期刊
ANTIBIOTICS-BASEL
卷 11, 期 8, 页码 -出版社
MDPI
DOI: 10.3390/antibiotics11081026
关键词
fusidic acid; antimicrobial; anti-inflammatory; molecular docking; molecular dynamic
资金
- National Natural Science Foundation of China [81803390, 22077020]
- Guangdong Basic and Applied Basic Research Foundation [2021A1515010221]
- Science and Technology Innovation Strategy of Guangdong Province [Jiangke(2018)352, Jiangke(2020)182]
- Jiangmen City Social Welfare Innovation Platform Construction Project [2018090103460022105]
- Foundation of Department of Education of Guangdong Province [2021ZDZX4041, 2020KZDZX1202, 2018KTSCX236, 2017KSYS010]
Fusidic acid and its derivatives show good antibacterial activity against Gram-positive bacteria without cross-resistance. They also exhibit similar bacteriostatic characteristics and effectively reduce inflammation-induced ear edema.
Fusidic acid (FA), a narrow-spectrum antibiotics, is highly sensitive to various Gram-positive cocci associated with skin infections. It has outstanding antibacterial effects against certain Gram-positive bacteria whilst no cross-resistance with other antibiotics. Two series of FA derivatives were synthesized and their antibacterial activities were tested. A new aromatic side-chain analog, FA-15 exhibited good antibacterial activity with MIC values in the range of 0.781-1.563 mu M against three strains of Staphylococcus spp. Furthermore, through the assessment by the kinetic assay, similar characteristics of bacteriostasis by FA and its aromatic derivatives were observed. In addition, anti-inflammatory activities of FA and its aromatic derivatives were evaluated by using a 12-O-tetradecanoylphorbol-13-acetate (TPA) induced mouse ear edema model. The results also indicated that FA and its aromatic derivatives effectively reduced TPA-induced ear edema in a dose-dependent manner. Following, multiform computerized simulation, including homology modeling, molecular docking, molecular dynamic simulation and QSAR was conducted to clarify the mechanism and regularity of activities. Overall, the present work gave vital clues about structural modifications and has profound significance in deeply scouting for bioactive potentials of FA and its derivatives.
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