tailieunhanh - Whole-cell fungal-mediated structural transformation of anabolic drug metenolone acetate into potent anti-inflammatory metabolites

Study indicated that F. lini was able to catalyze dehydrogenation reactions selectively. Structures of compounds 1–14 were determined through NMR, HRFAB-MS, and IR spectroscopic data. Compounds 1–14 were identified as non-cytotoxic against BJ human fibroblast cell line (ATCC CRL-2522). Metabolite 5 ( ± ) showed a potent activity against TNF-a production, as compared to the substrate 1 ( ± ). Metabolites 2 ( ± ), 8 ( ± ), 10 ( ± ), 11 ( ± ), and 12 ( ± ), also showed a good inhibition of TNF-a production. Compounds 3 (IC50 = ± mg/mL), and 5 (IC50 = ± mg/mL) showed a significant activity against T-cell proliferation. Identification of selective inhibitors of TNF-a production, and T-cell proliferation is a step forward towards the development of anti-inflammatory drugs. | Nội dung Text Whole-cell fungal-mediated structural transformation of anabolic drug metenolone acetate into potent anti-inflammatory metabolites

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