Targeting bacterial efflux pump effectively enhances the efficacy of Ru-based antibacterial agents against Gram-negative pathogen.

The rise of antibiotic resistance has posed a great threat to human's life, thus develop novel antibacterial agents is urgently needed. It worthies to noted that Ru-based antibacterial agents often showed robust potency against Gram-positive pathogens, disrupted bacterial membrane and avoided bacterial resistance, making they promising antibiotic candidates. However, they are generally less active when applied to negative pathogens.

AIE-based ruthenium complexes as photosensitizers for specifically photo-inactivate gram-positive bacteria.

The emergence of multidrug-resistant bacterial have caused severe burden for public health. Particularly, Staphylococcus aureus as one of ESKAPE pathogens have induced various infectious diseases and resulted in increasing deaths. Developing new antibacterial agents is still urgent and challenging.

Discovery of quaternized pyridine-thiazole-ruthenium complexes as potent anti-Staphylococcus aureus agents.

Quaternization of ruthenium complexes may be a promising strategy for the development of new antibiotics. In response to the increasing bacterial resistance, we integrated the quaternary amine structure into the design of ruthenium complexes and evaluated their antibacterial activity. All the ruthenium complexes showed good antibacterial activity against the tested Staphylococcus aureus (S.

Integrated Analysis of scRNA-Seq and Bulk RNA-Seq Reveals Metabolic Reprogramming of Liver Cancer and Establishes a Prognostic Risk Model.

Liver cancer manifests as a profoundly heterogeneous malignancy, posing significant challenges in terms of both therapeutic intervention and prognostic evaluation. Given that the liver is the largest metabolic organ, a prognostic risk model grounded in single-cell transcriptome analysis and a metabolic perspective can facilitate precise prevention and treatment strategies for liver cancer. Hence, we identified 11 cell types in a scRNA-seq profile comprising 105,829 cells and found that the metabolic activity of malignant cells increased significantly.

Morpholine-modified Ru-based agents with multiple antibacterial mechanisms as metalloantibiotic candidates against infection.

Multidrug-resistant bacteria resulting from the abuse and overuse of antibiotics have become a huge crisis in global public health security. Therefore, it is urgently needed to develop new antibacterial drugs with unique mechanisms of action. As a versatile moiety, morpholine has been widely employed to enhance the potency of numerous bioactive molecules.

Evaluation of multi-target iridium(iii)-based metallodrugs in combating antimicrobial resistance and infections caused by .

The rapid emergence and spread of multidrug-resistant bacteria pose a serious challenge to human life and health, necessitating the development of novel antibacterial agents. Herein, to address this challenge, three iridium-based antibacterial agents were prepared and their antimicrobial activity were explored. Importantly, the three complexes all showed robust potency against with MIC values in the range of 1.

Design, synthesis, anti-infective potency and mechanism study of novel Ru-based complexes containing substituted adamantane as antibacterial agents.

Infections caused by Staphylococcus aureus (S. aureus) are increasing difficult to treat because this pathogen is easily resistant to antibiotics. However, the development of novel antibacterial agents with high antimicrobial activity and low frequency of resistance remains a huge challenge.

Polypyridyl ruthenium complexes with benzothiazole moiety as membrane disruptors and anti-resistance agents for Staphylococcus aureus.

Developing new antimicrobials to combat drug-resistant bacterial infections is necessary due to the increasing problem of bacterial resistance. In this study, four metallic ruthenium complexes modified with benzothiazoles were designed, synthesized and subjected to bio-evaluated. Among them, Ru-2 displayed remarkable inhibitory activity against Staphylococcus aureus (S.

DeepION: A Deep Learning-Based Low-Dimensional Representation Model of Ion Images for Mass Spectrometry Imaging.

