Citation: Hanxue LIU, Shijie LI, Meng REN, Xuling XUE, Hongke LIU. Design and antitumor properties of dehydroabietic acid functionalized cyclometalated iridium(Ⅲ) complex[J]. Chinese Journal of Inorganic Chemistry, ;2025, 41(8): 1483-1494. doi: 10.11862/CJIC.20250031 shu

Design and antitumor properties of dehydroabietic acid functionalized cyclometalated iridium(Ⅲ) complex

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  • A novel cyclometalated iridium complex, CycIr-DHA, was successfully synthesized by incorporating the natural product dehydroabietic acid (DHA) into the cyclometalated iridium framework, and the ligand and complex were characterized by 1H NMR. The complex showed strong antitumor effects on various cancer cells, especially michigan cancer foundation-7 (MCF-7) cells, with a half maximal inhibitory concentration (IC50) of 2.5 μmol·L-1, superior to that of the traditional chemotherapeutic drug cisplatin. Experimental results indicated that CycIr-DHA primarily accumulated in the mitochondria of MCF-7, leading to a significant increase in intracellular reactive oxy- gen species levels and subsequent mitochondrial dysfunction. Furthermore, the complex modulated the expression of apoptosis - related proteins (Bax and Bcl - 2), promoting apoptosis, and upregulates LC3 - Ⅱ protein, inducing autophagy. In a 3D cell spheroid model, CycIr-DHA significantly inhibited the growth of the spheroids.
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