NC0604, a new analogue of bleomycin, was isolated from fermentation broth of Streptomyces verticillus var. pingyangensis n.var. The structure of NC0604 was elucidated by spectroscopic analyses. NC0604 had the same kernel structure as bleomycin, but a different terminal amine moiety determined as amidepropyl spermidine. NC0604 exhibited antibacterial activity against a wide range of bacterial species and showed cytotoxicity in vitro against human HepG(2), KB, MCF-7, HCT116, BGC-823 and MCF-7/DOX cells with IC(50) values of 1.18, 1.21, 1.41, 1.83, 2.02, 1.45 muM, respectively. The antitumor activity of NC0604 against these cells was 3~9 times higher than that of bleomycin; and the pulmonary toxicity of NC0604 was much lower than that of bleomycin.

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http://dx.doi.org/10.1038/ja.2008.88DOI Listing

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