title: Effect of norcantharidin on N-acetyltransferase activity in HepG2 cells.
abstract: The inhibition ofarylamine N-acetyltransferase (NAT) activity by norcantharidin (NCTD), the demethylated form of cantharidin, in human hepatocellular carcinoma HepG2 cells was investigated. By using high performance liquid chromatography, NAT activity on acetylation of 2-aminofluorene (AF) and p-aminobenzoic acid (PABA) were examined. Two assay systems were performed, one with cellular cytosols, the other with intact HepG2 cell suspensions. The NAT activity in HepG2 cell line was inhibited by norcantharidin in a dose-dependent manner in both types of examined systems: i.e. the greater the concentration of norcantharidin in the reaction, the greater the inhibition of NAT activities. This report is the first to show that norcantharidin has an inhibitory effect on NAT activity in HepG2 cell.
authors.affiliation: Department of Microbiology, China Medical College, Taichung, Taiwan.
authors.forename: L T
authors.initials: LT
authors.lastname: Wu
authors.forename: J G
authors.initials: JG
authors.lastname: Chung
authors.forename: J C
authors.initials: JC
authors.lastname: Chen
authors.forename: W
authors.initials: W
authors.lastname: Tsauer
mesh_terms: D010129:4-Aminobenzoic Acid / Q000378:metabolism; D000107:Acetylation; D000970:Antineoplastic Agents / Q000494:pharmacology*; D001191:Arylamine N-Acetyltransferase / Q000037:antagonists & inhibitors*; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000494:pharmacology*; D002273:Carcinogens / Q000378:metabolism; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004365:Drugs, Chinese Herbal; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005449:Fluorenes / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D013379:Substrate Specificity; D013997:Time Factors; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D019086:Bridged Bicyclo Compounds, Heterocyclic; D002273:Carcinogens; D004365:Drugs, Chinese Herbal; D004791:Enzyme Inhibitors; D005449:Fluorenes; C012177:2-aminofluorene; C069741:norcantharidin; D001191:Arylamine N-Acetyltransferase; D010129:4-Aminobenzoic Acid