Table 1.
.Specific Activity of Mammalian and Human Liver Carboxylesterases toward Pyrethroid-like Fluorescent Substratesa
substrates | porcineb | rabbitb | humanc hCE1 | moused NM_133960 | moused BAC36707 |
---|---|---|---|---|---|
Cypermethrin Analogues | |||||
1R cis, αR | 2.35(0.17) | 5.67(0.49) | 0.60(0.02) | 3.94(0.37) | 19.74(2.18) |
1S cis, αR | 2.45(0.22) | 5.71(0.83) | 0.36(0.13) | 7.44(0.66) | 8.44(0.37) |
1R trans, αR | 26.8(1.8)e | 12.2(1.4) | 16.0(1.60)e | 7.63 (0.27) | 26.2(2.8)e |
1S trans, αR | 51.0(2.6)e | 37.5(2.6)e | 21.3(2.2)e | 85.1(3.2)e | 281(24)e |
1R cis, αS | 33.4(4.5)e | 7.41(0.04) | 0.64(0.06) | 20.3(0.1)e | 2.28(0.31) |
1S cis, αS | 6.62(0.46) | 3.73(0.37) | 0.66(0.05) | 8.69(0.85) | 6.69(1.06) |
1R trans, αS | 42.4(3.8)e | 55.6(7.5)e | 55.2(3.1)e | 7.34(0.76) | 14.6(1.2)e |
1S trans, αS | 61.2(1.8)e | 83.4(11.3)e | 14.7(1.3)e | 155(2)e | 327(25)e |
Fenvalerate Analogues | |||||
2R,αR | 1.62(0.07) | 17.1(1.0)e | 0.38(0.01)e | 10.3(0.4)e | 40.3(2.6)e |
2R, αS | 8.34(0.35) | 15.0(0.4)e | 0.58(0.10)e | 15.2(0.3)e | 54.2(3.4)e |
2S,αR | 4.31 (0.32) | 0.25(0.04) | NDf | 0.63(0.05) | NDf |
2S, αS | 2.66(0.20) | 4.61(0.04) | 0.04(0.03) | 0.79(0.11) | NDf |
Values stand for mean activities ((nmol/min)/mg protein, SD in parentheses) based on triplicate assays.
Porcine and rabbit liver carboxylesterases are commercial from Sigma-Aldrich; they were mixtures of multiple isozymes.
Human (hCE1) carboxy-lesterase was expressed in insect cells with a recombinant bacu-lovirus expression system, then recombinant hCE1 was sequentially purified by anion-exchange chromatography, preparative electrophoresis, and gel-filtration chromatography.
Mouse: two recombinant mouse liver carboxylesterase (NCBI accession nos. NM_133960 and BAC36707) were recently purified (12), and data were presented in ref 13.
Preference was considered if one stereoisomer is hydrolyzed by one carboxylesterase over 5 times faster than the least favored isomer in a single series.
ND = not detectable under the same protein as other stereoisomers.