共查询到20条相似文献,搜索用时 15 毫秒
1.
Marta Jakubaszek Jeremie Rossier Johannes Karges Joachim Delasoie Bruno Goud Gilles Gasser Fabio Zobi 《Helvetica chimica acta》2019,102(7)
The current photosensitizers (PSs) for photodynamic therapy (PDT) lack selectivity for cancer cells. To tackle this drawback, in view of selective cancer delivery, we envisioned conjugating two ruthenium polypyridyl complexes to vitamin B12 (Cobalamin, Cbl) to take advantage of the solubility and active uptake of the latter. Ultimately, our results showed that the transcobalamin pathway is unlikely involved for the delivery of these ruthenium‐based PDT PSs, emphasizing the difficulty in successfully delivering metal complexes to cancer cells. 相似文献
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Qian‐Xiong Zhou Dr. Wan‐Hua Lei Jing‐Rong Chen Chao Li Yuan‐Jun Hou Xue‐Song Wang Prof. Bao‐Wen Zhang 《Chemistry (Weinheim an der Bergstrasse, Germany)》2010,16(10):3157-3165
Ruthenium(II) polypyridyl complexes with long‐wavelength absorption and high singlet‐oxygen quantum yield exhibit attractive potential in photodynamic therapy. A new heteroleptic RuII polypyridyl complex, [Ru(bpy)(dpb)(dppn)]2+ (bpy=2,2′‐bipyridine, dpb=2,3‐bis(2‐pyridyl)benzoquinoxaline, dppn=4,5,9,16‐tetraaza‐dibenzo[a,c]naphthacene), is reported, which exhibits a 1MLCT (MLCT: metal‐to‐ligand charge transfer) maximum as long as 548 nm and a singlet‐oxygen quantum yield as high as 0.43. Steady/transient absorption/emission spectra indicate that the lowest‐energy MLCT state localizes on the dpb ligand, whereas the high singlet‐oxygen quantum yield results from the relatively long 3MLCT(Ru→dpb) lifetime, which in turn is the result of the equilibrium between nearly isoenergetic excited states of 3MLCT(Ru→dpb) and 3ππ*(dppn). The dppn ligand also ensures a high binding affinity of the complex towards DNA. Thus, the combination of dpb and dppn gives the complex promising photodynamic activity, fully demonstrating the modularity and versatility of heteroleptic RuII complexes. In contrast, [Ru(bpy)2(dpb)]2+ shows a long‐wavelength 1MLCT maximum (551 nm) but a very low singlet‐oxygen quantum yield (0.22), and [Ru(bpy)2(dppn)]2+ shows a high singlet‐oxygen quantum yield (0.79) but a very short wavelength 1MLCT maximum (442 nm). 相似文献
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Kai Xiong Chen Qian Yixian Yuan Lin Wei Xinxing Liao Liting He Thomas W. Rees Yu Chen Jian Wan Liangnian Ji Hui Chao 《Angewandte Chemie (International ed. in English)》2020,59(38):16631-16637
Inducing necroptosis in cancer cells is an effective approach to circumvent drug‐resistance. Metal‐based triggers have, however, rarely been reported. Ruthenium(II) complexes containing 1,1‐(pyrazin‐2‐yl)pyreno[4,5‐e][1,2,4]triazine were developed with a series of different ancillary ligands ( Ru1 ‐ 7 ). The combination of the main ligand with bipyridyl and phenylpyridyl ligands endows Ru7 with superior nucleus‐targeting properties. As a rare dual catalytic inhibitor, Ru7 effectively inhibits the endogenous activities of topoisomerase (topo) I and II and kills cancer cells by necroptosis. The cell signaling pathway from topo inhibition to necroptosis was elucidated. Furthermore, Ru7 displays significant antitumor activity against drug‐resistant cancer cells in vivo. To the best of our knowledge, Ru7 is the first Ru‐based necroptosis‐inducing chemotherapeutic agent. 相似文献
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Chemical Swarming: Depending on Concentration,an Amphiphilic Ruthenium Polypyridyl Complex Induces Cell Death via Two Different Mechanisms 下载免费PDF全文
Dr. Bianka Siewert Vincent H. S. van Rixel Eva J. van Rooden Dr. Samantha L. Hopkins Miriam J. B. Moester Freek Ariese Dr. Maxime A. Siegler Dr. Sylvestre Bonnet 《Chemistry (Weinheim an der Bergstrasse, Germany)》2016,22(31):10960-10968
