivityControl Activity
50 μM2 mM50 μM2 mMSubstrate (500 μM)2 mM
nmol min−1mg−1 nmol min−1 mg−1 nmol min−1 mg−1
UGT1A10.0020.036, 0.0261-a N.D.N.D.Octylgallate0.81
UGT1A6N.D.N.D.N.D.N.D.1-Naphthol1.4
UGT1A90.171.30.0100.73Propofol0.78
UGT2B70.0060.0730.0020.0344-Hydroxyestrone0.45
UGT2B150.0030.0450.001N.D.8-Hydroxyquinoline0.36
HLM0.142.00.0080.69
HKM0.082.30.0150.76
  • N.D., not detectable; HLM, human liver microsomes; HKM, human kidney microsomes.

  • 1-a  Two peaks detected.