评价新型3,5-二取代吡唑啉衍生物抗人肺癌细胞株(A549)的潜能  

Potential Evaluation of a New 3,5 Disubstituted Pyrazoline Derivative Against Human Lung Cancer Cell Line (A549)

作　　者：卢致辉[1] 辜茜娟 LU Zhihui;GU Xijuan(Department of Oncology,Nanchang University the First Affiliated Hospital,Nanchang,JIANG xi 330019;Neurosurgery Department,Nanchang University the First Affiliated Hospital,Nanchang,JIANG xi 330019)

机构地区：[1]南昌大学第一附属医院肿瘤科,江西南昌330019 [2]南昌大学第一附属医院神经外科,江西南昌330019

出　　处：《智慧健康》2023年第18期154-157,共4页Smart Healthcare

摘　　要：目的 评估新型3,5-二取代吡唑啉衍生物抗人肺癌细胞株(A549)的潜能。方法 制备新型吡唑啉衍生物,评价这种衍生物在体外对抗人非小细胞肺癌(NSCLC)细胞株A549的效能。利用MTT法与SRB法筛查全部最终衍生物的抗癌潜力,测定其存在的细胞毒性。结果 本文条件下制备最终化合物用时10d,在表达抗A549中存在细胞毒性潜能,占比约为71.24%,对照药物为阿奇霉素,阿奇霉素所具有的细胞毒性为80.55%,两组相较并无差异(P>0.05)。所制备的新型吡唑啉衍生物的抗癌活性SRB检查结果与MTT法检查所得的细胞毒性结果类似,其成分为具有甲硫基、氟基团、甲氧基官能团的化合物,10d对抗A549的GI50水平为11.41μg/mL,对照药物ADR的TGI水平>100μm,化合物10d为46.76μm。结论 新型吡唑啉衍生物抗NSCLC的A549细胞株的潜力理想,细胞毒性水平较为合理。Objective To observe anti human lung cancer cell line(A549)of a new 3,5 disubstituted pyrazoline derivative and analyze the potential of A549.Methods The paper prepared a new Pyrazoline derivative and evaluated its effect against human non-small cell lung cancer(NSCLC)cell line A549 in vitro,screened all final derivatives for their anticancer potential with MTT and SRB methods and determined their cytotoxicity.Results Final compound of chemical reaction process and conditions in the paper was 10d,with cytotoxicity potential in expression of anti A549,accounting for 71.24%.Control drug was azithromycin with cytotoxicity of 80.55%.There was no difference between two groups(P>0.05).Anti-cancer activity SRB test results of synthesized compounds were similar to those of MTT method.for compounds of methylthio,fluoro and methoxy functional groups,GI50 level was 11.41μG/ml against A549 in 10d,TGI level in control drug ADR>100μm,that of compound 10d was 46.76μM.Conclusion Final compound can achieve ideal potential of anti NSCLC A549 cell line,reasonable level of cytotoxicity,especially derivatives with methylthio,fluoro and methoxy functional groups have good potential.

关 键 词：新型3 5-二取代吡唑啉衍生物 人肺癌细胞株 细胞潜能 最终化合物 

分 类 号：R96[医药卫生—药理学]