Auranofin and related heterometallic gold(I)-thiolates as potent inhibitors of methicillin-resistant Staphylococcus aureus bacterial strains

作者：Hokai Yozane; Jurkowicz Boruch; Fernandez Gallardo Jacob; Zakirkhodjaev Nuruddinkodja; Sanau Mercedes; Muth Theodore R; Contel Maria^*

来源：Journal of Inorganic Biochemistry, 2014, 138: 81-88.

DOI：10.1016/j.jinorgbio.2014.05.008

• Antimicrobial
• Auranofin
• Heterometallic gold-thiolates
• MRSA

A series of new heterometallic gold(I) thiolates containing ferrocenyl-phoshines were synthesized. Their antimicrobial properties were studied and compared to that of FDA-approved drug, auranofin (Ridaura), prescribed for the treatment of rheumatoid arthritis. MIC in the order of one digit micromolar were found for most of the compounds against Gram-positive bacteria Staphylococcus aureus and CA MRSA strains US300 and US400. Remarkably, auranofin inhibited S. aureus, US300 and US400 in the order of 150-300 nM. This is the first time that the potent inhibitory effect of auranofin on MRSA strains has been described. The effects of a selected heterometallic compound and auranofin were also studied in a non-tumorigenic human embryonic kidney cell line (HEK-293).

• 出版日期2014-9