K1115 A, a new anthraquinone derivative that inhibits the binding of activator protein-1 (AP-1) to its recognition sites. I. Biological activities.
K1115 A, a new anthraquinone derivative, was isolated from the culture broth of Streptomyces griseorubiginosus (Mer-K1115). K1115A inhibited the direct binding of activator protein-1 (AP-1) to AP-1 oligonucleotide (IC50 = 100 microM), and the production of collagenase in IL-1 alpha-stimulated rat synovial cells (IC50 = 60 microM). In vivo, the application of K1115 A decreased phorbol myristate acetate (PMA)-induced mouse ornithine decarboxylase (ODC) activity. These results indicated that K1115 A is able to attenuate the inflammatory response mediated by AP-1.
Eisai Tsukuba Research Laboratories, Ibaraki, Japan.
M
M
Goto
M
M
Masegi
T
T
Yamauchi
K
K
Chiba
Y
Y
Kuboi
K
K
Harada
N
N
Naruse
D000818:Animals; D000880:Anthraquinones / Q000302:isolation & purification / Q000494:pharmacology*; D017364:Collagenases / Q000187:drug effects / Q000378:metabolism; D015342:DNA Probes; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D008812:Mice, Hairless; D009955:Ornithine Decarboxylase / Q000187:drug effects / Q000378:metabolism; D011500:Protein Synthesis Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D051381:Rats; D011917:Rats, Inbred Lew; D013302:Streptomyces / Q000378:metabolism*; D018808:Transcription Factor AP-1 / Q000378:metabolism*
D000880:Anthraquinones; D015342:DNA Probes; D011500:Protein Synthesis Inhibitors; D018808:Transcription Factor AP-1; D017364:Collagenases; D009955:Ornithine Decarboxylase