BIOMACROMOLECULES
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2014
·
IF 5.788
Xin Yang,Kan Hu,Guantai Hu,Danyao Shi,Yunjiang Jiang,Liwei Hui,Rui Zhu,Yuntao Xie,Lihua Yang
We show that simply converting the hydrophobic moiety of an antimicrobial peptide (AMP) or synthetic mimic of AMPs (SMAMP) into a hydrophilic one could be a different pathway toward membrane-active antimicrobials preferentially acting against bacteria over host cells. Our biostatistical analysis on natural AMPs indicated that shorter AMPs tend to be more hydrophobic, and the hydrophilic-and-cationic mutants of a long AMP experimentally demonstrated certain membrane activity against bacteria. To isolate the effects of antimicrobials’ hydrophobicity and systematically examine whether hydrophilic-and-cationic mutants could inherit the membrane activity of their parent AMPs/SMAMPs, we constructed a minimal prototypical system based on methacrylate-based polymer SMAMPs and compared the antibacterial membrane activity and hemolytic toxicity of analogues with and without the hydrophobic moiety. Antibacterial assays showed that the hydrophobic moiety of polymer SMAMPs consistently promoted the antibacterial activity but diminished in effectiveness for long polymers, and the resultant long hydrophilic-and-cationic polymers were also membrane active against bacteria. What distinguished these long mutants from their parent SMAMPs were their drastically reduced hemolytic toxicities and, as a result, strikingly enhanced selectivity. Similar toxicity reduction was observed with the hydrophilic-and-cationic mutants of long AMPs. Taken together, our results suggest that long hydrophilic-and-cationic polymers could offer preferential membrane activity against bacteria over host cells, which may have implications in future antimicrobial development.
研究领域:
微生物学
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生物化学
·
药物开发
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产品关联
DOI
PubMed
高影响因子
Microbiology Spectrum
·
2022
·Vol. 10
·期 5
·
IF 9.043
Wen Wang,Xuerui Bao,Mona Bové,Petra Rigole,Xiaofeng Meng,Jianyu Su,Tom Coenye
Phytochemicals are promising antibacterials for the development of novel antibiofilm drugs, but their antibiofilm activity in physiologically relevant model systems is poorly characterized. As the host microenvironment can interfere with the activity of the phytochemicals, mimicking the complex environment found in biofilm associated infections is essential to predict the clinical potential of novel phytochemical-based antimicrobials. In the present study, we examined the antibiofilm activity of borneol, citral, and combinations of both as well as their Pickering emulsions against Staphylococcus aureus and Pseudomonas aeruginosa in an in vivo-like synthetic cystic fibrosis medium (SCFM2) model, an in vitro wound model (consisting of an artificial dermis and blood components at physiological levels), and an in vivo Galleria mellonella model. The Pickering emulsions demonstrated an enhanced biofilm inhibitory activity compared to both citral and the borneol/citral combination, reducing the minimum biofilm inhibitory concentration (MBIC) values up to 2 to 4 times against P. aeruginosa PAO1 and 2 to 8 times against S. aureus P8-AE1 in SCMF2. In addition, citral, the combination borneol/citral, and their Pickering emulsions can completely eliminate the established biofilm of S. aureus P8-AE1. The effectiveness of Pickering emulsions was also demonstrated in the wound model with a reduction of up to 4.8 log units in biofilm formation by S. aureus Mu50. Furthermore, citral and Pickering emulsions exhibited a significant degree of protection against S. aureus infection in the G. mellonella model. The present findings reveal the potential of citral- or borneol/citral-based Pickering emulsions as a type of alternative antibiofilm candidate to control pathogenicity in chronic infection.IMPORTANCE There is clearly an urgent need for novel formulations with antimicrobial and antibiofilm activity, but while there are plenty of studies investigating them using simple in vitro systems, there is a lack of studies in which (combinations of) phytochemicals are evaluated in relevant models that closely resemble the in vivo situation. Here, we examined the antibiofilm activity of borneol, citral, and their combination as well as Pickering emulsions (stabilized by solid particles) of these compounds. Activity was tested against Staphylococcus aureus and Pseudomonas aeruginosa in in vitro models mimicking cystic fibrosis sputum and wounds as well as in an in vivo Galleria mellonella model. The Pickering emulsions showed drastically increased antibiofilm activity compared to that of the compounds as such in both in vitro models and protected G. mellonella larvae from S. aureus-induced killing. Our data show that Pickering emulsions from phytochemicals are potentially useful for treating specific biofilm-related chronic infections.
