Anti-methicillin-resistant Staphylococcus aureus assay of azalomycin F5a and its derivatives.
10.1016/S1875-5364(14)60061-3
- Author:
Gan-Jun YUAN
1
;
Pei-Bo LI
2
;
Jun YANG
3
;
Hui-Zhong PANG
3
;
Ying PEI
3
Author Information
1. College of Bioscience and Engineering, Jiangxi Agricultural University, Nanchang 330045, China. Electronic address: sqlygj@126.com.
2. School of Life Science, Sun Yat-sen University, Guangzhou 510275, China.
3. College of Bioscience and Engineering, Jiangxi Agricultural University, Nanchang 330045, China.
- Publication Type:Journal Article
- Keywords:
Anti-MRSA;
Azalomycin F(5a);
Demalonyl Derivatives;
Macrocyclic antibiotics
- MeSH:
Anti-Bacterial Agents;
chemistry;
pharmacology;
Humans;
Macrolides;
chemistry;
pharmacology;
Methicillin-Resistant Staphylococcus aureus;
drug effects;
Microbial Sensitivity Tests;
Molecular Structure;
Staphylococcal Infections;
microbiology;
Structure-Activity Relationship
- From:
Chinese Journal of Natural Medicines (English Ed.)
2014;12(4):309-313
- CountryChina
- Language:English
-
Abstract:
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.
