1,8-萘二甲酰亚胺衍生物NA-17对肝癌细胞株HepG2的体外抗肿瘤作用研究

doi:10.16088/j.issn.1001-6600.2016.03.014

广西师范大学学报（自然科学版） ›› 2016, Vol. 34 ›› Issue (3): 102-108.doi: 10.16088/j.issn.1001-6600.2016.03.014

1,8-萘二甲酰亚胺衍生物NA-17对肝癌细胞株HepG2的体外抗肿瘤作用研究

吴亦明¹, 李亮萍², 曾淑兰², 李晓红², 周祖平¹, 彭艳²

1. 广西师范大学生命科学学院,广西桂林541006;
2. 广西师范大学化学与药学学院,广西桂林541004

收稿日期:2015-11-24 出版日期:2016-09-30 发布日期:2018-09-17
通讯作者: 彭艳(1968—),女,辽宁锦州人,广西师范大学教授,博士。E-mail: pengyan630@gxnu.edu.cn
基金资助:
广西自然科学基金资助项目(2014GXNSFAA118165,2015GXNSFDA139010);教育部创新团队项目(IRT1225);广西医药产业人才小高地资助项目(1309,1312,1507);药用资源化学与药物分子工程省部共建国家重点实验室主任基金资助项目(CMEMR2015-A09,CMEMR2014-A11);广西研究生教育创新计划项目(JGY2015023);八桂学者计划资助项目

The Anti-Tumor Mechanism of 1,8-Naphthalate FormylImide Derivative NA-17 in HepG2 Cells

WU Yiming¹, LI Liangping², ZENG Shulan², LI Xiaohong², ZHOU Zuping¹, PENG Yan²

1. College of Life Sciences,Guangxi Normal University,Guilin Guangxi 541006,China;
2. College of Chemistry & Pharmaceutical Sciences,Guangxi Normal University,Guilin Guangxi 541004,China

Received:2015-11-24 Online:2016-09-30 Published:2018-09-17

摘要/Abstract

摘要： 本文对1,8-萘二甲酰亚胺衍生物NA-17(N-(3,4-亚甲二氧苯乙基)-4-(3-N,N-二甲氨基)丙胺基-1,8-萘二甲酰亚胺)在肝癌细胞中的抗肿瘤活性进行了研究。对多种肿瘤细胞的抗肿瘤活性筛选表明NA-17对肿瘤细胞具有一定的选择性,其中对肝癌细胞(HepG2)有较好的抑制效果,但对正常肝细胞(HL-7702)毒性较低。初步的机制研究显示,NA-17通过诱发HepG2细胞发生早期凋亡杀死HepG2细胞,但对细胞周期无明显影响,进一步的分子机制研究表明NA-17通过下调抗凋亡蛋白Bcl-2、Bcl-xL的表达,同时上调凋亡蛋白Bak的表达,从而诱导HepG2细胞发生细胞凋亡。

关键词: NA-17, 细胞凋亡, HepG2, 选择性抑制, 抗肿瘤活性

Abstract: The antitumor effects of a novel 1,8-naphthalate formyl imide derivative NA-17 in human liver cancer cells was researched. The inhibition effects of NA-17 in various human cancer cell lines showed that NA-17 exhibited highly selective inhibition in human liver cancer cell line HepG2, but with low toxicity to normal hepatic cell HL-7702. Preliminary research indicated that NA-17 induced apoptosis to suppress proliferation in HepG2 cells. Further studies showed that NA-17 induced the increase in the levels of Bak, while the decrease in Bcl-2 and Bcl-xL to trigger cell apoptosis.

Key words: NA-17, apoptosis, HepG2, selective inhibition, antineoplastic activity

吴亦明, 李亮萍, 曾淑兰, 李晓红, 周祖平, 彭艳. 1,8-萘二甲酰亚胺衍生物NA-17对肝癌细胞株HepG2的体外抗肿瘤作用研究[J]. 广西师范大学学报（自然科学版）, 2016, 34(3): 102-108.

WU Yiming, LI Liangping, ZENG Shulan, LI Xiaohong, ZHOU Zuping, PENG Yan. The Anti-Tumor Mechanism of 1,8-Naphthalate FormylImide Derivative NA-17 in HepG2 Cells[J]. Journal of Guangxi Normal University(Natural Science Edition), 2016, 34(3): 102-108.

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1,8-萘二甲酰亚胺衍生物NA-17对肝癌细胞株HepG2的体外抗肿瘤作用研究

The Anti-Tumor Mechanism of 1,8-Naphthalate FormylImide Derivative NA-17 in HepG2 Cells

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