研究领域:
微生物学
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药理学
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感染病学
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DOI
高影响因子
ACS Infectious Diseases
·
2024
·
IF 4
Shu Li,Zhaopeng Wang,Shibo Song,Yuanyuan Tang,Jingjing Zhou,Xiaojing Liu,Xingjiao Zhang,Min Chang,Kairong Wang,Yali Peng
Multidrug resistance against conventional antibiotics has dramatically increased the difficulty of treatment and accelerated the need for novel antibacterial agents. The peptide Tat (47–57) is derived from the transactivating transcriptional activator of human immunodeficiency virus 1, which is well-known as a cell-penetrating peptide in mammalian cells. However, it is also reported that the Tat peptide (47–57) has antifungal activity. In this study, a series of membrane-active hydrocarbon-stapled α-helical amphiphilic peptides were synthesized and evaluated as antibacterial agents against Gram-positive and Gram-negative bacteria, including multidrug-resistant strains. The impact of hydrocarbon staple, the position of aromatic amino acid residue in the hydrophobic face, the various types of aromatic amino acids, and the hydrophobicity on bioactivity were also investigated and discussed in this study. Among those synthesized peptides, analogues P3 and P10 bearing a l-2-naphthylalanine (Φ) residue at the first position and a Tyr residue at the eighth position demonstrated the highest antimicrobial activity and negligible hemolytic toxicity. Notably, P3 and P10 showed obviously enhanced antimicrobial activity against multidrug-resistant bacteria, low drug resistance, high cell selectivity, extended half-life in plasma, and excellent performance against biofilm. The antibacterial mechanisms of P3 and P10 were also preliminarily investigated in this effort. In conclusion, P3 and P10 are promising antimicrobial alternatives for the treatment of the antimicrobial-resistance crisis.
研究领域:
微生物学
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药物化学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
APPLIED MICROBIOLOGY AND BIOTECHNOLOGY
·
2021
·Vol. 105
·期 11
·4709-4718
·
IF 4.813
Fan Qiuxia,Yuan Yahong,Jia Hang,Zeng Xuejun,Wang Zhouli,Hu Zhongqiu,Gao Zhenpeng,Yue Tianli
Abstract Shigella flexneri ( Sh. flexneri ), a common foodborne pathogen, has become one of the main threats to food safety and human health due to its high pathogenicity and persistent infection. The objective of this study was to explore the antimicrobial and anti-biofilm activities and the possible mechanism of thymoquinone (TQ) against Sh. flexneri . The minimum inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) of TQ against Sh. flexneri were 0.4 and 0.5 mg/mL, respectively. TQ showed bactericidal activity against Sh. flexneri in culture medium and milk system. Scanning electron microscopy (SEM) and confocal laser scanning microscopy (CLSM) observations demonstrated that TQ could induce abnormal cell morphology and destroy cell membrane. Sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) analysis suggested that TQ could inhibit protein synthesis in Sh. flexneri . Also, at sub-inhibitory concentrations (SICs), TQ exhibited an inhibitory effect on Sh. flexneri biofilm formation, which was confirmed by crystal violet quantitative analysis and SEM observation. Real-time quantitative PCR (RT-qPCR) analyses revealed that TQ downregulated the expression of genes involved in Sh. flexneri biofilm formation. Thus, TQ has potential as a natural antimicrobial and anti-biofilm agent to address the contamination and infection caused by Sh. flexneri . Key points • Antimicrobial and anti-biofilm activity of TQ on Shigella flexneri were investigated.
• TQ inhibited biofilm formation by Shigella flexneri.
• TQ provided a new strategy for Shigella flexneri control.
研究领域:
微生物学
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食品安全
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分子生物学
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DOI
PubMed
高影响因子
BIOLOGICAL TRACE ELEMENT RESEARCH
·
2023
·
IF 3.9
Celebı Demet,Celebı Ozgur,Aydin Elif,Baser Sumeyye,Güler Mustafa Can,Yildirim Serkan,Taghizadehghalehjoughi Ali
Multidrug-resistant bacteria is one of the most important public health problems. Increasing rates of antibacterial resistance also affect the outcomes of medical approaches. Cancer treatment because of immune system deficiency (chemotherapy or steroids usage) commonly can cause infection. Lung cancer is the dominant cause of cancer-related deaths, and infection is the most common cause of death among those patients. In this study, it was aimed to determine the antimicrobial, antibiofilm, and anticancer activity of boron compounds. A549 lung cancer cell line was infected with Acinetobacter baumannii (ATCC 19606), Klebsiella pneumoniae (ATCC 700603), and Pseudomonas aeruginosa (ATCC 27853). In order to determine the fractional inhibitory concentration (FIC) index, antibiotics and boron compound concentrations prepared according to the minimum inhibitory concentration (MIC) values were determined by the checkerboard method. In our study results, the antibiofilm activity was an average of 46% in A. baumannii +boron compounds, 45% in P. aeruginosa +boron compounds, and 43% in K. pneumoniae . Cell culture analysis results show a decrease in viability and antioxidant capacity and an increase in total oxidant status after adding boron compounds to the culture. Immunofluorescence results show a correlation with MTT, and boron compounds increased 8-OHdG expression in comparison to antibiotic administration. In conclusion, boron compounds have promising effects on bacteria, especially in resistant bacteria spp.
研究领域:
医学
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微生物学
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肿瘤学
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DOI
PubMed
高影响因子
MACROMOLECULES
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2025
·
IF 5.2
Xiangbin Sun,Yuanyuan Xie,Xiaobing Ma,Yufeng He,Pengfei Song,Rongmin Wang
Bacterial biofilm contamination poses a substantial threat to public health and safety while also leading to considerable economic losses. In this study, a series of both offensive and defensive poly(quaternary phosphonium salt-borneol) copolymers (P(QPx-BOy)), utilizing stereochemically structured borneol as the membrane breaking arrow and quaternary phosphonium salt cations as the electrostatic driving force, were successfully synthesized. Notably, this work exemplifies a novel integration of natural borneol with quaternary phosphonium cations. Subsequently, the molecular structure, molecular weight distribution, microstructure, and corresponding physicochemical properties of the P(QPx-BOy) were characterized using NMR, FT-IR, GPC, SEM, EDS, CA, and DLS. Leveraging the electrostatic interaction between the phosphonium cation and the stereochemical antibacterial mechanism of borneol, P(QPx-BOy) exhibited remarkable antibacterial efficacy against both E. coli and S. aureus, achieving a 100% antibacterial rate with MIC value as low as 30 μg/mL. Furthermore, crystal violet staining assays revealed that borneol’s unique antibiofilm mechanism exerts a significant inhibitory effect on bacterial biofilm formation. Finally, the biocompatibility and antibacterial potential of P(QPx-BOy) were evaluated through cytotoxicity assays and fabric antibacterial tests. Specifically, the integration of borneol essential oil with hydrophilic quaternary phosphonium salt cations effectively addresses the hydrophobic nature of borneol essential oil while mitigating the cytotoxic effects associated with quaternary phosphonium salts. This synergistic combination leverages the strengths of both components, thereby enhancing their suitability for applications in healthcare and public health sectors.
