Zhang Jian-Xin, Wang Jun-Xia, Zhang Yu, Zuo Jian-Ping, Wu Jin-Ming, Sui Yi, Li Ying
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Yao Xue Xue Bao. 2006 Jan;41(1):65-70.
AIM: To search for new artemisinin derivatives with higher immunosuppressive activity. METHODS: Two kinds of new artemisinin derivatives containing polyethylene glycol group were synthesized from dihydroartemisinin via condensation and esterification. These compounds were assayed for their inhibitory activity on ConA-induced T cell proliferation and LPS-induced B cell proliferation. RESULTS: Twenty three new compounds (2a - 2f, 3a - 3d, 4a - 4f, 6a, 6b and 7a - 7g) were synthesized and identified by 1H NMR and elemental analysis. CONCLUSION: These compounds had immunosuppressive activity in vitro. Among them, the symmetrical substituted compound 2 and 6 had higher activity than mono-substituted compound 3, 4 and 7. Especially, compounds 2a - 2f remarkably exhibited higher inhibition in comparison with artemisinin and artesunate.
目的：寻找具有更高免疫抑制活性的新型青蒿素衍生物。 方法：以二氢青蒿素为原料，通过缩合和酯化反应合成了两种含聚乙二醇基团的新型青蒿素衍生物。检测这些化合物对刀豆蛋白A诱导的T细胞增殖和脂多糖诱导的B细胞增殖的抑制活性。 结果：合成了23种新化合物（2a - 2f、3a - 3d、4a - 4f、6a、6b和7a - 7g），并通过1H NMR和元素分析进行了鉴定。 结论：这些化合物在体外具有免疫抑制活性。其中，对称取代的化合物2和6比单取代的化合物3, 4和7具有更高的活性。特别是，与青蒿素和青蒿琥酯相比，化合物2a - 2f表现出显著更高的抑制作用。
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