Effects of luteolin on arylamine N-acetyltransferase activity in human liver tumour cells.

Cytobios Pub Date : 2000-01-01
J C Chen, J G Chung, K M Lin
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Abstract

The human liver tumour cell line (J5) was selected in order to evaluate whether or not luteolin affected arylamine N-acetyltransferase (NAT) activity. Using high performance liquid chromatography, the NAT activity for acetylation of arylamine substrates (2-aminofluorene and p-aminobenzoic acid) was determined. The cytosolic NAT activity in human liver tumour cells was 2.74+/-0.26 and 1.68+/-0.20 nmol/min/mg of protein for 2-aminofluorene and p-aminobenzoic acid, respectively. Luteolin displayed a dose-dependent inhibition to cytosolic NAT activity and intact human liver tumour cells. Time-course experiments showed that NAT activity measured from intact human liver tumour cells was inhibited by luteolin for up to 24 h. Using standard steady-state kinetic analysis, it was shown that luteolin was a possible noncompetitive inhibitor to NAT activity in cytosols. This report is the first to show how luteolin affects NAT activity in human liver tumour cells.

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木犀草素对人肝肿瘤细胞芳胺n -乙酰转移酶活性的影响。
以人肝癌细胞株J5为实验材料,研究木犀草素对芳胺n -乙酰转移酶(NAT)活性的影响。采用高效液相色谱法测定了芳胺底物(2-氨基芴和对氨基苯甲酸)乙酰化的NAT活性。人肝肿瘤细胞中2-氨基芴和对氨基苯甲酸的胞质NAT活性分别为2.74+/-0.26和1.68+/-0.20 nmol/min/mg。木犀草素对细胞质内NAT活性和完整的人肝癌细胞具有剂量依赖性的抑制作用。时间过程实验表明,木犀草素可以抑制完整的人肝肿瘤细胞的NAT活性长达24小时。通过标准稳态动力学分析,木犀草素可能是细胞质中NAT活性的非竞争性抑制剂。该报告首次展示了木犀草素如何影响人类肝脏肿瘤细胞的NAT活性。
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