Mass spectrometry imaging (MSI) is a high-throughput imaging technique capable of the qualitative and quantitative in situ detection of thousands of ions in biological samples. Ion image representation is a technique that produces a low-dimensional vector embedded with significant spectral and spatial information on an ion image, which further facilitates the distance-based similarity measurement for the identification of colocalized ions. However, given the low signal-to-noise ratios inherent in MSI data coupled with the scarcity of annotated data sets, achieving an effective ion image representation for each ion image remains a challenge.

Metal-ruthenium complex based on dipyridylamine group as membrane-active antibacterial agent effectively decrease the development of drug-resistance on Staphylococcus aureus.

Staphylococcus aureus (S. aureus), one of the Gram-positive bacteria, is easily to develop drug-resistance. Drug-resistant S.

Coupling a Virulence-Targeting Moiety with Ru-Based AMP Mimics Efficiently Improved Its Anti-Infective Potency and Therapeutic Index.

The surge of antibiotic resistance in calls for novel drugs that attack new targets. Developing antimicrobial peptides (AMPs) or antivirulence agents (AvAs) is a promising strategy to tackle this challenge. However, AMPs, which kill bacteria by disrupting cell membranes, suffer from low stability and high synthesis cost, while AvAs, which inhibit toxin secretion, have relatively poor bactericidal activity.

Ruthenium polypyridine complexes containing prenyl groups as antibacterial agents against Staphylococcus aureus through a membrane-disruption mechanism.

Four new ruthenium polypyridyl complexes with prenyl groups, [Ru(bpy) (MHIP)](PF ) (Ru(II)-1), [Ru(dtb) (MHIP)](PF ) (Ru(II)-2), [Ru(dmb) (MHIP)](PF ) (Ru(II)-3), and [Ru(dmob) (MHIP)](PF ) (Ru(II)-4) (bpy = 2,2'-bipyridine, dtb = 4,4'-di-tert-butyl-2,2'-bipyridine, dmb = 4,4'-dimethyl-2,2'-bipyridine, dmob = 4,4'-dimethoxy-2,2'-bipyridine, and MHIP = 2-(2,6-dimethylhepta-1,5-dien-1-yl)-1H-imidazo[4,f][1,10]phenanthroline), were synthesized and characterized. Their antibacterial activities against Staphylococcus aureus were assessed, and the minimum inhibition concentration (MIC) value of Ru(II)-2 against S. aureus was only 0.

Coumarin-modified ruthenium complexes by disrupting bacterial membrane to combat Gram-positive bacterial infection.

Antibiotic abuse has caused the generation of drug-resistant bacteria and a series of infections induced by multidrug-resistant bacteria have become a threat to human health. Facing the failure of traditional antibiotics, antibacterial drugs with new molecular and action modes urgently need to be developed. In this study, ruthenium complexes containing coumarin were designed and synthesized.

Synthesis and biological evaluation of ruthenium complexes bearing the 1,2,4-triazole group as potential membrane-targeting antibacterial agents towards .

Bacterial infection is one of the most serious public health problems, being harmful to human health and expensive. Nowadays, the misuse and overuse of antibiotics have led to the emergence of drug resistance. Therefore, it is an urgent need to develop new antimicrobial agents to address the current situation.

Multi-target antibacterial mechanism of ruthenium polypyridine complexes with anthraquinone groups against .

Three new Ru(ii) complexes, [Ru(dtb)PPAD](PF) (), [Ru(dmob)PPAD](PF) () and [Ru(bpy)PPAD](PF) () (dtb = 4,4'-di-butyl-2,2'-bipyridine, dmob = 4,4'-dimethyl-2,2'-bipyridine, bpy = 2,2'-bipyridine and PPAD = 2-(pyridine-3-yl)-1-imidazo[4,5][1.10]phenanthracene-9,10-dione), were synthesized and characterized by H NMR and C NMR spectroscopy, HRMS and HPLC. Among them, showed excellent antimicrobial activity against Gram-positive bacteria (minimum inhibitory concentration (MIC) = 1 μg mL) and low hemolytic and cytotoxic activity.

