[Synthesis and immunosuppressive activity of new artemisinin derivatives containing polyethylene glycol group].
OBJECTIVE
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.


CONCLUSIONS
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.
Zhang
Jian-Xin
JX
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Wang
Jun-Xia
JX
Zhang
Yu
Y
Zuo
Jian-Ping
JP
Wu
Jin-Ming
JM
Sui
Yi
Y
Li
Ying
Y