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INDUSTRIAL CROPS AND PRODUCTS · 2022 · IF 6.449

Ultrasonic preparation of Tween-essential oil (Zanthoxylum schinifolium Sieb. et Zucc) oil/water nanoemulsion: Improved stability and alleviation of Staphylococcus epidermidis biofilm

Shenglan Liao,Gang Yang,Zhirong Wang,Yuheng Ou,Shan Huang,Bin Li,Aijun Li,Jianquan Kan

Staphylococcus epidermidis has been identified as a pathogen in ready-to-eat foods, and its biofilm can cause devastating chronic infections in affected hosts. For the demand of natural antibacterial reagents and overcoming their inherent properties, nanoemulsions are increasingly being used in the delivery of natural drugs. The nanoemulsion obtained by ultrasonic technology has the advantages of small droplet size , low polydispersity index (PDI), high stability and small amount of surfactant. Therefore, ultrasonic technology was used to prepare Zanthoxylum schinifolium Sieb. et Zucc essential oil nanoemulsion (ZEO-NE), a novel antibiofilm nanoemulsion with a mean particle size of 105.6 nm, polydispersity index of 0.278, and Zeta potential of − 22.3 mV. Assessment of antibacterial activity defined the minimum inhibitory concentration (MIC) and minimum bactericidal concentration of ZEO-NE against S. epidermidis as 2.5 and 5.0 mg/mL, respectively. Meanwhile, the antibiofilm assays revealed that the inhibition rate of ZEO-NE at sub-MIC levels (1/16–1/2 MIC) against S. epidermidis biofilm formation was 4.65–81.38 %. Further studies showed that sub-MIC ZEO-NE can effectively inhibit the formation of biofilms by extracellular polymeric substances and regulate gene expression of biofilm initial adhesion, formation, and quorum-sensing systems. Meanwhile, the inhibition rates of ZEO-NE (1/2–4 MIC) on preformed biofilm biomass and cell metabolic activity were 45.06–72.40 % and 30.72–62.54 %, respectively. In addition, electron microscopy analysis showed that ZEO-NE can destroy the established biofilms to a great extent. Finally, cytotoxicity evaluation experiments showed that ZEO-NE could damage human immortalized keratinocytes . These findings indicate that nanotechnology is an effective strategy to increase ZEO stability and solubility, and the prepared ZEO-NE is a viable candidate to inhibit S. epidermidis and its biofilms.

研究领域: 纳米技术 · 微生物学 · 药学 · 食品科学 · 生物技术
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ACS Applied Bio Materials · 2024 · IF 4.6

Preparation and Antibacterial Properties of Polyelectrolyte Complexed Nanoparticles Aggregated from PHMG and Sodium Caffeate

Mingyuan Tang,Xiaoxian Hao,Yuanyuan Kang,Xiaofeng He,Haichao Zhao

In this study, we synthesized polyelectrolyte complexed nanoparticles using an ion exchange reaction between poly(hexamethylene guanidine hydrochloride) and sodium caffeate. The morphology of the obtained antiparticle was observed by scanning electron microscopy, and FT-IR and XPS were employed for the structural characterization. The antimicrobial properties of E. coli and S. aureus were characterized through minimum inhibitory concentration (MIC), growth curve analysis, plate colony counting method, and crystal violet method. Notably, the sample showed a 100% bactericidal rate against E. coli at 0.095 μg/mL and against S. aureus at 0.375 μg/mL within 1 h, demonstrating excellent antimicrobial performance against E. coli and S. aureus. The CA-PHMG-containing acrylic resin coatings exhibited exceptional antimicrobial and antiadhesive properties when examined under an inverted fluorescence microscope, particularly at a 4% weight concentration of the antibacterial agent. This study holds vast potential for development in the field of antimicrobial coatings.

