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George Psomas - One of the best experts on this subject based on the ideXlab platform.
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zinc ii complexes with the quinolone Antibacterial Drug flumequine structure dna and albumin binding
New Journal of Chemistry, 2013Co-Authors: Alketa Tarushi, Jakob Kljun, Iztok Turel, George Psomas, Anastasia A. Pantazaki, Dimitris P KessissoglouAbstract:The interaction of Zn(II) with the quinolone Antibacterial Drug flumequine (Hflmq) in the presence or absence of an N,N′-donor heterocyclic ligand, 2,2′-bipyridine (bipy), is being investigated. Interaction of equimolar quantities of ZnCl2 with flumequine and 2,2′-bipyridine results in the formation of a structurally characterized [Zn(flmq)(bipy)Cl] (2) complex, while excess of flumequine leads to a structurally characterized [Zn(flmq)2(bipy)] (3) compound. The reaction of ZnCl2 with flumequine in the absence of 2,2′-bipyridine leads to formation of complex [Zn(flmq)2(H2O)2] (1). In all these complexes, the deprotonated bidentate flumequinato ligands are coordinated to zinc ions through pyridone and carboxylato oxygens. The complexes exhibit good binding propensity to human or bovine serum albumin protein having relatively high binding constant values. UV study of interaction of the complexes with calf-thymus DNA (CT DNA) has shown that they bind to CT DNA and [Zn(flmq)(bipy)Cl] exhibits the highest binding constant. A competitive study with ethidium bromide (EB) has shown that the complexes can displace DNA-bound EB, indicating that they bind to DNA in strong competition with EB. The complexes bind to CT DNA in an intercalative binding mode which has also been verified by DNA solution viscosity measurements. DNA electrophoretic mobility experiments showed that all complexes bind to pDNA possibly in an intercalative manner resulting in catenanes formation as well as in double-stranded cleavage reflecting (or ending) in the formation of linear DNA.
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zinc ii complexes of the second generation quinolone Antibacterial Drug enrofloxacin structure and dna or albumin interaction
Bioorganic & Medicinal Chemistry, 2010Co-Authors: Alketa Tarushi, George Psomas, Catherine P. Raptopoulou, Vassilis Psycharis, Aris Terzis, Dimitris P KessissoglouAbstract:Zinc mononuclear complexes with the second-generation quinolone Antibacterial Drug enrofloxacin in the absence or presence of a nitrogen donor heterocyclic ligand 1,10-phenanthroline or 2,2′-bipyridine have been synthesized and characterized. Enrofloxacin is on deprotonated mode acting as a bidentate ligand coordinated to zinc ion through the ketone and a carboxylato oxygen atoms. The crystal structure of bis(enrofloxacinato)(1,10-phenanthroline)zinc(II), 2, has been determined by X-ray crystallography. The biological activity of the complexes has been evaluated by examining their ability to bind to calf-thymus DNA (CT DNA) with UV and fluorescence spectroscopies. UV studies of the interaction of the complexes with DNA have shown that they can bind to CT DNA and the DNA binding constants have been calculated. Competitive studies with ethidium bromide (EB) have shown that the complexes exhibit the ability to displace the DNA-bound EB indicating that they bind to DNA in strong competition with EB for the intercalative binding site. The complexes exhibit good binding propensity to human and bovine serum albumin proteins having relatively high binding constant values.
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zinc complexes of the Antibacterial Drug oxolinic acid structure and dna binding properties
Journal of Inorganic Biochemistry, 2009Co-Authors: Alketa Tarushi, George Psomas, Catherine P. Raptopoulou, Dimitris P KessissoglouAbstract:The neutral mononuclear zinc complexes with the quinolone Antibacterial Drug oxolinic acid in the absence or presence of a nitrogen donor heterocyclic ligand 2,2′-bipyridine or 1,10-phenanthroline have been synthesized and characterized. The experimental data suggest that oxolinic acid is on deprotonated mode acting as a bidentate ligand coordinated to the metal ion through the ketone and one carboxylato oxygen atoms. The crystal structures of (chloro)(oxolinato)(2,2′-bipyridine)zinc(II), 2, and bis(oxolinato)(1,10-phenanthroline)zinc(II), 3, have been determined with X-ray crystallography. The biological activity of the complexes has been evaluated by examining their ability to bind to calf-thymus DNA (CT DNA) with UV and fluorescence spectroscopies. UV studies of the interaction of the complexes with DNA have shown that they can bind to CT DNA and the DNA-binding constants have been calculated. Competitive studies with ethidium bromide (EB) have shown that complex 3 exhibits the ability to displace the DNA-bound EB indicating that it binds to DNA in strong competition with EB.
