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Journal of Inorganic Biochemistry

Elisa Palma, Filipa Mendes, Goreti Ribeiro Morais, Inês Rodrigues, Isabel Cordeiro Santos, Maria Paula C Campello, Paula Raposinho, Isabel Correia, Sofia Gama, Dulce Belo, Vítor Alves, Antero J Abrunhosa, Isabel Santos, António Paulo
Aiming to explore alternative mechanisms of cellular uptake and cytotoxicity, we have studied a new family of copper(II) complexes (CuL(1)-CuL(4)) with bis(thiosemicarbazone) (BTSC) ligands containing pendant protonable cyclic amines (morpholine and piperidine). Herein, we report on the synthesis and characterization of these new complexes, as well as on their biological performance (cytotoxic activity, cellular uptake, protein and DNA binding), in comparison with the parental Cu(II)ATSM (ATSM=diacetyl-bis(N4-methylthiosemicarbazonate) complex without pendant cyclic amines...
November 23, 2016: Journal of Inorganic Biochemistry
Eduardo Henrique Silva Sousa, Luiz Gonzaga de França Lopes, Gonzalo Gonzalez, Marie-Alda Gilles-Gonzalez
Heme-based sensors have emerged during the last 20years as being a large family of proteins that occur in all kingdoms of life. A myriad of biological adaptations are associated with these sensors, which include vasodilation, bacterial virulence, dormancy, chemotaxis, biofilm formation, among others. Due to the key activities regulated by these proteins along with many other systems that use similar output domains, there is a growing interest in developing small molecules as their regulators. Here, we review the development of potential activators and inhibitors for many of these systems, including human soluble guanylate cyclase, c-di-GMP-related enzymes, Mycobacterium tuberculosis DevR/DevS/DosT (differentially expressed in virulent strain response regulator/sensor/dormancysurvival sensorT), the Rev-erb-α and β nuclear receptor, among others...
November 20, 2016: Journal of Inorganic Biochemistry
Claudia Palopoli, Guillermo Gómez, Ana Foi, Fabio Doctorovich, Sonia Mallet-Ladeira, Christelle Hureau, Sandra Signorella
Two mononuclear Mn(III) complexes [Mn(3,5-F2salpn)(H2O)2][B(C6H5)4]·2H2O (1·2H2O) and [Mn(3,5-Cl2salpn)(OAc)(H2O)]·H2O (2·H2O), where H2salpn=1,3-bis(salicylidenamino)propane, have been prepared and characterized. The crystal structure of 1·H2O shows that this complex forms μ-aqua dimers with a short Mn⋯Mn distance of 4.93Å. Under anaerobic conditions, the two complexes are stable in solution and possess trans-diaxial symmetry with the tetradentate Schiff base ligand symmetrically arranged in the equatorial plane...
November 18, 2016: Journal of Inorganic Biochemistry
Xiaofang Yang, Weiwei Zhang, Zhiwei Zhao, Nuan Li, Zhipeng Mou, Dongdong Sun, Yongping Cai, Weiyun Wang, Yi Lin
Quercetin (Qe) plays an important role in inflammation, antibacterial, anticancer, and aging. However, Qe has extremely low water solubility, which is a major challenge in drug absorption. In this study, we described a simple method for synthesis of Qe/CdSe/ZnS nanoparticles (QCZ NPs). The QCZ NPs had an average diameter of 10nm and prominent yellow emission under UV irradiation. We investigated the antibacterial activity of QCZ NPs against drug-resistant Escherichia coli (E. coli) and Bacillus subtilis (B...
November 17, 2016: Journal of Inorganic Biochemistry
Mauro Ravera, Elisabetta Gabano, Stefano Tinello, Ilaria Zanellato, Domenico Osella
A small series of Pt(IV) prodrugs containing Gln-like (Gln=glutamine) axial ligands has been designed with the aim to take advantage of the increased demand of Gln showed by some cancer cells (glutamine addiction). In complex 4 the Gln, linked through the α-carboxylic group is recognized by the Gln transporters, in particular by the solute carrier transporter SLC1A5. All compounds showed cellular accumulation, as well as antiproliferative activity, related to their lipophilicity, as already demonstrated for the majority of Pt(IV) prodrugs, that enter cells mainly by passive diffusion...