CAS / MDL: 331-39-5
研究领域: 材料科学 · 纳米技术 · 生物医学工程 · 微生物学
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MOLECULES · 2024 ·Vol. 29 ·期 7 ·1534 · IF 4.2

Exploration of the Antibacterial and Anti-Inflammatory Activity of a Novel Antimicrobial Peptide Brevinin-1BW

Zhizhi Chen,Lei Wang,Dongxia He,Qi Liu,Qinqin Han,Jinyang Zhang,A-Mei Zhang,Yuzhu Song

Antibiotic resistance has emerged as a grave threat to global public health, leading to an increasing number of treatment failures. Antimicrobial peptides (AMPs) are widely regarded as potential substitutes for traditional antibiotics since they are less likely to induce resistance when used. A novel AMP named Brevinin-1BW (FLPLLAGLAASFLPTIFCKISRKC) was obtained by the Research Center of Molecular Medicine of Yunnan Province from the skin of thePelophylax nigromaculatus. Brevinia-1BW had effective inhibitory effects on Gram-positive bacteria, with a minimum inhibitory concentration (MIC) of 3.125 μg/mL againstEnterococcus faecalis(ATCC 29212) and 6.25 μg/mL against bothStaphylococcus aureus(ATCC 25923) and multidrug-resistantStaphylococcus aureus(ATCC 29213) but had weaker inhibitory effects on Gram-negative bacteria, with a MIC of ≥100 μg/mL. Studies using scanning electron microscopy (SEM) and flow cytometry have revealed that it exerts its antibacterial activity by disrupting bacterial membranes. Additionally, it possesses strong biofilm inhibitory and eradication activities as well as significant lipopolysaccharide (LPS)-binding activity. Furthermore, Brevinin-1BW has shown a significant anti-inflammatory effect in LPS-treated RAW264.7 cells. In conclusion, Brevinin-1BW is anticipated to be a promising clinical agent with potent anti-Gram-positive bacterial and anti-inflammatory properties.

CAS / MDL: 7727-21-1
研究领域: 微生物学 · 药理学 · 传染病学 · 分子生物学
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EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES · 2019 · IF 3.532

Design and synthesis of new norfloxacin-1,3,4-oxadiazole hybrids as antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA)

Yong Guo,Ting Xu,Chongnan Bao,Zhiyan Liu,Jiangping Fan,Ruige Yang,Shangshang Qin

Toward the search of new antibacterial agents to control methicillin-resistant Staphylococcus aureus (MRSA), a class of new norfloxacin-1,3,4-oxadiazole hybrids were designed and synthesized. Antibacterial activities against drug-sensitive bacteria S. aureus and clinical drug resistant isolates of MRSA were evaluated. Compound 5k exhibited excellent antibacterial activities against S. aureus (MIC: 2 μg/mL) and MRSA1–3 (MIC: 0.25–1 μg/mL). The time-kill kinetics demonstrated that compound 5k had an advantage over commonly used antibiotics vancomycin in killing S. aureus and MRSA. Moreover, compound 5k could inhibit the bacteria and destroy their membranes in a short time, and showed very low cytotoxicity to NRK-52E cells. Some interesting structure-activity relationships (SARs) were also discussed. These results indicated that these norfloxacin-1,3,4-oxadiazole hybrids could be further developed into new antibacterial agents against MRSA.

CAS / MDL: 79-04-9 10025-87-3
研究领域: 药物化学 · 微生物学 · 药理学
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ANTIMICROBIAL AGENTS AND CHEMOTHERAPY · 2023 · IF 4.9

CDBN-YGXZ, a Novel Small-Molecule Drug, Shows Efficacy against Clostridioides difficile Infection and Recurrence in Mouse and Hamster Infection Models

Xiaojun Hu,Renhan Dong,Sheng Huang,Yisheng Zeng,Wei Zhan,Xiaofang Gao,Dong Tian,Jian Peng,Jiewei Xu,Ting Wang,Yaying Zhang,Xiaohui Wang,Xiaoxia Zhang,Jin Liu,Bing Guang,Tai Yang

