Abstract
7b, a novel amonafide analog, has shown high antitumor activity against Raji B-cell lymphoma. We report here that 7b also shows high cytotoxicity against various T lymphoma cells, with the highest IC(50) (concentration for 50% cytotoxicity) value in Jurkat cells. In a previous study, p53-mutant Raji cells were sensitive to 7b treatment. In the present study, the Jurkat T lymphoma cells were characterized as p53-null. Additional assays showed that 7b could induce G1/S phase arrest and mitochondrial apoptosis in Jurkat cells, suggesting 7b as a potential drug candidate for treatment of T-cell lymphoma. This action was not affected by p53 status. Further analysis of molecular mechanisms revealed that up-regulation of p21 and the Bak/Bcl-2 ratio and down-regulation of UHRF1 and c-Myc were attributed to p73 activation. In turn, up-regulation of p73 was initiated by DNA damage-induced reactive oxygen species (ROS) formation. Interestingly, at non-toxic drug concentrations, 7b could also inhibit phorbol 12-myristate 13-acetate/phytohemagglutinin (PMA/PHA)-induced inflammatory responses of Jurkat T cells owing to the suppression of nuclear factor-κB (NF-κB) DNA-binding. Indeed, electrophoretic mobility shift assay and NF-κB binding assay showed that NF-κB DNA-binding was inhibited by 7b, and correspondingly, proinflammatory cytokine production was also decreased. In conclusion, 7b exhibits both antiproliferative and anti-inflammatory activities in T lymphoma cells.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Inflammatory Agents / pharmacology*
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Antineoplastic Agents / pharmacology*
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Apoptosis / drug effects
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Cell Cycle Checkpoints / drug effects
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Cell Cycle Proteins / genetics
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Cell Cycle Proteins / metabolism
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cytokines / biosynthesis
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DNA Damage
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DNA-Binding Proteins / metabolism*
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Gene Expression Regulation, Neoplastic / drug effects
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Humans
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Inflammation / chemically induced
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Inflammation / metabolism
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Inflammation Mediators / metabolism
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Jurkat Cells
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Mitochondria / drug effects
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Mitochondria / metabolism
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NF-kappa B / metabolism*
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Naphthalimides / pharmacology*
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Nuclear Proteins / metabolism*
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Oxidation-Reduction / drug effects
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Phytohemagglutinins
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Proto-Oncogene Proteins c-myc / genetics
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Proto-Oncogene Proteins c-myc / metabolism
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Reactive Oxygen Species / metabolism
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Tetradecanoylphorbol Acetate / analogs & derivatives
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Tumor Protein p73
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Tumor Suppressor Protein p53 / deficiency
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Tumor Suppressor Proteins / metabolism*
Substances
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6-(dodecylamino)-2-(3-(4-methylpiperazin-1-yl)propyl)-1H-benzo-(de)isoquinoline-1,3(2H)-dione
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Anti-Inflammatory Agents
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Antineoplastic Agents
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Cell Cycle Proteins
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Cytokines
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DNA-Binding Proteins
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Inflammation Mediators
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NF-kappa B
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Naphthalimides
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Nuclear Proteins
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Phytohemagglutinins
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Proto-Oncogene Proteins c-myc
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Reactive Oxygen Species
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TP73 protein, human
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Tumor Protein p73
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Tumor Suppressor Protein p53
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Tumor Suppressor Proteins
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phorbolol myristate acetate
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Tetradecanoylphorbol Acetate