November 17, 2016: Journal of Inorganic Biochemistry
Shinobu Sato, Shigeori Takenaka
Seven ferrocenyl naphthalene diimide (FND) ligands were synthesized. Each had a higher affinity for tetraplex DNA than for either single- or double-stranded DNA. The FND binding affinities were >10(5)M(-1) in 0.10M AcOH-AcONa or AcOH-AcOK (pH5.5) containing 0.10M NaCl or KCl. The FNDs with the highest binding affinities for tetraplex DNA showed 23- or 8-times higher preference for tetraplex DNA than for single- or double-stranded DNA, respectively. The current signals generated from the seven FNDs bound to the tetraplex DNA immobilized on the electrode were found to correlate with the binding affinities of these ligands for the tetraplex DNA...
November 17, 2016: Journal of Inorganic Biochemistry
Veronika Farkasová, Sayed Ali Drweesh, Andrea Lüköová, Danica Sabolová, Ivana D Radojević, Ljiljana R Čomić, Sava M Vasić, Helena Paulíková, Stanislav Fečko, Tatiana Balašková, Mária Vilková, Ján Imrich, Ivan Potočňák
Starting from well-defined NH2(CH3)2[PdCl2(XQ)] complexes, coordination compounds of general formula Cat[PdCl2(XQ)] have been prepared by cationic exchange of NH2(CH3)2(+) and Cat cations, where XQ are biologically active halogen derivatives of quinolin-8-ol (5-chloro-7-iodo-quinolin-8-ol (CQ), 5,7-dibromo-quinolin-8-ol (dBrQ) and 5,7-dichloro-quinolin-8-ol (dClQ)) and Cat is K(+) or Cs(+). The cation exchange of all prepared complexes, K[PdCl2(CQ)] (1), K[PdCl2(dClQ)] (2), K[PdCl2(dBrQ)] (3), Cs[PdCl2(CQ)] (4), Cs[PdCl2(dClQ)] (5) and Cs[PdCl2(dBrQ)] (6) was approved using IR spectroscopy, their structures in DMSO solution were elucidated by one- and two-dimensional NMR experiments, whereas their stability in solution was verified by UV-VIS spectroscopy...
November 16, 2016: Journal of Inorganic Biochemistry
S Scintilla, L Brustolin, A Gambalunga, F Chiara, A Trevisan, C Nardon, D Fregona
Since the discovery of cisplatin in the 1960s, other metal complexes have been investigated as potential antitumor agents to overcome the side-effects associated with the administration of the Pt-based drug. In line with our previous research, in this work we report the synthesis and characterization of mono- and dinuclear Ru(III) complexes with the pyrrolidinedithiocarbamate (PDT) ligand and the more sterically-hindered carbazole-dithiocarbamato ligand (CDT), to compare their properties (both at the chemical and antiproliferative level), in an attempt to assess a structure-activity rationale...
November 16, 2016: Journal of Inorganic Biochemistry
Antoine Ziller, Rajiv Kumar Yadav, Mercè Capdevila, Mondem Sudhakara Reddy, Laurent Vallon, Roland Marmeisse, Silvia Atrian, Òscar Palacios, Laurence Fraissinet-Tachet
Metallothioneins are cysteine-rich proteins, which function as (i) metal carriers in basal cell metabolism and (ii) protective metal chelators in conditions of metal excess. Metallothioneins have been characterized from different eukaryotic model and cultivable species. Presently, they are categorized in 15 families but evolutionary relationships between these metallothionein families remain unresolved. Several cysteine-rich protein encoding genes that conferred Cd-tolerance in Cd-sensitive yeast mutants have previously been isolated from soil eukaryotic metatranscriptomes...
November 12, 2016: Journal of Inorganic Biochemistry
Jiafeng Geng, Lu Huo, Aimin Liu
The diheme enzyme MauG utilizes H2O2 to perform oxidative posttranslational modification on a protein substrate. A bis-Fe(IV) species of MauG was previously identified as a key intermediate in this reaction. Heterolytic cleavage of the OO bond of H2O2 drives the formation of the bis-Fe(IV) intermediate. In this work, we tested a hypothesis that a glutamate residue, Glu113 in the distal pocket of the pentacoordinate heme of MauG, facilitates heterolytic OO bond cleavage, thereby leading to bis-Fe(IV) formation...
November 9, 2016: Journal of Inorganic Biochemistry
Luca Mazzei, Michele Cianci, Francesco Musiani, Gábor Lente, Marta Palombo, Stefano Ciurli
Urease is a Ni(II)-containing enzyme that catalyzes the hydrolysis of urea to yield ammonia and carbamate at a rate 10(15) times higher than the uncatalyzed reaction. Urease is a virulence factor of several human pathogens, in addition to decreasing the efficiency of soil organic nitrogen fertilization. Therefore, efficient urease inhibitors are actively sought. In this study, we describe a molecular characterization of the interaction between urease from Sporosarcina pasteurii (SPU) and Canavalia ensiformis (jack bean, JBU) with catechol, a model polyphenol...
November 9, 2016: Journal of Inorganic Biochemistry
Gonzalo Scalese, Isabel Correia, Julio Benítez, Santiago Rostán, Fernanda Marques, Filipa Mendes, António Pedro Matos, João Costa Pessoa, Dinorah Gambino
Searching for prospective vanadium-based drugs for cancer treatment, a new series of structurally related [V(IV)O(L-2H)(NN)] compounds (1-8) was developed. They include a double deprotonated salicylaldimine Schiff base ligand (L-2H) and different NN-polypyridyl co-ligands having DNA intercalating capacity. Compounds were characterized in solid state and in solution. EPR spectroscopy suggests that the NN ligands act as bidentate and bind through both nitrogen donor atoms in an axial-equatorial mode. The cytotoxicity was evaluated in human tumoral cells (ovarian A2780, breast MCF7, prostate PC3)...
November 9, 2016: Journal of Inorganic Biochemistry
Lei He, Zhenyu Meng, Yi-Qun Xie, Xiang Chen, Tianhu Li, Fangwei Shao
Two platinum complexes with an aza-bridged bis(1,10-phenanthrolin-2-yl)amine (bpa) were synthesized. The two phenanthrolines in bpa entered a flat plane prior to binding of nucleic acids, which bestowed on the two Pt complexes a significantly high stabilizing ability on both DNA and RNA G-quadruplexes. Further extending alkyl tail from aromatic coordination core enabled the complexes to distinguish GQ sequence based upon the topological folding structures and enhanced the selectivity of the complex against duplex DNA...
November 9, 2016: Journal of Inorganic Biochemistry
Zhize Ou, Yunqing Wang, Yunyan Gao, Xiaobing Wang, Yimeng Qian, Yi Li, Xuesong Wang
The interactions between alkynylplatinum(II) terpyridine complexes 1-3 and the G-quadruplex DNA, including c-myc and telomeric quadruplex DNA, are investigated both in dilute solution and under molecular crowding conditions. The UV-vis absorption spectroscopy, circular dichroism and molecular docking studies suggest that 1-3 associate with telomeric and c-myc G-quadruplexes via groove binding, and electrostatic interactions. Experimental studies indicate that under molecular crowding conditions (in the presence of 40wt% PEG 200), 1-2 show weak affinity for c-myc, while 3 still displays high affinity and selectivity for c-myc...
November 9, 2016: Journal of Inorganic Biochemistry
Nicol Romero, José Benítez, David Garcia, Arlette González, Leonardo Bennun, María A García-Robles, Vasthi López, Liam A Wilson, Gerhard Schenk, Nelson Carvajal, Elena Uribe
Agmatine (1-amino-4-guanidinobutane) plays an important role in a range of metabolic functions, in particular in the brain. Agmatinases (AGMs) are enzymes capable of converting agmatine to the polyamine putrescine and urea. AGMs belong to the family of Mn(2+)-dependent ureahydrolases. However, no AGM from a mammalian source has yet been extracted in catalytically active form. While in human AGM the six amino acid ligands that coordinate the two Mn(2+) ions in the active site are conserved, four mutations are observed in the murine enzyme...