Synthesis and biological evaluation of ruthenium complexes containing phenylseleny against Gram-positive bacterial infection by damage membrane integrity and avoid drug-resistance.

Compounds modified with selenium atom as potential antibacterial agents have been exploited to combat the nondrug-resistant bacterial infection. In this study, we designed and synthesized four ruthenium complexes retouching of selenium-ether. Fortunately, those four ruthenium complexes shown excellent antibacterial bioactive (MIC: 1.

Ruthenium polypyridine complexes with triphenylamine groups as antibacterial agents against with membrane-disruptive mechanism.

Due to the emergence and wide spread of methicillin-resistant , the treatment of this kind of infection becomes more and more difficult. To solve the problem of drug resistance, it is urgent to develop new antibiotics to avoid the most serious situation of no drug available. Three new Ru complexes [Ru (dmob)PMA] (PF6) () [Ru (bpy)PMA] (PF6) () and [Ru (dmb)PMA] (PF6) () (dmob = 4,4'-dimethoxy-2,2'-bipyridine, bpy = 2,2'-bipyridine, dmb = 4,4'-dimethyl-2,2'-bipyridine and PMA = N-(4-(1H-imidazo [4,5-f] [1,10] phenanthrolin-2-yl) -4-methyl-N-(p-tolyl) aniline) were synthesized and characterized by 1H NMR, 13C NMR and HRMS.

The synthesis and antibacterial activity study of ruthenium-based metallodrugs with a membrane-disruptive mechanism against .

The wide spread of drug-resistant bacteria, especially methicillin-resistant (MRSA), poses a tremendous threat to global health. Of particular concern, resistance to vancomycin, linezolid, and daptomycin has already been reported in clinical MRSA strains. New antibacterial agents are urgently needed to overcome this crisis.

Synthesis of ruthenium polypyridine complexes with benzyloxyl groups and their antibacterial activities against Staphylococcus aureus.

Four new ruthenium polypyridyl complexes, [Ru(bpy)(BPIP)](PF) (Ru(II)-1), [Ru(dtb)(BPIP)](PF) (Ru(II)-2), [Ru(dmb)(BPIP)](PF) (Ru(II)-3) and [Ru(dmob)(BPIP)](PF) (Ru(II)-4) (bpy = 2,2'-bipyridine, dtb = 4,4'-di-tert-butyl-2,2'-bipyridine, dmb = 4,4'-dimethyl-2,2'-bipyridine, dmob = 4,4'-dimethoxy-2,2'-bipyridine and BPIP = 2-(3,5-bis(benzyloxyl)phenyl)-1H-imidazo[4,5-f][1,10]phenanthroline) had been synthesized and characterized. Their antimicrobial activities were investigated against Staphylococcus aureus (S. aureus) and four complexes showed obvious antibacterial effect, especially the minimum inhibition concentration (MIC) value of Ru(II)-3 was only 4 μg/mL.

Design, synthesis, and evaluation of aryl-thioether ruthenium polypyridine complexes: A multi-target antimicrobial agents against gram-positive bacteria.

With the increase in bacterial resistance, new antimicrobial agents are urgently need for developing to combat multidrug-resistant pathogens and with low cytotoxicity. In this study, four new ruthenium polypyridine complexes bearing 4-tBu-phenyl sulfide Ru(bpy)(TBPIP)](PF)(Ru(Ⅱ)-1), Ru(dmb)(TBPIP)](PF)(Ru(Ⅱ)-2), Ru(dmob)(TBPIP)](PF)(Ru(Ⅱ)-3) and Ru(dtb)(TBPIP)](PF)(Ru(Ⅱ)-4) were designed, synthesized and evaluated. Those ruthenium complexes showed strong activity against Staphylococcus aureus (S.

Ruthenium(II) complexes targeting membrane as biofilm disruptors and resistance breakers in Staphylococcus aureus bacteria.

