Thiocoraline

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).

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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 activities. J. 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 thiodepsipeptide. J. Med. Chem. 50(14), 3322-3333 (2007).