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Actinonin

CAS No. : 13434-13-4

MCE 站：Actinonin

产品活性：Actinonin ((-)-Actinonin) 是一种由放线菌产生的天然抗菌剂。Actinonin 抑制氨肽酶 M，氨肽酶 N 和亮氨酸氨肽酶。Actinonin 是一种有效的可逆肽去甲酰基酶 (PDF) 抑制剂，K_i 为 0.28 nM。Actinonin 还抑制 MMP-1，MMP-3，MMP-8，MMP-9 和 hmeprin α 的 K_i 值分别为 300 nM，1,700 nM，190 nM，330 nM 和 20 nM。Actinonin 是一种凋亡诱导剂，具有抗增殖和抗肿瘤活性。

研究领域：Anti-infection  |  Metabolic Enzyme/Protease  |  Apoptosis

作用靶点：Aminopeptidase  |  Bacterial  |  MMP  |  Apoptosis  |  Antibiotic

In Vitro: 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.
HsPDF is a critical target of actinonin and that the inhibition of this protein in the mitochondria leads to cell death in tumor cells. Actinonin treatment of cells led to a tumor-specific mitochondrial membrane depolarization and ATP depletion in a time- and dose-dependent manner.
Actinonin is a potent inhibitor of all three forms (Zn-, Ni-, and Fe-) of peptide deformylases from both S. aureus and E. coli bacteria. Under the assay conditions, the IC₅₀ values for Actinonin are 90, 3, 0.8, and 11 nM for Zn-PDF (E. coli), Ni-PDF (E. coli), Fe-PDF (E. coli), and Ni-PDF (S. aureus), respectively.
Actinonin is active against Gram-positive bacteria, including S. aureus (MIC value of 8-16 ?g/mL), Streptococcus pyogenes (MIC value of 8 ?g/mL) and Streptococcus epidermidis (MIC value of 2-4 ?g/mL). Actinonin is also active against fastidious Gramne-gative bacteria, such as H. influenzae (MIC value of 1-2 ?g/mL), Moraxella catarrhalis (MIC value of 0.5 ?g/mL), and Neisseria gonorrheae (MIC value of 1-4 ?g/mL). Actinonin is very active against the H. influenzae acr (MIC value of 0.13 ?g/mL) and E. coli acr (MIC value of 0.25 ?g/mL) efflux pump mutants.

In Vivo: Actinonin has been safely administered to mice as an antibiotic at doses up to 400 mg/kg. Actinonin does not appear to have significant toxicity to normal tissues, despite its antitumor activity in vitro. Remarkably, Actinonin exhibits significant antitumor activity when given i.p. or orally in a CWR22 human prostate tumor xenograft model in nude mice. During treatment, the animals show no signs of toxicity.

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