金属配合物抗癌活性的研究进展

介绍了铂配合物、Schiff碱金属配合物及稀土金属配合物的抗癌活性研究现状。     

抗癌金属配合物的研究新进展

自从Rosenberg等人偶然发现顺铂具有抗癌活性以来,金属配合物的药用性引起了人们的广泛关注,开辟了金属配合物抗癌药物研究的新领域。综合评述近年来不同金属配合物在抗癌药物中的研究应用新进展,同时还对金属配合物的抗癌机理进行初探。     

抗癌钌配合物NAMI-A和ICR的合成、水解及其与DNA的相互作用

以RuCl3、DMSO、Im为原料合成了抗癌钌配合物NAMI-A和ICR,进行必要的表征.利用紫外-可见吸收光谱研究了它们在水、DMSO的水溶液、磷酸缓冲溶液(PBS)中的水解情况及其在磷酸缓冲溶液中与DNA相互作用.结果表明,钌配合物在水、DMSO的水溶液和磷酸缓冲溶液(PBS)中的水解性质有较大的差距,与DNA可能以配体嵌插或沟槽作用方式结合.     

槲皮素金属配合物的研究进展

槲皮素具有广泛的生物活性和多方面的药理作用,有完整的大π键共轭体系、强配位氧原子及合适的空间构型,可与多种金属离子螯合成稳定的环状配合物。研究表明:槲皮素金属配合物具有抗癌、抗炎、抗氧化、清除自由基和降血糖等作用。槲皮素金属配合物生物活性明显高于槲皮素,药理作用显著。综述了槲皮素金属配合物的研究进展,介绍了槲皮素与主族、副族和稀土金属元素形成配合物的研究现状,为此类化合物的研究提供科学依据。     

新型铂（Ⅱ）配合物的合成、表征及抗肿瘤活性

为合成铂配合物顺式-1,1环丁基二羧酸一正丁胺／环戊胺合铂（II）,以顺式-二碘-正丁胺／环戊胺合铂（II）为原料,先后与硝酸银和1,1环丁基二羧酸钾反应合成标题产物。采用元素分析、质谱、核磁共振氢谱和红外光谱分析其组成和结构,利用MTT体外检测法进行了初步的体外活性评价。结果显示合成的化合物结构与理论一致,具有一定的体外肿瘤生长抑制活性。     

甘氨酸铂配合物的合成与表征

氯亚铂酸钾与甘氨酸在水溶液中合成了甘氨酸铂配合物。通过薄层色谱、差动热分析、红外、元素分析和体外抗癌活性实验对甘氨酸铂配合物进行了初步表征。     

磺胺类药物金属配合物的研究进展

磺胺类药物配体因具有特殊的芳香环结构、丰富的配位原子以及良好的抗菌、抗癌药物活性等优势,成为新型金属配合物抗菌/抗癌药物研究的热点。重点综述磺胺类药物金属配合物的合成方法、配位模式、抗菌性能和抗癌性能的研究进展,探讨合适的合成方法、有效的配位模式、抗菌/抗癌作用规律等。通过对已报道磺胺类药物金属配合物的系统研究,为设计开发高效、低毒、抗耐药性的新型抗菌/抗癌药物奠定基础。     

钌及其配合物应用研究进展

钌及其配合物具有较好的催化活性及抗肿瘤活性,在化工及医学领域的应用较广泛。查阅大量相关资料,对其在催化方面及抗肿瘤等领域的研究现状进行综述。     

丝氨酸铂配合物的合成、表征及抗肿瘤活性初探

用二碘二氨合铂与L-丝氨酸在水溶液中合成了丝氨酸铂配合物。通过薄层色谱、差动热分析、红外光谱、元素分析对丝氨酸铂配合物进行了初步表征。利用MTT体外检测法初步体外抗癌活性实验结果表明:L-丝氨酸铂配合物对人体的宫颈癌细胞(Hela)和胃癌细胞株(BGC-823)生长有明显抑制作用。     