Clostridioides difficile infection (CDI) causes severe diarrhea and colitis, leading to significant morbidity, mortality, and high medical costs worldwide. Oral vancomycin, a first-line treatment for CDI, is associated with a high risk of recurrence, necessitating novel therapies for primary and recurrent CDI. A novel small-molecule compound, CDBN-YGXZ, was synthesized by modifying the benzene ring of nitazoxanide with lauric acid. The mechanism of action of CDBN-YGXZ was validated using a pyruvate:ferredoxin/flavodoxin oxidoreductase (PFOR) inhibition assay. The efficacy of CDBN-YGXZ was evaluated using the MIC test and CDI infection model in mice and hamsters. Furthermore, metagenomics was used to reveal the underlying reasons for the effective reduction or prevention of CDI after CDBN-YGXZ treatment. The inhibitory activity against PFOR induced by CDBN-YGXZ. MIC tests showed that the in vitro activity of CDBN-YGXZ against C. difficile ranging from 0.1 to 1.5 μg/mL. In the mouse and hamster CDI models, CDBN-YGXZ provided protection during both treatment and relapse, while vancomycin treatment resulted in severe relapse and significant clinical scores. Compared with global effects on the indigenous gut microbiota induced by vancomycin, CDBN-YGXZ treatment had a mild influence on gut microbes, thus resulting in the disappearance or reduction of CDI recurrence. CDBN-YGXZ displayed potent activity against C. difficile in vitro and in vivo, reducing or preventing relapse in infected animals, which could merit further development as a potential drug candidate for treating CDI.

研究领域: 药理学 · 传染病学 · 微生物学 · 药物开发
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2024 · IF 7.7

Natural polysaccharide hydrogel with bioadhesion characters to synergistically enhance berberine's antibacterial effect by regulating the PTS system of Staphylococcus aureus

Yaozhi Zhang,Zhijia Wang,ShuChang Yao,Xiaoyu Lin,Xiang Zhang,Xinru Tan,Liuyang Zhang,Ran Xu,Yihang Zhao,Chen Zhao,Fuhao Chu,Wenguang Jing,Xuemei Huang,Penglong Wang

The global spread of Staphylococcus aureus ( S. aureus ) not only causes significant economic losses but also poses a serious threat to public health. Consequently, there is an urgent need for multidimensional strategies to develop antimicrobial dressings to combat bacterial infections. In response, we have developed a plant polysaccharide antibacterial hydrogel formed through the self-assembly of edible Kudzu powder (KP) and the natural star molecule berberine (BBR). Rheological tests show that natural polysaccharide KP-BBR hydrogel (BBR@KP) exhibits excellent injectability and adhesion. And the degradation of the hydrogel exceeded 90 % within 3 days. The synergistic effect of these two ingredients enhances the antibacterial activity of BBR and can increase the MIC of BBR to 0.05 mM. Specifically, KP promotes the affinity of the Phosphoenolpyruvate Phosphotransferase System (PTS) of S. aureus , enabling KP, with its bioadhesive properties, to adhere to the bacterial surface and continuously release BBR. Subsequently, BBR effectively exerts its antibacterial effect by inhibiting the synthesis of histidine and isoleucine. Furthermore, the BBR@KP hydrogel exhibits negligible cytotoxicity and hemolytic toxicity, underscoring its favorable biosafety profile. This synergistic natural antibacterial hydrogel, formulated through a green and straightforward methodology, not only holds promise for broad clinical applications but also provides novel perspectives for the utilization and development of plant polysaccharides in the biomedical field.

