五倍子抗炎、抗菌活性指导下的有效成分分离与抗口腔溃疡网络药理学评价  

Separation of active components and evaluation of network pharmacology of anti-ulcer were guided by the anti-inflammatory and antibacterial activities of GallaChinensis

作　　者：齐云云 温鹏 于诗怡 李全凯 李晓娟 陈文 韩博 QI Yunyun;WEN Peng;YU Shiyi;LI Quankai;LI Xiaojuan;CHEN Wen;HAN Bo(School of Pharmacy/Key Laboratory of Xinjiang Phytomedicine Resource and Utilization,Ministry of Education,Shihezi University,Shihezi,Xinjiang 832000)

机构地区：[1]石河子大学药学院/新疆植物药资源利用教育部重点实验室,新疆石河子832000

出　　处：《石河子大学学报（自然科学版）》2020年第5期620-628,共9页Journal of Shihezi University(Natural Science)

基　　金：国家自然科学基金项目(81760756,U1903211);石河子大学成果转化与技术推广计划项目(CGZH201806)。

摘　　要：目的寻找五倍子(GallaChinensis,GCE)中具有抗口腔溃疡的活性成分,并初步分析其作用机理。方法(1)利用柱层析分离五倍子中的成分,并建立五倍子化合物库。预测五倍子化合物潜在靶点并构建可视化相互作用网络。(2)二倍稀释法测定各组分最小抑菌浓度(MIC),牛津杯法测定活性组分的抑菌圈及药物敏感性。(3)分析各组分在口腔溃疡大鼠体内干预过程中的疗效,酶联免疫吸附试验(ELISA)测定溃疡组织中TNF-α、IL-1β和IL-6表达水平。结果(1)将五倍子中化合物分离为GCE-1、GCE-2、GCE-3三段组分,经LC-MS分析得到7个成分,其中3个成分与口腔溃疡治疗的靶点相关。(2)GCE-2段具有较好的抗菌活性,MIC均为5 mg·mL-1。(3)与其他组分相比,GCE-2治疗效果最好,组织中TNF-α、IL-1β表达水平显著降低(P<0.05),溃疡组织病理状态改变。结论GCE-2具有较好的抗口腔溃疡活性。本工作系统分析五倍子治疗口腔溃疡的物质基础及可能作用机制,为五倍子在抗炎、抗菌领域的应用提供有益参考。Objective To investigate the effective components of GallaChinensis(GCE)in treating oral ulcer,preliminary analyze its mechanism of action.Methods(1)Column chromatography was used to separate components of GallaChinensis,and compounds library of GallaChinensis was established,potential targets of GallaChinensis components were predicted and a visual interaction network was constructed.(2)The minimum inhibitory concentration(MIC)value of each component was assessed by double dilution method,and the inhibition zone of effective components were measured by Oxford cup method.(3)The therapeutic effect of each components in oral ulcer rats was analyzed,the levels of TNF-α,IL-1βand IL-6 in ulcer organization were detected by ELISA.Results(1)The compounds in GallaChinensiswere divided into 3 fractions:GCE-1,GCE-2 and GCE-3,7 compounds in these fractions were analyzed by LC-MS.(2)GCE-2 showed good antibacterial activity,and its MIC was both 5 mg·mL-1.(3)Compared to other fractions,GCE-2 showed good therapeutic effect.The levels of TNF-α、IL-1βand IL-6 in tissue were significantly decreased(P<0.05).Conclusion GCE-2 showed good therapeutic activity on oral ulcer.This work systematically analyzed the material basis and possible action mechanism of GallaChinensis in the treatment of oral ulcer,and provided beneficial reference for the application in anti-inflammatory and antibacterial fields.

关 键 词：五倍子 多酚 口腔溃疡 系统药理学 活性成分 

分 类 号：R285.5[医药卫生—中药学]