阿扎霉素 F5a 及其衍生物抗耐甲氧西林金黄色葡萄球菌活性测定。
Anti-methicillin-resistant Staphylococcus aureus assay of azalomycin F5a and its derivatives.
机构信息
College of Bioscience and Engineering, Jiangxi Agricultural University, Nanchang 330045, China.
School of Life Science, Sun Yat-sen University, Guangzhou 510275, China.
出版信息
Chin J Nat Med. 2014 Apr;12(4):309-13. doi: 10.1016/S1875-5364(14)60061-3.
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.
目的
发现抗耐甲氧西林金黄色葡萄球菌（anti-MRSA）的微生物天然产物或其衍生物。
方法
通过发酵吸水链霉菌吸水亚种制备阿扎霉素 F5a（1），并通过在烃基醇-AcOH（4：1）中的烃化和随后用 2mol·L（-1）KOH 在 MeOH-H2O（7：3）中脱琥珀酰化来合成其衍生物。通过琼脂扩散和肉汤微量稀释法评估它们对 MRSA ATCC 33592 和三种临床分离的 MRSA 的活性。
结果
合成了四个脱琥珀酰基阿扎霉素 F5a 衍生物 2 至 5。抗-MRSA 活性测定表明，化合物 1 至 5 对 MRSA 表现出显著的活性，其最小抑菌浓度（MIC）分别为 3.0-4.0、0.5-1.0、0.67-1.0、0.67-0.83 和 0.5-0.83μg·mL（-1）。
结论
阿扎霉素 F5a 和脱琥珀酰基阿扎霉素 F5a 衍生物 2-5 表现出显著的抗-MRSA 活性，2-5 的抗-MRSA 活性高于 1，而 2-5 的抗-MRSA 活性没有明显差异。还表明，阿扎霉素 F5a 的丙二酰单酯基对其抗-MRSA 活性不太重要。
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