基于新的非对称的沙洛芬类型配体的Ni (II) 和Zn (II) 复合物的抗癌活性:合成,表征和单晶X射线衍射
David Villaman1, Andrés Vega2, Lucía Santa Maria de la Parra3
1Laboratorio de Química Inorgánica y Organometálica, Facultad de Cs. Química, Universidad de Concepción, Chile. dvillaman@udec.cl.
Dalton transactions (Cambridge, England : 2003)
|July 24, 2023
概括
新的 (NiII) 和 (ZnII) 协调化合物被合成为潜在的抗癌剂. NiII-L2对骨髓瘤和结肠癌细胞表现出显著的功效,表现优于思丁,对瘤细胞具有很高的选择性.
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:
- 基于的化疗药物有严重的副作用,推动了对新型抗癌剂的研究.
- 不对称的N2O2-四酸连接体及其金属复合物为开发新的癌症治疗提供了有前途的途径.
研究的目的:
- 通过非对称的N2O2-四酸连接物合成和描述新的Ni(II) 和Zn(II) 协调化合物.
- 评估这些合成化合物的体外抗癌活性和对各种癌症细胞系的选择性.
主要方法:
- 合成和对不对称的N2O2-四聚酸联体 (H2L1,H2L2) 和它们的Ni (II) 和Zn (II) 复合物的完整表征.
- 使用1H NMR,UV-Vis光谱和单晶X射线衍射进行结构阐明.
- 在体外细胞毒性测定对人类骨髓瘤 (MG-63),结肠癌 (HCT-116),乳腺癌 (MDA-MB-231) 细胞系和非癌性L929细胞.
主要成果:
- 合成的配体和复合物,包括NiII-L1,NiII-L2,ZnII-L1和ZnII-L2,在相关的生物介质中表现出稳定性.
- NiII-L2,ZnII-L1和ZnII-L2复合物对癌细胞系产生了显著的细胞毒性作用,而配体则没有表现出细胞毒性.
- NiII-L2对具有低微分子IC50值的MG-63和HCT-116细胞表现出强烈的活性,并且与西斯普拉丁相比,对测试的癌症细胞系表现出更高的疗效.
- 三种复合物对瘤细胞表现出显著的选择性,选择性指数 (SI) 值在1.6到7.4之间.
结论:
- 合成的Ni (II) 和Zn (II) 复合物,特别是NiII-L2,显示出作为新型抗癌剂的显著前景.
- NiII-L2对癌细胞表现出强烈和选择性的细胞毒性,这表明它有可能成为化疗开发的主要化合物.
- 需要对这些化合物的作用机制和体内疗效进行进一步的研究.
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