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  1. Article ; Online: Coagulation factors: a novel class of endogenous host antimicrobial proteins against drug-resistant gram-negative bacteria.

    Li, Congran / You, Xuefu

    Signal transduction and targeted therapy

    2019  Volume 4, Page(s) 46

    Language English
    Publishing date 2019-11-08
    Publishing country England
    Document type Journal Article
    ZDB-ID 2886872-9
    ISSN 2059-3635 ; 2095-9907
    ISSN (online) 2059-3635
    ISSN 2095-9907
    DOI 10.1038/s41392-019-0083-4
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Deletion of the

    Lu, Yun / Chen, Hongtong / Shao, Zhiyuan / Sun, Lang / Li, Congran / Lu, Yu / You, Xuefu / Yang, Xinyi

    Frontiers in microbiology

    2024  Volume 15, Page(s) 1301204

    Abstract: Introduction: Mycobacterium tuberculosis: Methods: In our study, to discover the function and targetability of CYP138, a : Results and discussion: The knockout ... ...

    Abstract Introduction: Mycobacterium tuberculosis
    Methods: In our study, to discover the function and targetability of CYP138, a
    Results and discussion: The knockout of
    Language English
    Publishing date 2024-03-25
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2587354-4
    ISSN 1664-302X
    ISSN 1664-302X
    DOI 10.3389/fmicb.2024.1301204
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Discovery of Gambogic acid as an antibacterial adjuvant against vancomycin-resistant enterococci in vitro and in vivo.

    Pang, Jing / Guo, Xixi / Zhang, Zhimeng / Guo, Wei / Yuan, Min / Li, Zhenjun / Lu, Xi / Wang, Yanxiang / You, Xuefu

    Phytomedicine : international journal of phytotherapy and phytopharmacology

    2024  Volume 128, Page(s) 155400

    Abstract: Background: The emergence and spread of vancomycin-resistant enterococci (VRE) have posed a significant challenge to clinical treatment, underscoring the need to develop novel strategies. As therapeutic options for VRE are limited, discovering ... ...

    Abstract Background: The emergence and spread of vancomycin-resistant enterococci (VRE) have posed a significant challenge to clinical treatment, underscoring the need to develop novel strategies. As therapeutic options for VRE are limited, discovering vancomycin enhancer is a feasible way of combating VRE. Gambogic acid (GA) is a natural product derived from the resin of Garcinia hanburyi Hook.f. (Clusiaceae), which possesses antibacterial activity.
    Purpose: This study aimed to investigate the potential of GA as an adjuvant to restore the susceptibility of VRE to vancomycin.
    Methods: In vitro antibacterial and synergistic activities were evaluated against vancomycin-susceptible and resistant strains by the broth microdilution method for the Minimal Inhibitory Concentrations (MICs) determination, and checkerboard assay and time-kill curve analysis for synergy evaluation. In vivo study was conducted on a mouse multi-organ infection model. The underlying antibacterial mechanism of GA was also explored.
    Results: GA showed a potent in vitro activity against all tested strains, with MICs ranging from 2 to 4 μg/ml. The combination of GA and vancomycin exhibited a synergistic effect against 18 out of 23 tested VRE strains, with a median fractional inhibitory concentration index (FICI) of 0.254, and demonstrated a synergistic effect in the time-kill assay. The combination therapy exhibited a significant reduction in tissue bacterial load compared with either compound used alone. GA strongly binds to the ParE subunit of topoisomerase IV, a bacterial type II DNA topoisomerase, and suppresses its activity.
    Conclusions: The study suggests that GA has a significant antibacterial activity against enterococci, and sub-MIC concentrations of GA can restore the activity of vancomycin against VRE in vitro and in vivo. These findings indicate that GA has the potential to be a new antibacterial adjuvant to vancomycin in the treatment of infections caused by VRE.
    MeSH term(s) Xanthones/pharmacology ; Animals ; Microbial Sensitivity Tests ; Vancomycin-Resistant Enterococci/drug effects ; Anti-Bacterial Agents/pharmacology ; Vancomycin/pharmacology ; Drug Synergism ; Mice ; Garcinia/chemistry ; Female ; Gram-Positive Bacterial Infections/drug therapy
    Chemical Substances Xanthones ; gambogic acid (8N585K83U2) ; Anti-Bacterial Agents ; Vancomycin (6Q205EH1VU)
    Language English
    Publishing date 2024-02-01
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 1205240-1
    ISSN 1618-095X ; 0944-7113
    ISSN (online) 1618-095X
    ISSN 0944-7113
    DOI 10.1016/j.phymed.2024.155400
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Isolation, Structure Elucidation, and First Total Synthesis of Quinomycins K and L, Two New Octadepsipeptides from the Maowei Sea Mangrove-Derived Streptomyces sp. B475

