铁-氟尿嘧啶配合物抗肿瘤活性研究

›› 2017, Vol. 2 ›› Issue (2): 11-19.

铁-氟尿嘧啶配合物抗肿瘤活性研究

（1.昆明医科大学药学院，昆明650500；2.云南开放大学化学学院，昆明650223；3.昆明医科大学
基础医学院，昆明650500；4.昆明学院化学系，昆明650214）

收稿日期:2016-04-06 修回日期:2016-06-14 出版日期:2017-02-15 发布日期:2017-02-15
作者简介:杜馨娥，硕士研究生，主要从事肿瘤药理研究.
基金资助:
云南省科技厅-昆明医科大学应用基础研究联合专项资助项目（2014FB011）；云南省教育厅科学研究基金资
助项目（2014Z060）

Research on Anti-tumor Activity of Iron-fluorouracil Complex

（1. Pharmaceutical Science, Kunming Medical University, Kunming 650500, China; 2. College of Chemistry, Yunnan Open University,
Kunming 650223, China; 3 School of Basic Medicine, Kunming Medical University, Kunming 650500, China; 4. Department of
Chemistry, Kunming University, Kunming 650214, China）

Received:2016-04-06 Revised:2016-06-14 Online:2017-02-15 Published:2017-02-15

摘要/Abstract

摘要：

目的：探讨铁-氟尿嘧啶配合物的抗肿瘤活性和对人胃癌细胞凋亡的影响。方法：采用MTT法检测配合物及其配体对
K562、HCT-116、SGC-7901、MCF-7和HEPG-2 细胞的增殖抑制作用；Hoechst 33342/PI双染法和流式细胞术检测对人胃癌
细胞凋亡的影响；RT-qPCR 检测对Caspase-3、Bax、Bcl-2 基因表达的影响。结果：配合物作用5株细胞后的IC50值分别为
7.8×10-5、5.4×10-5、3.5×10-5、1.1×10-4和2.2×10-5 mol/L，能明显抑制细胞的增殖。配合物以10-5 mol/L浓度作用SGC-7901细胞36 h
后，凋亡率为9.8%，能明显促进SGC-7901细胞凋亡（P＜0.01），作用强于其配体5-Fu和Phen（P＜0.01）；使凋亡相关基因
Caspase-3表达上调至4.9（P＜0.01）；Bcl-2 表达下调至0.2（P＜0.01）。结论：铁-氟尿嘧啶配合物具有良好的体外抗肿瘤活性，
其发挥抗肿瘤作用可能与诱导肿瘤细胞凋亡有关，而其诱导凋亡的作用可能与Caspase-3 基因上调和Bcl-2基因下调有关。

关键词: 铁-氟尿嘧啶配合物, 细胞毒活性, 凋亡

Abstract:

Objective: To explore iron- fluorouracil complex's anti- tumor activity and effect to human gastric carcinoma cells
apoptosis. Methods: MTT method was used to detect inhibition rate of the complex on tumor cell lines: K562, HCT-116, SGC-7901,
MCF-7 and HEPG-2; Hoechst 33342/PI and flow cytometry（FCM）methods were used to exhibit apoptosis of SGC-7901 cells; RTqPCR
was used to measure the mRNA expression of apoptosis related factors: Caspase-3, Bax and Bcl-2. Results: Iron-fluorouracil
complex obviously inhibited the proliferation of 5 tumor cell lines. IC50 were 7.8×10-5, 5.4×10-5, 3.5×10-5, 1.1×10-4 and 2.2×10-5 mol/L,
respectively. After 36 hours' treatment on SGC-7901 cell with a concentration 10- 5 mol/L, its apoptosis rate was 9.8%, which could
promote SGC-7901 cell apoptosis than its ligands 5-Fu and Phen（P＜0.01）; the mRNA expression of Caspase-3 gene was up-regulated
to 4.9（P＜0.01）, while Bcl-2 was down-regulated to 0.2（P＜0.01）. Conclusion: The complex showed good anti-tumor activity in
vitro, up regulation of Caspase-3 as well as down regulation Bcl-2 may be one of its mechanisms of action.

Key words: iron-fluorouracil complex, cytotoxicity, apoptosis

中图分类号:

杜馨娥，周云，陈英杰，施敏，钟文远，周轶平. 铁-氟尿嘧啶配合物抗肿瘤活性研究[J]. , 2017, 2(2): 11-19.

Du Xin'e, Zhou Yun, Chen Yingjie, Shi Min, Zhong Wenyuan, Zhou Yiping. Research on Anti-tumor Activity of Iron-fluorouracil Complex[J]. , 2017, 2(2): 11-19.

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