青藤碱衍生物4EDB的合成、鉴定以及对实验性自身免疫性心肌炎的治疗作用观察  

Synthesis and identification of sinomenine derivate 4EDB and its therapeutic effects on mice with experimental autoimmune myocarditis

作　　者：苏晓莲 吕宏祥[1] 姜媛媛[1] 周姗姗[1] 唐晴[2] 苏兆亮[1] 邵晓轶[2] 

机构地区：[1]江苏大学免疫研究所,镇江212013 [2]南通大学医学院免疫学系,南通226001

出　　处：《上海交通大学学报（医学版）》2017年第4期453-457,共5页Journal of Shanghai Jiao tong University:Medical Science

基　　金：国家自然科学基金(81370084);江苏省普通高校研究生实践创新计划项目(省立校助SJLX15_0518);南通市科技计划项目(MS12016007)~~

摘　　要：目的·制备青藤碱衍生物4EDB,研究体内4EDB对实验性自身免疫性心肌炎(EAM)小鼠的治疗作用。方法·采用随机分组方法,将BALB/c小鼠分为空白对照组、EAM+4EDB组和EAM组,每组6只。免疫开始的第14日开始灌胃给药,5 mg/(kg·d)。第21日处死小鼠,取出心脏做病理切片,并进行天狼星红染色和苏木精-伊红染色(H-E染色);real-time PCR检测心肌组织相关炎症因子白介素-1(IL-1)、IL-6、IL-17A、转化生长因子-β(TGF-β)的表达。结果·与EAM组相比,EAM+4EDB组心肌炎症病理评分降低(P=0.020),纤维化得到缓解,心肌组织炎症因子IL-1、IL-6、IL-17A、TGF-β水平下降(P<0.05)。结论·新合成的青藤碱衍生物4EDB对EAM模型小鼠的心肌炎症有缓解作用,其机制可能与其抑制炎症因子表达有关。Objective· To synthesize 4EDB, the derivative of sinomenine, and to observe its therapeutic effects on mice with experimental autoimmune myocarditis （EAM）. Methods. The BALB/c mice were randomly divided into three groups： control group, EAM group and EAM＋4EDB group with 6 mice in each group, and then treated with 4EDB [5 mg/（kg·d）] by intragastric administration from the 14th day of immunization until sacrificed on the 2 lth day. Hematoxylin-eosin （H-E） staining was used to identify the areas of inflammation, and the hematoxylin-picrosirius red staining was used to detect the degree of myocardial fibrosis. The expression levels of related inflammatory factors including IL-1, IL-6, IL-17A and TGF-β in myocardial tissues were detected by real-time PCR. Results · Compared with EAM group, the pathological score of myocardial inflammation decreased in EAM＋4EDB group （P=0.020）, with myocardial fibrosis alleviated, and the expression levels of inflammatory eytokines including IL-1, IL-6, IL-17A and TGF-β in myocardium reduced （P〈0.05）. Conclusion · The new derivative of sinomenine, 4EDB, can alleviate the myocarditis in EAM mice, and the inhibition of inflammatory factors may play an important role.

关 键 词：青藤碱 4EDB 实验性自身免疫性心肌炎 炎症 

分 类 号：R284[医药卫生—中药学] R285.5[医药卫生—中医学]