2-(N-丙基)-6-三氟甲氧基苯并噻唑抗肿瘤活性研究  

Research on anti-tumour activity of 2-(N-propylamine)-6-trifluoromethoxy-benzothiazole

作　　者：张飞 刘振国[2] 王海芳 武祥龙 刘柳 蔺旭彬 吕文君 刘浩 ZHANG Fei;LIU Zhen-guo;WANG Hai-fang;WU Xiang-long;LIU Liu;LIN Xu-bin;LYU Wen-jun;LIU Hao(Key Lab for Space Bioscience and Biotechnology,School of Life Sciences,Northwestern PolytechnicalUniversity,Xi’an710072,China;Intensive Care Unit,Shaanxi Provincial People’s Hospital,Xi’an710068,China;Shaanxi Key Lab of Integrated Traditional and Western Medicine for Prevention and Treatmentof Cardiovascular Diseases,Shaanxi University of Chinese Medicine,Xi’an712046,China)

机构地区：[1]西北工业大学生命学院空间生物实验模拟技术重点实验室,陕西西安710072 [2]陕西省人民医院重症医学科,陕西西安710068 [3]陕西中医药大学陕西省中西医结合心血管病防治重点实验室,陕西西安712046

出　　处：《中国药理学通报》2019年第5期644-648,共5页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目(No 21202130);大学生创新创业训练计划项目(No 201710699335)

摘　　要：目的研究2-(N-丙基)-6-三氟甲氧基苯并噻唑的抗肿瘤活性和机制。方法采用CCK-8法测定药物对HeLa、HepG2、MCF-7和SP2/0肿瘤细胞增殖的影响;Hoechst 33258染色和Annexin V-FITC/PI双染法,检测药物对MCF-7细胞的促凋亡作用,观察药物作用后肿瘤细胞的形态;采用细胞划痕实验,检测药物对肿瘤细胞迁移能力的影响。结果 2-(N-丙基)-6-三氟甲氧基苯并噻唑能明显抑制4种肿瘤细胞的增殖,且具有较好的选择性,特别是对MCF-7作用最明显,其IC_(50)值为(12.91±0.69)μmol·L^(-1)。对MCF-7细胞有比较强的抗迁移作用,划痕愈合率较对照组明显降低,还可诱导MCF-7细胞的早期凋亡。结论 2-(N-丙基)-6-三氟甲氧基苯并噻唑可抑制肿瘤细胞的增殖,并且通过诱导MCF-7细胞的早期凋亡,抑制MCF-7细胞迁移,从而发挥其增殖抑制作用。Aim To study the anti-tumour activity and mechanism of 2-(N-propylamine)-6-trifluoromethoxy-benzothiazole. Methods The anti-proliferative activities against HeLa,HepG2,MCF-7 and SP2/0 cancer cell lines were assessed by CCK-8 assay.The morphological changes of cancer cells were observed by Hoechst staining.Effects on the cell migration were evaluated by monolayer cells wound healing assay.The cell apoptosis analysis was evaluated by using the flow cytometric analysis. Results Compound 2-(N-propylamine)-6-trifluoromethoxy-benzothiazole showed good selectivity and inhibitory effects against four tumor cell lines.Especially,the effects on MCF-7 cells were very significant.This compound could inhibit the migration of MCF-7 cells and induce early apoptosis. Conclusions 2-(N-propylamine)-6-trifluoromethoxy-benzothiazole can inhibit the proliferation of four tumor cell lines.It shows inhibitory effects on MCF-7 cells by inducing early apoptosis.

关 键 词：苯并噻唑 肿瘤 肿瘤细胞 迁移 增殖 凋亡 

分 类 号：R329.24[医药卫生—人体解剖和组织胚胎学] R329.25[医药卫生—基础医学]