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Chiral ruthenium(ii) complex as potent radiosensitizer of I-125 through DNA-damage-mediated apoptosis

机译:手性钌(II)通过DNA损伤介导的细胞凋亡作为I-125的有效放射胶剂复合物

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摘要

A chiral ruthenium(ii) complex, -[Ru(bpy)(2)(o-tFMPIP)] (ClO4)(2) (o-tFMPIP = 2-trifluoromethylphenyl) imidazo [4,5-f][1,10]phenanthroline, was prepared and evaluated for its enhancement of the radiosensitivity of I-125 seeds. The synthetic Ru(ii) complex, LR042, effectively enhanced growth inhibition against HepG2 human hepatocellular liver carcinoma cells induced by I-125 seeds and consequently effectively promoted the apoptosis of tumor cells with increasing level of cleave-caspase-3. Furthermore, the results of immunofluorescence indicated that LR042 enhanced the phosphorylation of H2AX by I-125 seeds vigorously in response to damaged DNA. LR042 improved DNA damage induced by I-125 seeds, which resulted in apoptosis through the activation of the p53/AKT signal. In conclusion, synthetic LR042 can be further developed as a potential radiosensitizer of I-125 seed radiotherapy for cancer therapy.
机译:手性钌(II)复合物, - [Ru(BPY)(2)(O-TFMPIP)](CLO 4)(2)(O-TFMPIP = 2-三氟甲基苯基)咪唑[4,5-F] [1,10] 制备菲咯啉,并评价其增强I-125种子的放射敏感性。 合成ru(ii)复合物,LR042,有效地增强了对I-125种子诱导的HepG2人肝细胞癌细胞的生长抑制,从而有效地促进了肿瘤细胞的凋亡随着裂解水溶液-3的水平。 此外,免疫荧光的结果表明,LR042响应于受损DNA致响应于损坏的DNA,LR042通过I-125种子增强H2AX的磷酸化。 LR042改善了I-125种子诱导的DNA损伤,通过激活P53 / AKT信号导致细胞凋亡。 总之,合成的LR042可以进一步开发为癌症治疗的I-125种子放射治疗的潜在放射胶质剂。

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  • 来源
    《RSC Advances》 |2018年第37期|共7页
  • 作者单位

    Sun Yat Sen Univ Affiliated Hosp 3 Dept Vasc Intervent Radiol 600 Tianhe Rd Guangzhou 510630 Guangdong Peoples R China;

    Sun Yat Sen Univ Affiliated Hosp 3 Dept Vasc Intervent Radiol 600 Tianhe Rd Guangzhou 510630 Guangdong Peoples R China;

    Guangdong Pharmaceut Univ Sch Pharm Guangzhou 510006 Guangdong Peoples R China;

    Guangdong Pharmaceut Univ Sch Pharm Guangzhou 510006 Guangdong Peoples R China;

    Sun Yat Sen Univ Affiliated Hosp 3 Dept Vasc Intervent Radiol 600 Tianhe Rd Guangzhou 510630 Guangdong Peoples R China;

    Sun Yat Sen Univ Affiliated Hosp 3 Dept Vasc Intervent Radiol 600 Tianhe Rd Guangzhou 510630 Guangdong Peoples R China;

    Sun Yat Sen Univ Affiliated Hosp 3 Dept Vasc Intervent Radiol 600 Tianhe Rd Guangzhou 510630 Guangdong Peoples R China;

    Sun Yat Sen Univ Affiliated Hosp 3 Dept Vasc Intervent Radiol 600 Tianhe Rd Guangzhou 510630 Guangdong Peoples R China;

    Sun Yat Sen Univ Affiliated Hosp 3 Dept Vasc Intervent Radiol 600 Tianhe Rd Guangzhou 510630 Guangdong Peoples R China;

    Sun Yat Sen Univ Affiliated Hosp 3 Dept Vasc Intervent Radiol 600 Tianhe Rd Guangzhou 510630 Guangdong Peoples R China;

    Guangdong Pharmaceut Univ Sch Pharm Guangzhou 510006 Guangdong Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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