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乙酰吉他霉素临床前药理学研究
Study on the preclinical pharmacology of acetylkitasamycin
【摘要】 乙酰吉他霉素对临床分离的革兰氏阳性球菌有较好的抑菌活力,其对金葡球菌、β-溶血性链球菌、表葡球菌的MIC50分别为1、0.22和4mg/L,对耐红霉素、青霉素的金葡球菌、表葡球菌半数以上较敏感,与吉他霉素相似,但其对革兰氏阴性菌无明显作用。乙酰吉他霉素对小鼠实验性细菌感染有明显保护作用。对金葡球菌、肺炎双球菌感染小鼠口服用药的ED50分别为79.6和25.1mg/kg。其疗效与吉他霉素、麦白霉素、乙酰螺旋霉素相似。乙酰吉他霉素小鼠1次口服的LD50>15g/kg,与吉他霉素相比毒性无差异。
【Abstract】 Acetylkitasamycin has a strong antibacterial activity against Gram-positive bacteria,especially against Gram-positive coccus. The MIC50 of acetylkitasamycin were 0.39mg/L against Staphylococcus aureus,0. 22mg/L against β-hemolytic Streptococcus, 4mg/L against Staphylococcus epidermidis. Its activity was the same as kitasamycin but stronger than mileumycin and acetylspiramycin.It was susceptible to erythromycin -resistant Staphylococus aureus and Staphylococcus epidermidis.It has no effects on Gram-negative bacteris.The protective effects of acetylkitasamycin against systemic infection in mice were as good as kitasamycin, meleumycin, and acetylspiramycin. The ED50 of acetylkitasamycin against Staphylococcus-32 and Pneumococcus 31001-18 were 79. 6 and 25. 1 mg/kg respectively. The LD50 values of acetylkitasamycin in mice were 15g/kg(op) and 2g/kg(ip)respectively.
- 【文献出处】 中国抗生素杂志 ,CHINESE JOURNAL OF NATIBIOTICS , 编辑部邮箱 ,1996年01期
- 【分类号】R978.15
- 【被引频次】4
- 【下载频次】226