Abstract
To discover new lead compounds against methicillin-resistant Staphylococcus aureus (MRSA), trimethylhydroquinone, vitamins K1, K2, K3 and menadione sodium bisulfite were targeted for anti-MRSA assay. Their anti-MRSA activities were evaluated by agar diffusion method, and their minimum inhibitory concentrations (MICs) were determined by broth microdilution method. The results showed that trimethylhydroquinone, vitamin K3 and menadione sodium bisulfite presented obvious anti-MRSA activity, and their MICs against MRSA ATCC 33592 and three clinical MRSA isolates were successively 16 to 32, 8 to 16 and 16 µg/ml. Vitamins K1 and K2 showed no anti-MRSA activity when the test discs respectively carried 1024 µg of them. These indicated that the anti-MRSA activity would disappear when the methyl of vitamin K3 was substituted by alkyl that contained four isopentenyl units, and vitamin K3 probably has an ancillary effect on the treatment of MRSA infection. Key words: Vitamin K3, menadione sodium bisulfate, trimethylhydroquinone, methicillin-resistant Staphylococcus aureus (MRSA).
Highlights
Methicillin-resistant Staphylococcus aureus (MRSA)poses a serious threat to public health because of its resistance to multiple antibiotics (Payne, 2008; Taubes, 2008)
The results showed that trimethylhydroquinone, vitamin K3 and menadione sodium bisulfite presented obvious anti-MRSA
It is worth noticing that discovering anti-MRSA compounds from known compounds and drugs should be an economical and effective method (Berger, 2007; Chong and Jr Sullivan, 2007)
Summary
Poses a serious threat to public health because of its resistance to multiple antibiotics (Payne, 2008; Taubes, 2008). Various efforts at discovery of novel antibiotics were carried forward, such as classic screening methods, chemical modification of known antimicrobials, improving antimicrobial activity of known compounds, hybrid agents and new targets (Moellering, 2011). Base on the structure-activity analysis of anti-MRSA natural products (Saleem et al, 2010; Gibbons, 2004), some phenols and quinones contained hydrophobic groups were deduced to present potential anti-MRSA activity. Three potential anti-MRSA compounds as trimethylhydroquinone (compound 1) (Figure 1), αtocopherol and phloroglucinol were selected for antiMRSA assays. The results showed that compound 1 presented obvious anti-MRSA activity with daptomycin as a positive control, while α-tocopherol and phloroglucinol
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