穿心莲内酯3,19-缩醛(酮)衍生物对小鼠脾淋巴细胞增殖活性的影响

Modulation of the proliferation of mouse spleen lymphocytesby 3,19-ketal andrographolide derivatives

目的：评价穿心莲内酯及其衍生物对小鼠脾淋巴细胞增殖活性的影响，用于指导以穿心莲内酯为先导化合物的新型免疫调节剂的合成。方法：采用MTT法，在1．56～12．50umol·L^-1定量考察穿心莲内酯及其3，19-缩醛（酮）衍生物对小鼠脾淋巴细胞增殖反应的影响。结果：穿心莲内酯对丝裂原诱导的淋巴细胞增殖活性有显著的抑制作用。通过半合成改造得到的3，19-缩醛（酮）衍生物可使抑制活性显著提高，但是部分衍生物在1．56～6．25umol·L^-1。内表现出促进T或／和B淋巴细胞增殖的作用。结论：穿心莲内酯3，19-缩醛（酮）衍生物对穿心莲内酯作为开发免疫调节剂的先导化合物有重要价值和潜力。

Objective ： To evaluate whether andrographolide and its 3,19-ketal derivatives impact the proliferation of mouse spleen lymphocytes. Methods： Andrographolide derivatives （ 1.56 - 12.50 umol· L^-1 ） were incubated with mouse spleen lymphocytes and the spleen lymphocytes were then quantified by a MTT assay. Results：Andrographolide significantly inhibited the proliferation of mitogen-induced lymphocytes. 3, 19- ketal andrographolide derivatives showed more potent inhibitory activities on the lym- phocytes, but some（ 1.56 -6.25 umol·L^-1） enhanced the proliferation of T and/or B lymphocytes. Conclusion： The andrographolide derivatives had the potential to be further developed as a lead compound of immunomodulators.