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INTERNATIONAL JOURNAL OF FOOD SCIENCE AND TECHNOLOGY · 2013 ·Vol. 49 ·期 4 ·969-975 · IF 1.24

Membrane-disruptive property of a novel antimicrobial peptide from anchovy (Engraulis japonicus) hydrolysate

Wenting Tang,Hui Zhang,Li Wang,Haifeng Qian

Summary A novel antimicrobial peptide named Pep39 has been isolated from anchovy hydrolysate using ÄKTA protein liquid chromatography and reverse-phase high-performance liquid chromatography. Its amino acid sequence was RLFRHAFKAVLRL with a molecular weight of 1626.92. Pep39 demonstrated antimicrobial ability against Escherichia coli ATCC 25922, Salmonella typhi ATCC 50013, Staphylococcus aureus ATCC 25923 and Bacillus subtilis ATCC 9372, with minimal inhibitory concentration (MIC) ranging from 4 to 32 μg mL −1 . No cytotoxicity to mouse red blood cells was observed when its concentration was lower than 30 μg mL −1 . Pep39 induced the influx of fluorescent probe 8-Anilino-1-naphthalenesulfonic acid and the outflow of β-galactosidase by increasing E. coli outer and inner membrane permeabilities, respectively. Flow cytometric analysis also demonstrated that Pep39 disrupted E. coli cell membrane. These results suggested that the antimicrobial mechanism of Pep39 involved cytoplasmic membrane damage.

研究领域: 微生物学 · 分子生物学 · 食品科学
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ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY · 2022 · IF 7.129

Efficient Microcystis aeruginosa coagulation and removal by palladium clusters doped g-C3N4 with no light irradiation

Shihuan Lu,Xizi Li,Bingzhi Yu,Jiafeng Ding,Yuchi Zhong,Hangjun Zhang

Efficient treatment of cyanobacterial blooms in eutrophication waters by safe and reliable nanomaterials is a big challenge for reducing environmental health risks. Herein, a novel strategy combining palladium clusters (Pd n ) with g-C 3 N 4 nanocomposite was presented to achieve high-efficient removal of Microcystis aeruginosa cells through coagulation and breakage. Interestingly, 95.17% of algal cells (initial concentration of 5.6 × 10 6 cells mL −1 ) were promptly removed in the Pd/g-C 3 N 4 (5%) system within only 10 min and without visible light irradiation and persulfate activation. Both the release of potassium ion and microcystin during the removal process and the transmission electron microscope observations of Microcystis aeruginosa cells proved that the integrity of the algal cell membrane was destroyed. The removal of Microcystin-LR (MC-LR) were further confirmed in the next process. Pd metal interaction and breakage against algal cells may cause disruption of algal cells. This study describes a novel technology for the superfast removal of harmful algae and may provide a new insight into the control of cyanobacterial blooms in practical applications.

研究领域: 环境科学 · 微生物学
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BIORESOURCE TECHNOLOGY · 2024 · IF 9.7

Oxidation effects on Microcystis aeruginosa inactivation through various reactive oxygen species: Degradation efficiency, mechanisms, and physiological properties

Heshan Zheng,Yongjie Zheng,Le Yuan,Shuo Li,Junfeng Niu,Xu Dong,Yoong Kit Leong,Duu-Jong Lee,Jo-Shu Chang

The study investigated the inactivation of Microcystis aeruginosa using a combined approach involving thermally activated peroxyacetic acid (Heat/PAA) and thermally activated persulfate (Heat/PDS). The Heat/PDS algal inactivation process conforms to first-order reaction kinetics. Both hydroxyl radical (•OH) and sulfate radical (SO 4 - •) significantly impact the disruption of cell integrity, with SO 4 - • assuming a predominant role. PAA appears to activate organic radicals (RO•), hydroxyl (•OH), and a minimal amount of singlet oxygen ( 1 O 2 ). A thorough analysis underscores persulfate's superior ability to disrupt algal cell membranes. Additionally, SO 4 - • can convert small-molecule proteins into aromatic hydrocarbons, accelerating cell lysis. PAA can accelerate cell death by diffusing into the cell membrane and triggering advanced oxidative reactions within the cell. This study validates the effectiveness of the thermally activated persulfate process and the thermally activated peroxyacetic acid as strategies for algae inactivation.

