单核无氧化物与双核氧化物VIV 金属药物:溶液行为,生物分子结合,细胞毒性和细胞内化
Pratikshya Das Pattanayak1, Sushree Aradhana Patra1, Sanchita Das1
1Department of Chemistry, National Institute of Technology, Rourkela, Odisha 769008, India.
Inorganic chemistry
|February 4, 2026
概括
新的复合体显示出显著的抗癌活性. 单核复合物在溶液中稳定,向溶酶体,线粒体和核,导致癌细胞死亡.
科学领域:
- 无机化学 无机化学
- 药用化学 医学化学
- 生物化学 生物化学
背景情况:
- 硫化甲 (TSC) 连接物是金属复合体合成的多功能支架.
- 复合物已经显示出有前途的生物活性,包括抗癌性质.
研究的目的:
- 使用素替代的TSC连接物合成和表征新型单核和双核 (IV) 复合物.
- 研究这些复合物的溶液相稳定性,DNA/蛋白质结合和细胞毒性作用.
主要方法:
- 使用物理化学技术合成和表征复合物.
- 溶液相稳定性研究.
- 谱学方法,密度函数理论 (DFT) 和对接研究用于相互作用分析.
- 对A549和MCF-7癌细胞系的细胞毒性测定.
- 细胞内化研究使用溶解体,线粒体和核作为目标.
主要成果:
- 成功合成单核[VIV(L2,3) 2 (1-2) 和双核[VIVO) 2(L1-3) 2 (3-5) VIV复合体.
- 复合体1-2在水溶液中保持稳定,而3-5部分转化.
- 复合物及其转化产物通过非共价和共价结合与BSA和CT-DNA相互作用.
- 所有复合物都对肺癌 (A549) 和乳腺癌 (MCF-7) 细胞系表现出显著的细胞毒性活性 (IC50:8.919.2μM).
- 复合体5及其碎片是最有效的;复合体1-2显示出高效的细胞吸收,准溶酶体,线粒体和细胞核,诱导ROS和亡.
结论:
- 合成的复合物表现出强大的抗癌活性.
- 单核复合体是稳定的,并通过溶酶体破坏和ROS生成诱导亡.
- 这些发现突出了这些复合物的抗癌药物的潜力.
相关概念视频
01:31Internal Receptors
74.7K
Many cellular signals are hydrophilic and therefore cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind to internal, or intracellular, receptors that reside within the cell. Many mammalian steroid hormones use this mechanism of cell signaling, as does nitric oxide (NO) gas.
74.7K
03:14Oxidation Numbers
42.8K
In redox reactions, the transfer of electrons occurs between reacting species. Electron transfer is described by a hypothetical number called the oxidation number (or oxidation state). It represents the effective charge of an atom or element, which is assigned using a set of rules.
42.8K
02:00Internal Energy
36.8K
The total of all possible kinds of energy present in a substance is called the internal energy (U), sometimes symbolized as E. Suppose a system with initial internal energy, Uinitial, undergoes a change in energy (transfer of work or heat), and the final internal energy of the system is Ufinal. Change in internal energy equals the difference between Ufinal and Uinitial.
36.8K
02:18The Equilibrium Binding Constant and Binding Strength
15.1K
The equilibrium binding constant (Kb) quantifies the strength of a protein-ligand interaction. Kb can be calculated as follows when the reaction is at equilibrium:
15.1K
01:27Cytotoxic T Cells-mediated Immune Response
7.5K
Cytotoxic T cells are a vital component of the immune system. They have the remarkable ability to identify and target antigens on infected or abnormal cells. These antigens often originate from intracellular pathogens such as viruses or abnormal proteins cancer cells produce.
Immunological surveillance is the ability of immune cells to monitor and eliminate infected cells with intracellular pathogens, neoplastically transformed cells, and cells with non-self antigens. Cytotoxic T cells and NK...
Immunological surveillance is the ability of immune cells to monitor and eliminate infected cells with intracellular pathogens, neoplastically transformed cells, and cells with non-self antigens. Cytotoxic T cells and NK...
7.5K
01:15Pyruvate Oxidation
169.0K
After glycolysis, the charged pyruvate molecules enter the mitochondria via active transport and undergo three enzymatic reactions. These reactions ensure that pyruvate can enter the next metabolic pathway so that energy stored in the pyruvate molecules can be harnessed by the cells.
First, the enzyme pyruvate dehydrogenase removes the carboxyl group from pyruvate and releases it as carbon dioxide. The stripped molecule is then oxidized and releases electrons, which are then picked up by NAD+...
First, the enzyme pyruvate dehydrogenase removes the carboxyl group from pyruvate and releases it as carbon dioxide. The stripped molecule is then oxidized and releases electrons, which are then picked up by NAD+...
169.0K