Hypericin as a non-antioxidant inhibitor of NF-kappa B.
NF-kappa B is a transcription factor involved in immune and inflammatory responses. Here we show that micromolar concentrations of hypericin inhibited the PMA- and TNF-alpha-induced activation of NF-kappa B in HeLa and TC10 cells, respectively. In contrast, NF-kappa B activated by H2O2 was not influenced by hypericin, indicating a pathway-specificity of hypericin. Hyperforin and a Hypericum perforatum extract standardised on 0.15% hypericin and 5% hyperforin were not active at pharmacologically relevant concentrations. The PMA/TNF-alpha-induced transcription of a reporter gene, which is under the control of the NF-kappa B-dependent IL-6 promoter, was strongly reduced by preincubation with hypericin.
Bork
P M
PM
Institute of Pharmaceutical Biology, Albert-Ludwigs University, Freiburg, Germany.
Bacher
S
S
Schmitz
M L
ML
Kaspers
U
U
Heinrich
M
M
D000818:Animals; D000873:Anthracenes; D002460:Cell Line; D006367:HeLa Cells; D006801:Humans; D051379:Mice; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010569:Perylene / Q000031:analogs & derivatives* / Q000494:pharmacology; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology; D014409:Tumor Necrosis Factor-alpha / Q000494:pharmacology
D000873:Anthracenes; D016328:NF-kappa B; D014409:Tumor Necrosis Factor-alpha; D010569:Perylene; C004965:hypericin; D013755:Tetradecanoylphorbol Acetate