研究领域: 环境科学 · 微生物学
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Biology-Basel · 2025 ·Vol. 14 ·期 3 ·226 · IF 3.5

The Antimicrobial Peptide D-CONGA-Q7 Eradicates Drug-Resistant E. coli by Disrupting Bacterial Cell Membranes

Zonghan Jiang,Leisheng Sun,Yuanyuan Li,Haoyu Li,Yu Fu,Jiyun Li,Zhiliang Sun

Simple SummaryEscherichia coliis a ubiquitous pathogen, with certain strains causing severe diarrhea and intestinal illnesses, which pose significant health risks to both children and animals. As antimicrobial resistance continues to rise, traditional antibiotics are increasingly ineffective, highlighting the urgent need for novel therapeutic strategies. In this study, we investigated the antimicrobial peptide D-CONGA-Q7, aiming to evaluate its efficacy and underlying mechanism against drug-resistantE. colistrains. Our results demonstrate that D-CONGA-Q7 effectively disrupts bacterial cell membranes, leading to bacterial death, and exhibits comparable activity against polymyxin- and meropenem-resistant strains. In vivo experiments revealed that D-CONGA-Q7 significantly alleviated intestinal inflammation, reduced inflammatory cytokine levels, and promoted the repair of damaged intestinal tissues. Furthermore, D-CONGA-Q7 displayed good stability. These findings suggest that D-CONGA-Q7 not only represents a promising new approach to combat drug-resistant bacterial infections but also holds potential for clinical application.Escherichia coli(E. coli) is a zoonotic bacterium widespread in the environment, highly transmissible, and responsible for significant economic losses and millions of cases of illness annually. The rise of multidrug-resistant (MDR) strains has rendered last-line antibiotics such as polymyxin and meropenem ineffective, making the development of new antibiotics urgent. Although D-CONGA-Q7 has broad-spectrum bactericidal activity, its underlying mechanism remains poorly understood. In this study, we used in vitro and in vivo experiments to demonstrate that D-CONGA-Q7 effectively kills both antibiotic-sensitive and multidrug-resistant strains ofE. coli. D-CONGA-Q7 disrupts the cell membranes of Gram-negative bacteria, and the treatment ofE. colistrainLN175with D-CONGA-Q7 resulted in a significant up-regulation of theMlacgene, suggesting that D-CONGA-Q7 may interact with phospholipids in the cell membrane. Furthermore, in treatingK88-induced bacterial enteritis in the small intestine, D-CONGA-Q7 significantly reduced intestinal inflammation. In conclusion, this study provides a novel approach to combat drug-resistantE. coli.

CAS / MDL: 90-30-2 25535-16-4
研究领域: 微生物学 · 药理学 · 传染病学
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Journal of Advanced Research · 2025 · IF 13

Development of novel broad-spectrum amphipathic antimicrobial peptides against multidrug-resistant bacteria through a rational combination strategy

Jing Zhang,Liang Luan,Youdong Xu,Shuyuan Jiang,Wenpeng Zhang,Long Tian,Weifeng Ye,Jiaqi Han,Changhao Zhang,Taoran Wang,Qingbing Meng

