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利用自建的快速高效的次黄嘌呤一磷酸盐脱氢酶(Inosine monophosphate dehydrogenase,IMPDH)抑制剂的高通量筛选模型,筛选分离得到两个活性化合物2264 A和B,通过对其紫外、质谱、核磁等理化数据的分析确定2264 A为cyclopenol,2264 B为viridicatol。2264 A和B对IMPDH的IC50分别为69.68、11.86μmol/L;体外脾淋巴细胞增殖实验显示2264 A和B分别在322.6和65.8μmol/L浓度下可完全抑制由ConA活化的脾淋巴细胞增殖,表明2264 B在分子水平和细胞水平均表现出较好的免疫抑制活性,2264 A的活性相对较弱。
By using a high-throughput screening model of a fast and efficient inhibitor of inosine monophosphate dehydrogenase (IMPDH), two active compounds, 2264 A and B, were isolated and screened by ultraviolet spectrophotometry , NMR and other physical and chemical data analysis to determine 2264 A for cyclopenol, 2264 B for viridicatol. The IC50 of 2264 A and B for IMPDH were 69.68 and 11.86 μmol / L, respectively. In vitro proliferation experiments of spleen lymphocytes showed that 2264 A and B could completely inhibit the proliferation of spleen lymphocytes activated by ConA at 322.6 and 65.8 μmol / L, respectively. The results indicated that 2264 B showed good immunosuppressive activity both at the molecular level and cellular level, and the activity of 2264 A was relatively weaker.