The development of ruthenium-based complexes or antimicrobial peptides are identified as a promising strategy for combating drug-resistant bacteria. In this work, four biphenyl-based antibacterial ruthenium complexes by targeting membrane integrity, which act as antimicrobial peptides mimics, were designed and synthesized. In vitro antimicrobial screening demonstrated that four complexes could absolutely inhibit the growth of Staphylococcus aureus (S.

Regulation of DNA-binding activity of the Staphylococcus aureus catabolite control protein A by copper (II)-mediated oxidation.

Catabolite control protein A (CcpA) of the human pathogen Staphylococcus aureus is an essential DNA regulator for carbon catabolite repression and virulence, which facilitates bacterial survival and adaptation to a changing environment. Here, we report that copper (II) signaling mediates the DNA-binding capability of CcpA in vitro and in vivo. Copper (II) catalyzes the oxidation of two cysteine residues (Cys216 and Cys242) in CcpA to form intermolecular disulfide bonds between two CcpA dimers, which results in the formation and dissociation of a CcpA tetramer of CcpA from its cognate DNA promoter.

Synthesis and biological evaluation of ruthenium polypyridine complexes with 18β-glycyrrhetinic acid as antibacterial agents against .

Four new ruthenium(II) polypyridine complexes bearing 18β-glycyrrhetinic acid derivatives, [Ru(bpy)L](PF) (Ru1), [Ru(dmb)L](PF) (Ru2), [Ru(dtb)L](PF) (Ru3) and [Ru(phen)L](PF) (Ru4) (bpy = 2,2-bipyridine, dmb = 4,4'-dimethyl-2,2'-bipyridine, dtb = 4,4'-di--butyl-2,2'-bipyridine, phen = 1,10-phenanthroline and L is the GA modified new ligand) were designed and synthesized. Their antimicrobial activities against () were evaluated and all complexes showed an obvious inhibitory effect, especially, the minimum inhibitory concentration (MIC) value of Ru2 was 3.9 μg mL.

Identification of ruthenium (II) complexes with furan-substituted ligands as possible antibacterial agents against Staphylococcus aureus.

The growing burden of antibiotic resistance worldwide calls for developing new classes of antimicrobial strategy. Recently years, the use of adjuvants that rescue antibiotics identified as a promising strategy for overcoming bacterial resistance. In this study, three ruthenium complexes functionalized with furan-substituted ligands([Ru(phen) (CAPIP)](ClO ) (Ru(Ⅱ)-1), [Ru(dmp) (CAPIP)](ClO ) (Ru(Ⅱ)-2) and [Ru(dmb) (CAPIP)](ClO ) (Ru(Ⅱ)-3) (dmb=4,4'-dimethyl-2,2'-bipyridine, phen=1,10-phenanthroline, dmp=2,9-dimethyl-1,10-phenanthroline, CAPIP=(E)-2- (2-(furan-2-yl)vinyl)-1H-imidazo[4,5-f][1,10]phenanthroline)) were designed and synthesized.

Synthesis of ruthenium complexes functionalized with benzothiophene and their antibacterial activity against Staphylococcus aureus.

New effective antimicrobial agents with novel modes of action are urgently needed due to the continued emergence of drug-resistant bacteria. Here, three ruthenium complexes functionalized with benzothiophene: [Ru(phen)(BTPIP)](ClO) (Ru(II)-1), [Ru(dmp)(BTPIP)](ClO) (Ru(II)-2) and [Ru(dmb)(BTPIP)](ClO) (Ru(II)-3) (dmb = 4,4'-dimethyl-2,2'-bipyridine, phen = 1,10-phenanthroline, dmp = 2,9-dimethyl-1,10-phenanthroline) have been synthesized and their antimicrobial activities in vitro were assessed. Minimum inhibitory concentration (MIC) assays indicated that the three Ru(II)-1, Ru(II)-2 and Ru(II)-3 complexes all showed antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa.