An inhibitor of mammalian collagenase active at micromolar concentrations from an actinomycete culture broth.
Anti-collagenase activity was detected in the culture supernatant of an Actinomycete strain S 4373. The molecule was purified by solvent extraction, medium pressure and high pressure reverse phase chromatography and finally by HPLC gel filtration. The pure product was analyzed by mass spectroscopy and was identified as actinonin, a known pseudopeptide antibiotic. The Ki was determined as 1.4 microM and this value was confirmed using pure synthetic actinonin.
Faucher
D C
DC
Rhône Poulenc Santé, Centre de Recherches de Monts, France.
Lelièvre
Y
Y
Cartwright
T
T
D000192:Actinomycetales / Q000201:enzymology*; D002851:Chromatography, High Pressure Liquid; D004791:Enzyme Inhibitors / Q000302:isolation & purification*; D006877:Hydroxamic Acids / Q000302:isolation & purification / Q000494:pharmacology; D013058:Mass Spectrometry; D003012:Microbial Collagenase / Q000037:antagonists & inhibitors*; D010455:Peptides / Q000302:isolation & purification
D004791:Enzyme Inhibitors; D006877:Hydroxamic Acids; D010455:Peptides; D003012:Microbial Collagenase; C010531:actinonin