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2 Acta Biochimica Polonica

2 2002

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Effect of natural phenols on the catalytic activity of cytochrome P450 2E1

100%

Mikstacka R. , Gnojkowski J. , Baer-Dubowska W.

tom 49

nr 4

917-925

The effect of protocatechuic acid, tannic acid and trans-resveratrol on the activity of p-nitrophenol hydroxylase (PNPH), an enzymatic marker of CYP2E1, was examined in liver microsomes from acetone induced mice. trans-Resveratrol was found to be the most potent inhibitor (IC50 = 18.5 ± 0.4 mM) of PNPH, while protocatechuic acid had no effect on the enzyme activity. Tannic acid with IC50 = 29.6 ± 3.3 mM showed mixed- and trans-resveratrol competitive inhibition kinetics (Ki = 1 mM and 2.1 mM, respectively). Moreover, trans-resveratrol produced a NADPH-dependent loss of PNPH activity, suggesting mechanism-based CYP2E1 inactivation. These results indicate that trans-resveratrol and tannic acid may modulate cytochrome P450 2E1 and influence the metabolic activation of xenobiotics mediated by this P450 isoform.

Effect of natural phenols on the catalytic activity of cytochrome P450 2E1

67%

Mikstacka R. , Gnojkowski J. , Baer-Dubowska W.

Acta Biochimica Polonica

2002

tom 49

nr 4

The effect of protocatechuic acid, tannic acid and trans-resveratrol on the activity of p-nitrophenol hydroxylase (PNPH), an enzymatic marker of CYP2E1, was examined in liver microsomes from acetone induced mice. trans-Resveratrol was found to be the most potent inhibitor (IC50 = 18.5 ± 0.4 uM) of PNPH, while protocatechuic acid had no effect on the enzyme activity. Tannic acid with IC50 = 29.6 ± 3.3 uM showed mixed- and trans-resveratrol competitive inhibition kinetics (Ki = 1 uM and 2.1 uM, respectively). Moreover, trans-resveratrol produced a NADPH-dependent loss of PNPH activity, suggesting mechanism-based CYP2E1 inactivation. These results indicate that trans-resveratrol and tannic acid may modulate cytochrome P450 2E1 and influence the metabolic activation of xenobiotics mediated by this P450 isoform.