细叶勾儿茶部分化合物抗炎活性的实验研究  

Experimental study of the anti⁃inflammatory activity of some compounds in Berchemia lineata(L.)DC.

作　　者：刘军洋 滕红丽 赵金妹 洪精 LIU Jun-yang;TENG Hong-li;ZHAO Jin-mei;HONG Jing(Guangxi University of Chinese Medicine,Nanning 530001,China;Guangxi International Zhuang Medical Hospital,Nanning 530201,China)

机构地区：[1]广西中医药大学,广西南宁530001 [2]广西国际壮医医院,广西南宁530201

出　　处：《海南医学院学报》2023年第11期825-830,共6页Journal of Hainan Medical University

基　　金：国家重点研发计划课题(2022YFC3502201);国家自然科学基金课题(81960762);广西中医药重点学科(GZXK⁃Z⁃20⁃62);广西科技基地和人才专项(桂科AD19245183、AD22035052);广西中医外治法示范基地项目(桂中医药医发〔2019〕14号);全国名中医传承工作室、全国名老中医药专家传承工作室建设项目、全国名中医黄汉儒学术思想及临床经验传承推广中心(2022V004)。

摘　　要：目的:筛选细叶勾儿茶[Berchemia lineata(L.)DC.]中分离出的具有抗炎活性的单体化合物并探究21号简单的酚类化合物基于NF⁃κB信号通路的抗炎作用机制。方法:采用脂多糖(lipopolysaccharide,LPS)诱导小鼠巨噬细胞(RAW264.7)建立细胞炎症反应模型;采用CCK⁃8法检测单体化合物对RAW264.7细胞活性的影响;采用Griess法检测细胞上清液中一氧化氮(nitric oxide,NO)释放量并计算NO抑制率,对部分单体化合物进行抗炎活性梯度检测;采用酶联免疫吸附法(ELISA)检测21号单体化合物对LPS诱导RAW264.7细胞分泌IL⁃6、TNF⁃α、NF⁃κB、COX⁃2、iNOS的影响。结果:细叶勾儿茶单体化合物浓度为50μmol/L,给药24 h,结果显示19号蒽醌类化合物有明显的药物毒性,其他化合物毒性较弱或无明显药物毒性;浓度为50μmol/L,给药12 h,结果显示其单体化合物均可不同程度的抑制NO的释放量,NO抑制率最高可达90%以上,具有明显的抗炎活性;01号新骨架化合物NO抑制率可达到70.81%。抗炎活性梯度结果显示,细叶勾儿茶单体化合物可不同程度抑制NO释放且呈剂量依赖性。ELISA结果显示,21号简单的酚类化合物可抑制RAW264.7细胞分泌IL⁃6、TNF⁃α、NF⁃κB、COX⁃2、iNOS。结论:细叶勾儿茶单体化合物具有一定抗炎活性,其中黄酮类及首次从该植物中分离得到的联苄类成分可能是其发挥抗炎活性的物质基础;21号简单的酚类化合物可能通过调控NF⁃κB信号通路发挥抗炎作用。Objective:To screen the anti⁃inflammatory monomeric compounds isolated from Berchemia lineata(L.)DC and explore the anti⁃inflammatory mechanism of some compounds based on NF⁃κB signaling pathway.Methods:LPS was used to induce RAW264.7 to establish a model of cellular inflammatory reaction.CCK⁃8 method was used to detect the effect of monomer compounds on the activity of RAW264.7 cells.The release of nitric oxide(NO)in the superneant was measured by Griess meth⁃od,and NO inhibition rate was calculated.The anti⁃inflammatory activity gradient of some monomeric compounds was also mea⁃sured.The effects of monomer compound 21 on the secretion of IL⁃6,TNF⁃α,NF⁃κB,COX⁃2 and iNOS induced by LPS were detected by ELISA.Results:The concentration of monomer compound of Berchemia lineata(L.)DC.was 50μmol/L,and it was administered for 24 h.The results showed that anthraquinone compound No.19 had obvious drug toxicity,while other compounds had weak or no obvious drug toxicity.The concentration was 50μmol/L,and the drug was administered for 12 h.The results showed that all the monomer compounds could inhibit the release of NO to varying degrees,and the highest NO inhibition rate was over 90%,which showed obvious anti⁃inflammatory activity.NO inhibition rate of No.01 new skeleton compound can reach 70.81%.The results of anti⁃inflammatory activity gradient showed that the monomer compound of Berchemia lineata(L.)DC.could inhibit the release of NO in a dose⁃dependent manner.The results of ELISA showed that phenolic compound 21 could inhibit the secretion of IL⁃6,TNF⁃α,NF⁃κB,COX⁃2 and iNOS in RAW264.7 cells.Conclusion:The monomer compound of Berchemia lineata(L.)DC.has a certain anti⁃inflammatory activity,among which flavonoids and bibenzyl components isolated from this plant for the first time may be the material basis for its anti⁃inflammatory activity.The simple phenolic monomer com⁃pound 21 may play an anti⁃inflammatory role by regulating NF⁃κB signaling pathway.

关 键 词：铁包金 细叶勾儿茶 RAW264.7 抗炎 

分 类 号：R285.5[医药卫生—中药学]