The crystal structure and in vitro cytotoxicity of the amphiphilic ruthenium complex [ 3 ](PF6)2 are reported. Complex [ 3 ](PF6)2 contains a Ru?S bond that is stable in the dark in cell‐growing medium, but is photosensitive. Upon blue‐light irradiation, complex [ 3 ](PF6)2 releases the cholesterol–thioether ligand 2 and an aqua ruthenium complex [ 1 ](PF6)2. Although ligand 2 and complex [ 1 ](PF6)2 are by themselves not cytotoxic, complex [ 3 ](PF6)2 was unexpectedly found to be as cytotoxic as cisplatin in the dark, that is, with micromolar effective concentrations (EC50), against six human cancer cell lines (A375, A431, A549, MCF‐7, MDA‐MB‐231, and U87MG). Blue‐light irradiation (λ=450 nm, 6.3 J cm?2) had little influence on the cytotoxicity of [ 3 ](PF6)2 after 6 h of incubation time, but it increased the cytotoxicity of the complex by a factor 2 after longer (24 h) incubation. Exploring the unexpected biological activity of [ 3 ](PF6)2 in the dark elucidated an as‐yet unknown bifaceted mode of action that depended on concentration, and thus, on the aggregation state of the compound. At low concentration, it acts as a monomer, inserts into the membrane, and can deliver [ 1 ]2+ inside the cell upon blue‐light activation. At higher concentrations (>3–5 μm ), complex [ 3 ](PF6)2 forms supramolecular aggregates that induce non‐apoptotic cell death by permeabilizing cell membranes and extracting lipids and membrane proteins. 相似文献
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Wenbing Hu Qun Luo Dr. Xiaoyan Ma Kui Wu Jianan Liu Yi Chen Prof. Dr. Shaoxiang Xiong Dr. Jianping Wang Prof. Dr. Peter J. Sadler Prof. Dr. Fuyi Wang Prof. Dr. 《Chemistry (Weinheim an der Bergstrasse, Germany)》2009,15(27):6586-6594
Arene control : Anticancer complexes [Ru(arene)Cl(en)]+ (arene=p‐cymene or biphenyl; en=ethylenediamine) bind to surface histidine (His128, His247, His510) and methionine (Met298) residues in human albumin, but only the p‐cymene complex can gain entry to the crevice containing the free cysteine thiolate (Cys34) and induce oxidation to sulfinate.
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A Deadly Organometallic Luminescent Probe: Anticancer Activity of a ReI Bisquinoline Complex 下载免费PDF全文
Dr. Igor Kitanovic Suzan Can Dr. Hamed Alborzinia Dr. Ana Kitanovic Vanessa Pierroz Anna Leonidova Dr. Antonio Pinto Priv. Doz. Dr. Bernhard Spingler Priv. Doz. Dr. Stefano Ferrari Roberto Molteni Dr. Andreas Steffen Prof. Dr. Nils Metzler‐Nolte Prof. Dr. Stefan Wölfl Prof. Dr. Gilles Gasser 《Chemistry (Weinheim an der Bergstrasse, Germany)》2014,20(9):2496-2507
The photophysical properties of [Re(CO)3(L ‐N3)]Br (L ‐N3=2‐azido‐N,N‐bis[(quinolin‐2‐yl)methyl]ethanamine), which could not be localized in cancer cells by fluorescence microscopy, have been revisited in order to evaluate its use as a luminescent probe in a biological environment. The ReI complex displays concentration‐dependent residual fluorescence besides the expected phosphorescence, and the nature of the emitting excited states have been evaluated by DFT and time‐dependent (TD) DFT methods. The results show that fluorescence occurs from a 1LC/MLCT state, whereas phosphorescence mainly stems from a 3LC state, in contrast to previous assignments. We found that our luminescent probe, [Re(CO)3(L ‐N3)]Br, exhibits an interesting cytotoxic activity in the low micromolar range in various cancer cell lines. Several biochemical assays were performed to unveil the cytotoxic mechanism of the organometallic ReI bisquinoline complex. [Re(CO)3(L ‐N3)]Br was found to be stable in human plasma indicating that [Re(CO)3(L ‐N3)]Br itself and not a decomposition product is responsible for the observed cytotoxicity. Addition of [Re(CO)3(L ‐N3)]Br to MCF‐7 breast cancer cells grown on a biosensor chip micro‐bioreactor immediately led to reduced