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氯化两面针碱抑制肿瘤血管生成相关靶标蛋白的初步筛选

傅宣皓 秦悦 黄焱燚 谢雪平 成晓静 刘华钢 赖泽锋

广西医科大学学报2017,Vol.34Issue(5):650-653,4.
广西医科大学学报2017,Vol.34Issue(5):650-653,4.DOI:10.16190/j.cnki.45-1211/r.2017.05.003

氯化两面针碱抑制肿瘤血管生成相关靶标蛋白的初步筛选

A preliminary screening of molecular targets for anti-tumor angiogenesis effect of nitidine chloride

傅宣皓 1秦悦 1黄焱燚 1谢雪平 1成晓静 2刘华钢 1赖泽锋1

作者信息

  • 1. 广西医科大学药学院,南宁 530021
  • 2. 广西医科大学生命科学研究院,南宁530021
  • 折叠

摘要

Abstract

Objective:To preliminarily screen the molecular targets of nitidine chloride (NC) relevant to its anti-tumor angiogenesis effect.Methods:Human umbilical vein endothelial cells (HUVECs) were divided into a control group and two different doses (30 μmol/L and 60μmol/L) NC groups.The migration ability of HUVECs was detected by wound healing assay after exposure to NC for 24 h and 48 h.The protein expression of vascular endothelial growth factor (VEGF) in HUVECs was determined by western blotting after NC treatment.The computer-aided drug design (CADD) software SYBYL 2.0 was employed to conduct the molecular docking between NC and the receptors from the tumor angiogenesis signals,and the Pymol software was used to draw the 3-dimension structures of the docking results.The interaction between NC and the receptors was analyzed.Results:Compared with the control group,the cell migration rate in 30 μmol/L and 60 μmol/L NC groups was significantly decreased (P <0.001).The protein expression of VEGF in NC groups was down-regulated (P <0.01).The molecular docking results indicated that NC had strong affinity to both phosphatidylinositol 3-kinase (PI3K) and non-receptor tyrosine kinase (c-Src) and their interactions were dominantly hydrogen bonds and hydrophobic interaction.Conclusion:NC inhibited the migration of HUVECs via suppressing the expression of VEGF.PI3K and c-Src might be potential molecular targets relevant to anti-tumor and anti-angiogenesis effects of NC.

关键词

氯化两面针碱/血管生成/分子对接/靶标/PI3K/c-Src

Key words

snitidine chloride/angiogenesis/molecular docking/target/PI3K/c-Src

分类

医药卫生

引用本文复制引用

傅宣皓,秦悦,黄焱燚,谢雪平,成晓静,刘华钢,赖泽锋..氯化两面针碱抑制肿瘤血管生成相关靶标蛋白的初步筛选[J].广西医科大学学报,2017,34(5):650-653,4.

基金项目

国家自然科学基金资助项目(No.81260657) (No.81260657)

广西医科大学学报

OACSTPCD

1005-930X

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