Introduction In recent years, cationic amphipathic antimicrobial peptides (AMPs) have shown great promise in combating antibiotic resistance on account of their distinctive membrane-disruptive mechanism. However, the clinical application of AMPs is restricted by their unsatisfactory stability and safety. Although attempts have been made to improve the stability and safety of AMPs, many of them are accompanied by a decline in their antimicrobial activity and bacterial selectivity. Objectives To develop AMPs with excellent and balanced antimicrobial activity, stability, and safety using a combination strategy. Methods A series of sC18 4b -derived peptide analogues were designed by a combination strategy of subtly adjusting the charges, hydrophobic properties, and introducing specific unnatural amino acids in a well-balanced manner. The antimicrobial activity, cytotoxicity, hemolytic activity, stability, anti-biofilm activity, mechanism of action, synergistic effects, in vivo efficacy, and pharmacokinetics of the analogues were evaluated. Results Among these analogues, P-α-02-B stood out for its broad-spectrum and potent antimicrobial activity, anti-biofilm activity, desirable bacterial selectivity, high plasma stability, and synergistic effect with antibiotic levofloxacin. P-α-02-B exhibited strong membrane disturbance effect, which could be explained by its rigid α-helical structure revealed by molecular dynamics simulations. More importantly, P-α-02-B showed favorable therapeutic efficacy in vivo , whether used alone or in combination with levofloxacin. Conclusion P-α-02-B is a promising antimicrobial agent for MDR bacterial infections, demonstrating the effectiveness of the combination strategy for AMP development.

研究领域: 微生物学 · 药物开发 · 分子生物学
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Nanoscale · 2016 ·Vol. 8 ·期 21 ·11143-11152 · IF 7.76

Antibacterial properties and mechanisms of gold–silver nanocages

Yulan Wang,Jiangshan Wan,Richard J. Miron,Yanbin Zhao,Yufeng Zhang

Despite the number of antibiotics used in routine clinical practice, bacterial infections continue to be one of the most important challenges faced in humans. The main concerns arise from the continuing emergence of antibiotic-resistant bacteria and the difficulties faced with the pharmaceutical development of new antibiotics. Thus, advancements in the avenue of novel antibacterial agents are essential. In this study, gold (Au) was combined with silver (Ag), a well-known antibacterial material, to form silver nanoparticles producing a gold–silver alloy structure with hollow interiors and porous walls (gold–silver nanocage). This novel material was promising in antibacterial applications due to its better biocompatibility than Ag nanoparticles, potential in photothermal effects and drug delivery ability. The gold–silver nanocage was then tested for its antibacterial properties and the mechanism involved leading to its antibacterial properties. This study confirms that this novel gold–silver nanocage has broad-spectrum antibacterial properties exerting its effects through the destruction of the cell membrane, production of reactive oxygen species (ROS) and induction of cell apoptosis. Therefore, we introduce a novel gold–silver nanocage that serves as a potential nanocarrier for the future delivery of antibiotics.

CAS / MDL: 107-21-1
研究领域: 材料科学 · 微生物学 · 药理学
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FOOD CHEMISTRY · 2025 · IF 9.8

Renewable rosin-based bisquaternary ammonium salt with pyridyl design, synthesis and antifungal activity

Bin Wu,Chaoji Xiong,Zhuo Xu,Kun Liang,Chunhua Wu,Wei Wu,Qian Chen

In order to synthesize green, low-toxicity, and novel antifungal agents. In this study, a rosin-based bisquaternary ammonium salt (Rbs) was synthesized using rosin amine and evaluated for its antifungal activity against F. oxysporum f. sp. niveum, F. graminearum, V. mali, P. capsica and A. solani . The results show that compared to benzalkonium bromide, Rbs has stronger inhibitory activity against five types of fungi, with the best activity against V. mali (EC 50  = 3.071 μg/mL), and has excellent sustained antifungal activity. In vivo tests have shown that Rbs has significant protective and therapeutic effects on apples . Using SEM, TEM, relative membrane permeability and density functional theory calculations, we found that Rbs causes organelle and cell membrane disruption, leading to leakage of cell contents and ultimately cell death. In addition, mouse toxicology showed that the toxicity of Rbs was low. These studies provide theoretical guidance for the development of subsequent fungicides.

