TABLE 1

Derived morphine glycosidation kinetic constants generated in the absence and presence of BSA (2% w/v) with morphine as the variable substrate

Data are shown as the mean ± S.D. for HLM from five separate livers.

PathwayCofactorWithout BSAWith BSA
Km or S50VmaxCLintnKm or S50VmaxCLintn
mMpmol/min/mgµl/min/mgmMpmol/min/mgµl/min/mg
Morphine 3-glucosideUDP-Glc5.56 ± 1.031581 ± 6310.30 ± 0.140.63 ± 0.12b1536 ± 5602.54 ± 1.29b
1:1e3.82 ± 0.26c260 ± 25d0.07 ± 0.01d0.89 ± 0.14b,c265 ± 18d0.30 ± 0.03b,d0.77 ± 0.01
M3GUDP-GlcUA3.63 ± 1.112803 ± 5990.82 ± 0.240.86 ± 0.030.45 ± 0.09b2429 ± 588a5.74 ± 2.32b0.83 ± 0.04
1:15.07 ± 0.29c2747 ± 1630.54 ± 0.02c0.93 ± 0.020.61 ± 0.09b,c2500 ± 1344.14 ± 0.35b0.89 ± 0.03
M6GfUDP-GlcUA2.88 ± 1.21387 ± 790.15 ± 0.050.89 ± 0.030.36 ± 0.07b353 ± 961.03 ± 0.41b
1:14.72 ± 0.43c460 ± 400.10 ± 0.02c0.51 ± 0.08b,c396 ± 200.78 ± 0.08b
  • a P < 0.05; comparisons for each glycoside ± BSA for single cofactor experiments.

  • b P < 0.01; comparisons for each glycoside ± BSA for single cofactor experiments.

  • c P < 0.05; comparisons for each glycoside between single and mixed cofactor experiments.

  • d P < 0.01; comparisons for each glycoside between single and mixed cofactor experiments.

  • e 1:1; combination of 5 mM UDP-Glc and 5 mM UDP-GlcUA.

  • f Ksi for M6G formation in presence of BSA = 62 ± 6 mM.