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详细内容
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Thiocoraline is a depsipeptide and DNA bis-intercalator originally isolated from Micromonospora with antibacterial and anticancer activities.1,2 It is active against the Gram-positive bacteria S. aureus, B. subtilis, and M. luteus (MICs = 0.05, 0.05, and 0.03 μg/ml, respectively) but not Gram-negative E. coli, K. pneumoniae, or P. aeruginosa (MICs = >100 μg/ml for all).1 Thiocoraline inhibits RNA and DNA polymerase and thymidylate synthase (IC50s = 6, 6, and 15 μg/ml, respectively), as well as RNA and DNA synthesis in vitro (IC50s = 0.008 and 0.4 μg/ml, respectively). It is cytotoxic to P388, A549, HT-29, and MEL-28 cancer cells (IC50s = 0.002, 0.002, 0.01, and 0.002 μg/ml, respectively).
1.Romero, F., Espilego, F., Pérez Baz, J., et al.Thiocoraline, a new depsipeptide with antitumor activity produced by a marine Micromonospora. I. Taxonomy, fermentation, isolation, and biological activitiesJ. Antibiot. (Tokyo)50(9)734-737(1997) 2.Negri, A., Marco, E., García-Hernández, V., et al.Antitumor activity, X-ray crystal structure, and DNA binding properties of thiocoraline A, a natural bisintercalating thiodepsipeptideJ. Med. Chem.50(14)3322-3333(2007)
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