Actinonin is an isolated antibiotic and shown to be an inhibitor of aminopeptidase M, inhibits enkephalin-degrading enzymes from guinea-pig striatum (enkephalin-aminopeptidase), striatal membrane neutral endopeptidase and soluble dipeptidylaminopeptidase in rat whole brain homogenate with IC50 of 0.39, 5.6 and 1.1 uM, respectively.
Actinonin administered intracisternally (i.cist., 50 micrograms) or intraperitoneally (i.p., 100 mg/kg), potentiated the analgesic action of met-enkephalin (50 micrograms i.cist.). analgesia by a tail-flick test.
Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with Ki of 0.28 nM. inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively.
Actinonin inhibits cell growth in various human tumor cell lines. The IC50 of 4, 6.9, 12.8, 16.6, 27.4, 15.7 and 49.3 μM for Raji cells, MDA-MB-468 cells,PC3 cells, SK-LC-19 cells, Hela cells, HT-1080 cells and AL67 cells, respectively.
Actinonin is active against Gram-positive bacteria, including S. aureus (MIC value of 8-16 µg/mL), Streptococcus pyogenes (MIC value of 8 µg/mL) and Streptococcus epidermidis (MIC value of 2-4 µg/mL).