替加环素杂质9-硝基米诺环素的致突变Ames试验研究  

Study for Ames test of 9-nitrominocycline of tigecycline impurity

作　　者：张晓燕 杜加秋 张冲 徐慧娟 ZHANG Xiao-yan;DU Jia-qiu;ZHANG Chong(Hanhui Pharmaceuticals Co.,Ltd,Hangzhou 310000,China;不详)

机构地区：[1]瀚晖制药有限公司,杭州310000 [2]浙江海正药业股份有限公司,浙江台州318000

出　　处：《中国处方药》2021年第8期25-28,共4页Journal of China Prescription Drug

摘　　要：目的通过组氨酸营养缺陷型鼠伤寒沙门氏菌回复突变试验评价替加环素杂质9-硝基米诺环素的潜在致突变性。方法采用平板渗入法进行实验,以二甲基亚砜(DMSO)为溶剂,计数TA97a、TA98、TA100、TA102及TA1535菌株在活化和非活化条件下的回变菌落数,评价其致突变性。结果受试物9-硝基米诺环素在菌株TA100间接(+S9)和直接(-S9)致突变实验中,回复突变数均显著增加,并为溶剂对照的2倍以上;在菌株TA1535直接(-S9)致突变实验中,回复突变菌落数为溶剂对照的2倍以上,但未达到3倍,在间接(+S9)致突变实验中,回复突变菌落数显著增加,并为溶剂对照的3倍以上。结论在本实验条件下,受试物9-硝基米诺环素具有潜在致突变性。Objective To determine the mutagenic potential of 9-nitrominocycline of tigecycline impurity with the Ames(Salmonella typhimurium)(his-)/microsome mutagenicity assay.Methods The plate incorporation assay was taken and DMSO was used as solvent.Count the number of spontaneously induced revertant colonies formed by 5 standard tester strains of TA97a,TA98,TA100,TA102 and TA1535 with or without S9 homogenate.Results In the indirect(+S9)and direct(-S9)mutagenicity assay of strain TA100,the number of revertant mutations was increased significantly,which was more than 2 times that of solvent control.In the direct(-S9)mutagenicity assay of strain TA1535,the number of revertant colonies was more than 2 times that of solvent control,but not up to 3 times.In the indirect(+S9)mutagenicity assay,the number of revertant mutations was increased significantly and was more than 3 times that of solvent control.Conclusion Under the conditions of this assay,9-nitrominocycline was considered to be mutagenic.

关 键 词：替加环素 9-硝基米诺环素 AMES试验 二甲基亚砜 

分 类 号：R965[医药卫生—药理学]