CAS / MDL: 298-93-1 1232133-62-8
研究领域: 生物医学工程 · 药学 · 微生物学 · 材料科学
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CHEMICAL ENGINEERING JOURNAL · 2023 · IF 15.1

Totally-green cellulosic fiber with prominent sustained antibacterial and antiviral properties for potential use in spunlaced non-woven fabric production

Jinxin Lan,Yao Wu,Changmei Lin,Jiazhen Chen,Ruiqi Zhu,Xiaojuan Ma,Shilin Cao

The worldwide spread of COVID-19 has put a higher requirement for personal medical protective clothing, developing protective clothing with sustained antibacterial and antiviral performance is the priority for safe and sustaining application. For this purpose, we develop a novel cellulose based material with sustained antibacterial and antiviral properties. In the proposed method, the chitosan oligosaccharide (COS) was subjected to a guanylation reaction with dicyandiamide in the presence of Scandium (III) triflate; because of the relatively lower molecular weight and water solubility of the COS, GCOS (guanylated chitosan oligosaccharide) with high substitution degree (DS) could be successfully synthetized without acid application. In this instance, the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the GCOS were only 1/8 and 1/4 of that of COS. The introduction of GCOS onto the fiber endowed the fiber with extremely high antibacterial and antiviral performance, showing 100% bacteriostatic rate against Staphylococcus aureus and Escherichia coli and 99.48% virus load reduction of bacteriophage MS2. More importantly, the GCOS modified cellulosic fibers (GCOS-CFs) exhibit excellent sustained antibacterial and antiviral properties; namely, 30 washing cycles had negligible effect on the bacteriostatic rate (100%) and inhibition rate of bacteriophage MS2 (99.0%). Moreover, the paper prepared from the GCOS-CFs still exhibited prominent antibacterial and antiviral activity; inferring that the sheeting forming, press, and drying process have almost no effect on the antibacterial and antiviral performances. The insensitive of antibacterial and antiviral activity to water washing (spunlace) and heat (drying) make the GCOS-CFs a potential material applicable in the spunlaced non-woven fabric production.

研究领域: 材料科学 · 生物技术 · 纺织工程 · 微生物学
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JOURNAL OF FOOD QUALITY · 2023 · IF 3.3

Evaluation of Antibacterial and Antibiofilm Properties of Kojic Acid against Aeromonas sobria and Staphylococcus saprophyticus

Jing-Xin Ye,Yun-Fang Qian,Wei-Qing Lan,Jing Xie

Biofilms composed of microbes and extracellular polymeric substances (EPSs) pose a significant risk to human health and lead to economic loss in the food industry. In this study, the antimicrobial and antibiofilm properties of kojic acid (KA) against Aeromonas sobria (A. sobria) and Staphylococcus saprophyticus (S. saprophyticus) were investigated by determining the leakage of DNA and protein, cell morphology, biofilm formation, the metabolic activity of biofilms, excretion of EPS, and biofilm architecture. The results indicated that the values of minimum inhibitory concentration (MIC) of A. sobria and S. saprophyticus after KA treatment were 0.4 mg/mL and 1.6 mg/mL, respectively. 1 × MIC KA showed unignorable antimicrobial activity against the two bacteria, leading to alterations in the bacterial physicochemical characteristics and cell death. Sub-MICs of KA can inhibit biofilm formation and decrease the metabolic activity and excretion of EPS, and these inhibition effects were in a dose-dependent manner. These results were further confirmed by the visual images obtained from scanning electron microscopy (SEM) and confocal laser scanning microscopy (CLSM). Moreover, S. saprophyticus is more susceptible to KA in inhibiting biofilm formation, and for A. sobria, changes in the cell structure and the permeability of the cell membrane were more obvious. This research highlighted the antibacterial and antibiofilm activity of KA against A. sobria and S. saprophyticus.

研究领域: 微生物学 · 生物技术 · 食品科学
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JOURNAL OF CELLULAR AND MOLECULAR MEDICINE · 2024 ·Vol. 28 ·期 9 ·e18354 · IF 4.3

Fangchinoline inhibits growth and biofilm of Candida albicans by inducing ROS overproduction

