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New bisanthraquinone antibiotics and semi-synthetic derivatives with potent activity against clinical Staphylococcus aureus and Enterococcus faecium isolates |
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| Authors: | Socha Aaron M LaPlante Kerry L Rowley David C |
| Affiliation: | aDepartments of Biomedical and Pharmaceutical Sciences, University of Rhode Island, 53 Fogarty Hall Kingston, RI 02881, USA bPharmacy Practice, University of Rhode Island, Kingston, RI 02881, USA cCollege of Pharmacy, Veterans Affairs Medical Center, Providence, RI 02908, USA |
| Abstract: | The escalation of antibiotic resistance among Gram-positive pathogens presents increasing treatment challenges and requires the development of innovative therapeutic agents. Here, we present the antimicrobial properties of structurally unusual bisanthraquinone metabolites produced by a marine streptomycete and four semi-synthetic derivatives. Biological activities were measured against clinically derived isolates of vancomycin-resistant Enterococcus faecium (VRE), and methicillin-susceptible, methicillin-resistant, and tetracycline-resistant Staphylococcus aureus (MSSA, MRSA, and TRSA, respectively). The most potent antibiotic displayed MIC50 values of 0.11, 0.23, and 0.90 μM against a panel (n = 25 each) of clinical MSSA, MRSA, and VRE, respectively, and was determined to be bactericidal by time-kill analysis. |
| Keywords: | Antibiotics Marine streptomycete Semi-synthesis Bisanthraquinone |
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