Anti-methicillin-resistant Staphylococcus aureus assay of azalomycin F5a and its derivatives

Abstract

AimTo discover anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) microbial natural products or their derivatives. MethodAzalomycin F5a (1) was prepared through fermentation of Streptomyces hygroscopicus var. azalomyceticus, and its derivatives were synthesized through hydrocarbylation in hydrocarbyl alcoholic-AcOH (4 : 1) and subsequent demalonylation with 2 mol·L−1 KOH in MeOH-H2O (7 : 3). Their activities against MRSA ATCC 33592 and three clinical MRSA isolates were evaluated by the agar diffusion and broth microdilution methods. ResultsFour demalonylazalomycin F5a derivatives 2 to 5 were synthesized. The anti-MRSA activity assay indicated that compounds 1 to 5 showed remarkable activity against MRSA, and their minimum inhibitory concentrations (MICs) were respectively 3.0–4.0, 0.5–1.0, 0.67–1.0, 0.67–0.83, and 0.5–0.83 μg·mL−1. ConclusionAzalomycin F5a and the demalonylazalomycin F5a derivatives 2–5 showed remarkable anti-MRSA activity, and the anti-MRSA activities of 2 to 5 were higher than that of 1, while the anti-MRSA activities of 2 to 5 showed no obvious differences. It was also shown that the malonyl monoester group of azalomycin F5a was less important for its anti-MRSA activity.