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10.3389/fmicb.2017.01251

http://scihub22266oqcxt.onion/10.3389/fmicb.2017.01251
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suck abstract from ncbi


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pmid28725220
      Front+Microbiol 2017 ; 8 (ä): 1251
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  • A Novel Derivative of (-)mycousnine Produced by the Endophytic Fungus Mycosphaerella nawae, Exhibits High and Selective Immunosuppressive Activity on T Cells #MMPMID28725220
  • Wang LW ; Wang JL ; Chen J ; Chen JJ ; Shen JW ; Feng XX ; Kubicek CP ; Lin FC ; Zhang CL ; Chen FY
  • Front Microbiol 2017[]; 8 (ä): 1251 PMID28725220 show ga
  • An endophytic fungus, Mycosphaerella nawae ZJLQ129, was isolated from the leaves of the traditional Chinese medicine Smilax china. From the fermentation broth and mycelium, a dibenzofurane compound (-)mycousnine (1) was isolated. Chemical modification of it to the amide derivative (-)mycousnine enamine (2), which is new to science, was found to have high and selective immunosuppressive activity: similar to cyclosporin A, (-)mycousnine enamine (2) selectively inhibited T cell proliferation, suppressed the expression of the surface activation antigens CD25 and CD69 and the formation and expression of the cytokines interleukin-2 as well as interferon ? in activated T cells, but did not show any effect on the proliferation of B cells and cancer cells (PANC-1 and A549) and the activation of macrophages. Furthermore, the cytotoxicity of (-)mycousnine enamine was lower than that of cyclosporin A, and its therapeutic index (TC50/EC50) was 4,463.5, which is five-fold higher than that of cyclosporin A. We conclude that (-)mycousnine enamine (2), the semi-synthestic product prepared from the native product (-)mycousnine (1) of the endophyte M. nawae is a novel effective immunosuppressant showing low toxicity and high selectivity.
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