In silico and in vitro genotoxicity evaluation of descarboxyl levofloxacin,an impurity in levofloxacin
In silico and in vitro genotoxicity evaluation of descarboxyl levofloxacin,an impurity in levofloxacin作者机构:Shandong Institute for Food and Drug Control
出 版 物:《中国药理学与毒理学杂志》 (Chinese Journal of Pharmacology and Toxicology)
年 卷 期:2013年第3期
页 面:470-471页
核心收录:
学科分类:1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100706[医学-药理学] 100602[医学-中西医结合临床] 10[医学]
主 题:genotoxicity impurity descarboxyl levofloxacin SARs CHL chromosomal aberration
摘 要:OBJECTIVE To evaluate the genotoxicity of Descarboxyl Levofloxacin by In silico and In vitro *** Assessment of genotoxicity using Derek for Windows We used DEREK for Windows(DfW,Lhasa Ltd.,Leeds,UK) version 11.0 for toxicity *** structures are entered into the program in *** *** program applies structure-activity relationships 〔(Q) SARs〕and other expert knowledge rules to derive a reasoned prediction about the potential toxicity of the query *** reverse mutation assay(Ames test) The Salmonella histidine point mutation assay proposed by Maron and Ameswas *** *** histidine autotrophic strains(TA97,TA98,TA100 and TA102) used in this test were obtained from Shandong center for disease *** saline(NS) was used as a vehicle control.2-Aminofluorene(2-AF,10 μg /plate),1,8-dihydroxyanthraquinone(50 μg /plate),Sodium azide(NaN3,1.5 μg /plate),and Dexon(50 μg /plate) were used as positive *** levofloxacin was assayed at concentrations of 31.25,62.5,125,250,and 500 μg /***,0.1 ml of test substance(or control solution),0.1 ml of bacterial culture 〔(1-2) × 1012 L-1 〕and 0.5 ml of S9 mix(NS for treatment without activation) were mixed and poured onto the agar plates after addition of 1.8 ml of top agar(0.6% agar Difco,0.5% NaCl,50 μmol·L-1 L-histidine,50 μmol·L-1 biotin,45℃) at 45℃.Plates were inverted and incubated for 48h at 37℃ in the *** colonies were counted and the background lawn was inspected for signs of toxicity or compound *** assay was performed two times in triple and included negative and positive *** al aberrations in Chinese ham ster lung cells Chinese Hamster Lung(CHL) cells were obtained from Shandong center for disease *** cells were grown in DMEM medium supplemented with 10% heat-inactivated calf serum at 37℃ in an atmosphere containing 5% of *** test for Chromosomal aberrations in CHL cells was con