Development of ruthenium(II) complexes as topical antibiotics against methicillin resistant Staphylococcus aureus.
A series of ruthenium(II) bis(2,2'-bipyridyl) complexes containing N-phenyl-substituted diazafluorenes (Ru-C1, Ru-C6, Ru-C7 and Ru-F) was synthesized and their potential antibacterial activity against methicillin resistant Staphylococcus aureus (MRSA) was investigated. The Ru-C7 complex showed significant improvement in both minimum inhibitory concentration (MIC, 6.25 μg mL(-1)) and minimum bactericidal concentration (MBC, 25 μg mL(-1)) towards MRSA when compared with those of methicillin (positive control) (MIC = 25 μg mL(-1) and MBC = 100 μg mL(-1)). The Ru-C7 complex possessed much stronger antibacterial effects than the Ru-C6 complex (MIC, 25 μg mL(-1), MBC, >100 μg mL(-1)). Both Ru-C6 and Ru-C7 complexes were also demonstrated to be biologically safe when tested on normal human skin keratinocytes.
State Key Laboratory of Chirosciences, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong, P.R. China.
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Gambari
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D000287:Administration, Topical; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D056831:Coordination Complexes / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D005449:Fluorenes / Q000737:chemistry; D006801:Humans; D015603:Keratinocytes / Q000187:drug effects; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D012428:Ruthenium / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D056831:Coordination Complexes; D005449:Fluorenes; D012428:Ruthenium