    Lu, Qinpei / Wu, Gang / Hao, Xiaomeng / Hu, Xinxin / Cai, Hao / Liu, Xiujun / You, Xuefu / Guo, Hongwei / Sun, Chenghang

    Mar Drugs. 2023 Feb. 23, v. 21, no. 3

    2023  

    Abstract: Mangrove actinomycetia have been proven to be one of the promising sources for discovering novel bioactive natural products. Quinomycins K (1) and L (2), two rare quinomycin-type octadepsipeptides without intra-peptide disulfide or thioacetal bridges, ... ...

    Abstract Mangrove actinomycetia have been proven to be one of the promising sources for discovering novel bioactive natural products. Quinomycins K (1) and L (2), two rare quinomycin-type octadepsipeptides without intra-peptide disulfide or thioacetal bridges, were investigated from the Maowei Sea mangrove-derived Streptomyces sp. B475. Their chemical structures, including the absolute configurations of their amino acids, were elucidated by a combination of NMR and tandem MS analysis, electronic circular dichroism (ECD) calculation, advanced Marfey’s method, and further unequivocally confirmed by the first total synthesis. The two compounds displayed no potent antibacterial activity against 37 bacterial pathogens and had no significant cytotoxic activity against H460 lung cancer cells.
    Keywords Streptomyces ; antibacterial properties ; circular dichroism spectroscopy ; cytotoxicity ; disulfides ; lung neoplasms
    Language English
    Dates of publication 2023-0223
    Publishing place Multidisciplinary Digital Publishing Institute
    Document type Article ; Online
    ZDB-ID 2175190-0
    ISSN 1660-3397
    ISSN 1660-3397
    DOI 10.3390/md21030143
    Database NAL-Catalogue (AGRICOLA)

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  5. Article ; Online: Isolation, Structure Elucidation, and First Total Synthesis of Quinomycins K and L, Two New Octadepsipeptides from the Maowei Sea Mangrove-Derived

    Lu, Qinpei / Wu, Gang / Hao, Xiaomeng / Hu, Xinxin / Cai, Hao / Liu, Xiujun / You, Xuefu / Guo, Hongwei / Sun, Chenghang

    Marine drugs

    2023  Volume 21, Issue 3

    Abstract: Mangrove actinomycetia have been proven to be one of the promising sources for discovering novel bioactive natural products. Quinomycins K ( ...

    Abstract Mangrove actinomycetia have been proven to be one of the promising sources for discovering novel bioactive natural products. Quinomycins K (
    MeSH term(s) Streptomyces/metabolism ; Echinomycin/metabolism ; Anti-Bacterial Agents/chemistry ; Magnetic Resonance Spectroscopy ; Molecular Structure
    Chemical Substances quinomycin (11113-76-1) ; Echinomycin (512-64-1) ; Anti-Bacterial Agents
    Language English
    Publishing date 2023-02-23
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2175190-0
    ISSN 1660-3397 ; 1660-3397
    ISSN (online) 1660-3397
    ISSN 1660-3397
    DOI 10.3390/md21030143
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: The Prediction of LptA and LptC Protein-Protein Interactions and Virtual Screening for Potential Inhibitors.

