UGT Activity in Liver Microsomes (nmol/min/mg protein)b | ||||||||||||||||||||||||||||
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Treatmenta | Dose/kg | 1-OHP | Entacapone | 1-Naphthol | ||||||||||||||||||||||||
1 μM | % | 15 μM | % | 100 μM | % | 150 μM | % | 250 μM | % | 1 mM | % | 500 μM | % | |||||||||||||||
Olive oil | 2.5 ml | 0.47 ± 0.13 | 100 | 3.60 ± 0.50 | 100 | 12.8 ± 1.5 | 100 | 21.6 ± 3.1 | 100 | 0.124 ± 0.030 | 100 | 0.202 ± 0.034 | 100 | 5.99 ± 0.88 | 100 | |||||||||||||
Aroclor 1254 | 550 mg | 7.67 ± 2.59*** | 1628 | 36.52 ± 10.34*** | 1014 | 52.0 ± 6.3*** | 406 | 116.4 ± 10.4*** | 539 | 1.000 ± 0.228*** | 806 | 1.456 ± 0.378*** | 721 | 32.87 ± 5.69*** | 549 | |||||||||||||
Sucrose | 100 mg | 0.42 ± 0.04 | 100 | 4.74 ± 0.34 | 100 | 9.5 ± 1.1 | 100 | 19.3 ± 2.9 | 100 | 0.100 ± 0.010 | 100 | 0.160 ± 0.015 | 100 | 6.22 ± 0.60 | 100 | |||||||||||||
4-Methylcatechol | 100 mg | 0.50 ± 0.07* | 121 | 5.25 ± 0.26* | 111 | 11.9 ± 1.0* | 125 | 23.3 ± 1.6* | 120 | 0.134 ± 0.018** | 134 | 0.200 ± 0.017** | 125 | 7.73 ± 0.43*** | 124 | |||||||||||||
4-Methylcatechol | 150 mg | 0.45 ± 0.09 | 107 | 5.14 ± 0.78 | 108 | 11.0 ± 1.4 | 116 | 19.2 ± 4.3 | 99 | 0.111 ± 0.016 | 111 | 0.165 ± 0.023 | 103 | 6.59 ± 1.64 | 106 | |||||||||||||
4-Nitrocatechol | 100 mg | 0.44 ± 0.06 | 106 | 4.94 ± 0.32 | 104 | 10.7 ± 1.5 | 113 | 18.6 ± 2.7 | 96 | 0.107 ± 0.016 | 107 | 0.158 ± 0.011 | 99 | 6.26 ± 1.04 | 101 | |||||||||||||
4-Nitrocatechol | 200 mg | 0.48 ± 0.09 | 115 | 4.89 ± 0.98 | 103 | 9.8 ± 1.4 | 103 | 17.6 ± 3.3 | 91 | 0.128 ± 0.008*** | 128 | 0.165 ± 0.020 | 103 | 6.93 ± 0.79 | 111 | |||||||||||||
Olive oil | 3.0 ml | 0.45 ± 0.10 | 100 | 4.00 ± 0.47 | 100 | 11.4 ± 1.6 | 100 | 21.1 ± 3.5 | 100 | 0.111 ± 0.027 | 100 | 0.147 ± 0.038 | 100 | 6.40 ± 1.60 | 100 | |||||||||||||
2,3-DHN | 300 mg | 0.61 ± 0.14* | 136 | 4.18 ± 0.22 | 105 | 10.8 ± 1.6 | 95 | 25.5 ± 3.7* | 121 | 0.159 ± 0.012** | 143 | 0.221 ± 0.013** | 150 | 7.85 ± 0.83 | 123 | |||||||||||||
Olive oil | 3.0 ml | 0.33 ± 0.06 | 100 | 3.17 ± 0.32 | 100 | 11.0 ± 1.7 | 100 | 25.7 ± 4.5 | 100 | 0.085 ± 0.017 | 100 | N.D. | 6.05 ± 1.03 | 100 | ||||||||||||||
Entacapone | 200 mg | 0.35 ± 0.05 | 107 | 3.68 ± 0.51* | 116 | 13.6 ± 0.9* | 123 | 30.1 ± 2.7* | 117 | 0.112 ± 0.021* | 132 | N.D. | 7.86 ± 1.09* | 130 | ||||||||||||||
Tolcapone | 200 mg | 0.46 ± 0.06** | 139 | 4.15 ± 0.94* | 131 | 12.2 ± 3.5 | 111 | 28.2 ± 6.2 | 110 | 0.115 ± 0.022* | 135 | N.D. |
| 7.30 ± 1.78 | 121 |