山豆根抗鼻咽癌活性成分的筛选
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篇名: 山豆根抗鼻咽癌活性成分的筛选
TITLE: Screening of active components of Euchresta japonica against nasopharyngeal carcinoma
摘要: 目的 筛选山豆根抗鼻咽癌的活性成分。方法选择山豆根主要化学成分,并在SwissTargetPrediction数据库中预测其作用靶点,同时借助GeneCards数据库获取鼻咽癌相关靶点。将山豆根化学成分靶点与鼻咽癌相关靶点取交集后构建蛋白互作(PPI)网络,再利用Cytoscape3.6.1软件对PPI网络进行分析,筛选山豆根抗鼻咽癌的潜在活性成分和核心靶点。利用分子对接技术评估山豆根潜在活性成分与核心靶点的结合能力,筛选可能的抗鼻咽癌活性成分。利用细胞增殖实验验证山豆根潜在活性成分的抗鼻咽癌活性。结果共筛选出山豆根抗鼻咽癌潜在活性成分7个(越南槐醇、槲皮素、山豆根素、苦参酮、染料木素、山豆根色烯素、高丽槐素),核心靶点10个(SRC、PIK3CA、MAPK1、MAPK3、AKT1、MAPK8、MAP2K1、PTK2、EGFR、JAK3)。分子对接结果显示,上述山豆根潜在活性成分均具有一定抗鼻咽癌活性;进一步细胞增殖实验结果显示,越南槐醇、山豆根素、高丽槐素对人鼻咽癌CNE-1细胞均具有较好的抑制作用。结论越南槐醇、山豆根素、高丽槐素可能是山豆根抗鼻咽癌的主要药效物质基础。
ABSTRACT: OBJECTIVE To screen t he active component s of Euchresta japonica against nasopharyngeal carcinoma. METHODS Main chemical components of E. japonica were selected ,and their target proteins were predicted in Swiss Target Prediction database. The target proteins of nasopharyngeal cancer were obtained with GeneCards database. Protein-protein interaction(PPI)network was established after the target of chemical components of E. japonica was intersected with the target of nasopharyngeal carcinoma ;PPI network was analyzed by using Cytoscape 3.6.1 software,and the potential active components and key targets of E. japonica against nasopharyngeal carcinoma were screened. The molecular docking technology was used to evaluate binding ability of active component-key target ;active components of E. japonica against nasopharyngeal carcinoma were screened. The anti-nasopharyngeal cancer effect of potential active components of E. japonica was verified by cell proliferation experiment. RESULTS Seven potential active components (tonkinensisol,quercetin,sophoranone,matrine,genistein,coumarin,maackiain) and 10 core targets (SRC,PIK3CA,MAPK1,MAPK3,AKT1,MAPK8,MAP2K1,PTK2,EGFR,JAK3)of E. japonica against nasopharyngeal carcinoma were screened. The molecular docking results showed that above potential active components all possessed certain anti-nasopharyngeal cancer effect. Cell proliferation activity test showed that tonkinensisol ,sophoranone and maackiain had a very significant inhibitory activity on nasopharyngeal carcinoma cells CNE- 1. CONCLUSIONS Tonkinensisol, sophoranone and maackiain might be the main active components of E. japonica against nasopharyngeal carcinoma.
期刊: 2022年第33卷第11期
作者: 南俊伶,王超众,闫广利,吴芳芳,宋志军,王硕,周小雷,缪剑华,王喜军
AUTHORS: NAN Junling,WANG Chaozhong, YAN Guangli,WU Fangfang,SONG Zhijun,WANG Shuo,ZHOU Xiaolei,MIAO Jianhua,WANG Xijun
关键字: 山豆根;鼻咽癌;活性成分;越南槐醇;山豆根素;高丽槐素
KEYWORDS: Euchresta japonica ;nasopharyngeal carcinoma ;active components ;tonkinensisol;sophoranone;maackiain
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