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Z24系列化合物遗传毒性的优化筛选
引用本文:秦爱平,袁素波,马华智,吴纯启,廖明阳. Z24系列化合物遗传毒性的优化筛选[J]. 中国新药杂志, 2006, 15(10): 773-776
作者姓名:秦爱平  袁素波  马华智  吴纯启  廖明阳
作者单位:军事医学科学院毒物药物研究所,北京,100850
摘    要:
目的:对Z24系列化合物进行遗传毒性优化筛选,从中选出毒性较低的候选新药作进一步开发.方法:采用Ames波动试验,SOS显色试验和双核细胞微核试验比较5种Z24系列化合物(Z24,SU5416,L1,L3和L4)的遗传毒性.结果:Ames波动试验结果表明除Z24外,其他4种化合物均显示致突变性;SOS显色试验则表明5种化合物均无致DNA原发损伤作用;双核细胞微核试验显示SU5416,L1,L3和L4具有致染色体断裂效应.结论:Z24是该系列化合物中最具开发前景的候选新药.

关 键 词:Z24系列化合物  遗传毒性  优化筛选
文章编号:1003-3734(2006)10-0773-04
修稿时间:2005-10-25

Optimization of Z24 serial chemicals with less genetic toxicity in vitro
QIN Ai-ping,YUAN Su-bo,MA Hua-zhi,WU Chun-qi,LIAO Ming-yang. Optimization of Z24 serial chemicals with less genetic toxicity in vitro[J]. Chinese Journal of New Drugs, 2006, 15(10): 773-776
Authors:QIN Ai-ping  YUAN Su-bo  MA Hua-zhi  WU Chun-qi  LIAO Ming-yang
Affiliation:Institute of Pharmacology and Toxicology, Academy of Military Medical Science, Beijing 100850, China
Abstract:
Objective:To make Z24 serial chemicals with less genetic toxicity optimized in vitro for further drug development.Methods:The genetic toxicities of five Z24 serial chemicals (Z24, SU5416,L1,L3 and L4)were evaluated by the Ames-fluctuation test,SOS chromotest and the cytokine- sis-block micronucleus assay.Results:All compounds but Z24 showed mutagenic effects in the Ames- fluctuation test on strain TA100,and had chromatic fragmentation effects in the binucleated micronucleus assay.No essential damnification to DNA by the five chemicals was found in the SOS chromotest.Con- clusion:Z24 with less genetic toxicity is warranted for further development.
Keywords:Z24 serial chemicals    genotoxicity   optimal screening
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