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<p>In this study, two Pt(II)–8-hydroxyquinoline derivatives, [Pt(Rob)(DMSO)Cl] (<b>RoPt</b>), and [Pt(Ah)(DMSO)Cl] (<b>AhPt</b>), incorporating robustine (H-Rob) and 5-amino-8-hydroxyquinoline (H-Ah), respectively, were synthesized and characterized. <b>RoPt</b> and <b>AhPt</b> exhibited antiproliferative effects in human cisplatin-resistant ovarian SK-OV-3/DDP (3SKD) and ovarian SK-OV-3 (3SK) cancer cells, with <b>RoPt</b> showing the strongest activity (IC<sub>50</sub> = 6.42 ± 0.21&#xa0;μM) compared with cisplatin, cis-Pt(DMSO)<sub>2</sub>Cl<sub>2</sub>, <b>AhPt</b>, H-Rob, and H-Ah. Notably, <b>RoPt</b> and <b>AhPt</b> induced apoptosis in 3SKD cells by triggering mitophagy pathways and inhibiting ATP and mitochondrial respiratory chain complex I/IV (MiRCC-I/MiRCC-IV) production. In vivo, <b>RoPt</b> displayed marked tumor suppression (ca. 37.1%) without causing notable body weight loss or mortality in 3SK tumor-bearing mice. These findings highlight the Pt(II)-robustine derivatives <b>RoPt</b> and <b>AhPt</b> as promising antiproliferative agents warranting further investigation.</p> Graphical abstract <p>Complexes <b>RoPt</b> and <b>AhPt</b> exerted cell apoptosis via induction of mitophagy pathways, inhibition of ATP and mitochondrial respiratory chain production.</p> <p></p>

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Synthesis and anticancer evaluation of platinum(II)-robustine complexes

  • 期刊论文

  • 发表日期：

    2026年2月23日

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  • Ju-Mei Zhang,
  • Xiao-Zhen Qin,
  • Fu-Liu Luo,
  • Zhen Zhou,
  • Ming-Xiong Tan,
  • Chun-Jie Liang,
  • Hong Liang,
  • Qi-Pin Qin

摘要

In this study, two Pt(II)–8-hydroxyquinoline derivatives, [Pt(Rob)(DMSO)Cl] (RoPt), and [Pt(Ah)(DMSO)Cl] (AhPt), incorporating robustine (H-Rob) and 5-amino-8-hydroxyquinoline (H-Ah), respectively, were synthesized and characterized. RoPt and AhPt exhibited antiproliferative effects in human cisplatin-resistant ovarian SK-OV-3/DDP (3SKD) and ovarian SK-OV-3 (3SK) cancer cells, with RoPt showing the strongest activity (IC50 = 6.42 ± 0.21 μM) compared with cisplatin, cis-Pt(DMSO)2Cl2, AhPt, H-Rob, and H-Ah. Notably, RoPt and AhPt induced apoptosis in 3SKD cells by triggering mitophagy pathways and inhibiting ATP and mitochondrial respiratory chain complex I/IV (MiRCC-I/MiRCC-IV) production. In vivo, RoPt displayed marked tumor suppression (ca. 37.1%) without causing notable body weight loss or mortality in 3SK tumor-bearing mice. These findings highlight the Pt(II)-robustine derivatives RoPt and AhPt as promising antiproliferative agents warranting further investigation.

Graphical abstract

Complexes RoPt and AhPt exerted cell apoptosis via induction of mitophagy pathways, inhibition of ATP and mitochondrial respiratory chain production.