NF-B inhibitors, unique -pyranol--lactams with sulfide and sulfoxide moieties from Hawaiian plant Lycopodiella cernua derived fungus Paraphaeosphaeria neglecta FT462.
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abstract
LC-UV/MS-based metabolomic analysis of the Hawaiian endophytic fungus Paraphaeosphaeria neglecta FT462 led to the identification of four unique mercaptolactated -pyranol--lactams, paraphaeosphaerides E-H (1-4) together with one -lactone (5) and the methyl ester of compound 2 (11). The structures of the new compounds (1-5 and 11) were elucidated through the analysis of HRMS and NMR spectroscopic data. The absolute configuration was determined by chemical reactions with sodium borohydride, hydrogen peroxide, -methoxy--(trifluoromethyl)phenylacetyl chlorides (Mosher reagents), and DP4+NMR calculations. All the compounds were tested against STAT3, A2780 and A2780cisR cancer cell lines, E. coli JW2496, and NF-B. Compounds 1 and 3 strongly inhibited NF-B with IC50 values of 7.1 and 1.5M, respectively.
