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
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-SrcKey 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)