<p>(+)-BE-7585A (<b>1</b>) and its derhodinosyl derivative (<b>2</b>), two rare 2-thiosugar-containing angucyclines, together with their biosynthetic precursor sakyomicin A (<b>3</b>), were isolated from the culture broth of the rare actinomycete <i>Amycolatopsis</i> sp. JS6. Their planar structures were determined by 1D/2D NMR and HRESI-MS data analyses, and the absolute configurations were established by comparison of ECD spectra. Compounds <b>1</b> and <b>2</b> exhibited weak to modest cytotoxicity against human cervical adenocarcinoma HeLa S3 cells and acute promyelocytic leukemia HL-60 cells, which was much less potent than that of <b>3</b>, indicating the hydroxy group at C-12b and the substitution at C-5 by the thiodisaccharide moiety of the aglycon may contribute to the cytotoxicity.</p><p></p>

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(+)-BE-7585A and its derhodinosyl derivative, two cytotoxic 2-thiosugar-containing angucyclines, derived from an actinomycete Amycolatopsis sp. JS6

  • Di Mao,
  • Yuhan Zhang,
  • Lei Zhang,
  • Pengwei Yu,
  • Naoya Shinzato,
  • Sayaka Kobayashi,
  • Shan Lu,
  • Hideaki Kakeya

摘要

(+)-BE-7585A (1) and its derhodinosyl derivative (2), two rare 2-thiosugar-containing angucyclines, together with their biosynthetic precursor sakyomicin A (3), were isolated from the culture broth of the rare actinomycete Amycolatopsis sp. JS6. Their planar structures were determined by 1D/2D NMR and HRESI-MS data analyses, and the absolute configurations were established by comparison of ECD spectra. Compounds 1 and 2 exhibited weak to modest cytotoxicity against human cervical adenocarcinoma HeLa S3 cells and acute promyelocytic leukemia HL-60 cells, which was much less potent than that of 3, indicating the hydroxy group at C-12b and the substitution at C-5 by the thiodisaccharide moiety of the aglycon may contribute to the cytotoxicity.