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

SU Xiao-lian1, Lü Hong-xiang1, JIANG Yuan-yuan1, ZHOU Shan-shan1, TANG Qing2, SU Zhao-liang1, SHAO Xiao-yi1, 2   

  1. 1. Institute of Immunology, Jiangsu University, Zhenjiang 212013, China; 2. Department of Immunology, Medical School, Nantong University, Nantong 226001, China
  • Online:2017-04-28 Published:2017-05-04
  • Supported by:

    National Natural Science Foundation of China, 81370084; Practice Innovation Program of Ordinary University Graduate Students in Jiangsu Province, SJLX15_0518; Project of Nantong Municipal Science and Technology Bureau, MS12016007


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 21th 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 cytokines 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.

Key words: sinomenine, 4EDB, experimental autoimmune myocarditis, inflammation