新氨基糖苷类抗生素vertimicin的体内抗菌活性研究

In vivo antibacterial activity of a new aminoglycoside antibiotic,vertimicin

目的评价新氨基糖苷类抗生素vertimicin(VTM)的体内抗菌活性。方法采用小鼠全身感染模型,观察VTM对临床分离大肠埃希菌(E.coli)、肺炎克雷伯菌(K.pneumoniae)、铜绿假单胞菌(Ps.aeruginosa)和金葡菌(S.aureus)腹腔感染小鼠的体内疗效;采用兔皮肤烫伤感染模型、小鼠泌尿道上行性感染模型观察VTM对临床分离大肠埃希菌局部感染的体内疗效,并与对照药进行比较。结果VTM皮下或静脉给药对E.coli 96-12、K.pneumoniae 93-5、Ps.aeruginosa 94-17和S.aureus 93-44腹腔感染小鼠具有相似的体内疗效,皮下给药的ED50值分别为0.67、0.29、2.41和0.99mg/kg,静脉给药的ED50值分别为0.46、0.23、0.99和1.52mg/kg,体内疗效与奈替米星相近。兔皮肤烫伤感染模型中,VTM各剂量组兔皮肤组织活菌落数明显低于对照组(P<0.05或0.01)。小鼠泌尿道上行性感染模型中,VTM各剂量组肾组织活菌落数明显低于对照组,肾剖面盖印细菌阴性率明显高于对照组(P<0.01),抗菌活性优于庆大霉素。结论VTM对全身和局部感染动物均显示较好保护作用,体内疗效与奈替米星相近。

Objective To investigate the in vivo antibacterial activity of vertimicin. Methods The in vivo efficacies of vertimicin were evaluated in mice with experimental systemic infection caused by E. coli, K. pneumoniae, Ps. aeruginosae and S. aureus, skin-burned rabbits infected with E. coli 96-12 and mice transurethrally infected with E. coli 96-12, and compared with those of the control. Results Vertimicin given by s.c. or i.v. had similar effects on mice systemically infected with E. coli 96-12, K. pneumoniae 93-5, Ps. aeruginosae 94-17 and S. aureus 93-44, the EDs0s of vertimicin given by s.c. were 0.67, 0. 29, 2.41 and 0.99 mg/kg respectively, and those given by i.v. were 0.46, 0.23, 0. 99 and 1.52 mg/kg respectively, the in vivo activity was similar to that of netilmicin. In skin-burned rabbits infected with E. coli, and treated with vertimicin were significantly reduced the skin bacteria counts compared to the control （P〈0.05 or P〈0.01）. In mice transurethrally infected with E. coli, the renal colony counts for the vertimicin treated groups were significantly lower than that of the control, and the negative ratios of kidney stamping were significantly higher than that of the control （P〈0.01） ,the activity of vertimicin was better than that of gentamicin. Conclusion Vertimicin had relatively good protection to animals with systemic or local infections, and the in vivo activity was similar to that of netilmicin.