新化合物(Z)-7-氟-6-甲基-3(哌嗪-1-亚甲基)硫色满-4-酮体外抗肿瘤作用  

Antitumor Effect of (Z)-7-fluoro-6-methyl-3-(piperazin-1-methylene) thiochroman-4-ketone in Vitro

作　　者：崔世怡[1,2] 刘玉欣[1] 杨更亮 方保岭 田伟 

机构地区：[1]河北大学药学院细胞药理研究室,河北保定071002 [2]保定市第三中心医院 [3]河北省药物质量分析控制重点实验室

出　　处：《中国药师》2010年第5期612-614,共3页China Pharmacist

基　　金：河北大学研究基金资助(编号:y2008118)

摘　　要：目的:研究(Z)-7-氟-6-甲基-3(哌嗪-1-亚甲基)硫色满-4-酮(FMTK)对人宫颈癌HeLa细胞系,肺癌A549细胞系,肝细胞癌HepG2细胞系,低分化胃腺癌BGC-823细胞系的抗肿瘤活性,为深入研究FMTK抗肿瘤作用提供实验依据。方法:4种肿瘤细胞培养于含有不同浓度的FMTK培养液中,实验设受试药物组、阴性对照组、阳性对照组、空白对照组、溶剂对照组,采用四甲基偶氮唑蓝微量酶比色法(MTT法)检测FMTK对以上4种肿瘤细胞增殖的影响;采用大鼠小肠隐窝上皮细胞IEC-6检测FMTK对正常细胞的毒性。结果:通过检测以上细胞的增殖情况,得出FMTK半数抑制浓度(IC_(50))如下:HeLa(80.09±1.48μg·ml^(-1)),BGC-823(55.87±1.14μg·ml^(-1)),HePG2(35.06±2.68μg·ml^(-1)),FMTK对A549几乎没有抑制作用。FMTK对人宫颈癌HeLa细胞系,肝细胞癌HepG2细胞系,低分化胃腺癌BGC-823细胞系抑制作用随着剂量和时间的增加而增高,与阴性对照组相比,差异有统计学意义(P<0.05);FMTK对大鼠小肠隐窝上皮细胞IEC-6没有抑制作用。结论:FMTK具有体外抗肿瘤活性,对正常细胞IEC-6无毒性。Objective： To explore the inhibitory effect of （ Z ） -7-fluoro-6-methyl-3- （ piperazin-1 -methylene ） thiochroman-4-ketone （FMTK） on the growth of cancer cell lines （HeLa, BGC-823, HepG2, A549 cells） and IEC-6 cells. Method： Four human cancer cell lines and IEC-6 cells were subjected to various concentration of FMTK in culture medium, the inhibitory rate of FMTK was masured by MTT assay and compared with a negative contral, solvent control, blank and cisplatin positive control. Result： FMTK inhibited HeLa, BGC-823 and HepG2 cells growth in concentration and time dependent manner, and has no inhibitory effect on A549 cells the 50% inhibiting concentration （ IC50 ） of FMTK was showed by studying the growth of the four cancer cell lines as fllow：uterine cervix cancer （ HeLa cells ： 80.09 ± 1.48 μg · ml^-1 ）, gastric cancer（ BGC-823 ceils ： 55.87 ± 1.14 μg · ml^-1 ）, liver cancer（ HePG2 ceils： 35.06 ± 2.68 μg · ml^-1 ） ,lung cancer （A549 cells： nearly no inhibitory effect）, the inhibitory rate of IEC-6 was less than eisplatin . Conclusion： FMTK has an antitumor effect and its toxicity to IEC-6 cells is less than cisplatin in vitro.

关 键 词：(Z)-7-氟-6-甲基-3(哌嗪-1-亚甲基)硫色满-4-酮 抗肿瘤作用 体外 

分 类 号：R965.1[医药卫生—药理学]