SM 934
- Ethanamine, 2-[(decahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin-10-yl)oxy]-, [3R-(3α,5aβ,6β,8aβ,9α,10α,12β,12aR*)]-, (Z)-2-butenedioate (1:1)
- 3,12-Epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin, ethanamine deriv.
- SM 934
- β-Aminoarteether maleate
CAS 133162-25-1
MF C17 H29 N O5 . C4 H4 O4
Ethanamine, 2-[(decahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin-10-yl)oxy]-, (3R,5aS,6R,8aS,9R,10S,11aR)-, (2Z)-2-butenedioate (1:1)
TLR7/9 signal transduction modulator
IND FILED
2.5 and 5 mg/kg, ig (MRL/lpr mice);
10 mg·kg−1·d−1, ig (NZB/W F1 mice)
10 mg·kg−1·d−1, ig (NZB/W F1 mice)
Autoimmune diseases; SLE
SM934, an artemisinin derivative, possesses potent antiproliferative and antiinflammatory properties.
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.
PATENT
PAPER
Volume 9, Issues 13–14, December 2009, Pages 1509–1517
Inflammatory Mediators Long Term after Sulfur Mustard Exposure (Sardasht-Iran Cohort Study)
SM934, a water-soluble derivative of arteminisin, exerts immunosuppressive functions in vitro and in vivo
- a State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, People's Republic of China
- b Department of Synthetic Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, People's Republic of China
- c Laboratory of Immunology and Virology, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, People's Republic of China
- Hou LF, He SJ, Wang JX, Yang Y, Zhu FH, Zhou Y, et al. SM934, a water-soluble derivative of arteminisin, exerts immunosuppressive functions in vitro and in vivo. Int Immunopharmacol 2009; 9: 1509–17. | Article |
- Hou LF, He SJ, Li X, Yang Y, He PL, Zhou Y, et al. Oral administration of artemisinin analog SM934 ameliorates lupus syndromes in MRL/lpr mice by inhibiting Th1 and Th17 cell responses. Arthritis Rheum 2011; 63: 2445–55. | Article
- Hou LF, He SJ, Li X, Wan CP, Yang Y, Zhang XH, et al. SM934 treated lupus-prone NZB x NZW F1 mice by enhancing macrophage interleukin-10 production and suppressing pathogenic T cell development. PLoS One 2012; 7: e 32424.
- Wu Y, He S, Bai B, Zhang L, Xue L, Lin Z, et al. Therapeutic effects of the artemisinin analog SM934 on lupus-prone MRL/lpr mice via inhibition of TLR-triggered B-cell activation and plasma cell formation. Cell Mol Immunol 2015 Mar 16. doi: 10.1038/cmi.2015.13. [Epub ahead of print].
/////////TLR7/9 signal transduction modulator, SM 934, IND FILED, 133162-25-1, β-Aminoarteether maleate
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