| 齐墩果酸-环金属铱配合物的点击化学合成及抗肿瘤性能 | |
| Click-chemistry synthesis and antitumor properties of cyclometalated iridium(Ⅲ) complex based on oleanolic acid | |
| 摘要: 选择天然产物齐墩果酸进行炔基化修饰（OA-alkyne），与环金属铱前体CycloIr-N3在铜催化条件下发生叠氮-炔环加成（CuAAC）反应，得到新的环金属铱配合物CycloIr-OA，通过1H NMR、ESI-MS对配体及配合物进行了表征。配合物具有良好的脂溶性，可以快速进入细胞。用MTT法、激光共聚焦成像及流式细胞术对CycloIr-OA的抗肿瘤活性和抗癌机制进行了研究。结果表明，连接齐墩果酸后，配合物CycloIr-OA的抗癌活性有较大提升。CycloIr-OA富集在肿瘤细胞的线粒体中，导致活性氧产生，同时将细胞周期阻滞在S期，最终诱导肿瘤细胞坏死。 | |
| 关键词: 环金属铱配合物 齐墩果酸 抗肿瘤 坏死 | |
| 基金项目: 国家自然科学基金（No.21771109，22077066，21807060）资助 | |
| Abstract: Herein, we modified the natural product oleanolic acid with alkyne to synthesize the ligand OA-alkyne, and tethered it with cyclic metal iridium precursor CycloIr-N3 to obtain the final complex CycloIr-OA via copper(Ⅰ)-catalyzed azide-alkyne cycloaddition (CuAAC) reaction. The ligand and the complex were characterized by 1H NMR and ESI-MS. The results show that the complex had good lipophilicity, which was helpful to enter the cells quickly. The antitumor activity of CycloIr-OA and the mechanism of inducing tumor cell death were further studied by MTT, confocal imaging, and flow cytometry. After oleanolic acid was linked, the anti-cancer activity of complex CycloIr-OA was greatly improved. CycloIr-OA is enriched in the mitochondria of tumor cells, leading to the production of reactive oxygen species, and at the same time, it blocks the cell cycle in the S phase, ultimately inducing tumor cell necrosis. | |
| Keywords: cyclometalated iridium complex oleanolic acid antitumor necrosis | |
| 投稿时间：2022-08-20 修订日期：2022-11-09 | |
| 摘要点击次数: 3150 | |
| 全文下载次数: 476 | |
| 李世杰,钱晓婷,黄元镭,薛旭玲,钱勇,苏志,刘红科.齐墩果酸-环金属铱配合物的点击化学合成及抗肿瘤性能[J].无机化学学报,2023,39(2):317-326. | |
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| Support information: 相关附件： 220379_齐墩果酸-环金属铱配合物的合成和抗肿瘤性能研究SI.doc | |
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