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<p>In the preliminary screening, falcarinol and falcarindiol, C<sub>17</sub> polyacetylenes from the roots of <i>Glehnia littoralis</i> F. Schmidt ex Miq (Umbelliferae), displayed cytotoxic activity both against oxaliplatin-sensitive/resistant colorectal cancer (CRC) and gefitinib-sensitive/resistant non-small cell lung cancer (NSCLC) cells. In this study, 13 polyacetylenes including a new (3<i>R</i>,11<i>R</i>)-11-hyroxy-isofalcarinolone (<b>1</b>) were isolated from <i>G. littoralis</i>, and the chemical structures were elucidated through NMR, HRMS, and optical rotation analysis as well as DP4 plus calculation. (3<i>S</i>,8<i>S</i>)-Oplopandiol (<b>5</b>) showed cytotoxic activities against oxaliplatin-sensitive and -resistant CRC (HCT116 and HCT116-OxR) cells. Unexpectedly, (3<i>R</i>,8<i>S</i>)-falcarindiol (<b>3</b>) and (3<i>S</i>)-falcarinol (<b>12</b>), newly purified from <i>G</i>. <i>littoralis</i>, did not show cytotoxic activity. It was confirmed that both falcarinol and falcarindiol, previously evaluated, were decomposed, which seems to be the cause of inconsistent biological results. These findings indicated that C<sub>17</sub> polyacetylene could be a good starting compound for the development of anticancer leads against drug-resistant CRC and NSCLC cells, however, the stability of C<sub>17</sub> polyacetylens should be considered for further studies.</p> Graphical Abstract <p></p>

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Cytotoxic activity of C17 polyacetylenes from the roots of Glehnia littoralis against drug-resistant colorectal and lung cancer cells

  • 期刊论文

  • 发表日期：

    2025年1月6日

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  • Jisu Park,
  • Sihyun Jang,
  • Seung-On Lee,
  • InWha Park,
  • Sainan Li,
  • A-Young Nam,
  • Jung-Hyun Shim,
  • MinKyun Na

摘要

In the preliminary screening, falcarinol and falcarindiol, C17 polyacetylenes from the roots of Glehnia littoralis F. Schmidt ex Miq (Umbelliferae), displayed cytotoxic activity both against oxaliplatin-sensitive/resistant colorectal cancer (CRC) and gefitinib-sensitive/resistant non-small cell lung cancer (NSCLC) cells. In this study, 13 polyacetylenes including a new (3R,11R)-11-hyroxy-isofalcarinolone (1) were isolated from G. littoralis, and the chemical structures were elucidated through NMR, HRMS, and optical rotation analysis as well as DP4 plus calculation. (3S,8S)-Oplopandiol (5) showed cytotoxic activities against oxaliplatin-sensitive and -resistant CRC (HCT116 and HCT116-OxR) cells. Unexpectedly, (3R,8S)-falcarindiol (3) and (3S)-falcarinol (12), newly purified from G. littoralis, did not show cytotoxic activity. It was confirmed that both falcarinol and falcarindiol, previously evaluated, were decomposed, which seems to be the cause of inconsistent biological results. These findings indicated that C17 polyacetylene could be a good starting compound for the development of anticancer leads against drug-resistant CRC and NSCLC cells, however, the stability of C17 polyacetylens should be considered for further studies.

Graphical Abstract