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synthesis characterization Antibacterial activity and interaction with dna of the vanadyl enrofloxacin complex
Bioorganic & Medicinal Chemistry Letters, 2007Co-Authors: Eleni K Efthimiadou, Nikos Katsaros, Alexandra Karaliota, George PsomasAbstract:The neutral mononuclear vanadyl complex with the quinolone Antibacterial Drug enrofloxacin has been prepared and characterized with physicochemical and spectroscopic techniques and molecular mechanics calculations. The interaction of the complex with calf-thymus DNA has also been investigated and the antimicrobial activity has been evaluated against three different microorganisms.
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structure and biological properties of the copper ii complex with the quinolone Antibacterial Drug n propyl norfloxacin and 2 2 bipyridine
Journal of Inorganic Biochemistry, 2007Co-Authors: Eleni K Efthimiadou, Catherine P. Raptopoulou, Hellinida Thomadaki, Yiannis Sanakis, Nikos Katsaros, Andreas Scorilas, Alexandra Karaliota, George PsomasAbstract:Abstract The neutral mononuclear copper complex with the quinolone Antibacterial Drug N -propyl-protected norfloxacin, Hpr-norfloxacin, in the presence of the nitrogen donor heterocyclic ligand 2,2′-bipyridine has been prepared and characterized. The crystal structure of (chloro)(2,2′-bipyridine)(pr-norfloxacinato)copper(II), 1 , has been determined and refined with X-ray crystallography. X-band electron paramagnetic resonance (=EPR) spectroscopy at liquid helium temperatures from powdered samples indicates the presence of dimeric units in consistency with the crystal structure. In aqueous solutions of 1 the EPR behavior indicates mixture of dimeric and monomeric species. The antimicrobial activity of the complex has been tested on three different microorganisms and the best inhibition (MIC = 0.25 μg mL −1 ) has been exhibited against Escherichia coli . The study of the interaction of the complex with calf-thymus DNA has been performed with diverse spectroscopic techniques and has shown that complex 1 is bound to calf-thymus DNA by the intercalative mode. Potential anticancer cytostatic and cytotoxic effects of complex 1 on human promyelocytic leukemia HL-60 and human chronic myelogenous leukemia K562 cell lines have been investigated. Complex 1 shows an increased antiproliferative and necrotic effect on both HL-60 and K562 human leukemia cells in comparison to the free pr-norfloxacin.
Matylda Zietek - One of the best experts on this subject based on the ideXlab platform.
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Species-specific activity of Antibacterial Drug combinations
Nature, 2018Co-Authors: Ana Rita Brochado, Anja Telzerow, Jacob Bobonis, Joel Selkrig, Emily Huth, Stefan Bassler, Jordi Zamarreño Beas, Manuel Banzhaf, André Mateus, Matylda ZietekAbstract:Screening pairwise combinations of antibiotics and other Drugs against three bacterial pathogens reveals that antagonistic and synergistic Drug–Drug interactions are specific to microbial species and strains. The spread of antimicrobial resistance has become a serious public health concern, making once-treatable diseases deadly again and undermining the achievements of modern medicine^ 1 , 2 . Drug combinations can help to fight multi-Drug-resistant bacterial infections, yet they are largely unexplored and rarely used in clinics. Here we profile almost 3,000 dose-resolved combinations of antibiotics, human-targeted Drugs and food additives in six strains from three Gram-negative pathogens— Escherichia coli , Salmonella enterica serovar Typhimurium and Pseudomonas aeruginosa —to identify general principles for Antibacterial Drug combinations and understand their potential. Despite the phylogenetic relatedness of the three species, more than 70% of the Drug–Drug interactions that we detected are species-specific and 20% display strain specificity, revealing a large potential for narrow-spectrum therapies. Overall, antagonisms are more common than synergies and occur almost exclusively between Drugs that target different cellular processes, whereas synergies are more conserved and are enriched in Drugs that target the same process. We provide mechanistic insights into this dichotomy and further dissect the interactions of the food additive vanillin. Finally, we demonstrate that several synergies are effective against multi-Drug-resistant clinical isolates in vitro and during infections of the larvae of the greater wax moth Galleria mellonella , with one reverting resistance to the last-resort antibiotic colistin.
