生物活性 | |||
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描述 | Neomycin B sulfate (Framycetin sulfate), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Neomycin B sulfate competes for specific divalent metal ion binding sites in RNase P RNA. Neomycin B sulfate inhibits hammerhead ribozyme with a Ki of 13.5 μM. Neomycin B sulfate is sensitive to pH and an increase in pH suppresses the inhibition in other systems[1]. 5″-azido neomycin B and Framycetin sulfate selectively inhibit production of the mature miRNA, boosts a downstream protein, and inhibits invasion in HCC (hepatocellular carcinoma) cell line[2]. Neomycin B exhibits poor antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa, while kanamycin A shows weak activity against MRSA, methicillin-resistant Staphylococcus epidermidis (MRSE) and P. aeruginosa. Polyguanidinylation of the neomycin B-derived headgroup lowers the hydrophobic requirement of the lipid tail segment to provide broad-spectrum antibacterial activity from C16 to C12. Moreover, guanidinylation of the polycationic headgroup in neomycin B-derived cationic lipids enhances antibacterial activity against a neomycin B-, kanamycin A- and gentamicin-resistant P. aeruginosa strain, and reduces haemolytic activity[3]. Neomycin B has been found to block the binding of HIV-1 Rev protein to its viral RNA recognition site, thereby inhibiting the production of the virus[4]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.10mL 0.22mL 0.11mL |
5.50mL 1.10mL 0.55mL |
11.00mL 2.20mL 1.10mL |
参考文献 |
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