Page 46 - 《中国药房》2022年11期
P. 46
山豆根抗鼻咽癌活性成分的筛选 Δ
1 #
2
2
2
1
1,2
2
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 (1.黑龙江中医药大学国家
1*
2
中医药管理局中医方证代谢组学研究中心/教育部经典名方有效性评价及产业化开发工程研究中心,哈尔滨
150040;2.广西壮族自治区药用植物园/西南濒危药材资源开发国家工程实验室,南宁 530023)
中图分类号 R917;R965 文献标志码 A 文章编号 1001-0408(2022)11-1320-05
DOI 10.6039/j.issn.1001-0408.2022.11.07
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Swiss Target Prediction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Cytoscape 3.6.1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。
关键词 山豆根;鼻咽癌;活性成分;越南槐醇;山豆根素;高丽槐素
Screening of active components of Euchresta japonica against nasopharyngeal carcinoma
1
2
2
NAN Junling ,WANG Chaozhong ,YAN Guangli ,WU Fangfang ,SONG Zhijun ,WANG Shuo ,ZHOU Xiaolei ,
2
2
1
1
MIAO Jianhua ,WANG Xijun (1. Chinmedomics Research Center of National Administration of Traditional
2
1,2
Chinese Medicine/Research Center for Effectiveness Evaluation and Industrialization Development Engineering of
Classical Formula of the Ministry of Education,Heilongjiang University of Chinese Medicine,Harbin 150040,
China;2. Guangxi Botanical Garden of Medical Plants/Southwest National Engineering Laboratory for the
Resources Development of Endangered Medicinal Materials,Nanning 530023,China)
ABSTRACT OBJECTIVE To screen the active components 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.
KEYWORDS Euchresta japonica;nasopharyngeal carcinoma;active components;tonkinensisol;sophoranone;maackiain
Δ 基金项目:广西创新驱动发展专项(No.桂科 AA18242040);广
西科技基地和人才专项(No.桂科AD18126013);广西特色药用资源开 山豆根为豆科植物越南槐Sophora tonkinensis Gag-
发科技创新基地建设项目(No.桂科ZY21195044)
nep.的干燥根和根茎,又名广豆根,具有清热解毒、消肿
*硕士研究生。研究方向:中药药效物质基础及新药开发。
利咽的功效,可用于治疗火毒蕴结、乳蛾喉痹、咽喉肿
E-mail:1065913709@qq.com
[1]
# 通信作者:副研究员,硕士生导师。研究方向:中药药效物质基 痛、齿龈肿痛、口舌生疮 。现代药理学研究表明,山豆
础及新药开发。E-mail:gancaosuan@163.com 根具有抗肿瘤、抗病毒及增强免疫等药理作用 [2-3] 。鼻
·1320 · China Pharmacy 2022 Vol. 33 No. 11 中国药房 2022年第33卷第11期