卤代3-芳基香豆素体外抗肿瘤活性研究  

Study on Antitumor Activity of Halogenated 3-Aryl Coumarin in Vitro

作　　者：肖春芬[1] 黄秋妹[1] 刘卫海[1] 沈小莉[1] XIAO Chun-fen;HUANG Qiu-mei;LIU Wei-hai;SHEN Xiao-li(Guangdong Food and Drug Vocational College,Guangzhou 510520,China)

机构地区：[1]广东食品药品职业学院

出　　处：《广州化学》2019年第4期61-64,共4页Guangzhou Chemistry

基　　金：广东省医学科学技术研究基金项目（A2017437）;广东食品药品职业学院自然科学研究项目（2016YZ015）

摘　　要：从24个卤代3-芳基香豆素化合物中筛选抗肿瘤化合物,为开发新型抗肿瘤药物提供参考。采用MTT法测定24个卤代3-芳基香豆素化合物对人前列腺癌细胞PC-3、人乳腺癌细胞MCF-7、人肝癌细胞HepG2的生长抑制作用,用抑制率评价增殖抑制效果。结果表明,试药浓度为25μg/mL时,24种化合物对PC-3、MCF-7、HepG2细胞株均有不同程度的增殖抑制作用,绝大部分化合物增殖抑制率超过50%。其中化合物A6、B6表现出较强的增殖抑制活性,对PC-3细胞株的抑制率分别为72.09%和73.3%,对HepG2细胞株的抑制率分别为80.17%和81.02%,与阳性对照星孢菌素的抑制率接近。试药浓度为5μg/mL时,24种化合物对MCF-7细胞株的抑制率均没有超过50%,对HepG2细胞株有3个化合物抑制率超过50%,对PC-3细胞株有18个化合物抑制率超过50%。3-芳基香豆素化合物具有潜在的肿瘤细胞增殖抑制活性,有发展为抗肿瘤药物的潜力。The anti-tumor compounds were screened from 24 3-arylcoumarins,which could provide a reference for the development of new anti-tumor drugs.The inhibitory effects of 24 3-arylcoumarins on the growth of human prostate cancer cell line PC-3 and human breast cancer cell line MCF-7 and human hepatocellular carcinoma cell line HepG2 were determined by MTT assay,and the inhibitory effect was evaluated by inhibition rate.At the concentration of 25μg/mL,24 compounds showed anti-proliferation inhibition activity of cell lines PC-3,MCF-7 and HepG2 to some extent.Most of the compounds had more than 50%inhibitory effect.Compound A6 and B6 showed strong inhibitory activity on proliferation.The inhibitory rates of A6 and B6 were 72.09%and 73.3%on PC-3 cell lines and 80.17%and 81.02%on HepG2 cell lines,respectively.The inhibitory effect of compound A6 and B6 on PC-3,HepG2 cell line was close to that of staurosporine.At the concentration of 5μg/mL,the inhibition rates of 24 compounds on MCF-7 cell lines were not more than 50%,3 compounds on HepG2 cell lines were more than 50%,and 18 compounds on PC-3 cell lines were more than 50%.3-Arylcoumarin compounds have the potential to inhibit the proliferation of tumor cells and have the potential to develop into anti-tumor drugs.

关 键 词：卤代3-芳基香豆素 人前列腺癌细胞PC-3 人乳腺癌细胞MCF-7 人肝癌细胞HEPG2 

分 类 号：R73-3[医药卫生—肿瘤]