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Species-specific activity of Antibacterial Drug combinations
Nature, 2018Co-Authors: Ana Rita Brochado, Anja Telzerow, Jacob Bobonis, Joel Selkrig, Emily Huth, Stefan Bassler, Jordi Zamarreño Beas, Manuel Banzhaf, André Mateus, Matylda ZietekAbstract:The spread of antimicrobial resistance has become a serious public health concern, making once treatable diseases deadly again and undermining breakthrough achievements of modern medicine 1,2. Drug combinations can aid in fighting multi-Drug resistant (MDR) bacterial infections, yet, are largely unexplored and rarely used in clinics. To identify general principles for Antibacterial Drug combinations and understand their potential, we profiled ~3,000 dose-resolved combinations of antibiotics, human-targeted Drugs and food additives in 6 strains from three Gram-negative pathogens, Escherichia coli, Salmonella Typhimurium and Pseudomonas aeruginosa. Despite their phylogenetic relatedness, more than 70% of the detected Drug-Drug interactions are species-specific and 20% display strain specificity, revealing a large potential for narrow-spectrum therapies. Overall, antagonisms are more common than synergies and occur almost exclusively between Drugs targeting different cellular processes, whereas synergies are more conserved and enriched in Drugs targeting the same process. We elucidate mechanisms underlying this dichotomy and further use our resource to dissect the interactions of the food additive, vanillin. Finally, we demonstrate that several synergies are effective against MDR clinical isolates in vitro and during Galleria mellonella infections with one reverting resistance to the last-resort antibiotic, colistin.
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Species-specific activity of Antibacterial Drug combinations
Nature, 2018Co-Authors: Ana Rita Brochado, Anja Telzerow, Jacob Bobonis, Joel Selkrig, Emily Huth, Stefan Bassler, Jordi Zamarreño Beas, Artur Mateus, Manuel Banzhaf, Matylda ZietekAbstract:The spread of antimicrobial resistance has become a serious public health concern, making once-treatable diseases deadly again and undermining the achievements of modern medicine1,2. Drug combinations can help to fight multi-Drug-resistant bacterial infections, yet they are largely unexplored and rarely used in clinics. Here we profile almost 3,000 dose-resolved combinations of antibiotics, human-targeted Drugs and food additives in six strains from three Gram-negative pathogens—Escherichia coli, Salmonella enterica serovar Typhimurium and Pseudomonas aeruginosa—to identify general principles for Antibacterial Drug combinations and understand their potential. Despite the phylogenetic relatedness of the three species, more than 70% of the Drug–Drug interactions that we detected are species-specific and 20% display strain specificity, revealing a large potential for narrow-spectrum therapies. Overall, antagonisms are more common than synergies and occur almost exclusively between Drugs that target different cellular processes, whereas synergies are more conserved and are enriched in Drugs that target the same process. We provide mechanistic insights into this dichotomy and further dissect the interactions of the food additive vanillin. Finally, we demonstrate that several synergies are effective against multi-Drug-resistant clinical isolates in vitro and during infections of the larvae of the greater wax moth Galleria mellonella, with one reverting resistance to the last-resort antibiotic colistin.
K Balasubramanian - One of the best experts on this subject based on the ideXlab platform.
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polyacrylonitrile syzygium aromaticum hierarchical hydrophilic nanocomposite as a carrier for Antibacterial Drug delivery systems
RSC Advances, 2015Co-Authors: Ramdayal Yadav, K BalasubramanianAbstract:Correction for ‘Polyacrylonitrile/Syzygium aromaticum hierarchical hydrophilic nanocomposite as a carrier for Antibacterial Drug delivery systems’ by Ramdayal Yadav et al., RSC Adv., 2015, 5, 3291–3298.
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Polyacrylonitrile/Syzygium aromaticum hierarchical hydrophilic nanocomposite as a carrier for Antibacterial Drug delivery systems
RSC Advances, 2014Co-Authors: Ramdayal Yadav, K BalasubramanianAbstract:Correction for ‘Polyacrylonitrile/Syzygium aromaticum hierarchical hydrophilic nanocomposite as a carrier for Antibacterial Drug delivery systems’ by Ramdayal Yadav et al., RSC Adv., 2015, 5, 3291–3298.
Ana Rita Brochado - One of the best experts on this subject based on the ideXlab platform.
