水解稳定的Ti-IV-水基金属药物:蛋白相互作用和抗癌潜力
Gurunath Sahu1, Kausik Sahu1, Sushree Aradhana Patra1
1Department of Chemistry, National Institute of Technology, Rourkela, Odisha 769008, India.
ACS applied bio materials
|November 29, 2023
概括
合成和表征了三个新的 (IV) 复合物. 这些稳定复合体对牛血清白蛋白具有高度亲和力,并表现出有前途的抗癌活性,其中一个复合体对HeLa细胞特别有效.
科学领域:
- 协调化学 协调化学
- 材料科学 材料科学 材料科学
- 药用化学 医学化学
背景情况:
- 酸连接体是协调化学中的多功能构建块.
- 复合物在各种生物应用中显示出潜力.
- 了解金属-连接体相互作用对于开发新的治疗剂至关重要.
研究的目的:
- 为了合成和表征新的 (IV) 复合物与酸连接体.
- 研究这些复合物的稳定性和生物相互作用.
- 为了评估它们的抗癌潜力与选定的细胞系对比.
主要方法:
- 使用元素分析,FT-IR,UV-vis,NMR,HR-ESI-MS和X射线晶体学进行合成和表征.
- 在DMSO-d/D2O中的水性稳定性研究.
- 使用光和吸收光谱的牛血清白蛋白 (BSA) 相互作用研究.
- 在体外抗癌活性测定对HeLa,A549和NIH-3T3细胞系.
- 使用共聚焦显微镜和流细胞计的亡诱导研究.
主要成果:
- 三种 (IV) 复合物,[Ti (L1-3) ] (1-3),已成功合成并从结构上阐明.
- 综合体1-3在DMSO-d/D2O介质中表现出良好的水解稳定性.
- 观察到对牛血清白蛋白 (BSA) 的高度亲和力,通过静态火表示.
- 综合体1对HeLa细胞表现出显著的细胞毒性 (IC50 = 11.6 ± 1.1μM).
- 发现复合物诱导了亡,通过显微镜和流细胞计验证了这一点.
结论:
- 合成的 (IV) - 水复合物是稳定的,并与BSA强烈相互作用.
- 复合物1显示有前途的抗癌活性,并通过亡诱导细胞死亡.
- 这些发现凸显了这些复合物作为抗癌剂的潜力.
更多相关视频
11:09Constructing Thioether/Vinyl Sulfide-tethered Helical Peptides Via Photo-induced Thiol-ene/yne Hydrothiolation
Published on: August 1, 2018
10.8K
07:20Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
14.0K
相关概念视频
Drugs that Stabilize Microtubules
2.1K
Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
2.1K
EDTA: Chemistry and Properties
1.9K
Polydentate ligands are most widely used in complexometric titrations because they form more stable complexes with the metal ions than mono- or bidentate ligands due to the chelate effect. Examples of polydentate ligands are ethylenediaminetetraacetic acid (EDTA), crown ethers, and cryptands. The most important feature of optimal polydentate ligands is the ability to form 1:1 complexes in a single-step process. Amino carboxylic acid derivatives are frequently used as complexing agents. EDTA is...
1.9K
Metal-Ligand Bonds
20.8K
The hemoglobin in the blood, the chlorophyll in green plants, vitamin B-12, and the catalyst used in the manufacture of polyethylene all contain coordination compounds. Ions of the metals, especially the transition metals, are likely to form complexes.
In these complexes, transition metals form coordinate covalent bonds, a kind of Lewis acid-base interaction in which both of the electrons in the bond are contributed by a donor (Lewis base) to an electron acceptor (Lewis acid). The Lewis acid in...
In these complexes, transition metals form coordinate covalent bonds, a kind of Lewis acid-base interaction in which both of the electrons in the bond are contributed by a donor (Lewis base) to an electron acceptor (Lewis acid). The Lewis acid in...
20.8K
Complexation Equilibria: Factors Influencing Stability of Complexes
376
In complexation reactions, metal cations are the electron pair acceptors, and the ligands are the electron pair donors. The stability of the metal complexes depends primarily on the complexing ability of the central metal ion and the nature of the ligands. Generally, the complexing ability of the metal ion depends on the size and charge of the ion. As the metal ion size increases, the stability of the metal complexes decreases, provided that the valency of the metal ion and the ligands remain...
376
Drugs that Destabilize Microtubules
2.0K
Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
2.0K