CAS / MDL: 1195-59-1
研究领域: 植物病理学 · 绿色化学 · 毒理学
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2019 · IF 3.571

Biocatalytic Synthesis of Lipophilic Baicalin Derivatives as Antimicrobial Agents

Xuan Xin,Mengmeng Zhang,Xiao-Feng Li,Guanglei Zhao

Enzymatic acylation is commonly used to increase the lipophilicity of flavonoids. However, the absence of primary hydroxyl groups makes it challenging to acylate baicalin using traditional acylation methods. In this study, an enzymatic esterification strategy was developed to introduce fatty-acid chains into baicalin at its carboxyl group, hence successfully synthesizing a new series of baicalin ester derivatives in nonaqueous media. Under the optimal reaction conditions, up to 95% conversion of baicalin was achieved. Antimicrobial evaluation of the baicalin ester derivatives indicated a corresponding increase to that of C log P values, with a cutoff effect at C log P = 5.2. Baicalin ester derivatives with C log P values of 4.9–5.2 exhibited the most potent antimicrobial activity. Interestingly, the introduction of medium-length fatty alcohol chains not only increased lipophilicity but also endowed them with membrane-disrupting properties. This study, therefore, provides an understanding of the esterification of flavonoid glycosides and a prospective application of the ester derivatives.

研究领域: 药理学 · 生物催化 · 有机合成
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JOURNAL OF BIOMATERIALS APPLICATIONS · 2022 · IF 2.712

The effect of alkyl chain length of (R)-3-Hydroxybutyric alkyl ester on antibacterial activity and its antibacterial mechanism

Zao Cheng,Junfei Gao,Qianqian Liu,Qun Gu

This work describes the relationship between the antibacterial activity and the ester chain length (C1-C8) of (R)-3-Hydroxybutyric ((R)-3-HB) alkyl esters that synthesized from (R)-3-HB acid ((R)-3-HBA) by esterification reaction. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) decrease as the length of the (R)-3-HB alkyl ester chain increases from 1 to 6, but (R)-3-HB-C7 and (R)-3-HB-C8 have their own rules for different microorganisms. Among them, the (R)-3HB-C6 has the relatively best antibacterial and antifungal properties, which MIC were 1.95 mg mL−1 against E. coli and S. aureus; 0.98 mg mL−1 against C. albicans and B. subtilis; 0.49 mg mL−1 against A. niger. Finally, the antimicrobial mechanisms of the (R)-3HB-C6 are revealed, and these include disruption of biofilm and the bacterial wall/membrane, leakage of the intracellular content, and change in the transmembrane potential. These results imply the potential application of (R)-3-HB alkyl ester as new antimicrobial agents; future research can use this as an antibacterial element to synthesize new polymer materials or agents with high-efficiency antibacterial activity.

研究领域: 药物化学 · 微生物学 · 有机化学
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Small · 2025 · IF 12.1

Enhancement Effect of Static Magnetic Field on Bactericidal Activity

Min Zhang,Yongshun Song,Jun Wang,Xinlei Shi,Qiang Chen,Rui Ding,Junjie Mou,Haiping Fang,Yunlong Zhou,Ruoyang Chen

The biological effects of magnetic fields are pervasive in microorganisms, with significant attention given to alternating magnetic fields (AMFs). However, AMFs induce electrical and magnetothermal effects, which complicate the interpretation of magnetic field-induced biological effects and introduce uncertainties regarding cytotoxicity in practical applications. The static magnetic field (SMF) with few variables and high biocompatibility presents a promising alternative for both understanding biological mechanisms and ensuring safe applications, but has a remaining problem on weak interactions with microorganisms. Here we show that the combination of SMF with paramagnetic calcium-polypyrrole nanoparticles (Ca-PPy) remarkably enhances bactericidal activity. Our experiments indicate that the synergistic action of SMF and Ca-PPy significantly promotes the generation of reactive oxygen species (ROS), i.e., singlet oxygen and superoxide anion radicals, in Escherichia coli ( E. coli ) and Staphylococcus aureus ( S. aureus ), coupled with the physical disruption of bacterial membrane, exhibiting the extraordinary bactericidal performance (the bactericidal rate is over 94%). The mechanism disclosed by computations is that the singlet-to-triplet transition of radical pairs can be increased by the introduction of magnetic fields. These findings offer new insights into the biological effects of magnetic fields and pave the way for their safe, highly effective use in bactericidal applications.

