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MOLECULES · 2017 ·Vol. 22 ·期 6 ·970 · IF 2.861

Synthesis and Bioactivity Evaluation of N-Arylsulfonylindole Analogs Bearing a Rhodanine Moiety as Antibacterial Agents

Ming-Xia Song,Song-Hui Li,Jiao-Yang Peng,Ting-Ting Guo,Wen-Hui Xu,Shao-Feng Xiong,Xian-Qing Deng

Due to the rapidly growing bacterial resistance to antibiotics and the scarcity of novel agents under development, bacterial infections are still a pressing global problem, making new types of antibacterial agents, which are effective both alone and in combination with traditional antibiotics, urgently needed. In this paper, seven series ofN-arylsulfonylindole analogs5–11bearing rhodanine moieties were synthesized, characterized, and evaluated for antibacterial activity. According to the in vitro antimicrobial results, half of the synthesized compounds showed potent inhibition against four Gram-positive bacteria, with MIC values in the range of 0.5–8 µg/mL. For multidrug-resistant strains, compounds6aand6cwere the most potent, with MIC values of 0.5 µg/mL, having comparable activity to gatifloxacin, moxiflocaxin and norfloxacin and being 128-fold more potent than oxacillin (MIC = 64 µg/mL) and 64-fold more active than penicillin (MIC = 32 µg/mL) againstStaphylococcus aureusATCC 43300.

研究领域: 药物化学 · 微生物学 · 感染与免疫
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ACS Applied Materials & Interfaces · 2018 · IF 8.097

Mechanistic Insight into the Light-Irradiated Carbon Capsules as an Antibacterial Agent

Qiuwen Wu,Gen Wei,Zhuobin Xu,Jing Han,Juqun Xi,Lei Fan,Lizeng Gao

Infections caused by bacteria are a growing global challenge for public health as bacteria develop resistance, which will cause the failure of anti-infective treatment eventually. An effective alternative strategy to traditional antibacterial therapy is utilizing reactive oxygen species (ROS) to kill bacteria. Here, we report a simple route to prepare PEGylated nitrogen-doped carbon capsules (PEG-N-CCs) as an antibacterial agent. The PEG-N-CCs can translate near-infrared light (NIR) into heat and produce a high concentration of ROS triggered by NIR irradiation. Both heating and ROS are critical to destroy the outer membranes and rupture cell bodies, causing DNA fragmentation and glutathione oxidation both in Gram-negative Escherichia coli, Gram-positive Staphylococcus aureus, and their multidrug-resistant strains. Moreover, PEG-N-CCs plus NIR irradiation can efficiently scavenge the existing biofilms and prevent the formation of new biofilms, killing planktonic bacteria as well as those within the biofilm. Our studies prove that the PEG-N-CCs plus NIR irradiation can provide a simple and effective platform for combating bacteria, employing carbon nanomaterials as an antibacterial alternative for treatment of infectious diseases.

CAS / MDL: 548-62-9 7722-84-1
研究领域: 材料科学 · 微生物学 · 纳米技术 · 生物医学工程
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Research · 2024 · IF 8.5

Copper-Bearing Metal-Organic Framework with Mucus-Penetrating Function for the Multi-Effective Clearance of Mucosal Colonized Helicobacter pylori

Chunxi Shu,Wei Zhang,Yiwei Zhang,Yu Li,Xinbo Xu,Yanan Zhou,Yue Zhang,Qin Zhong,Cong He,Yin Zhu,Xiaolei Wang

Helicobacter pylori colonizes over 50% of people worldwide. Biofilm formation through penetrating gastric mucus and resistance acquired by H. pylori markedly reduces the efficacy of traditional antibiotics. The present triple therapy and bismuth-based quadruple therapy inevitably causes intestinal flora disturbance and fails to address the excessive H. pylori-triggered inflammatory response. Herein, a mucus-permeable therapeutic platform (Cu-MOF@NF) that consists of copper-bearing metal-organic framework (Cu-MOF) loaded with nitrogen-doped carbon dots and naturally active polysaccharide fucoidan is developed. The experimental results demonstrate that Cu-MOF@NF can penetrate the mucus layer and hinder H. pylori from adhering on gastric epithelial cells of the stomach. Notably, released Cu2+ can degrade the polysaccharides in the biofilm and interfere with the cyclic growing mode of “bacterioplankton ↔ biofilm”, thereby preventing recurrent and persistent infection. Compared with traditional triple therapy, the Cu-MOF@NF not only possesses impressive antibacterial effect (even include multidrug-resistant strains), but also improves the inflammatory microenvironment without disrupting the balance of intestinal flora, providing a more efficient, safe, and antibiotic-free new approach to eradicating H. pylori.