研究领域:
材料科学
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微生物学
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生物医学工程
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产品关联
DOI
高影响因子
MICROBIAL PATHOGENESIS
·
2024
·
IF 3.3
Kaviya Selvaraj,Lekha Sree Venkatesan,Dhanraj Ganapathy,Palanivel Sathishkumar
Biosynthesized gold nanoparticles (AuNPs) are highly attracted as a biocompatible nanodrug to treat various diseased conditions in humans. In this study, phytochemical tannic acid-mediated AuNPs (TA-AuNPs) are successfully synthesized and tested for antibacterial and antibiofilm activity against dental biofilm-forming Streptococcus mutans biofilm. The synthesized TA-AuNPs are appeared as spherical in shape with an average size of 19 nm. The antibacterial potential of TA-AuNPs was evaluated using ZOI and MIC measurements; while, antibiofilm efficacy was measured by checking the eradication of preformed biofilm on the tooth model. The ZOI and MIC values for TA-AuNPs are 25 mm in diameter and 4 μg/mL, respectively. The MTT assay, CLSM, and SEM results demonstrate that the preformed S. mutans biofilm is completely eradicated at 4xMIC (16 μg/mL) of TA-AuNPs. Finally, the present study reveals that the synthesized TA-AuNPs might be a great therapeutic drug to treat dental biofilm-forming bacterium S. mutans.
研究领域:
微生物学
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纳米医学
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口腔医学
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产品关联
DOI
PubMed
高影响因子
Polymers
·
2023
·Vol. 15
·期 16
·3462
·
IF 5
Yajie Wang,Chaoyue Zhao,Ziqi Cai,Lihong Wang,Liangxiang Zhu,Hui Huang,Guoping Zhang,Peng You,Chen Xie,Yaping Wang,Qing Bai,Tao Yang,Shunpu Li,Guangye Zhang
Organic solar cells (OSCs) have gained increasing attention. Among the various directions in OSCs, all-polymer solar cells (all-PSCs) have emerged as a highly promising and currently active research area due to their excellent film formation properties, mechanical properties, and thermal stabilities. However, most of the high-efficiency all-PSCs are processed from chloroform with an active layer thickness of ~100 nm. In order to meet the requirements for industrialization, a thicker active layer processed from low-vapor pressure solvents (preferentially a hydrocarbon solvent) is strongly desired. Herein, we employ toluene (a hydrocarbon solvent with a much higher boiling point than chloroform) and a method known as sequential processing (SqP) to mitigate the rapid decline in efficiency with increasing film thickness. We show that SqP enables a more favorable vertical phase segregation that leads to less trap-assisted recombination and enhanced charge extraction and lifetime than blend-cast devices at higher film thicknesses.Keywords:all-polymer solar cells;sequential processing;hydrocarbon solvent processing;thick-film active layer
研究领域:
材料科学
·
能源技术
✓ 已验证
DOI
PubMed
高影响因子
Frontiers in Chemistry
·
2022
·
IF 5.545
Fang Shanfang,Dang Yuan-Ye,Li Haizhou,Li Hongxia,Liu Jiayong,Zhong Rongcui,Chen Yongzhi,Liu Shouping,Lin Shuimu
Bacteria have developed increasing resistance to currently used antimicrobial agents. New classes of antimicrobial drugs are urgently required to fight drug-resistant pathogens. Here, we designed and synthesized a series of calix[4]arene derivatives as antibacterial agents by biomimicking the structural properties and biological functions of antibacterial peptides. After introducing cationic hydrophilic moieties and preliminary structural optimization, we obtained a lead compound (16) that exhibited excellent antibacterial activity against Gram-positive bacteria, low toxicity toward mammalian cells and poor hemolytic activity. The antibacterial mechanism studies showed that compound 16 can destroy bacterial cell membrane directly, leading to bacterial death and a low tendency to develop bacterial resistance.