cellular respiration and increased glycolysis, indicating a large shift in cellular metabolism and inhibition of mitochondrial activity. Further analysis of respiration of isolated mitochondria clearly showed that mitochondrial respiratory activity was a direct target of [Re(CO)3(L ‐N3)]Br and involved two modes of action, namely increased respiration at lower concentrations, potentially through increased proton transport through the inner mitochondrial membrane, and efficient blocking of respiration at higher concentrations. Thus, we believe that the direct targeting of mitochondria in cells by [Re(CO)3(L ‐N3)]Br is responsible for the anticancer activity. 相似文献
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多吡啶钌配合物作为DNA结构探针的研究 总被引:13,自引:2,他引:13
本文对多吡啶钌配合物作为DNA荧光或结构探针的研究背景、研究技术及其特点、钌配合物与DNA的键合模式及其结合力大小的影响因素、钌配合物与DNA键合的异构选择性及不同键合速率、非放射性核酸标记及DNA分子光开关等方面进行了简要述评 相似文献
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《化学:亚洲杂志》2017,12(2):254-264
Two new luminescent ruthenium(II) polypyridyl complexes, [Ru(bpy)2(tpt‐phen)]Cl2 ( 1 ; bpy=2,2′‐bipyridine, tpt‐phen=triptycenyl‐1,10‐phenanthroline) and [Ru(phen)2(tpt‐phen)]Cl2 ( 2 ; phen=1,10‐phenanthroline), have been developed as potential nonviral vectors for DNA delivery. Photophysical and electrochemical properties of the complexes have been investigated and corroborated with electronic structure calculations. DNA condensation by these complexes has been investigated by UV/Vis and emission spectroscopy, circular dichroism spectroscopy, atomic force microscopy, dynamic light scattering, confocal microscopy, and electrophoretic mobility studies. These complexes interact with DNA and efficiently condense DNA into globular nanoparticles that are taken up efficiently by HeLa cells. DNA cleavage inability and biocompatibility of complexes have been explored. Both complexes have good gene transfection abilities. 相似文献
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Dr. Shubhankar Gadre M. Manikandan Prakash Duari Sushant Chhatar Astha Sharma Subhash Khatri Dr. Jyoti Kode Madan Barkume Nirmal Kumar Kasinathan Manasi Nagare Meena Patkar Arvind Ingle Dr. Mukesh Kumar Prof. Ullas Kolthur-Seetharam Dr. Malay Patra 《Chemistry (Weinheim an der Bergstrasse, Germany)》2022,28(46):e202201259
Despite phenomenal clinical success, the efficacy of platinum anticancer drugs is often compromised due to inherent and acquired drug resistant phenotypes in cancers. To circumvent this issue, we designed two heterobimetallic platinum (II)-ferrocene hybrids that display multi-pronged anticancer action. In cancer cells, our best compound, 2 , platinates DNA, produces reactive oxygen species, and has nucleus, mitochondria, and endoplasmic reticulum as potential targets. The multi-modal mechanism of action of these hybrid agents lead to non-apoptotic cell death induction which enables circumventing apoptosis resistance and significant improvement in platinum cross resistance profile. Finally, in addition to describing detail mechanistic insights, we also assessed its stability in plasma and demonstrate anticancer efficacy in an in vivo A2780 xenograft model. Strikingly, compared to oxaliplatin, our compound displays better tolerability, safety profile and efficacy in vivo. 相似文献
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用紫外-可见吸收光谱和荧光光谱滴定、稳态荧光淬灭和反向盐滴定实验研究了双核钌(II)配合物[(bpy)2Ru(ebipcH2)Ru(bpy)2](ClO4)4 {bpy=2,2'-联吡啶; ebipcH2=N-乙基-4,7-二(咪唑-[4,5-f]-(1,10-邻菲啰啉)-2-基)咔唑}与酵母RNA 的相互作用. 结果表明该双核配合物以插入方式与酵母RNA 作用, 在生理盐浓度下(≈150 mmol/L NaCl)该配合物与RNA 的相互作用明显强于DNA. 相似文献
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Abdur Rauf Tareq Abu-Izneid Anees Ahmed Khalil Muhammad Imran Zafar Ali Shah Talha Bin Emran Saikat Mitra Zidan Khan Fahad A. Alhumaydhi Abdullah S. M. Aljohani Ishaq Khan Md. Mominur Rahman Philippe Jeandet Tanweer Aslam Gondal 《Molecules (Basel, Switzerland)》2021,26(23)