November 9, 2016: Journal of Inorganic Biochemistry
Anastasia M Cheplakova, Anastasiya O Solovieva, Tatiana N Pozmogova, Yuri A Vorotnikov, Konstantin A Brylev, Natalya A Vorotnikova, Elena V Vorontsova, Yuri V Mironov, Alexander F Poveshchenko, Konstantin A Kovalenko, Michael A Shestopalov
Inclusion compounds of photoluminescent hexamolybdenum cluster complexes in the chromium terephthalate metal-organic framework, MIL-101 (MIL, Matérial Institut Lavoisier) were successfully synthesized in two different ways and characterized by means of powder X-Ray diffraction, chemical analysis and nitrogen sorption. Some important functional properties of hexamolybdenum cluster complexes for biological and medical applications, in particular singlet oxygen generation ability, luminescence properties, cellular uptake behavior and cytotoxicity were studied...
November 9, 2016: Journal of Inorganic Biochemistry
Sara Rojas, Francisco J Carmona, Elisa Barea, Carmen R Maldonado
Two novel anthracene-based half-sandwich organometallic Ru(II) compounds, namely, [Ru(p-cymene)(L1)Cl2] (1) and [Ru(p-cymene)(L2)Cl2] (2) (L1=1-(anthracen-9-yl)-N-(pyridin-3-ylmethyl)methanamine; L2=1-(anthracen-9-yl)-N-(pyridin-4-ylmethyl)methanamine) have been synthesized and characterized. We demonstrate that the fluorescence properties of these complexes are highly affected by the linking position of the anthracene unit, as only 2 shows fluorescence emission in the blue region. Regarding their biological activity, both ruthenium metallodrugs show interaction with different biological targets such as S-donor amino acids (cysteine) and proteases (cysteine cathepsin B)...
November 7, 2016: Journal of Inorganic Biochemistry
Kathleen E Prosser, Stephanie W Chang, Felix Saraci, Phuc H Le, Charles J Walsby
The Cu(II) complex CuCl2(pbzH), pbzH=2-(2-pyridyl)benzimidazole, and derivatives modified at the non-coordinated nitrogen of the benzimidazole fragment, have been studied as anticancer agents. These compounds show promising cytotoxicity against A549 adenocarcinomic alveolar basal epithelial cells with IC50 values in the range of 5-10μM. Importantly, this activity is higher than either CuCl2·2H2O or the individual ligands, demonstrating that ligand coordination to the Cu(II) centres of the complexes is required for full activity...
November 5, 2016: Journal of Inorganic Biochemistry
Juan J Martínez Medina, Luciana G Naso, Ana L Pérez, Alberto Rizzi, Evelina G Ferrer, Patricia A M Williams
Based on the known antioxidant effect of flavonoids, baicalin (baic) found in roots of Scutellaria has been selected. Its coordination complex with the oxidovanadium(IV) cation, Na4[VO(baic)2].6H2O (V(IV)O(baic)), was synthesized at pH9 in ethanol and characterized by physicochemical methods. Spectrophotometric studies at pH9 showed a ligand: metal stoichiometry of 2:1. By vibrational spectroscopy a coordination mode through the cis 5-OH and 6-OH deprotonated groups is inferred. EPR spectroscopy shows an environment of four aryloxide (ArO(-)) groups in the equatorial plane of the VO moiety, both in solution and in the solid complex...
November 5, 2016: Journal of Inorganic Biochemistry
Jorge Serment-Guerrero, Maria Elena Bravo-Gomez, Eric Lara-Rivera, Lena Ruiz-Azuara
Casiopeinas is the generic name of a group of copper chelated complexes designed to be used as antineoplastic. Some of these compounds have shown promising results, and in fact, one of them named Casiopeina III-ia has completed preclinical trials and is ready to start clinical phase I in Mexico. As part of the tests that have to be done to every molecule intended to be used in humans, bacterial assays are required because of their sensitivity, speed and reproducibility and among them, Ames test and the SOS Chromotest are widely used to evaluate DNA damage...
November 5, 2016: Journal of Inorganic Biochemistry
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