研究领域:
微生物学
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药物化学
·
合成化学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF APPLIED MICROBIOLOGY
·
2022
·Vol. 133
·期 4
·2198-2209
·
IF 4.059
Yufang Li,Shijun Li,Kun Yang,Rongxiang Guo,Xin Zhu,Yanan Shi,Aixiang Huang
Aims Staphylococcus aureus has emerged as a serious threat to food safety owing to biofilm formation. The study aimed to examine the antibiofilm mechanism of a novel milk-derived antimicrobial peptide BCp12 against it. Methods and results Antibiofilm activity of BCp12 was studied by crystal violet staining, MTT assay, motility, SEM and CLSM. TMT proteome, real-time PCR and molecular docking in silico were conducted to evaluate the mechanism of BCp12 against S. aureus biofilm. The results showed that BCp12 had significant antibiofilm activity at 1 × MIC and sub-MIC. BCp12 induced the dispersion of structure of S. aureus biofilm BCp12 inhibited the movement of S. aureus . A total of 703 proteins were downregulated and 334 proteins were upregulated after BCp12 treatment. The proteins (agrA, agrB, agrC and psmβ) of the QS systems were downregulated. Additionally, the expression of the agr-related genes, agrA , agrB , agrC and psmβ , was downregulated. BCp12 was bound to the receptor proteins agrA and agrC through hydrogen bonds and π–π bonds. Conclusions The results showed the antibiofilm activity of BCp12 and it inhibits the biofilm formation by interfering agr QS system. Significance and Impact of Study BCp12 has the potential to be a novel antibiofilm agent against S. aureus biofilm and used in the food industry.
研究领域:
微生物学
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食品安全
·
分子生物学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2019
·Vol. 20
·期 18
·4565
·
IF 4.183
Shangyong Li,Yanan Wang,Xiao Li,Beom Suk Lee,Samil Jung,Myeong-Sok Lee
Bacterial biofilm causes severe antibiotic resistance. An extracellular polymeric substance (EPS) is the main component in the bacterial biofilm. Alginate is a key EPS component in the biofilm ofPseudomonas aeruginosaand responsible for surface adhesion and stabilization of biofilm. Alginate lyase has emerged as an efficient therapeutic strategy targeting to degrade the alginate in the biofilm ofP. aeruginosa. However, the application of this enzyme is limited by its poor stability. In this study, chitosan nanoparticles (CS-NPs) were synthesized using low molecular weight chitosan and alginate lyase Aly08 was immobilized on low molecular weight chitosan nanoparticles (AL-LMW-CS-NPs). As a result, the immobilization significantly enhanced the thermal stability and reusability of Aly08. In addition, compared with free Aly08, the immobilized AL-LMW-CS-NPs exhibited higher efficiency in inhibiting biofilm formation and interrupting the established mature biofilm ofP. aeruginosa, which could reduce its biomass and thickness confirmed by confocal microscopy. Moreover, the biofilm disruption greatly increased the antibiotic sensitivity ofP. aeruginosa. This research will contribute to the further development of alginate lyase as an anti-biofilm agent.Keywords:immobilization;chitosan nanoparticles;alginate lyase;anti-biofilm activity;antibiotics susceptibility
研究领域:
微生物学
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生物技术
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医学
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DOI
PubMed
高影响因子
CARBOHYDRATE POLYMERS
·
2019
·
IF 6.044
Maruthupandy Muthuchamy,Rajivgandhi Govindan,Kadaikunnan Shine,Veeramani Thangasamy,Naiyf S. Alharbi,Muneeswaran Thillaichidambaram,Jamal M. Khaled,Jun-Li Wen,Khalid F. Alanzi
In this study graphene/chitosan nanoparticles (GR/CS NCs) were developed. The homogenous combination of GR and CS was confirmed by FTIR spectroscopy. The combination of CS with GR sheets reduced the XRD intensity of the GR peak in GR/CS NCs, while TEM images revealed the immobile CS coating of GR sheets. Further, the anti-biofilm activity of GR/CS NCs was tested. The tests showed that the formation of biofilm by Pseudomonas aeruginosa and Klebsiella pneumoniae was inhibited at 40□g/mL GR/CS NCs up to 94 and 92 %, respectively. The intracellular and cell surface damage of the bacteria was observed by CLSM and SEM. Also, GR/CS NCs produced a toxic effect of 90 % on Artemia franciscana at 70□g/mL upon 24 h incubation. The recorded properties of the synthesized GR/CS NCs qualify them as potential agents against multi-drug resistant bacteria.
研究领域:
微生物学
·
纳米医学
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药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）