CAS / MDL: 10043-52-4 111-30-8
研究领域: 微生物学 · 生物物理学 · 材料科学
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Acta Biomaterialia · 2024 · IF 9.4

Rapid release of high-valent silver ions from water-soluble porphyrin complexes to enhance the direct killing of Methicillin-Resistant Staphylococcus aureus

Yanling Lin,Liyue Liu,Jiaqi He,Jianliang Shen,Qizhi Ren

The emergence of multidrug-resistant (MDR) bacteria represented by MRSA (Methicillin-resistant Staphylococcus aureus ) poses a great challenge to current anti-infection treatment. It is critical to develop efficient MRSA anti-bacteria drugs and explore simple therapeutic strategies with low MDR risk. Herein, we synthesized high-valent (Ag II /Ag III ) water-soluble porphyrins (cationic AgTMPyP and anionic AgTMPPS) and investigated their direct bactericidal property for MRSA without photoactivation in vitro and in vivo. The cationic porphyrin AgTMPyP exhibits well oxidase-like activity and has 100 % sterilizing rate at 8 μmol/L concentration. Besides, AgTMPyP can effectively destroy biofilms in vitro , mediate the polarization of macrophages from M1 to M2, and promote wound healing in vivo . Combined with DFT calculation, the related antibacterial mechanism is further discussed. High-valent silverporphyrins can maintain stable in water for at least 200 days. The moment they encounter MRSA, high-valent silver ions from AgTMPyP can be immediately released from the porphyrin ring and attack the MRSA with efficient sterilization. Together with the hemolysis, blood routine and blood biochemistry tests, it is proved that AgTMPyP can have great prospects in the direct treatment of bacterial infections in skin diseases in the future. Statement of significance The emergence of multidrug-resistant (MDR) bacteria represented by MRSA poses a great challenge to current anti-infection treatment. It has become critical to develop efficient MRSA anti-bacteria drugs and explore simple therapeutic strategies with low MDR risk. We synthesized high-valent (Ag II /Ag III ) water-soluble silver porphyrins (AgTMPyP and AgTMPPS), which can be stable for long periods in aqueous solutions. AgTMPyP can directly and efficiently kill bacteria and destroy biofilms without photoactivation in vitro and in vivo . Combined with DFT calculation, the related antibacterial mechanism is further discussed. AgTMPyP is a superior antimicrobial agent with good biocompatibility and it can have great prospects in the direct treatment of bacterial infections and wound healing in the future.

研究领域: 微生物学 · 药物化学 · 感染病学
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JOURNAL OF MEDICINAL CHEMISTRY · 2025 · IF 6.8

Terminally Symmetric β-Turn Peptides for Multidrug-Resistant Bacterial Infections

Long Tian,Taoran Wang,Liang Luan,Zhao Meng,Jiaqi Han,Chunhui Zhao,Yijie Xu,Chunlan Zeng,Weifeng Ye,Shuyuan Jiang,Li Zhang,Jiye Yin,Qingbin Meng,Song Li

Antimicrobial peptides (AMPs) are considered promising agents to solve the problem of antibiotic resistance due to their unique membrane-disruption mechanism. In this research, de novo terminally symmetric β-turn AMPs were designed by combining the β-turn sequences derived from Tritrpticin with alternately arranged cationic and hydrophobic amino acid sequences. The structure–activity relationship of the peptides was studied. Among the designed peptides, P-07 (KIKIKPWWWPKIKIK-NH2) exhibited potent antimicrobial activity against all the tested bacterial strains, showing the highest bacterial selectivity, relatively low cytotoxicity, high bactericidal efficiency, and low potential to induce bacterial resistance. The antimicrobial mechanisms of P-07 involving membrane-disruption and lipopolysaccharide-binding were proven. Moreover, the in vivo studies confirmed the wound-healing ability of P-07 using a mice bacteria-infected full-thickness wound model. Taken together, P-07 showed great promise in the treatment of multidrug-resistant bacterial infections.

研究领域: 微生物学 · 药物开发 · 分子生物学
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