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Species-specific activity of Antibacterial Drug combinations
Nature, 2018Co-Authors: Ana Rita Brochado, Anja Telzerow, Jacob Bobonis, Joel Selkrig, Emily Huth, Stefan Bassler, Jordi Zamarreño Beas, Manuel Banzhaf, André Mateus, Matylda ZietekAbstract:Screening pairwise combinations of antibiotics and other Drugs against three bacterial pathogens reveals that antagonistic and synergistic Drug–Drug interactions are specific to microbial species and strains. The spread of antimicrobial resistance has become a serious public health concern, making once-treatable diseases deadly again and undermining the achievements of modern medicine^ 1 , 2 . Drug combinations can help to fight multi-Drug-resistant bacterial infections, yet they are largely unexplored and rarely used in clinics. Here we profile almost 3,000 dose-resolved combinations of antibiotics, human-targeted Drugs and food additives in six strains from three Gram-negative pathogens— Escherichia coli , Salmonella enterica serovar Typhimurium and Pseudomonas aeruginosa —to identify general principles for Antibacterial Drug combinations and understand their potential. Despite the phylogenetic relatedness of the three species, more than 70% of the Drug–Drug interactions that we detected are species-specific and 20% display strain specificity, revealing a large potential for narrow-spectrum therapies. Overall, antagonisms are more common than synergies and occur almost exclusively between Drugs that target different cellular processes, whereas synergies are more conserved and are enriched in Drugs that target the same process. We provide mechanistic insights into this dichotomy and further dissect the interactions of the food additive vanillin. Finally, we demonstrate that several synergies are effective against multi-Drug-resistant clinical isolates in vitro and during infections of the larvae of the greater wax moth Galleria mellonella , with one reverting resistance to the last-resort antibiotic colistin.
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Species-specific activity of Antibacterial Drug combinations
Nature, 2018Co-Authors: Ana Rita Brochado, Anja Telzerow, Jacob Bobonis, Joel Selkrig, Emily Huth, Stefan Bassler, Jordi Zamarreño Beas, Manuel Banzhaf, André Mateus, Matylda ZietekAbstract:The spread of antimicrobial resistance has become a serious public health concern, making once treatable diseases deadly again and undermining breakthrough achievements of modern medicine 1,2. Drug combinations can aid in fighting multi-Drug resistant (MDR) bacterial infections, yet, are largely unexplored and rarely used in clinics. To identify general principles for Antibacterial Drug combinations and understand their potential, we profiled ~3,000 dose-resolved combinations of antibiotics, human-targeted Drugs and food additives in 6 strains from three Gram-negative pathogens, Escherichia coli, Salmonella Typhimurium and Pseudomonas aeruginosa. Despite their phylogenetic relatedness, more than 70% of the detected Drug-Drug interactions are species-specific and 20% display strain specificity, revealing a large potential for narrow-spectrum therapies. Overall, antagonisms are more common than synergies and occur almost exclusively between Drugs targeting different cellular processes, whereas synergies are more conserved and enriched in Drugs targeting the same process. We elucidate mechanisms underlying this dichotomy and further use our resource to dissect the interactions of the food additive, vanillin. Finally, we demonstrate that several synergies are effective against MDR clinical isolates in vitro and during Galleria mellonella infections with one reverting resistance to the last-resort antibiotic, colistin.
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Species-specific activity of Antibacterial Drug combinations
Nature, 2018Co-Authors: Ana Rita Brochado, Anja Telzerow, Jacob Bobonis, Joel Selkrig, Emily Huth, Stefan Bassler, Jordi Zamarreño Beas, Artur Mateus, Manuel Banzhaf, Matylda ZietekAbstract:The spread of antimicrobial resistance has become a serious public health concern, making once-treatable diseases deadly again and undermining the achievements of modern medicine1,2. Drug combinations can help to fight multi-Drug-resistant bacterial infections, yet they are largely unexplored and rarely used in clinics. Here we profile almost 3,000 dose-resolved combinations of antibiotics, human-targeted Drugs and food additives in six strains from three Gram-negative pathogens—Escherichia coli, Salmonella enterica serovar Typhimurium and Pseudomonas aeruginosa—to identify general principles for Antibacterial Drug combinations and understand their potential. Despite the phylogenetic relatedness of the three species, more than 70% of the Drug–Drug interactions that we detected are species-specific and 20% display strain specificity, revealing a large potential for narrow-spectrum therapies. Overall, antagonisms are more common than synergies and occur almost exclusively between Drugs that target different cellular processes, whereas synergies are more conserved and are enriched in Drugs that target the same process. We provide mechanistic insights into this dichotomy and further dissect the interactions of the food additive vanillin. Finally, we demonstrate that several synergies are effective against multi-Drug-resistant clinical isolates in vitro and during infections of the larvae of the greater wax moth Galleria mellonella, with one reverting resistance to the last-resort antibiotic colistin.
Dimitris P Kessissoglou - One of the best experts on this subject based on the ideXlab platform.
