Cochliobolic acid, a novel metabolite produced by Cochliobolus lunatus, inhibits binding of TGF-alpha to the EGF receptor in a SPA assay.
Cochliobolic acid (1), a novel biologically active natural product, is produced by submerged fermentation of Cochliobolus lunatus. Compound 1 was determined to be a novel polyketide possessing a substituted tetrahydrofuran ring, a conjugated polyene chain and a 1,2-diketone moiety, by interpretation of NMR, MS, and UV/vis spectroscopic data. Compound 1 inhibits the binding of TGF-alpha to the EGF receptor of the human epidermal cell line A431 in a SPA assay with an IC50 of 1.6 microM.
Robinson
N
N
Xenova Ltd., Slough, B erkshire, U.K.
Gibson
T M
TM
Chicarelli-Robinson
M I
MI
Cameron
L
L
Hylands
P J
PJ
Wilkinson
D
D
Simpson
T J
TJ
D055598:Chemical Phenomena; D002627:Chemistry, Physical; D066246:ErbB Receptors / Q000187:drug effects / Q000378:metabolism*; D005285:Fermentation; D005663:Furans / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D011090:Polyenes / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D013056:Spectrophotometry, Ultraviolet; D016211:Transforming Growth Factor alpha / Q000378:metabolism*; D013098:Xylariales / Q000737:chemistry*
D005663:Furans; D011090:Polyenes; D016211:Transforming Growth Factor alpha; C104549:cochliobolic acid; D066246:ErbB Receptors