    Ren, Yixin / Dong, Wenting / Li, Yan / Cao, Weiting / Xiao, Zengshuo / Zhou, Ying / Teng, Yun / You, Xuefu / Yang, Xinyi / Huang, Huoqiang / Wang, Hao

    Molecules (Basel, Switzerland)

    2024  Volume 29, Issue 8

    Abstract: Antibiotic resistance in Gram-negative bacteria remains one of the most pressing challenges to global public health. Blocking the transportation of lipopolysaccharides (LPS), a crucial component of the outer membrane of Gram-negative bacteria, is ... ...

    Abstract Antibiotic resistance in Gram-negative bacteria remains one of the most pressing challenges to global public health. Blocking the transportation of lipopolysaccharides (LPS), a crucial component of the outer membrane of Gram-negative bacteria, is considered a promising strategy for drug discovery. In the transportation process of LPS, two components of the LPS transport (Lpt) complex, LptA and LptC, are responsible for shuttling LPS across the periplasm to the outer membrane, highlighting their potential as targets for antibacterial drug development. In the current study, a protein-protein interaction (PPI) model of LptA and LptC was constructed, and a molecular screening strategy was employed to search a protein-protein interaction compound library. The screening results indicated that compound 18593 exhibits favorable binding free energy with LptA and LptC. In comparison with the molecular dynamics (MD) simulations on currently known inhibitors, compound 18593 shows more stable target binding ability at the same level. The current study suggests that compound 18593 may exhibit an inhibitory effect on the LPS transport process, making it a promising hit compound for further research.
    MeSH term(s) Anti-Bacterial Agents/pharmacology ; Anti-Bacterial Agents/chemistry ; Bacterial Proteins/antagonists & inhibitors ; Bacterial Proteins/metabolism ; Drug Discovery/methods ; Gram-Negative Bacteria/drug effects ; Lipopolysaccharides/metabolism ; Molecular Docking Simulation ; Molecular Dynamics Simulation ; Protein Binding ; Carrier Proteins/antagonists & inhibitors ; Carrier Proteins/metabolism
    Chemical Substances Anti-Bacterial Agents ; Bacterial Proteins ; Lipopolysaccharides ; Carrier Proteins
    Language English
    Publishing date 2024-04-17
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules29081827
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  7. Article ; Online: Strategies for Rapid Identification of

    Lu, Yun / Hu, Xinxin / Nie, Tongying / Yang, Xinyi / Li, Congran / You, Xuefu

    Frontiers in cellular and infection microbiology

    2021  Volume 11, Page(s) 734578

    Abstract: Acinetobacter ... ...

    Abstract Acinetobacter baumannii
    MeSH term(s) Acinetobacter baumannii ; Anti-Bacterial Agents/pharmacology ; Membrane Proteins ; Microbial Sensitivity Tests ; Polymyxin B/pharmacology ; Polymyxins ; Tandem Mass Spectrometry
    Chemical Substances Anti-Bacterial Agents ; Membrane Proteins ; Polymyxins ; Polymyxin B (J2VZ07J96K)
    Language English
    Publishing date 2021-09-21
    Publishing country Switzerland
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2619676-1
    ISSN 2235-2988 ; 2235-2988
    ISSN (online) 2235-2988
    ISSN 2235-2988
    DOI 10.3389/fcimb.2021.734578
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article: Recent Advances in Histidine Kinase-Targeted Antimicrobial Agents.

    Chen, Hongtong / Yu, Chengqi / Wu, Han / Li, Guoqing / Li, Congran / Hong, Wei / Yang, Xinyi / Wang, Hao / You, Xuefu

    Frontiers in chemistry

    2022  Volume 10, Page(s) 866392

    Abstract: The prevalence of antimicrobial-resistant pathogens significantly limited the number of effective antibiotics available clinically, which urgently requires new drug targets to screen, design, and develop novel antibacterial drugs. Two-component system ( ... ...

    Abstract The prevalence of antimicrobial-resistant pathogens significantly limited the number of effective antibiotics available clinically, which urgently requires new drug targets to screen, design, and develop novel antibacterial drugs. Two-component system (TCS), which is comprised of a histidine kinase (HK) and a response regulator (RR), is a common mechanism whereby bacteria can sense a range of stimuli and make an appropriate adaptive response. HKs as the sensor part of the bacterial TCS can regulate various processes such as growth, vitality, antibiotic resistance, and virulence, and have been considered as a promising target for antibacterial drugs. In the current review, we highlighted the structural basis and functional importance of bacterial TCS especially HKs as a target in the discovery of new antimicrobials, and summarize the latest research progress of small-molecule HK-inhibitors as potential novel antimicrobial drugs reported in the past decade.
    Language English
    Publishing date 2022-07-04
    Publishing country Switzerland
    Document type Journal Article ; Review
    ZDB-ID 2711776-5
    ISSN 2296-2646
    ISSN 2296-2646
    DOI 10.3389/fchem.2022.866392
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article: Parallel Reaction Monitoring Mass Spectrometry for Rapid and Accurate Identification of β-Lactamases Produced by

    Lu, Yun / Hu, Xinxin / Pang, Jing / Wang, Xiukun / Li, Guoqing / Li, Congran / Yang, Xinyi / You, Xuefu

    Frontiers in microbiology

    2022  Volume 13, Page(s) 784628

    Abstract: The increasing spread of drug-resistant bacterial strains presents great challenges to clinical antibacterial treatment and public health, particularly with regard to β-lactamase- ... ...

    Abstract The increasing spread of drug-resistant bacterial strains presents great challenges to clinical antibacterial treatment and public health, particularly with regard to β-lactamase-producing
    Language English
    Publishing date 2022-06-20
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2587354-4
    ISSN 1664-302X
    ISSN 1664-302X
    DOI 10.3389/fmicb.2022.784628
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article ; Online: A Novel Tigecycline Adjuvant ML-7 Reverses the Susceptibility of Tigecycline-Resistant

    Sun, Lilan / Sun, Lang / Li, Xue / Hu, Xinxin / Wang, Xiukun / Nie, Tongying / Zhang, Youwen / You, Xuefu

    Frontiers in cellular and infection microbiology

    2022  Volume 11, Page(s) 809542

    Abstract: The increasing incidence of tigecycline resistance undoubtedly constitutes a serious threat to global public health. The combination therapies had become the indispensable strategy against this threat. Herein, 11 clinical tigecycline- ... ...

    Abstract The increasing incidence of tigecycline resistance undoubtedly constitutes a serious threat to global public health. The combination therapies had become the indispensable strategy against this threat. Herein, 11 clinical tigecycline-resistant
    MeSH term(s) Anti-Bacterial Agents/pharmacology ; Anti-Bacterial Agents/therapeutic use ; Azepines ; Drug Resistance, Bacterial ; Humans ; Klebsiella Infections/drug therapy ; Klebsiella pneumoniae ; Microbial Sensitivity Tests ; Minocycline/pharmacology ; Naphthalenes ; Tigecycline/pharmacology
    Chemical Substances Anti-Bacterial Agents ; Azepines ; Naphthalenes ; ML 7 (109376-83-2) ; Tigecycline (70JE2N95KR) ; Minocycline (FYY3R43WGO)
    Language English
    Publishing date 2022-01-05
    Publishing country Switzerland
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2619676-1
    ISSN 2235-2988 ; 2235-2988
    ISSN (online) 2235-2988
    ISSN 2235-2988
    DOI 10.3389/fcimb.2021.809542
    Database MEDical Literature Analysis and Retrieval System OnLINE

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