2-苯基-3,4-噻二唑[3,2-α]并嘧啶-7-酮对宫颈癌HeLa细胞增殖、凋亡及相关因子表达的影响  

Effects of 2-phenyl-3, 4-thiadiazole [3,2-α]-pyrimidin-7-one on proliferation, apoptosis and expression of related factors in cervical cancer HeLa cells

作　　者：杨艳 常福厚 王敏杰[2,3] 白图雅[1,2] 吕晓丽 范蕾 YANG Yan;CHANG Fu-hou;WANG Min-jie;BAI Tu-ya;LU Xiao-li;FAN Lei(College of Pharmacy,Inner Mongolia Medical University,Hohhot INNER MONGOLIA 010110,China;Neiv Drug Safety Evaluation Center,Inner Mongolia Medical University,Hohhot INNER MONGOLIA 010110,China;School of Basic Medical Sciences,Inner Mongolia Medical University,Hohhot INNER MONGOLIA 010110,China)

机构地区：[1]内蒙古医科大学药学院,内蒙古呼和浩特010100 [2]内蒙古医科大学新药安全评价中心,内蒙古呼和浩特010100 [3]内蒙古医科大学基础医学院,内蒙古呼和浩特010100

出　　处：《中国新药与临床杂志》2020年第2期97-102,共6页Chinese Journal of New Drugs and Clinical Remedies

基　　金：内蒙古自治区自然科学基金项目（2015MS08111）;内蒙古医科大学博士启动基金（YKD2017BQ003

摘　　要：目的研究新化学合成药物2-苯基-3,4-噻二唑[3,2-α]并嘧啶-7-酮(TPh)对宫颈癌HeLa细胞增殖、凋亡及相关因子表达的作用。方法MTT法检测空白对照组和不同浓度TPh(0.6、0.4、0.2、0.1和0.05μmol·mL^-1)组培养24、48、72 h后对HeLa细胞增殖的作用,流式细胞术检测TPh对HeLa细胞周期的影响,Annexin-V FITC/PI双染检测TPh对HeLa细胞凋亡的影响,JC-1染色观察TPh对HeLa细胞线粒体膜电位的影响,Western blotting法检测凋亡相关因子表达情况。结果与空白对照组相比,TPh组Hela细胞增殖被显著抑制,HeLa细胞G0/G1期比例增加、G2/M期比例减少,HeLa细胞线粒体膜电位降低,HeLa细胞caspase-3、caspase-8、caspase-9表达增加、凋亡细胞比率增加(P<0.05,P<0.01),且呈剂量依赖性趋势。结论TPh可抑制宫颈癌HeLa细胞增殖,并促进凋亡,这可能与其激活细胞内源性和外源性凋亡途径有关。AIM To study the effect of the new chemical synthetic drug 2-phenyl-3,4-thiadiazole[3,2-α]-pyrimidin-7-one(TPh)on proliferation,apoptosis and expression of related factors of cervical cancer HeLa cells.METHODS MTT assay was used to detect the effect of different concentrations of TPh(0.6,0.4,0.2,0.1,0.05μmol·mL^-1)on HeLa cells proliferation compared with blank control after 24,48,72 h of culture.Flow cytometry was used to detect the effect of TPh on HeLa cell cycle.The effect of TPh on HeLa cell apoptosis was observed by Annexin-V FITC/PI double staining and mitochondrial membrane potential of HeLa cells was observed by JC-1 staining.The expression of apoptosis related factors were detected by Western blotting.RESULTS Compared with the blank control group,the Hela cell proliferation of TPh group was inhibited,the proportion of HeLa cells in G0/G1 phase increased and the proportion of G2/M phase decreased,the mitochondrial membrane potential decreased,and the expression of caspase-3,caspase-8 and caspase-9 and the ratio of apoptotic cells in HeLa cells increased(P<0.05,P<0.01).CONCLUSION TPh can inhibit HeLa cell proliferation and promote apoptosis,which is related to the activation of endogenous and exogenous apoptosis pathway.

关 键 词：宫颈肿瘤 HELA细胞 细胞增殖 细胞周期 细胞凋亡 2-苯基-3 4-噻二唑[3 2-α]并嘧啶-7-酮 

分 类 号：R979.1[医药卫生—药品] R737.3[医药卫生—药学]