Biotransformation and toxicity of the lipoxygenase inhibitor 2-hydroxy-5-methyllaurophenone oxime (FLM 5011) on Hep G2 cells.
2-Hydroxy-5-methyllaurophenone oxime (FLM 5011) is an inhibitor of lipoxygenase with antiinflammatory and antiallergic actions. We incubated FLM 5011 on the human immortal cell line Hep G2 and found a similar metabolite spectrum as in rat urine and faeces. We also measured the cytotoxicity of FLM 5011 on Hep G2 monolayers by the amido black assay and found that the influence of cell proliferation is partly due to apoptotic activities. Although the metabolic activity of Hep G2 cells is lower compared to rat hepatocyte cultures they are a suitable test system for biotransformation studies. Their higher proliferation rate allows toxicity to be characterised more exactly.
Mühlenfeld
K
K
Institut für Pharmazie, Humboldt Universität zu Berlin, Germany.
Langner
A
A
D000818:Animals; D018926:Anti-Allergic Agents / Q000378:metabolism / Q000633:toxicity; D000893:Anti-Inflammatory Agents / Q000378:metabolism / Q000633:toxicity; D017209:Apoptosis / Q000187:drug effects; D001711:Biotransformation; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D004247:DNA / Q000187:drug effects; D004587:Electrophoresis, Agar Gel; D006801:Humans; D007850:Lauric Acids; D016859:Lipoxygenase Inhibitors / Q000378:metabolism* / Q000633:toxicity; D008099:Liver / Q000166:cytology / Q000187:drug effects; D010091:Oximes; D051381:Rats; D014407:Tumor Cells, Cultured
D018926:Anti-Allergic Agents; D000893:Anti-Inflammatory Agents; D007850:Lauric Acids; D016859:Lipoxygenase Inhibitors; D010091:Oximes; C059535:FLM 5011; D004247:DNA