Research Article

硫普罗宁和杂环巯基四唑化合物的独特单体非均相双配位一价金配合物的细胞毒活性

卷 29, 期 22, 2022

发表于: 11 January, 2022

页: [3973 - 3982] 页: 10

弟呕挨: 10.2174/0929867328666211018094206

价格: $65

摘要

背景:NF-κB在癌症的恶性转化和转移等情况下起重要作用,抑制这种作用可能是癌症治疗策略之一。金制剂如金诺芬具有间接的NF-κB抑制作用。 目的:合成一种具有不同物理性质和化学结构的新型金配合物[硫普罗宁一价金-5-巯基-1-甲基四唑,简称TPN-Au(I)-MM4],并评价其对人THP1细胞的细胞毒活性和辐射增敏作用。 方法:用台盼蓝染料排除法计数活细胞数。通过FITC标记膜联蛋白V+和PI染色进行细胞死亡评估。为了研究TPN Au(I)-MM4的辐射增敏效应,在X射线照射前1小时将该化合物[10或25μM]添加到培养基中。 结果:在用25μM TPN-Au(I)-MM4处理72小时的细胞中,观察到THP1细胞的增殖减少[对照组和25μM处理组中活细胞的相对值分别约为6.8和4.2]。在25μM化合物治疗和X射线照射的组合中,与单独照射的情况相比,观察到在2 Gy照射下增加了约3.0倍,在4 Gy照射下增加了约1.4倍。 结论:TPN-Au(I)-MM4通过诱导细胞死亡而减少THP1细胞的增殖,TPN-Au(I)-MM4与X射线联合应用对THP1细胞具有有效的细胞毒性。

关键词: 金配合物,tpn-au[I]-mm4,辐射致敏效应,人类 thp1 细胞,抑制增殖,诱导细胞死亡

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