title: Luteolin-inhibited arylamine N-acetyltransferase activity and DNA-2-aminofluorene adduct in human and mouse leukemia cells.
abstract: N-Acetyltransferase enzyme is an important enzyme in the first step of arylamine compounds metabolism. Luteolin has been shown to exit antibacterial and antineoplastic activity. The purpose of this present study is to evaluate the question of whether luteolin could affect arylamine N-acetyltransferase (NAT) activity and DNA-2-aminofluorene adduct formation in human (HL-60) and mouse (L1210) leukemia cells. By using HPLC, N-acetylation of 2-aminofluorene was determined. Luteolin displayed a dose-dependent inhibition to cytosolic NAT activity and intact human and mice leukemia cells. Time-course experiments showed that N-acetylation of 2-aminofluorene measured from intact human and mice leukemia cells were inhibited by luteolin for up to 24 hours. Using standard steady-state kinetic analysis, it was demonstrated that luteolin was a possible uncompetitive inhibitor to NAT activity in cytosols. The DNA-2-aminofluorene adduct formation in human and mouse leukemia cells were inhibited by luteolin. This report is the first demonstration to show that luteolin affects human and mice leukemia cells NAT activity and DNA-2-aminofluorene on adduct formation.
authors.affiliation: Department of Medical Technology, Chung Tai Institute of Health Sciences and Technology, Taichung 400, ROC, Taiwan
authors.forename: Y C
authors.initials: YC
authors.lastname: Li
authors.forename: C F
authors.initials: CF
authors.lastname: Hung
authors.forename: F T
authors.initials: FT
authors.lastname: Yeh
authors.forename: J P
authors.initials: JP
authors.lastname: Lin
authors.forename: J G
authors.initials: JG
authors.lastname: Chung
mesh_terms: D015073:2-Acetylaminofluorene / Q000378:metabolism; D000107:Acetylation; D000818:Animals; D001191:Arylamine N-Acetyltransferase / Q000037:antagonists & inhibitors*; D003600:Cytosol / Q000378:metabolism; D018736:DNA Adducts / Q000032:analysis / Q000037:antagonists & inhibitors* / Q000737:chemistry; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000494:pharmacology; D005419:Flavonoids / Q000494:pharmacology*; D005449:Fluorenes / Q000737:chemistry; D006801:Humans; D007700:Kinetics; D007938:Leukemia / Q000378:metabolism*; D047311:Luteolin; D051379:Mice; D014407:Tumor Cells, Cultured
chemical_list: D018736:DNA Adducts; D004791:Enzyme Inhibitors; D005419:Flavonoids; D005449:Fluorenes; C012177:2-aminofluorene; D015073:2-Acetylaminofluorene; D001191:Arylamine N-Acetyltransferase; D047311:Luteolin