Longfei Yang,Xiaonan Wang,Zhiming Ma,Yujie Sui,Xin Liu

Infections caused by Candida species, especially Candida albicans , threaten the public health and create economic burden. Shortage of antifungals and emergence of drug resistance call for new antifungal therapies while natural products were attractive sources for developing new drugs. In our study, fangchinoline, a bis-benzylisoquinoline alkaloid from Chinese herb Stephania tetrandra S. Moore, exerted antifungal effects on planktonic growth of several Candida species including C. albicans , with MIC no more than 50 μg/mL. In addition, results from microscopic, MTT and XTT reduction assays showed that fangchinoline had inhibitory activities against the multiple virulence factors of C. albicans , such as adhesion, hyphal growth and biofilm formation. Furthermore, this compound could also suppress the metabolic activity of preformed C. albicans biofilms. PI staining, followed by confocal laser scanning microscope (CLSM) analysis showed that fangchinoline can elevate permeability of cell membrane. DCFH-DA staining suggested its anti- Candida mechanism also involved overproduction of intracellular ROS, which was further confirmed by N-acetyl-cysteine rescue tests. Moreover, fangchinoline showed synergy with three antifungal drugs (amphotericin B, fluconazole and caspofungin), further indicating its potential use in treating C. albicans infections. Therefore, these results indicated that fangchinoline could be a potential candidate for developing anti- Candida therapies.

CAS / MDL: 179463-17-3
研究领域: 微生物学 · 药理学 · 真菌学 · 天然产物 · 抗菌剂
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Frontiers in Microbiology · 2023 · IF 5.2

Alkyl ferulic acid esters: Evaluating their structure and antibacterial properties

Song Wei,Xin Jiaying,Yu Chong,Xia Chungu,Pan Yu

Ferulic acid (FA) is a natural antibacterial agent rich in plants, FA has excellent antioxidant and antibacterial properties. However, because of its short alkane chain and large polarity, FA is difficult to penetrate the soluble lipid bilayer in the biofilm to enter the cell to play an inhibitory role, limiting its biological activity. To improve the antibacterial activity of FA, with the catalytic condition of Novozym 435, four alkyl ferulic acid esters (FCs) with different alkyl chain lengths were obtained by fatty alcohols (including 1-propanol (C3), 1-hexanol (C6), nonanol (C9), and lauryl alcohol (C12)) modification. The effect of FCs on P. aeruginosa was determined by Minimum inhibitory concentrations (MIC), minimum bactericidal concentrations (MBC), Growth curves, alkaline phosphatase (AKP) activity, crystal violet method, scanning electron microscopy (SEM), membrane potential, PI, cell contents leakage. Results showed that the antibacterial activity of FCs increased after esterification, and the antibacterial activity significantly increased and then decreased with the extension of the alkyl chain of the FCs. Hexyl ferulate (FC6) showed the best antibacterial activities against E. coli and P. aeruginosa (MIC for E. coli was 0.5 mg/ml, MIC for P. aeruginosa was 0.4 mg/ml). And Propyl ferulate (FC3) and FC6 showed the best antibacterial activities S. aureus and B. subtilis (MIC for S. aureus was 0.4 mg/ml, The MIC of B. subtilis was 1.1 mg/ml). In addition, the growth, AKP activity, bacterial biofilm, bacterial cell morphology, membrane potential and cell contents leakage of P. aeruginosa after different FCs were investigated, which found that FCs could damage the cell wall of P. aeruginosa and showed different effects on the P. aeruginosa cell biofilm. FC6 showed the best inhibition on the biofilm formation of P. aeruginosa cells, which caused the surface of P. aeruginosa cells to be rough and wrinkled. Some P. aeruginosa cells showed aggregation and adhesion, even rupture. The membrane hyperpolarization was obvious, which appeared as holes, leading to cell contents leakage (protein and nucleic acid). All these results concluded that the antibacterial activities FCs against foodborne pathogens depended on different fatty alcohol esterification of FA. FC6 showed the best inhibition on P. aeruginosa due to its effect on P. aeruginosa cell walls and biofilms and the leak of the cell contents. This study provides more practical methods and a theoretical basis for giving full play to the bacteriostatic effect of plant FA.

研究领域: 药学化学 · 微生物学 · 食品科学
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