茶氨酸衍生物TClC脂质体对雌激素受体阳性的乳腺癌细胞生长和迁移的抑制作用

为研发抗癌新药,使用茶氨酸衍生物茶氯香酰胺TClC制备纳米脂质体(TClC-L),研究TClC-L对雌激素受体阳性的人乳腺癌MCF-7细胞生长和迁移的抑制作用,并深入探究可能的作用机制。分别采用MTT和Transwell chamber实验方法探究各浓度TClC-L对MCF-7细胞的生长和迁移的抑制作用;使用流式细胞术(FCM)检测TClC-L对MCF-7细胞凋亡的影响;应用Western blotting检测MCF-7细胞生长和迁移有关蛋白和酶的表达。实验结果显示,TClC-L对MCF-7细胞生长和迁移有显著的抑制、对癌细胞的凋亡表现促进作用;TClC-L明显下调受体蛋白p-VEGFR~2、Met和ER-α、抗凋亡蛋白Bcl-2、Cyclin D1、Akt和NF-?B的表达,上调促凋亡蛋白Bax、Caspase-3、p53和p21的表达。TClC-L作用的分子机制可能与抑制VEGFR/Met/ER-α-Akt/NF-?B信号传导通路有关。本研究显示了TClC-L有潜在的治疗雌激素受体阳性乳腺癌的作用。

Inhibitory effects of theanine derivative TClC liposome on the growth and migrations of ER-α-positive human breast cancer cells

The purpose of this study was to investigate the inhibitory effects of a theanine derivative TC1C-prepared liposome (TClC-L) on the growth and migrations of human breast cancer MCF-7 cells and its potential mechanism.The assays of MTT and transwell chamber were used to explore the effects of TC1C-L on the MCF-7 cell grown and migration,respectively.The flow cytometry (FCM) and Western blot were applied to analyzing the effects of TC1C-L on the apoptosis and related protein expressions in MCF-7 cells,respectively.The experimental results indicated that TC1C-L inhibited the cell growth and migration and promoted the apoptosis of human breast cancer cells.TC1C-L significantly down-regulated the protein expression and/or phosphorylation of Bcl-2,p-VEGFR2,Met,ER-α,Cyclin D 1,Akt and NF-κB,while it up-regulated the protein expression of Bax,caspase-3,p53,and p21 in MCF-7 cells.The possible molecular mechanism of the TC1C-L action against MCF-7 cells might be connected with the suppression of the signal pathway of VEGFR/Met/ER-α-Akt/NF-κB.TClC-L has a broad application prospect in treating estrogen receptor-positive human breast cancer.