Isolation and characterization of antibiotic NC0604, a new analogue of bleomycin.
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.
Chen
Caixia
C
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Tian Tan Xi Li No 1, Beijing 100050, P.R. China.
Si
Shuyi
S
He
Qiyang
Q
Xu
Hongzhang
H
Lu
Min
M
Xie
Yunying
Y
Wang
Yan
Y
Chen
Ruxian
R
D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology* / Q000633:toxicity; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology* / Q000633:toxicity; D001761:Bleomycin / Q000031:analogs & derivatives* / Q000302:isolation & purification / Q000494:pharmacology / Q000633:toxicity; D045744:Cell Line, Tumor; D003470:Culture Media / Q000737:chemistry*; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D013057:Spectrum Analysis; D013302:Streptomyces / Q000378:metabolism*
D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D003470:Culture Media; D001761:Bleomycin