【作者】 周雨朦； 李继安； 沈舜义； 林惠敏； 葛涵； 朱春宝； 陈代杰；

【Author】 ZHOU Yu-meng,ZHU Chun-bao,LI Ji-an,SHEN Shun-yi,GE Han,CHEN Dai-jie (China State Institute of Pharmaceutical Industry,Shanghai Institute of Pharmaceutical Industry,State Key Lab of New Drug and Pharmaceutical Process,Shanghai 200040)

【机构】 中国医药工业研究总院,上海医药工业研究院,创新药物与制药工艺国家重点实验室；

【摘要】 目的:建立秀丽隐杆线虫—甲氧西林耐药金黄色葡萄球菌感染模型,筛选抗耐药菌感染的活性化合物。方法:利用耐药菌对线虫进行感染,建立液体条件感染和抗生素救治模型,通过观察感染线虫的存活情况,考察筛选样品活性。结果:对456个样品孔进行考察,发现化合物sipi8294具有某种生物学活性,当浓度为16μg·mL^-1时,可以使感染线虫存活率达到60%。通过联合用药实验发现,sipi8294与青霉素类药物联用,具有明显的增效作用。8μg·mL^-1 sipi8294和8μg·mL^-1氨苄西林联用,可以使线虫存活率提高到80%以上。结论:该模型能反映病原菌在线虫体内的耐药性,并可以用于化合物的筛选,发现具有抗感染或是辅助抗感染作用的化合物。更多还原

【Abstract】 Objective:To establish C.elegans-MRSA infective model,and screen anti-infective compounds.Methods:Worms infected drug resistant bacteria were treated by antibiotics.We investigated the activity of the screening compounds using this model through measuring method of survival rate. Results:We used the method to screen 456 compound wells and found 16μg·mL^-1 sipi8294 which elevated the survival rate of infected nematodes to 60%.In combination experiment,we found sipi8294 associated with penicillins antibiotics could obviously increase the effect of anti-infection.8μg·mL^-1 sipi8294 associated with 8μg·mL^-1 ampicillin could increase survival rate more than 80%.Conclusion:The model can reflect the drug resistance of pathogen in C.elegans and may be used to screen antibacterial compounds and may also be useful bioactive compounds which most likely would not be identified in vitro.更多还原