夫西地酸对细胞外和细胞内金黄色葡萄球菌的活性：pH 值的影响及与利奈唑胺和克林霉素的比较。
Activity of fusidic acid against extracellular and intracellular Staphylococcus aureus: influence of pH and comparison with linezolid and clindamycin.
机构信息
Cellular and Molecular Pharmacology, Louvain Drug Research Institute, Université Catholique de Louvain, Brussels, Belgium.
出版信息
Clin Infect Dis. 2011 Jun;52 Suppl 7:S493-503. doi: 10.1093/cid/cir165.
BACKGROUND
Emergence of multidrug-resistant Staphylococcus aureus has triggered a reassessment of fusidic acid (CEM-102, sodium fusidate).
METHODS
Fusidic acid was examined for (1) activity against recent methicillin-resistant S. aureus (MRSA) isolates; (2) modulation of activity by acidic pH; and (3) accumulation by phagocytic cells and intracellular activity against methicillin-susceptible S. aureus (MSSA) and MRSA.
RESULTS
About 96% of strains (N = 94) were susceptible (European Committee on Antimicrobial Susceptibility Testing breakpoint [≤ 1 mg/L]). Activity was enhanced at pH 5.5 (6 dilutions decrease for minimum inhibitory concentration) in parallel with an increase of drug bacterial accumulation (opposite effects for clindamycin; linezolid remained unaffected). Fusidic acid accumulated in THP-1 cells (about 5.5 fold), with further accumulation at pH 5.5 vs pH 7.4. The intracellular activity of Fusidic acid was similar to that of clindamycin and linezolid (maximal relative activity, 0.4-0.6 log(10) colony-forming unit decrease). No cross-resistance to vancomycin or daptomycin was observed.
CONCLUSIONS
Fusidic acid is active against S. aureus in broth as well as intracellularly, with no cross-resistance to other antibiotics.
背景
耐多药金黄色葡萄球菌的出现促使人们重新评估了夫西地酸（CEM-102，夫西地酸钠）。
方法
检测了夫西地酸（1）对近期耐甲氧西林金黄色葡萄球菌（MRSA）分离株的活性；（2）酸性 pH 值对其活性的调节作用；（3）吞噬细胞对夫西地酸的蓄积作用及其对甲氧西林敏感金黄色葡萄球菌（MSSA）和 MRSA 的细胞内活性。
结果
约 96%的菌株（N=94）对夫西地酸敏感（欧洲抗菌药物敏感性试验委员会折点[≤1mg/L]）。在 pH5.5 时，活性增强（最低抑菌浓度降低 6 个稀释度），同时药物细菌蓄积增加（克林霉素的作用相反；利奈唑胺不受影响）。夫西地酸在 THP-1 细胞中蓄积（约 5.5 倍），在 pH5.5 时比 pH7.4 时蓄积更多。夫西地酸的细胞内活性与克林霉素和利奈唑胺相似（最大相对活性下降 0.4-0.6log10 菌落形成单位）。未观察到与万古霉素或达托霉素的交叉耐药性。
结论
夫西地酸对金黄色葡萄球菌在肉汤中的活性以及细胞内活性均有效，与其他抗生素无交叉耐药性。
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