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<p>Non-platinum (non-Pt) coordination compounds display great potential as antineoplastic drugs. Herein, two new 8-hydroxyquinoline-<i>N</i>-oxide (H-8QOL) non-Pt coordination compounds, [Co<sup>II</sup>(8QOL)<sub>2</sub>(biq)] (Yulin Normal University-2a, <b>YNU-2a</b>) and [Co<sup>III</sup>(8QOL)<sub>2</sub>(phe)]NO<sub>3</sub>·CH<sub>3</sub>OH (<b>YNU-2b</b>), bearing 2,2′-biquinoline (biq) and 1,10-phenanthroline (phe) as auxiliary ligands, respectively, were synthesized and evaluated for their potential anticancer efficacy. A third compound, [Co<sub>2</sub>(biq)<sub>2</sub>(NO<sub>3</sub>)<sub>2</sub>(OCH<sub>3</sub>)<sub>2</sub>] (<b>YNU-2c</b>), was used as the control. <b>YNU-2a</b> demonstrated superior antineoplastic activity compared to cisplatin (CCDP), <b>YNU-2b</b>, and <b>YNU-2c</b> against human cisplatin-resistant lung adenocarcinoma A549/DDP (A549C) cells. And <b>YNU-2a</b>–<b>YNU-2c</b> exhibited lower cytotoxicity towards normal embryonic kidney (HEK293) cells than that of CCDP. The different cytotoxicities of <b>YNU-2a</b>–<b>YNU-2c</b> against the A549C cells depended on auxiliary ligands, following the order phe &lt; biq. Further analyses revealed that <b>YNU-2a</b> more obviously suppressed A549C cancer cell proliferation via triggering mitophagy, inhibiting the production of ATP and mitochondrial respiration complexes I (MR1) and IV (MR4), and inducing mitochondrial dysfunction compared with <b>YNU-2c</b>. This study demonstrates that <b>YNU-2a</b> facilitates targeted mitophagy, highlighting its potential as an anticancer drug.</p> Graphical abstract <p></p>

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Two new 8-hydroxyquinoline-N-oxide cobalt coordination compounds: synthesis, crystal structures, and in vitro anticancer efficacy evaluation

  • 期刊论文

  • 发表日期：

    2025年7月1日

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  • Qi-Pin Qin,
  • Yue-Jiao Liang,
  • Li Ruan,
  • Ling-Qi Du,
  • Qiu-Ji Xie,
  • Li-Qin Qin,
  • Ming-Xiong Tan

摘要

Non-platinum (non-Pt) coordination compounds display great potential as antineoplastic drugs. Herein, two new 8-hydroxyquinoline-N-oxide (H-8QOL) non-Pt coordination compounds, [CoII(8QOL)2(biq)] (Yulin Normal University-2a, YNU-2a) and [CoIII(8QOL)2(phe)]NO3·CH3OH (YNU-2b), bearing 2,2′-biquinoline (biq) and 1,10-phenanthroline (phe) as auxiliary ligands, respectively, were synthesized and evaluated for their potential anticancer efficacy. A third compound, [Co2(biq)2(NO3)2(OCH3)2] (YNU-2c), was used as the control. YNU-2a demonstrated superior antineoplastic activity compared to cisplatin (CCDP), YNU-2b, and YNU-2c against human cisplatin-resistant lung adenocarcinoma A549/DDP (A549C) cells. And YNU-2a–YNU-2c exhibited lower cytotoxicity towards normal embryonic kidney (HEK293) cells than that of CCDP. The different cytotoxicities of YNU-2a–YNU-2c against the A549C cells depended on auxiliary ligands, following the order phe < biq. Further analyses revealed that YNU-2a more obviously suppressed A549C cancer cell proliferation via triggering mitophagy, inhibiting the production of ATP and mitochondrial respiration complexes I (MR1) and IV (MR4), and inducing mitochondrial dysfunction compared with YNU-2c. This study demonstrates that YNU-2a facilitates targeted mitophagy, highlighting its potential as an anticancer drug.

Graphical abstract