Cyclothialidine, a novel DNA gyrase inhibitor. II. Isolation, characterization and structure elucidation.
Cyclothialidine is a novel DNA gyrase inhibitor produced by Streptomyces filipinensis NR 0484. It was isolated from the culture broth by charcoal adsorption, Diaion HP-21, Amberlite CG-50, DEAE Toyopearl, and Toyopearl HW-40 SF column chromatography. The structure of cyclothialidine was determined to be a unique twelve membered lactone by amino acid analysis and various 2D-NMR experiments. Cyclothialidine inhibited Escherichia coli DNA gyrase with an IC50 of 30 ng/ml.
Kamiyama
T
T
Nippon Roche Research Center, Kanagawa, Japan.
Shimma
N
N
Ohtsuka
T
T
Nakayama
N
N
Itezono
Y
Y
Nakada
N
N
Watanabe
J
J
Yokose
K
K
D000595:Amino Acid Sequence; D000596:Amino Acids / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D004926:Escherichia coli; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008969:Molecular Sequence Data; D010456:Peptides, Cyclic; D011758:Pyrroles / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D013302:Streptomyces / Q000378:metabolism*; D059005:Topoisomerase II Inhibitors
D000596:Amino Acids; D006571:Heterocyclic Compounds; D010456:Peptides, Cyclic; D011758:Pyrroles; D059005:Topoisomerase II Inhibitors; C085889:cyclothialidine