Burkholone, a new cytotoxic antibiotic against IGF-I dependent cells from Burkholderia sp.
In the course of our screening program for new inhibitors of IGF-I signaling, we isolated a new cytotoxic antibiotic, burkholone, from the culture broth of Burkholderia sp. QN15488. The structure of burkholone was determined to be (E)-3-methyl-2-(2-octenyl)-4-quinolone by a series of NMR analyses. Burkholone induced cell death 32D/GR15 cells with an IC50 value of 160 nM in IGF-I containing medium, while no cell death was observed in IL-3 containing medium even at the concentration of 37 microM.
Somatech Center, House Foods Corporation, Yotsukaido, Chiba, Japan.
Toshiya
T
Mori
Tomoki
T
Yamashita
Kazuo
K
Furihata
Koji
K
Nagai
Ken-Ichi
K
Suzuki
Yoichi
Y
Hayakawa
Kazuo
K
Shin-Ya
D000903:Antibiotics, Antineoplastic / Q000096:biosynthesis / Q000737:chemistry / Q000494:pharmacology*; D019117:Burkholderia / Q000378:metabolism*; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007334:Insulin-Like Growth Factor I / Q000037:antagonists & inhibitors*; D009682:Magnetic Resonance Spectroscopy; D015363:Quinolones / Q000737:chemistry / Q000494:pharmacology*
C527232:3-methyl-2-(2-octenyl)-4-quinolone; D000903:Antibiotics, Antineoplastic; D015363:Quinolones; D007334:Insulin-Like Growth Factor I