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zinc ii complexes with the quinolone Antibacterial Drug flumequine structure dna and albumin binding
New Journal of Chemistry, 2013Co-Authors: Alketa Tarushi, Jakob Kljun, Iztok Turel, George Psomas, Anastasia A. Pantazaki, Dimitris P KessissoglouAbstract:The interaction of Zn(II) with the quinolone Antibacterial Drug flumequine (Hflmq) in the presence or absence of an N,N′-donor heterocyclic ligand, 2,2′-bipyridine (bipy), is being investigated. Interaction of equimolar quantities of ZnCl2 with flumequine and 2,2′-bipyridine results in the formation of a structurally characterized [Zn(flmq)(bipy)Cl] (2) complex, while excess of flumequine leads to a structurally characterized [Zn(flmq)2(bipy)] (3) compound. The reaction of ZnCl2 with flumequine in the absence of 2,2′-bipyridine leads to formation of complex [Zn(flmq)2(H2O)2] (1). In all these complexes, the deprotonated bidentate flumequinato ligands are coordinated to zinc ions through pyridone and carboxylato oxygens. The complexes exhibit good binding propensity to human or bovine serum albumin protein having relatively high binding constant values. UV study of interaction of the complexes with calf-thymus DNA (CT DNA) has shown that they bind to CT DNA and [Zn(flmq)(bipy)Cl] exhibits the highest binding constant. A competitive study with ethidium bromide (EB) has shown that the complexes can displace DNA-bound EB, indicating that they bind to DNA in strong competition with EB. The complexes bind to CT DNA in an intercalative binding mode which has also been verified by DNA solution viscosity measurements. DNA electrophoretic mobility experiments showed that all complexes bind to pDNA possibly in an intercalative manner resulting in catenanes formation as well as in double-stranded cleavage reflecting (or ending) in the formation of linear DNA.
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zinc ii complexes of the second generation quinolone Antibacterial Drug enrofloxacin structure and dna or albumin interaction
Bioorganic & Medicinal Chemistry, 2010Co-Authors: Alketa Tarushi, George Psomas, Catherine P. Raptopoulou, Vassilis Psycharis, Aris Terzis, Dimitris P KessissoglouAbstract:Zinc mononuclear complexes with the second-generation quinolone Antibacterial Drug enrofloxacin in the absence or presence of a nitrogen donor heterocyclic ligand 1,10-phenanthroline or 2,2′-bipyridine have been synthesized and characterized. Enrofloxacin is on deprotonated mode acting as a bidentate ligand coordinated to zinc ion through the ketone and a carboxylato oxygen atoms. The crystal structure of bis(enrofloxacinato)(1,10-phenanthroline)zinc(II), 2, has been determined by X-ray crystallography. The biological activity of the complexes has been evaluated by examining their ability to bind to calf-thymus DNA (CT DNA) with UV and fluorescence spectroscopies. UV studies of the interaction of the complexes with DNA have shown that they can bind to CT DNA and the DNA binding constants have been calculated. Competitive studies with ethidium bromide (EB) have shown that the complexes exhibit the ability to displace the DNA-bound EB indicating that they bind to DNA in strong competition with EB for the intercalative binding site. The complexes exhibit good binding propensity to human and bovine serum albumin proteins having relatively high binding constant values.
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zinc complexes of the Antibacterial Drug oxolinic acid structure and dna binding properties
Journal of Inorganic Biochemistry, 2009Co-Authors: Alketa Tarushi, George Psomas, Catherine P. Raptopoulou, Dimitris P KessissoglouAbstract:The neutral mononuclear zinc complexes with the quinolone Antibacterial Drug oxolinic acid in the absence or presence of a nitrogen donor heterocyclic ligand 2,2′-bipyridine or 1,10-phenanthroline have been synthesized and characterized. The experimental data suggest that oxolinic acid is on deprotonated mode acting as a bidentate ligand coordinated to the metal ion through the ketone and one carboxylato oxygen atoms. The crystal structures of (chloro)(oxolinato)(2,2′-bipyridine)zinc(II), 2, and bis(oxolinato)(1,10-phenanthroline)zinc(II), 3, have been determined with X-ray crystallography. The biological activity of the complexes has been evaluated by examining their ability to bind to calf-thymus DNA (CT DNA) with UV and fluorescence spectroscopies. UV studies of the interaction of the complexes with DNA have shown that they can bind to CT DNA and the DNA-binding constants have been calculated. Competitive studies with ethidium bromide (EB) have shown that complex 3 exhibits the ability to displace the DNA-bound EB indicating that it binds to DNA in strong competition with EB.