己内酰胺铂配合物的合成与表征

用氯亚铂酸钾和己内酰胺在水溶液中合成了己内酰胺铂配合物。通过差动热分析、红外光谱、元素分析和体外癌细胞杀伤实验对己内酰胺铂配合物进行了表征。结果表明,己内酰胺铂配合物具有一定抗癌活性,有应用价值。     

量子化学在金属配合物中的应用进展

量子化学的发展经历了价键理论、分子轨道理论和密度泛函理论等的发展,并最终产生了量子化学Gunssian程序。金属配合物在工业、医药和生物学等方面的应用日益广泛,而量子化学理论与方法为其研究提供了有力的计算工具。文章综述了量子化学在研究金属配合物分子结构、稳定性、分子磁性、分子轨道等方面的应用及其研究进展。     

Platinum and Palladium Complexes as Promising Sources for Antitumor Treatments

There is a need for new, safer, and more effective agents to treat cancer. Cytostatics that have transition metals at their core have attracted renewed interest from scientists. Researchers are attempting to use chemotherapeutics, such as cisplatin, in combination therapy (i.e., in order to enhance their effectiveness). Moreover, studies are being carried out to modify molecules, by developing them into multinuclear structures, linking different compounds to commonly used drugs, or encapsulating them in nanoparticles to improve pharmacokinetic parameters, and increase the selectivity of these drugs. Therefore, we attempted to organize recent drug findings that contain palladium and platinum atoms in their structures.     

新型过渡金属配合物的合成、表征及生物活性研究

为了寻找更好的生物活性化合物,以1-苯基-3-甲基-5-吡唑啉酮和苯甲酰氯为原料,二氧六环为溶剂,回流反应合成了4-酰基吡唑啉酮配体及4种过渡金属配合物,通过元素分析、红外光谱、差热-热重分析、紫外光谱等对其结构进行了表征,表明配合物组成分别为:Cu(L)2、Zn(L)2、Ni(L)2、Mn(L)2;同时利用抑菌圈大小...     

质谱技术在金属配合物研究中的应用进展

综述了质谱技术的原理及质谱技术在金属配合物研究中的各种应用,通过介绍金属配合物的表征、稳定性、反应过程及研究其质谱裂解规律等几方面的应用进行了概述。     

Polypyridyl CoII-Curcumin Complexes as Photoactivated Anticancer and Antibacterial Agents

Four new Co^II complexes, [Co(bpy)₂(acac)]Cl ( 1 ), [Co(phen)₂(acac)]Cl ( 2 ), [Co(bpy)₂(cur)]Cl ( 3 ), [Co(phen)₂(cur)]Cl ( 4 ), where bpy=2,2’-bipyridine ( 1 and 3 ), phen=1,10-phenanthroline ( 2 and 4 ), acac = acetylacetonate ( 1 and 2 ), cur=curcumin monoanion ( 3 and 4 ) have been designed, synthesized and fully characterized. The X-ray crystal structures of 1 and 2 indicated that the CoN₄O₂ core has a distorted octahedral geometry. The photoactivity of these complexes was tuned by varying the π conjugation in the ligands. Curcumin complexes 3 and 4 had an intense absorption band near 435 nm, which made them useful as visible-light photodynamic therapy agents; they also showed fluorescence with λ_em≈565 nm. This fluorescence was useful for studying their intracellular uptake and localization in MCF-7 breast cancer cells. The acetylacetonate complexes ( 1 and 2 ) were used as control complexes to understand the role of curcumin. The white-light-triggered anticancer profiles of the cytosol targeting complexes 3 and 4 were investigated in detail. These non-dark toxic complexes displayed significant apoptotic photo-cytotoxicity (under visible light) against MCF-7 cells through ROS generation. The control complexes 1 and 2 did not induce significant cell death in the light or dark. Interestingly, 1-4 produced a remarkable antibacterial response upon light exposure. Overall, the reported results here can increase the boundary of the Co^II-based anticancer and antibacterial drug development.     

