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首页> 外文期刊>RSC Advances >Microwave-assisted synthesis of polypyridyl ruthenium(II) complexes as potential tumor-targeting inhibitors against the migration and invasion of Hela cells through G2/M phase arrest
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Microwave-assisted synthesis of polypyridyl ruthenium(II) complexes as potential tumor-targeting inhibitors against the migration and invasion of Hela cells through G2/M phase arrest

机译：微波辅助合成聚吡啶钌（II）复合物作为潜在的靶向肿瘤抑制剂，通过G2 / M期阻滞阻止Hela细胞的迁移和侵袭

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A series of polypyridyl ruthenium(II) complexes coordinated by phenanthroimidazole derivatives [Ru(phen)2(R)](ClO4)2 (where 1 R = IP, 2 R = PIP, 3 R = p-HPIP, 4 R = p-OCH3PIP) was synthesized with an average yield of >85% under microwave irradiation at 140 °C for 30 min. The inhibitory effect of these complexes against various tumour cells were evaluated by MTT assay, and the results showed that these polypyridyl ruthenium(II) complexes exhibited acceptable inhibition against different tumour cells, especially 4, with an IC50 of 18.4 μM for Hela cells. The results showed that 4 inhibited the growth of cervical cancer Hela cells by inducing G2/M phase arrest, which was followed by slight apoptosis. Further studies showed that 4 displayed better inhibition against the invasion and metastasis of Hela cells than NAMI-A. Studies on the in vivo distribution and metabolism indicated that 4 was rapidly distributed in the entire body, absorbed by the tumour tissue and had only a small accumulation of toxicity in the body. These results demonstrated that this type of ruthenium(II) complex can block the growth of Hela cells and inhibit their migration and invasion through G2/M phase arrest, which suggests the complex could act as a potential tumour-targeting inhibitor in future clinical applications.
机译：菲并咪唑衍生物[Ru（phen） 2 （small）（R）]配位的一系列聚吡啶钌（ II ）配合物（ClO < sub> 4 ） 2 （其中1 R = IP，2 R = PIP，3 R = p -HPIP，4 R = p -OCH 3 PIP）在140°C的微波辐射下合成平均收率> 85％ 30分钟通过MTT分析评估了这些复合物对各种肿瘤细胞的抑制作用，结果表明，这些聚吡啶基钌（ II ）复合物对不同的肿瘤细胞表现出可接受的抑制作用，尤其是4种，IC <针对Hela细胞的small> 50 为18.4μM。结果表明，4通过诱导G2 / M期阻滞抑制了宫颈癌Hela细胞的生长，随后发生了轻微的凋亡。进一步的研究表明，与NAMI-A相比，4对Hela细胞的侵袭和转移具有更好的抑制作用。对体内分布和代谢的研究表明，4在整个体内迅速分布，被肿瘤组织吸收，在体内的毒性积累很小。这些结果表明，这种钌（ II ）复合物可以阻止Hela细胞的生长，并通过G2 / M期阻滞抑制其迁移和侵袭，这表明该复合物可以作为潜在的肿瘤-靶向抑制剂在未来的临床应用中。

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