BIOLOGICAL & PHARMACEUTICAL BULLETIN
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2015
·Vol. 38
·期 7
·1041-1048
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IF 1.828
Huixian Liu,Sui Xiao,Depeng Zhang,Shuhua Mu,Lifang Zhang,Xiaoyang Wang,Feiqun Xue
In this study we describe the design, synthesis, and antibacterial activity of novel pleuromutilin analogs. A series of new compounds containing piperazine and alkylamino or arylamino groups was synthesized. The new compounds were characterized via 1H-NMR, 13C-NMR, Fourier transform (FT)-IR and MS, and were further evaluated for their in vitro activity against seven Gram-positive, and one Gram-negative, pathogens. Antibacterial data revealed that all compounds exhibited moderate to good antibacterial activities against sensitive Gram-positive pathogens. Specifically, 9d displayed the best activity: its activity to Staphylococcus aureus (ATCC25923) is 0.125 µg/mL, which is equal to the control compound tiamulin. The antibacterial activities of 9d to Streptococcus suis (minimum inhibitory concentration (MIC) of 2 µg/mL), Streptococcus agalactiae (MIC of 0.5 µg/mL), and Streptococcus dysgalactiae (MIC of 0.5 µg/mL) were also excellent compared with the control drug erythromycin (MIC of >128 µg/mL). The binding modes of these compounds with active sites were calculated using the programs of Molecular Operating Environment (MOE) and Pymol.
研究领域:
药理学
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有机合成化学
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微生物学
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DOI
PubMed
高影响因子
Advanced Science
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2025
·
IF 14.1
Ke-Fei Xu,Zihao Wang,Macheng Cui,Yuhan Jiang,Chengcheng Li,Zi-Xi Wang,Ling-Yi Li,Chenyang Jia,Lijie Zhang,Fu-Gen Wu
Gram-positive bacteria pose significant threats to human health, necessitating the development of targeted bacterial detection and eradication strategies. Nevertheless, current approaches often suffer from poor targeting specificity. Herein, the study utilizes purple rice lixivium to synthesize biomass carbon dots (termed BCDs) with wheat germ agglutinin-like residues for precisely targeting Gram-positive bacteria. Subsequently, fluorescein isothiocyanate (FITC) molecules are grafted onto BCDs to yield FITC-labeled BCDs (termed CDFs), which can selectively and rapidly (≤5 min) stain bacterial cell wall and particularly target the peptidoglycan component. Strikingly, CDFs achieve superselective visualization of Gram-positive bacteria even in the presence of mammalian cells and Gram-negative bacteria. Furthermore, protoporphyrin (PpIX) molecules are conjugated onto BCDs to yield PpIX-modified BCDs (termed CDPs), which can induce bacterial aggregation and in situ generate singlet oxygen for realizing enhanced antibacterial photodynamic therapy (PDT). At the minimum bactericidal concentration of CDPs (PpIX: 5 µg mL −1 ), CDP-mediated PDT disrupts bacterial structure and metabolism pathways, thereby affecting bacterial interactions to eradicate biofilms. Importantly, CDP-mediated PDT efficiently modulates antiinflammatory responses to promote wound healing in the bacteria-infected mice. This study underscores the significance of harnessing renewable and cost-effective biomass resources for preparing Gram-positive bacteria-targeting theranostic agents, which may find potential clinical applications in the future.
研究领域:
微生物学
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材料科学
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医学
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生物化学
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DOI
PubMed
高影响因子
ACS Sensors
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2022
·
IF 9.618
Leilei Sun,Sisi Shi,Zeming Wu,Yao Huang,Chenhui Ji,Craig A. Grimes,Xinxin Feng,Qingyun Cai
A material system enabling specific NIR-II fluorescence imaging of Gram-positive bacteria is described. The material system is based on the electrostatic binding of Cu2–xSe and vancomycin-modified NaGdF4:Nd,Yb@NaGdF4 downconversion nanoparticles (DCNPs), the fluorescence of which is weak owing to the spectral overlap of Cu2–xSe absorption with the DCNP NIR emission. The presence of Gram-positive bacteria precisely disconnects the bond between vancomycin-modified DCNPs and Cu2–xSe, thus enabling a strong fluorescent signal. In vivo studies show that the material system can be specifically activated at the site of Gram-positive bacterial infection but is essentially nonfluorescent in the area of Gram-negative bacterial infection.
研究领域:
生物医学工程
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材料科学
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感染性疾病研究
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PubMed
高影响因子
Materials Science & Engineering C-Materials for Biological Applications
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2017
·
IF 4.164
Yue Xu,Hang Gao,Yan Shen,Shigan Chai,Jinzhi Zhang,Qichao Zou
Novel Gemini quaternary ammonium salts (GQASs) with ester groups were synthesized. Cationic poly(styrene- co -butyl acrylate) (P(St- co -BA)) nanolatex was synthesized in the presence of GQASs as emulsifier. The structures of GQASs were characterized with Fourier transform infrared spectroscopy and nuclear magnetic resonance spectroscopy; the property of P(St- co -BA) nanolatex was characterized with dynamic light scattering. The results indicated that GQASs and P(St- co -BA) nanolatex with GQASs were successfully synthesized. GQASs, nanolatex, and the polymer films exhibited excellent antibacterial activities against Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli . The GQASs performed even better than the corresponding single-stranded quaternary ammoniums. The antibacterial mechanism was also preliminarily studied, and longer, softer hydrophobic chains of GQAS had stronger antibacterial activity. The work provided a novel, simple approach for developing high-efficiency antibacterial polymer material with a low cost, which has broad biomaterial applications.
研究领域:
材料科学
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生物学
·
医学
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产品关联
DOI
PubMed
高影响因子
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