Coinage Metal N-Heterocyclic Carbene Complexes: Recent Synthetic Strategies and Medicinal Applications

New weapons are constantly needed in the fight against cancer. The discovery of cisplatin as an anticancer drug prompted the search for new metal complexes. The successful history of cisplatin motivated chemists to develop a plethora of metal-based molecules. Among them, metal-N-heterocyclic carbene (NHC) complexes have gained significant attention because of their suitable qualities for efficient drug design. The enhanced applications of coinage metal-NHC complexes have encouraged a gradually increasing number of studies in the fields of medicinal chemistry that benefit from the fascinating chemical properties of these complexes. This review aims to present recent developments in synthetic strategies and medicinal applications of copper, silver and gold complexes supported by NHC ligands.     

In Vitro and In Vivo Biological Activity of Ruthenium 1,10-Phenanthroline-5,6-dione Arene Complexes

Ruthenium(II) arene complexes exhibit promising chemotherapeutic properties. In this study, the effect of the counter anion in Ru(II) complexes was evaluated by analyzing the biological effect of two Ru(II) p-cymene derivatives with the 1,10-phenanthroline-5,6-dione ligand of general-formula [(η⁶-arene)Ru(L)Cl][X] X = CF₃SO₃ (JHOR10) and PF₆ (JHOR11). The biological activity of JHOR10 and JHOR11 was examined in the ovarian carcinoma cell line A2780, colorectal carcinoma cell line HCT116, doxorubicin-resistant HCT116 (HCT116-Dox) and in normal human dermal fibroblasts. Both complexes JHOR10 and JHOR11 displayed an antiproliferative effect on A2780 and HCT116 cell lines, and low cytotoxicity in fibroblasts. Interestingly, JHOR11 also showed antiproliferative activity in the HCT116-Dox cancer cell line, while JHOR10 was inactive. Studies in A2780 cells showed that JHOR11 induced the production of reactive oxygen species (ROS) that trigger autophagy and cellular senescence, but no apoptosis induction. Further analysis showed that JHOR11 presented no tumorigenicity, with no effect in the cellular mobility, as evaluated by thye wound scratch assay, and no anti- or pro-angiogenic effect, as evaluated by the ex-ovo chorioallantoic membrane (CAM) assay. Importantly, JHOR11 presented no toxicity in chicken and zebrafish embryos and reduced in vivo the proliferation of HCT116 injected into zebrafish embryos. These results show that these are suitable complexes for clinical applications with improved tumor cell cytotoxicity and low toxicity, and that counter-anion alteration might be a viable clinical strategy for improving chemotherapy outcomes in multidrug-resistant (MDR) tumors.     

Reactions with Proteins of Three Novel Anticancer Platinum(II) Complexes Bearing N-Heterocyclic Ligands

Three novel platinum(II) complexes bearing N-heterocyclic ligands, i.e., Pt2c, Pt-IV and Pt-VIII, were previously prepared and characterized. They manifested promising in vitro anticancer properties associated with non-conventional modes of action. To gain further mechanistic insight, we have explored here the reactions of these Pt compounds with a few model proteins, i.e., hen egg white lysozyme (HEWL), bovine pancreatic ribonuclease (RNase A), horse heart cytochrome c (Cyt-c) and human serum albumin (HSA), primarily through ESI MS analysis. Characteristic and variegate patterns of reactivity were highlighted in the various cases that appear to depend both on the nature of the Pt complex and of the interacting protein. The protein-bound Pt fragments were identified. In the case of the complex Pt2c, the adducts formed upon reaction with HEWL and RNase A were further characterized by solving the respective crystal structures: this allowed us to determine the exact location of the various Pt binding sites. The implications of the obtained results are discussed in relation to the possible mechanisms of action of these innovative anticancer Pt complexes.