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: L T Wu, J G Chung, J C Chen, W Tsauer
• Journal: The American journal of Chinese medicine (Am J Chin Med) Vol. 29 Issue 1 Pg. 161-72 ( 2001) ISSN: 0192-415X [Print] Singapore
• PMID: 11321474 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Bridged Bicyclo Compounds, Heterocyclic
• Carcinogens
• Drugs, Chinese Herbal
• Enzyme Inhibitors
• Fluorenes
• 2-aminofluorene
• norcantharidin
• Arylamine N-Acetyltransferase
• 4-Aminobenzoic Acid

Topics

• 4-Aminobenzoic Acid (metabolism)
• Acetylation
• Antineoplastic Agents (pharmacology)
• Arylamine N-Acetyltransferase (antagonists & inhibitors)
• Bridged Bicyclo Compounds, Heterocyclic (pharmacology)
• Carcinogens (metabolism)
• Cell Survival (drug effects)
• Dose-Response Relationship, Drug
• Drugs, Chinese Herbal
• Enzyme Inhibitors (pharmacology)
• Fluorenes (metabolism)
• Humans
• Kinetics
• Substrate Specificity
• Time Factors
• Tumor Cells, Cultured