TABLE 2

Effect of human serum albumin preparations on the kinetics of zidovudine glucuronidation by human liver microsomes and recombinant UGT2B7

Data for HLM are the mean ± S.D. of four replicates, whereas data for UGT2B7 represent the mean of duplicate experiments. Crude refers to unmodified HSA.

Enzyme Source
Parameter
No Albumin
Crude
FAF
GF
FAFGF
0.1%
2.0%
0.1%
2.0%
0.1%
2.0%
0.1%
2.0%
HLM Km, μM 1113 ± 56 374 ± 16* 1575 ± 69 123 ± 1* 89 ± 4* 119 ± 3* 233 ± 13* 172 ± 6* 422 ± 7*
Vmax, pmol/min · mg 738 ± 13 893 ± 22 810 ± 59 751 ± 15 699 ± 8 725 ± 7 809 ± 18 565 ± 13 673 ± 13
CLint, μl/min · mg 0.663 2.39 0.514 6.10 7.88 6.11 3.48 3.28 1.60
UGT2B7 Km, μM 439 373 891 94 52 131 165 156 258
Vmax, pmol/min · mg 50 48 39 43 47 49 42 40 43
CLint, μl/min · mg
0.113
0.129
0.043
0.451
0.899
0.371
0.254
0.258
0.168

  • ↵* P < 0.05 compared with incubations conducted without albumin.