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

被引:0
作者
YUAN Gan-Jun [1 ]
LI Pei-Bo [2 ]
YANG Jun [1 ]
PANG Hui-Zhong [1 ]
PEI Ying [1 ]
机构
[1] College of Bioscience and Engineering, Jiangxi Agricultural University
[2] School of Life Science,Sun Yat-sen University
基金
中国国家自然科学基金;
关键词
Azalomycin F5a; Anti-MRSA; Demalonyl Derivatives; Macrocyclic antibiotics;
D O I
暂无
中图分类号
R96 [药理学];
学科分类号
100602 ; 100706 ;
摘要
AIM: To discover anti-methicillin-resistant Staphylococcus aureus(anti-MRSA) microbial natural products or their derivatives. METHOD: Azalomycin 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. RESULTS: Four 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. CONCLUSION: Azalomycin 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.
引用
收藏
页码:309 / 313
页数:5
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