有机化学 ›› 2015, Vol. 35 ›› Issue (5): 997-1008.DOI: 10.6023/cjoc201409048 上一篇    下一篇

综述与进展

KRN7000结构类似物及其免疫活性研究进展

冯俊娜a,b, 高芳a, 彭绍辉b, 陈华a, 李小六a   

  1. a 河北大学化学与环境科学学院 保定 071002;
    b 中国地质大学长城学院 保定 071000
  • 收稿日期:2014-09-30 修回日期:2014-12-06 发布日期:2014-12-18
  • 通讯作者: 陈华, 李小六 E-mail:hua-todd@163.com;lixl@hbu.cn
  • 基金资助:

    国家自然科学基金(Nos.20972039,21372060)、教育部博士点基金(No.20121301110004)、河北省自然科学基金石药集团医药联合基金(No.B2011201169)、河北省教育厅自然科学基金(No.ZH2011110)资助项目.

Research Advances of KRN7000 Analogues and Their Immune Activities

Feng Junnaa,b, Gao Fanga, Peng Shaohuib, Chen Hua, Li Xiaoliua   

  1. a College of Chemistry and Environmental Science, Hebei University, Baoding 071002;
    b China University of Geosciences Great Wall College, Baoding 071000
  • Received:2014-09-30 Revised:2014-12-06 Published:2014-12-18
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos.20972039, 21372060), the Research Fund for the Doctoral Program of Higher Education of China (No.20121301110004), the Medicinal Joint Funds of the Natural Science Foundation of Hebei and Shijiazhuang Pharmaceutical Group Foundation (No.B2011201169), and the Natural Science Foundations of Education Department of Hebei Province (No.ZH2011110).

KRN7000具有广泛的生物活性, 如抗肿瘤、抗结核病、抗真菌、抗病毒、消炎以及治疗自身免疫性疾病等. 作为免疫调节剂, 其免疫作用主要通过活化自然杀伤T细胞(NKT), 促进细胞因子IFN-γ和IL-4的释放. 由于IFN-γ抑制TH2活性, IL-4抑制TH1活性, TH1和TH2生物学效应的相互抑制限制了KRN7000在临床治疗上的应用. 因此, 对KRN7000的结构进行修饰, 以期得到免疫作用更好的药物是近年来研究的热点. 就KRN7000最新结构改造及免疫活性研究进展进行综述.

关键词: KRN7000, 免疫调节剂, TH1/TH2

KRN7000 has widely biological activities, such as anti-tumor, anti-tuberculosis, anti-fungal, anti-virus, anti-inflammation, and against auto-immune diseases. As the potential immunomodulator, KRN7000 can effectively activate the natural killer T cells (NKT cells) and induce the secretion of IFN-γ and IL-4 cytokines. However, IFN-γ inhibited the activity of T helper 2 cells (TH2) and IL-4 inhibited the activity of T helper 1 cells (TH1), which mediated humoral as well as celluar immune reactions, respectively. The concomitant of functions of TH1 and TH2 limits the therapeutic potential of KRN7000 against immune diseases. Therefore, developing new analogues of KRN7000 to find new immnostimulating drugs has drawn many attentions in the world. This review presents the recent progress in the study on the structure and immune activity of the synthesized KRN7000 derivatives.

Key words: KRN7000, immunomodulator, TH1/TH2