Actinonin is a natural antibacterial agent produced by Streptomyces, also serving as an effective PDF (peptide deformylase) inhibitor and apoptosis inducer. It inhibits APN (Aminopeptidase N), MMPs and heparin α, exhibiting antiproliferative and antitumour activity.

MMP1:300 nM (Ki), MMP3:1700 nM (Ki), MMP9:330 nM (Ki), MMP8:190 nM (Ki), hmeprin α:20 nM (Ki), Peptide deformylase:0.28 nM (Ki)

Actinonin exhibits significant proliferation-inhibitory effects on 16 tumor cell lines, with IC₅₀ values ranging from 5 to 60 μM, showing dose- and time-dependent characteristics, while demonstrating no significant impact on normal cell lines (such as WI-38, NIH-3T3, and hPBMCs) [1].
Treatment of RL lymphoma cells with Actinonin (10-100 μg/ml) induces time-dependent and dose-dependent mitochondrial membrane depolarization, with membrane potential recovering approximately 8 hours after Actinonin removal, suggesting its mechanism of action is mediated through indirect effects on the electron transport chain [1].

In the CWR22 human prostate cancer model, both intraperitoneal injection (250 mg/kg) and oral administration (500 mg/kg) of Actinonin significantly inhibited tumor growth. The significant effect of oral administration indicates that Actinonin has good oral bioavailability [1].