Guadinomines, Type III secretion system inhibitors, produced by Streptomyces sp. K01-0509. I: taxonomy, fermentation, isolation and biological properties.
Enteropathogenic Escherichia coli (EPEC) expressing the Type III secretion system (TTSS) induced hemolysis of sheep blood cells. Using this assay, six structurally related compounds designated as guadinomines were isolated as inhibitors of TTSS-induced hemolysis by ion exchange column chromatography and HPLC from the culture broth of Streptomyces sp. K01-0509. Guadinomines A and B showed potent inhibition with IC50 values of 0.02 and 0.007 microg/ml, respectively, guadinomine D showed moderate activity (IC50: 8.5 microg/ml), while guadinomines C1 and C2 and guadinomic acid had no activity.
Iwatsuki
Masato
M
The Kitasato Institute, Japan.
Uchida
Ryuji
R
Yoshijima
Hitomi
H
Ui
Hideaki
H
Shiomi
Kazuro
K
Matsumoto
Atsuko
A
Takahashi
Yoko
Y
Abe
Akio
A
Tomoda
Hiroshi
H
Omura
Satoshi
S
D000900:Anti-Bacterial Agents / Q000096:biosynthesis* / Q000302:isolation & purification / Q000494:pharmacology; D004151:Dipeptides / Q000097:blood* / Q000302:isolation & purification / Q000494:pharmacology; D005285:Fermentation; D048289:Imidazolidines / Q000097:blood* / Q000302:isolation & purification / Q000494:pharmacology; D013302:Streptomyces / Q000145:classification* / Q000378:metabolism*
D000900:Anti-Bacterial Agents; D004151:Dipeptides; D048289:Imidazolidines; C530702:guadinomine A; C530703:guadinomine B; C530704:guadinomine C; C530705:guadinomine D; C530706:guadinomine E