SM934, a water-soluble derivative of arteminisin, exerts immunosuppressive functions in vitro and in vivo

State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, People's Republic of China.
International immunopharmacology (Impact Factor: 2.71). 09/2009; 9(13-14):1509-17. DOI: 10.1016/j.intimp.2009.09.003
Source: PubMed

ABSTRACT In the present study, we investigated the immunosuppressive effects and underlying mechanisms of beta-aminoarteether maleate (SM934), a derivative of artemisinin, against T cell activation in vitro and in vivo. In vitro, SM934 significantly inhibited the proliferation of splenocytes induced by concanavalin A (Con A), lipopolysaccharide (LPS), mixed lymphocyte reaction (MLR), and anti-CD3 plus anti-CD28 (anti-CD3/28). SM934 significantly inhibited interferon (IFN)-gamma production and CD4(+) T cell division stimulated by anti-CD3/28. SM934 also promoted apoptosis of CD69(+) population in CD4(+) T cells stimulated by anti-CD3/28. Furthermore, SM934 inhibited interleukin (IL)-2 mediated proliferation and survival through blocking Akt phosphorylation in activated T cells. In ovalbumin (OVA)-immunized mice, oral administration of SM934 suppressed OVA-specific T cell proliferation and IFN-gamma production. SM934 treatment also significantly inhibited the sheep red blood cell (SRBC)-induced delayed type hypersensitivity (DTH) reactions in mice. Taken together, SM934 showed potent immunosuppressive activities in vitro and in vivo. Our results demonstrated that SM934 might be a potential therapeutic agent for immune-related diseases.

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Available from: Lifei Hou, Jul 27, 2015
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    • "Similar to SM735, the studies in Zuo group in SIMM found SM905 possessed potent immunoregulatory properties [5] [6] [7]. However, SM934 is quite distinct [11]. Similar to SM905 and artemether, in vitro, SM934 significantly inhibited the proliferation and IFN-í µí»¾ production of splenocytes or purified CD4+ T cells induced by mixed lymphocyte reaction (MLR) or TCR cross-linking. "
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