CAS / MDL: 64-17-5 68-12-2 67-56-1
研究领域: 生物医学工程 · 微生物学 · 药学 · 材料科学
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INORGANIC CHEMISTRY COMMUNICATIONS · 2024 · IF 4.4

Ga2Se3 nanosheets: Broad-spectrum antibacterial and antioxidant agents with low drug resistance

Henggang Wang,Shan Sun,Jin Yang,Haoyi Sun,Ke Cheng,Xinxin Wang,Si Li,Hengwei Lin

The efficient treatment of many infectious diseases is hindered by uncontrolled bacterial infections and inflammation induced by reactive oxygen species (ROS). Thus, there is an urgent need for the development of multifunctional therapeutic agents that possessing both antibacterial and antioxidant features. In this study, a novel antibacterial and antioxidant agent, Ga 2 Se 3 nanosheets (NSs), were firstly prepared by the liquid-phase exfoliation method. The Ga 2 Se 3 NSs exhibited broad-spectrum sterilization capabilities, even including multidrug-resistant strains. Noteworthily, Ga 2 Se 3 NSs showed a remarkable 800-fold enhancement in antibacterial efficacy compared to the bulk materials, while also demonstrating low drug resistance compared to the traditional antibiotics. Their superior antibacterial performance is primarily attributed to the disruption of basic bacterial metabolism induced by gallium and selenium components, as well as the dimensional engineering of Ga 2 Se 3 NSs. Cellular studies further confirmed the protective effects of pluronic F127 modified Ga 2 Se 3 NSs against oxidative stress damage, preserving cellular functions through ROS scavenging. This study highlights the superior antibacterial and antioxidant properties of Ga 2 Se 3 NSs, which offers an alternative opportunity for addressing the drug resistance issue in treatment of certain special diseases.

研究领域: 纳米技术 · 材料科学 · 生物医学工程 · 药学
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BIOCHEMICAL ENGINEERING JOURNAL · 2021 · IF 3.978

Novel ε-polylysine/polyethyleneimine -coated Ag nanoparticles for in vitro treatment of Pseudomonas aeruginosa

Jingjing Zhang,Feng Qu,Taobo Liang,Sidi Lv,Wen Li,Qixiu You,Bolu Chen,Hengyi Xu

Pseudomonas aeruginosa is one of the most commonly isolated nosocomial pathogens and is responsible for approximately 10 % of all hospital-acquired infections. P. aeruginosa is difficult to treat with known antibiotics due to its increasing antibiotic resistance. In our study, Ag NPs coated with ε-polylysine (ε-PL) and polyethyleneimine (PEI) were synthesized. These materials showed strong anti- P. aeruginosa capacity at an low concentration (IC50: 7.284 μg/mL). In addition, three drug-resistant clinical strains and biofilm formation were inhibited by ε-PL/PEI-coated Ag NPs (MBIC: 15.63 μg/mL). We further studied the antibacterial mechanism of Ag NPs on different levels and found that a) the amount of reactive oxygen species (ROS) increased, b) the expression of oxidative stress-related genes were up-regulated, c) the activity of total superoxide dismutase decreased, and d) the inhibitory rate is increased on P. aeruginosa cells. These antibacterial effects were dependent on an increasing concentration of Ag NPs but were neutralized by the ROS scavenger N-acetyl-L-cysteine. Therefore, we suggested that oxidative stress induced by ROS is the primary antibacterial mechanism of synthesized Ag NPs.

CAS / MDL: 7761-88-8
研究领域: 纳米技术 · 微生物学 · 药学 · 生物医学工程
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BMC MICROBIOLOGY · 2019 ·Vol. 19 ·期 1 ·1-13 · IF 3.287

Enhanced antifungal activity of bovine lactoferrin-producing probiotic Lactobacillus casei in the murine model of vulvovaginal candidiasis

Liao Hong,Liu Shanling,Wang He,Su Hang,Liu Zhenjun

Background Vulvovaginal candidiasis (VVC) is a common vaginitis caused by Candida species,a frequently recurring condition. Fungal azole-resistant strains with azole-resistance have developed for long and wide explosion to the first-line antifungal azole agent. Bovine lactoferrin (BLF) is a protein from transferrin family secreted by the bovine mammary tissue. Its various biological functions are well known, especially the pronounced antifungal activity. Results In the current study, we constructed a Lactobacillus casei strain ( L.casei /pPG612.1-BLF), which secreted BLF encoded by a mature secretion vector plasmid pPG612.1, and evaluated its antifungal activity in vitro and in vivo. In a two-layer agar plate in vitro assay, the number of C. albicans CFUs decreased and the average colony size shrunk upon exposure to L. casei /pPG612.1-BLF. In a murine VVC model, the infection burden of mice intra-vaginally pre-inoculated with L. casei /pPG612.1-BLF was lower than in control groups. Furthermore, the infection burden in mice with VVC was reduced when the animals were continually given L. casei /pPG612.1-BLF as a topical treatment for 5 days. Conclusion Combined, these results suggested that the L. casei /pPG612.1-BLF strain is a promising preventative and therapeutic anti-VVC agent, highlighting the possibility of employing the probiotic L. casei as a vehicle for biotherapy in the female genital tract and exploiting the natural antibiotic antimicrobial peptides for other applications.

