CAJ | 학술논문

目的：研究新型硫肽类抗生素诺卡沙星对临床常见革兰阳性致病菌的抗菌活性，探讨其抗菌机制，并与临床常用抗生素进行比较。方法：采用琼脂二倍稀释法测定最低抑菌浓度（Minimal Inhibition Concentration，MIC），采用微量肉汤二倍稀释法测定最低杀菌浓度（Minimal Bactericidal Concentration，MBC），采用小鼠体内抗菌保护实验测定体内抗菌活性。结果：诺卡沙星对甲氧西林耐药的葡萄球菌、青霉素耐药的肺炎球菌均显示较强的抗菌活性，对金黄色葡萄球菌MRSA、MSSA，表皮葡萄球菌MRSE、MSSE的MIC50值分别为0.016、0.016、0.0625、0.03125 mg· L-1，对肺炎球菌（PRSP/PISP）、化脓性链球菌、肠球菌的MIC50值为0.008、0.008、0.016 mg·L-1，其MIC50值为万古霉素的1/32~1/128，为莫西沙星的1/4~1/256，为利奈唑胺的1/32~1/256。注射用诺卡沙星经静脉给药后，对金黄色葡萄球菌感染小鼠均呈现体内保护作用，其ED50值明显低于对照药万古霉素和利奈唑胺，体内抗菌保护作用优于对照药。结论：诺卡沙星具有高效抗菌作用，明显优于万古霉素、利奈唑胺及莫西沙星，且与它们之间无交叉耐药现象。
목적：연구신형류태류항생소낙잡사성대림상상견혁란양성치병균적항균활성，탐토기항균궤제，병여림상상용항생소진행비교。방법：채용경지이배희석법측정최저억균농도（Minimal Inhibition Concentration，MIC），채용미량육탕이배희석법측정최저살균농도（Minimal Bactericidal Concentration，MBC），채용소서체내항균보호실험측정체내항균활성。결과：낙잡사성대갑양서림내약적포도구균、청매소내약적폐염구균균현시교강적항균활성，대금황색포도구균MRSA、MSSA，표피포도구균MRSE、MSSE적MIC50치분별위0.016、0.016、0.0625、0.03125 mg· L-1，대폐염구균（PRSP/PISP）、화농성련구균、장구균적MIC50치위0.008、0.008、0.016 mg·L-1，기MIC50치위만고매소적1/32~1/128，위막서사성적1/4~1/256，위리내서알적1/32~1/256。주사용낙잡사성경정맥급약후，대금황색포도구균감염소서균정현체내보호작용，기ED50치명현저우대조약만고매소화리내서알，체내항균보호작용우우대조약。결론：낙잡사성구유고효항균작용，명현우우만고매소、리내서알급막서사성，차여타문지간무교차내약현상。
To investigate the activity of a novel thiopeptide antibiotic nocathiacin against clinically isolated Gram-positive bacteria comparing with those commonly used antibiotics. Methods: MIC (Minimal Inhibitory Concentration) was determined by a two - fold agar dilution method. MBC (Minimal Bactericidal Concentration) was determined by a micro-broth dilution method. ED50 was determined by an infection-protection method. Results: Nocathiacin showed strong activities against MRSA and PRSP. MIC50 against MRSA, MSSA, MRSE, MSSE, PRSP/PISP, Streptococcus pyogenes, Enterococcus were 0.016, 0.016, 0.0625, 0.03125, 0.008, 0.008, 0.016 mg·L-1, respectively. Its MIC50 was 1/32~1/128 of vancomycin, 1/4~1/256 of moxifloxacin and 1/32~1/256 of linezolid, respectively. After intravenous injection, nocathiacin showed lower ED50 and stronger protective effect on infected mice than vancomycin or linezolid. Conclu-sions: Thiopeptide antibiotic nocathiacin has high antibacterial activities, which is obviously superior to vancomycin, linezolid and moxifloxacin, and there is no cross drug-resistance between them.