Artificial sodium channel amine ligands suppress growth and invasion in prostate cancer cells in vitro

周蕊; 卢宗亮; 刘凯; 杨柳娜; 胡叶敏; 常徽; 周永; 糜漫天; 李雁武; 许红霞

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Artificial sodium channel amine ligands suppress growth and invasion in prostate cancer cells in vitro

更新时间：2026-01-09

- Artificial sodium channel amine ligands suppress growth and invasion in prostate cancer cells in vitro
- Journal of Army Medical University Vol. 36, Issue 5, Pages: 422-426(2014)
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  CLC： R329.25;R737.25;R979.1
- Published：2014
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周蕊,卢宗亮,刘凯,杨柳娜,胡叶敏,常徽,周永,糜漫天,李雁武,许红霞.人工合成钠离子通道阻断剂抑制前列腺癌细胞的生长及侵袭[J].陆军军医大学学报(原第三军医大学学报),2014,36(05):422-426.

　Zhou Rui,Lu Zongliang,Liu Kai,Yang Liuna,Hu Yemin,Chang Hui,Zhou Yong,Mi Mantian,Li Yanwu,Xu Hongxia.Artificial sodium channel amine ligands suppress growth and invasion in prostate cancer cells in vitro[J].J Amry Med Univ (J Third Mil Med Univ),2014,36(05):422-426.
周蕊,卢宗亮,刘凯,杨柳娜,胡叶敏,常徽,周永,糜漫天,李雁武,许红霞.人工合成钠离子通道阻断剂抑制前列腺癌细胞的生长及侵袭[J].陆军军医大学学报(原第三军医大学学报),2014,36(05):422-426. DOI：

　Zhou Rui,Lu Zongliang,Liu Kai,Yang Liuna,Hu Yemin,Chang Hui,Zhou Yong,Mi Mantian,Li Yanwu,Xu Hongxia.Artificial sodium channel amine ligands suppress growth and invasion in prostate cancer cells in vitro[J].J Amry Med Univ (J Third Mil Med Univ),2014,36(05):422-426. DOI：

摘要

目的研究人工合成钠离子通道阻断剂(sodium channel amine ligands，SCALs)对前列腺癌细胞株（PC3细胞、DU145细胞）生长及侵袭的影响，以筛选高效的抗肿瘤药物。方法四甲基偶唑氮（MTT）法检测SCALs对肿瘤细胞的存活率的影响；Transwell侵袭实验检测SCALs干预后肿瘤细胞体外侵袭能力的变化；流式细胞仪检测SCALs促进细胞凋亡及阻滞细胞周期的能力，蛋白免疫印迹实验检测SCALs对钠离子通道蛋白α亚基Nav 1.7 蛋白表达的影响。结果 7种SCALs中的3种（S1127、S1169、S1180）对前列腺癌细胞敏感，在低浓度时对肿瘤细胞具有杀伤效应，且其抑制率与药物浓度呈剂量-效应关系，其中S1180对PC3和DU145细胞的IC

分别为2.9 μmol/L和2.5 μmol/L，在10 μmol/L时能促进12.89%的肿瘤细胞凋亡、抑制75.53%的细胞侵袭，并具有阻滞细胞周期的能力，以及能下调Nav 1.7 蛋白的表达水平。结论合成的钠离子通道阻断剂中3种SCALs尤其是S1180具有显著杀伤前列腺癌细胞效应，将来可能成为治疗肿瘤的一类新型药物。

Abstract

Objective To determine the effect of artificially synthesized sodium channel amine ligands (SCALs) on the growth and invasion of prostate cancer cell lines. Methods SCALs compounds

S1127

S1156

S1169

S1170

S1178

S1180

and S1182 were synthesized and confirmed. Prostate cancer cell lines

PC3 and DU145

were used in this study. The cell viability was assessed by MTT assay in the cells after the treatment of SCALs respectively. The cell apoptosis and cell cycle progression were assessed by flow cytometry. T

he cancer cell invasion was assessed by Transwell chamber assay. The protein expression of prostate cancer sodium channel α subunit

Nav 1.7 was determined by Western blotting. Results Three compounds

S1127

S1169

and S1180

inhibited the growth of tumor cells in a dose-dependent manner. S1180 was found to be the most potent among the 7 compounds. The IC

values of S1180 were 2.9 and 2.5 μmol/L respectively for PC3 and DU145 cells. At 10 μmol/L

S1180 improved cell apoptosis in 12.89% PC3 cells

and suppressed the cell invasion in 75.53% cells

and exerted significant effects on cell arrest

and down-regulated Nav 1.7 protein expression. Conclusion Three SCALs compounds

especially S1180

have obvious anti-tumor effect on prostate cancer cells

and might be a potential therapeutic agent for prostate cancer.

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