<p>Two new 2-pyridone alkaloids with unique structures, campyridones E (<b>1</b>) and F (<b>2</b>), together with other four known analogues (<b>3</b>–<b>6</b>), were isolated from the Beibu Gulf coral-derived fungus <i>Acremonium sclerotigenum</i> GXIMD 02501. The chemical structures and absolute configurations were determined by comprehensive spectroscopic interpretation and ECD calculation. Compound <b>3</b> exhibited antiproliferative activity against KTC-1 and MDA-MB-231 cells, with IC<sub>50</sub> values of (28.42±9.04) µmol/L and (31.91±5.58) µmol/L, respectively. Compound <b>4</b> showed cytotoxicity towards MDA-MB-231 cells with an IC<sub>50</sub> value of (29.23±0.53) µmol/L. Their structure-activity relationships are preliminarily discussed. Notably, compound <b>3</b> inhibited colony formation with a dose-dependent manner, blocked the G1 phase of cell cycle, and further induced apoptosis of MDA-MB-231 cells, revealing a potential promising anti-cancer compound.</p>

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Isolation and Cytotoxic Activities of Two New 2-Pyridone Alkaloids with Unique Structures from the Beibu Gulf Coral-Derived Acremonium sclerotigenum GXIMD 02501

  • Yuning Qin,
  • Xinjian Qu,
  • Miaoping Lin,
  • Hong Zhang,
  • Huangxue Qin,
  • Chenghai Gao,
  • Yonghong Liu,
  • Xuefeng Zhou,
  • Xiaowei Luo

摘要

Two new 2-pyridone alkaloids with unique structures, campyridones E (1) and F (2), together with other four known analogues (36), were isolated from the Beibu Gulf coral-derived fungus Acremonium sclerotigenum GXIMD 02501. The chemical structures and absolute configurations were determined by comprehensive spectroscopic interpretation and ECD calculation. Compound 3 exhibited antiproliferative activity against KTC-1 and MDA-MB-231 cells, with IC50 values of (28.42±9.04) µmol/L and (31.91±5.58) µmol/L, respectively. Compound 4 showed cytotoxicity towards MDA-MB-231 cells with an IC50 value of (29.23±0.53) µmol/L. Their structure-activity relationships are preliminarily discussed. Notably, compound 3 inhibited colony formation with a dose-dependent manner, blocked the G1 phase of cell cycle, and further induced apoptosis of MDA-MB-231 cells, revealing a potential promising anti-cancer compound.