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司帕沙星对白细胞减少小鼠实验性肺炎衣原体肺炎的保护作用。

Protective effects of sparfloxacin in experimental pneumonia caused by Chlamydia pneumoniae in leukopenic mice.

作者信息

Nakata K, Okazaki Y, Hattori H, Nakamura S

机构信息

Bioscience Research Laboratories, Dainippon Pharmaceutical Co., Ltd., Osaka, Japan.

出版信息

Antimicrob Agents Chemother. 1994 Aug;38(8):1757-62. doi: 10.1128/AAC.38.8.1757.

Abstract

The in vivo antichlamydial activities of sparfloxacin and reference drugs were examined in a experimental model of pneumonia caused by Chlamydia pneumoniae in leukopenic mice; their in vitro activities were also examined. The most potent agents in vitro were sparfloxacin (MICs for C. pneumoniae Kajaani and IOL 207, (0.031 and 0.031 micrograms/ml, respectively), clarithromycin (0.031 and 0.031 micrograms/ml, respectively), and minocycline (0.031 and 0.031 micrograms/ml, respectively); these were followed by tosufloxacin (0.063 and 0.125 micrograms/ml, respectively) and ofloxacin (0.5 and 0.5 micrograms/ml, respectively). The MBCs of sparfloxacin, tosufloxacin, ofloxacin, clarithromycin, and minocycline for these two strains were 0.063 and 0.063 micrograms/ml, 0.125 and 0.25 micrograms/ml, 1.0 and 1.0 micrograms/ml, 0.125 and 0.125 micrograms/ml, and 0.25 and 0.25 micrograms/ml, respectively. Fatal pneumonia was induced by intranasal inoculation of cyclophosphamide-treated leukopenic mice with C. pneumoniae IOL 207; infiltration of neutrophils and lymphocytes was observed in the lungs of these mice by histopathological examination. The 50% effective dose of sparfloxacin (oral dose of 0.97 mg/kg of body weight) against the pneumonia was the lowest among the drugs tested; this was followed by those of minocycline (2.22 mg/kg), tosufloxacin (3.47 mg/kg), clarithromycin (4.66 mg/kg), and ofloxacin (16.6 mg/kg). The results indicate that it may be worthwhile to use sparfloxacin against C. pneumoniae infections in humans.

摘要

在白细胞减少小鼠肺炎衣原体所致肺炎的实验模型中检测了司帕沙星及对照药物的体内抗衣原体活性;同时也检测了它们的体外活性。体外活性最强的药物是司帕沙星(肺炎衣原体卡亚尼株和IOL 207株的MIC分别为0.031和0.031微克/毫升)、克拉霉素(分别为0.031和0.031微克/毫升)和米诺环素(分别为0.031和0.031微克/毫升);其次是妥舒沙星(分别为0.063和0.125微克/毫升)和氧氟沙星(分别为0.5和0.5微克/毫升)。司帕沙星、妥舒沙星、氧氟沙星、克拉霉素和米诺环素对这两株菌的MBC分别为0.063和0.063微克/毫升、0.125和0.25微克/毫升、1.0和1.0微克/毫升、0.125和0.125微克/毫升、0.25和0.25微克/毫升。用环磷酰胺处理过的白细胞减少小鼠经鼻接种肺炎衣原体IOL 207株可诱发致死性肺炎;通过组织病理学检查在这些小鼠的肺中观察到中性粒细胞和淋巴细胞浸润。司帕沙星抗肺炎的50%有效剂量(口服剂量为0.97毫克/千克体重)在受试药物中最低;其次是米诺环素(2.22毫克/千克)、妥舒沙星(3.47毫克/千克)、克拉霉素(4.66毫克/千克)和氧氟沙星(16.6毫克/千克)。结果表明,使用司帕沙星治疗人类肺炎衣原体感染可能是值得的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a05f/284633/a2e3fc8d2285/aac00372-0066-a.jpg

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