CAS / MDL: 979-32-8
研究领域: 微生物学 · 传染病学 · 药理学 · 分子生物学
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JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH · 2014 · IF 0.968

A new dipeptide isolated from the bulb of garlic

Mei-Yun Zhou,Zhao-Jun Wu,Wen-Qing Li,Xing-Peng Hu,Rian Yan,Shi-Yi Ou,Hua Zhou

(R)-3-(allylthio)-2-((R)-3-(allylthio)-2-aminopropanamido)propanoic acid was isolated from the bulb of garlic, together with four known amino acids. Its structure was elucidated on the basis of 2D NMR and MS techniques. To the best of our knowledge, (R)-3-(allylthio)-2-((R)-3-(allylthio)-2-aminopropanamido)propanoic acid, which showed antibacterial activity against the Staphylococcus aureus antibiotic resistant strain, was the first example of dipeptide from garlic.

研究领域: 化学 · 药理学 · 微生物学
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Advanced Healthcare Materials · 2024 · IF 10

Action Programed Nanoantibiotics with pH-Induced Collapse and Negative-Charged-Surface-Induced Deformation Against Antibiotic-Resistant Bacterial Peritonitis

Xiao Zhang,Penghui Liu,Ran Zhang,Wenhong Zheng,Di Qin,Yinghang Liu,Xin Wang,Tongyi Sun,Yuanyuan Gao,Li-Li Li

The incorporation of well-designed antibiotic nanocarriers, along with an antibiotic adjuvant effect, in combination with various antibiotics, offers us an opportunity to combat drug-resistant strains. However, precise control over morphology and encapsulated payload release can significantly impact their antibacterial efficacy and synergistic effects when used alongside antibiotics. Here, we focus on developing lipopeptide-based nano-antibiotics, which demonstrate an antibiotic adjuvant effect by inducing pH-induced collapse and negative-charged-surface-induced deformation. This enhances the disruption of the bacterial outer membrane and facilitates drug penetration, effectively boosting the antimicrobial activity against drug-resistant strains. The modulation regulations of the lipopeptide nanocarriers with modular design were governed by us. The nanoantibiotics, made from lipopeptide and ciprofloxacin (Cip), have a drug loading efficiency of over 80%. The combination with Cip resulted in a significantly low fractional inhibitory concentration index (FIC) of 0.375 and a remarkable reduction in the minimum inhibitory concentration (MIC) of Cip against MDR E. coli (clinical isolated strains) by up to 32-fold. The survival rate of MDR E. coli peritonitis treated with our nanoantibiotics was significantly higher, reaching over 87%, compared to only 25% for Cip and no survival for the control group. Meanwhile, the nanoantibiotic showed no obvious toxicity to major organs. This article is protected by copyright. All rights reserved

研究领域: 药学 · 纳米技术 · 微生物学 · 传染病学
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JOURNAL OF HAZARDOUS MATERIALS · 2023 · IF 13.6

Attenuation effects of ZVI/PDS pretreatment on propagation of antibiotic resistance genes in bioreactors: Driven by antibiotic residues and sulfate assimilation

Qi Zhao,Qing-Lian Wu,Hua-Zhe Wang,Qi-Shi Si,Lu-Shi Sun,De-Nian Li,Nan-Qi Ren,Wan-Qian Guo

Sulfate radical-based advanced oxidation processes (AOPs) combined biological system was a promising technology for treating antibiotic wastewater. However, how pretreatment influence antibiotic resistance genes (ARGs) propagation remains largely elusive, especially the produced by-products (antibiotic residues and sulfate) are often ignored. Herein, we investigated the effects of zero valent iron/persulfate pretreatment on ARGs in bioreactors treating sulfadiazine wastewater. Results showed absolute and relative abundance of ARGs reduced by 59.8%− 81.9% and 9.1%− 52.9% after pretreatments. The effect of 90-min pretreatment was better than that of the 30-min. The ARGs reduction was due to decreased antibiotic residues and stimulated sulfate assimilation. Reduced antibiotic residues was a major factor in ARGs attenuation, which could suppress oxidative stress , inhibit mobile genetic elements emergence and resistant strains proliferation. The presence of sulfate in influent supplemented microbial sulfur sources and facilitated the in-situ synthesis of antioxidant cysteine through sulfate assimilation, which drove ARGs attenuation by alleviating oxidative stress. This is the first detailed analysis about the regulatory mechanism of how sulfate radical-based AOPs mediate in ARGs attenuation, which is expected to provide theoretical basis for solving concerns about by-products and developing practical methods to hinder ARGs propagation.

CAS / MDL: 68-35-9
研究领域: 环境工程 · 微生物学 · 废水处理 · 生物技术
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