摘要
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.
Abstract：
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.
冯俊娜, 高芳, 彭绍辉, 陈华, 李小六. KRN7000结构类似物及其免疫活性研究进展[J]. 有机化学, 2015, 35(5): 997-1008
