Synthesis and immunosuppressive activity of new artemisinin derivatives containing polyethylene glycol group

Zhang, J-Xin.; Wang, J-Xia.; Zhang, Y.; Zuo, J-Ping.; Wu, J-Ming.; Sui, Y.; Li, Y.

Yao Xue Xue Bao 41(1): 65-70

2006


ISSN/ISBN: 0513-4870
PMID: 16683530
Document Number: 599347
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.

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