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基于网络药理学的柴胡镇痛作用机制初探

Investigation of Analgesic Mechanisms of Bupleuri Radix with Network Pharmacology
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摘要 目的通过采用网络药理学方法,系统分析柴胡镇痛的主要作用机制及作用靶标,并初步阐明口服和注射两种给药方式下作用靶标差异,筛选可用于其质量评价的生物靶标并进行验证。方法基于数据库和文献检索收集柴胡的化学成分及其可能的作用靶标,以文献报道结合口服生物利用度和类药性作为区分口服制剂和注射用药药效成分的原则,从Gene Cards数据库中检索疼痛相关靶标,利用DIP蛋白质相互作用建立成分靶标与疼痛靶标的关联关系,构建柴胡镇痛的"药物成分-靶标-疾病"网络,通过网络分析筛选关键作用靶标并阐释其可能的机制。结果根据网络分析结果,共筛选出13个柴胡镇痛作用的主要靶标,包括胰蛋白酶原1、凝血酶原、二肽基肽酶4、乙酰胆碱酯酶、环氧化酶2、激素受体、雌激素受体、核受体辅助激活子1、一氧化氮合酶3等,主要影响细胞增殖、精氨酸分解代谢、血小板活化等过程。针对口服和注射两种不同给药方式下,主要作用靶点差异的分析结果表明,胰蛋白酶原1、环氧化酶2以及一氧化氮合酶3均为两种方式的主要作用靶标,可作为其生物评价的重要靶标;同时,注射剂成分对凝血酶原的过多作用可能与其不良反应有关。本研究选择环氧化酶2对柴胡的药效作用进行验证,体外试剂盒检测结果表明,柴胡质量浓度为3.125~50μg·m L^-1时可对环氧化酶2活性产生显著直接抑制作用。结论网络药理学可有效预测不同给药方式下柴胡镇痛的作用靶标及机制,亦可为构建基于镇痛作用的柴胡质量生物评价方法提供参考。 OBJECTIVE To analyze the major analgesic mechanism and target of Bupleuri Radix with a network pharmacology method,clarify the difference targets between oral administration and injection administration,and validate the possible biological target for its quality evaluation.METHODS The chemical components and potential targets of Bupleuri Radix were collected based on the database and literature searching and the analgesic associated targets were searched from Genecards database.All of the targets combined with interactional proteins from DIP database were used to construct a"compound-target-disease"network and the major analgesic mechanism of Bupleuri Radix were then predicted by the key function targets screened from it.RESULTS According to the results of network analysis,13 key targets were screened out,including trypsin-1,prothrombin,dipeptidyl peptidase 4,acetylcholinesterase,COX-2,androgen receptor,estrogen receptor,GABA receptorα1 and NOS-3,which might affect the process of cell proliferation,arginine catabolic process,platelet activation and so on.Trypsinogen-1,cyclooxygenase-2 and nitric oxide synthase-3 were the main targets for both of them,and could be used as the targets for biological evaluation of Bupleuri Radix.At the same time,there were some differences between oral administration and injection of Bupleuri Radix,the excessive effects of injection components on prothrombin may be associated with the adverse reactions of injection.Otherwise,inhibition of COX-2 enzyme activity by in vitro testing showed that Bupleuri Radix has good activity at the concentration of 3.125-50μg·m L-1.CONCLUSION Network pharmacology provides the potential to predict the analgesic mechanism and to establish new quality evaluation methods of Bupleuri Radix.
作者 谈英 杨晓娟 韩晓妮 张跃飞 代春美 牛明 TAN Ying;YANG Xiao-juan;HAN Xiao-ni;ZHANG Yue-fei;DAI Chun-mei;NIU Ming(China Resources Sanjiu Medical&Pharmaceutical Co.,Ltd.,Shenzhen 518110,China;NERC for the Pharmaceutics of Traditional Chinese Medicines,Benxi 117004,China;China Military Institute of Chinese Medicine,302 Military Hospital of China,Beijing 100039,China;Jinzhou Medical University,Jinzhou 121001,China)
出处 《中国药学杂志》 CAS CSCD 北大核心 2019年第2期98-104,共7页 Chinese Pharmaceutical Journal
基金 国家公益性行业专项课题资助(201507002) 国家中药标准化项目资助(ZYBZH-Y-TJ-43,ZYBZH-Y-BJ-07,ZYBZH-C-HUN-21) 全军医学科技“十二五”科研项目资助(BWS11J049) 全军医学科技青年培育项目资助(16QNP151).
关键词 柴胡 镇痛作用 网络药理学 Bupleuri Radix analgesic effect network pharmacology
作者简介 谈英,男,博士,高级工程师研究方向:中药学;通讯作者:牛明,男,工程师研究方向:生物信息学,Tel:(010)66933325 E-mail:nmbright@163.com.
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