基于新型Ni (II),Cu (II),Zn (II),Pd (II) 和Ag (I) 硫化碳基复合物的结构研究和生物活性
Bartłomiej Rogalewicz1, Marcin Świątkowski1, Magdalena Iwan2
1Institute of General and Ecological Chemistry, Faculty of Chemistry, Lodz University of Technology, Żeromskiego 116, 90-924 Lodz, Poland.
Journal of inorganic biochemistry
|June 11, 2025
概括
新的替代的尼托芬二氧化碳及其金属复合物显示出有前途的抗癌和抗菌活性. 值得注意的是,铜和复合体对癌细胞具有显著的有效性,对健康细胞的毒性较低.
科学领域:
- 协调化学 协调化学
- 药用化学 医学化学
- 材料科学 材料科学 材料科学
背景情况:
- 西米卡巴是多功能连接体,以其多样化的生物活动而闻名.
- 金属复合物通常与其母联体相比表现出增强的药理性质.
- 开发具有提高疗效和降低毒性的新型抗癌和抗微生物药物是一个关键的研究领域.
研究的目的:
- 合成和描述新的替代基化碳联体及其金属复合物.
- 评估这些化合物对特定癌症细胞系的抗癌活性.
- 调查针对各种细菌菌株的抗菌潜力,并评估它们的作用机制.
主要方法:
- 合成了三种新的二氧化碳联体 (HTSC-oCl,HTSC-mCl,HTSC-pCl) 和十五种金属复合物 (Ni(II),Cu(II),Zn(II),Pd(II),Ag(I)).
- 物理化学表征和单晶X射线衍射分析选择的配体和复合体.
- 在LN-229和T-47D细胞系上进行体外抗癌试验 (IC50测定),在BJ细胞上进行细胞毒性评估.
- 针对细菌菌株 (S. aureus,S. epidermidis,B. subtilis,E. coli) 的抗微生物敏感性测试 (MIC 确定).
- 行动研究的机制,包括ROS生产和DNA向调查.
主要成果:
- 在金属复合体中,N,S结合模式和连接体的脱质定被X射线衍射证实.
- Cu(TSC-oCl) 2,Cu(TSC-mCl) 2和Pd(TSC-oCl) 2表现出强烈的抗癌活性,IC50值低至1.52μM,对癌细胞系具有很强的抗癌作用.
- 复合铜 (Cu(TSC-oCl) 2,Cu(TSC-mCl) 2) 激活了抗氧化基因并产生了ROS,而Pd(TSC-oCl) 2则准了DNA.
- 所有测试的复合物对健康的BJ细胞有较低的毒性.
- 一些复合物,特别是基于Cu (II),Zn (II),Pd (II) 和Ag (I) 的复合物,表现出显著的抗菌活性,MIC值降至6.25 mg/L.
结论:
- 合成的替代的酸二氧化碳及其金属复合物代表了抗癌和抗菌药物开发的一类有前途的化合物.
- 铜和复合物显示出作为抗癌剂的优秀潜力,因为它们的高疗效和选择性.
- 独特的作用机制,包括ROS生成,DNA向和抗菌活性,突出显示了这些金属复合物的治疗多功能性.
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