Berberine (BBR), a potential bioactive agent, has remarkable health benefits. A substantial amount of research has been conducted to date to establish the anticancer potential of BBR. The present review consolidates salient information concerning the promising anticancer activity of this compound. The therapeutic efficacy of BBR has been reported in several studies regarding colon, breast, pancreatic, liver, oral, bone, cutaneous, prostate, intestine, and thyroid cancers. BBR prevents cancer cell proliferation by inducing apoptosis and controlling the cell cycle as well as autophagy. BBR also hinders tumor cell invasion and metastasis by down-regulating metastasis-related proteins. Moreover, BBR is also beneficial in the early stages of cancer development by lowering epithelial–mesenchymal transition protein expression. Despite its significance as a potentially promising drug candidate, there are currently no pure berberine preparations approved to treat specific ailments. Hence, this review highlights our current comprehensive knowledge of sources, extraction methods, pharmacokinetic, and pharmacodynamic profiles of berberine, as well as the proposed mechanisms of action associated with its anticancer potential. The information presented here will help provide a baseline for researchers, scientists, and drug developers regarding the use of berberine as a promising candidate in treating different types of cancers. 相似文献
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用紫外-可见吸收光谱和荧光光谱滴定、稳态荧光淬灭和反向盐滴定实验研究了双核钌(II)配合物[(bpy)2Ru(ebipcH2)Ru(bpy)2](ClO4)4 {bpy=2,2'-联吡啶; ebipcH2=N-乙基-4,7-二(咪唑-[4,5-f]-(1,10-邻菲啰啉)-2-基)咔唑}与酵母RNA的相互作用. 结果表明该双核配合物以插入方式与酵母RNA作用, 在生理盐浓度下(≈150 mmol/L NaCl)该配合物与RNA的相互作用明显强于DNA. 相似文献
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Dr. Mianli Bian Ying Sun Yuanhao Liu Dr. Zhongren Xu Rong Fan Ziwen Liu Prof. Dr. Wukun Liu 《Chemistry (Weinheim an der Bergstrasse, Germany)》2020,26(31):7092-7108
Many cancer cells critically rely on antioxidant systems for cell survival and are vulnerable to further oxidative impairment triggered by agents generating reactive oxygen species (ROS). Therefore, the classical design and development of inhibitors that target antioxidant defense enzymes such as thioredoxin reductase (TrxR) can be a promising anticancer strategy. Herein, it is shown that a gold(I) complex containing an oleanolic acid derivative ( 4 b ) induces apoptosis of ovarian cancer A2780 cells by activating endoplasmic reticulum stress (ERS). It can inhibit TrxR enzyme activity to elevate ROS, mediate ERS and mitochondrial dysfunction, and finally leads to cell cycle arrest and apoptosis of A2780 cells. Notably, this complex inhibits A2780 xenograft tumor growth accompanied by increased ERS level and decreased TrxR activity in tumor tissues. 相似文献
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设计合成含多个配位中心的多吡啶配体ODCIP (3,4-二氯基苯并咪唑并[4,5-f][1,10]邻菲咯啉)及其钌(II)多吡啶配合物[Ru(bpy)2ODCIP]2+. 运用元素分析、红外光谱、核磁谱和质谱对配体及配合物进行结构表征. 利用紫外吸收光谱、荧光光谱和粘度法研究了[Ru(bpy)2ODCIP]2+与DNA(脱氧核糖核酸)的作用机制、与Co2+配位后与DNA的作用机制及其荧光变化情况. 结果表明[Ru(bpy)2ODCIP]2+与DNA通过部分插入模式作用, [Ru(bpy)2ODCIP]2+与Co2+配位形成的双核配合物[Ru(bpy)2(ODCIP)Co]4+也能与DNA插入结合. 进一步利用稳态荧光发射光谱、荧光淬灭实验等方法研究了单核配合物[Ru(bpy)2ODCIP]2+和双核配合物[Ru(bpy)2(ODCIP)Co]4+的荧光性质. 相似文献
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Veronica Marin Elisabeth Holder Michael A. R. Meier Richard Hoogenboom Ulrich S. Schubert 《Macromolecular rapid communications》2004,25(7):793-798
Summary: An amino‐functionalized bipyridine ligand was prepared in order to serve as a bridging unit to an activated low‐molecular‐weight monomethyl ether of poly(ethylene glycol) (PEG). Coordination of a ruthenium(II ) phenantroline precursor onto the formed PEG‐containing bipyridine ligand yielded a metal‐containing polymer which shows interesting properties for solar cell applications.