Article
Chemistry, Multidisciplinary
Yuan Li, Xiangmei Liu, Zhenduo Cui, Yufeng Zheng, Hui Jiang, Yu Zhang, Yanqin Liang, Zhaoyang Li, Shengli Zhu, Shuilin Wu
Summary: This study presents a new NIR light catalyst that enhances the sensitivity of bacteria to reactive oxygen species and heat, resulting in the effective killing of bacteria under mild conditions. The catalyst alters bacterial metabolic processes and disrupts protein structures, exhibiting synergistic antibacterial effects with clinical antibiotics. Additionally, the catalyst stimulates immune responses and reduces complications.
Article
Engineering, Environmental
Qianqian Guo, Yongjun Luo, Honglei Guo, Tianyu Lan, Shengquan Wang, Kedui Geng, Xin Lu, Ling Tao, Xiangchun Shen
Summary: A novel antibacterial nanocomposite of AuNRs@PBArPEGMA was developed to treat drug-resistant P. aeruginosa infection in the lungs. The nanocomposite showed efficient antibacterial activity against MRPA and could kill biofilm bacteria using near-infrared irradiation.
CHEMICAL ENGINEERING JOURNAL
(2022)
Article
Pharmacology & Pharmacy
Maria S. Zharkova, Aleksey S. Komlev, Tatiana A. Filatenkova, Maria S. Sukhareva, Elizaveta V. Vladimirova, Andrey S. Trulioff, Dmitriy S. Orlov, Alexander V. Dmitriev, Anna G. Afinogenova, Anna A. Spiridonova, Olga V. Shamova
Summary: Antimicrobial peptides (AMPs) are a promising template for new antimicrobials, and their interaction with antiseptics is an interesting topic that requires further attention.
Article
Nanoscience & Nanotechnology
Yongjun Luo, Xiaoping Zhu, Jun Qian, Yiyi Yu, Jing Li, Zhiyong He, Suyan Duan, Honglei Guo, Xiangchun Shen, Qianqian Guo
Summary: The overuse of antibiotics has resulted in the emergence of drug-resistant pathogens, necessitating the development of effective strategies. Researchers have created pH-responsive polymer-coated gold nanorods for photothermal therapy against multidrug-resistant bacteria. These nanocomposites demonstrated enhanced photothermal efficiency and showed potential in treating drug-resistant bacterial infections in vivo.
ACS APPLIED NANO MATERIALS
(2022)
Article
Engineering, Biomedical
Qingqin Tan, Zhenxing Chen, Lei Liu, Xi Huang
Summary: In this study, new-generation rhodium nanoplates (RhNPs) and glycol chitosan- and polydopamine-functionalized RhNPs (Rh@GCS) were developed for the treatment of drug-resistant SSTIs. Rh@GCS exhibited enhanced antibacterial activity and promoted the healing of skin lesions in MRSA-induced SSTI mouse models. These results suggest that Rh@GCS is a promising nonantibiotic antimicrobial agent for the treatment of drug-resistant SSTIs.
ADVANCED HEALTHCARE MATERIALS
(2023)
Article
Chemistry, Medicinal
Wei Wang, You-Wen Zhang, Shang-Jiu Hu, Wei-Ping Niu, Guo-Ning Zhang, Mei Zhu, Ming-Hua Wang, Fan Zhang, Xue-Mei Li, Ju-Xian Wang
Summary: PFK-158 and its derivatives show potential antibacterial effects, especially against drug-resistant bacteria. This research provides new insights for the development of new antibiotics.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Biochemistry & Molecular Biology
Xiaofeng He, Wenjing Guo, Yuxuan Tang, Jianming Xiong, Yuanyuan Li, Rongrong Huang, Wenjun Miao
Summary: Due to the misuse of antibiotics, bacterial resistance has become a serious global problem, leading to an increase in associated diseases and medical burden. Antimicrobial photodynamic therapy (PDT), a safe and efficient treatment, has gained attention. In this study, an oxygen-supply antibacterial agent (Ce6@CS/CP) was developed, which enhanced the effectiveness of antibacterial PDT through O2 photosynthesis. Ce6@CS/CP had a strong interaction with bacteria, improving the delivery efficiency of Ce6. In vitro experiments showed that Ce6@CS/CP had significantly higher photodynamic bactericidal potency and antibiofilm activity compared to free Ce6. This new strategy offers a promising approach in fighting against drug-resistant bacteria.
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY
(2023)
Article
Public, Environmental & Occupational Health
Keke Liu, Hua Xu, Jian Sun, Yuqing Liu, Weiguang Li
Summary: A survey in Shandong Province, China, revealed significant regional differences in the detection rates of CRGN, with CRE having low detection and discovery rates, while CRAB had high rates. Larger hospitals showed increased use of carbapenem drugs, and economically developed regions also had higher usage levels.
FRONTIERS IN PUBLIC HEALTH
(2022)
Article
Engineering, Environmental
Yan Li, Zhihao Xu, Liqin Tang, Fujun Wang, Lu Wang
Summary: This study developed nano-fibrous wound dressings with synergistic antibacterial activity. The dressings were made by layerwise co-assembly of benzalkonium chloride (BC) and metal-organic framework nanoparticles (MOFs, PCN-224) onto electrospun nanofibrous membranes (ENMs) using a tannic acid (TA)-assisted adhesion strategy. The dressings exhibited high loading efficiency of PCN-224, good physiological stability, desirable biocompatibility, and were able to achieve bactericidal rates exceeding 99.99% against bacteria with only 10 minutes of irradiation. This breakthrough has important implications for wound disinfection in clinical settings.
CHEMICAL ENGINEERING JOURNAL
(2023)
Article
Infectious Diseases
Muhammad Imran Sajid, Sandeep Lohan, Shun Kato, Rakesh Kumar Tiwari
Summary: This study demonstrates the significant antimicrobial activity of the physical mixture of cyclic [R4W4] peptide and levofloxacin against various drug-resistant bacterial strains, and it is more effective than the covalent conjugate. The cytotoxicity of the cyclic [R4W4] peptide and levofloxacin conjugates is lower in breast cancer cells and normal kidney cells. The time-kill kinetic study shows rapid bactericidal action of the combination of [R4W4] and levofloxacin against drug-resistant bacteria.
Article
Biophysics
Shatabdi Das, Kumari Vishakha, Satarupa Banerjee, Debasish Nag, Arnab Ganguli
Summary: The study successfully eradicated diarrhoea-causing multi-drug resistant bacteria, including E. coli and S. flexneri, by loading tetracycline into biocompatible magnesium oxide nanoparticles. The nanoparticles also effectively reduced bacterial EPS production, antioxidant enzyme levels, and induced reactive oxygen species in bacterial cells.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2022)
Article
Nanoscience & Nanotechnology
Saeed Behzadinasab, Myra D. Williams, Mohsen Hosseini, Leo L. M. Poon, Alex W. H. Chin, Joseph O. Falkinham, William A. Ducker
Summary: Antimicrobial coatings, based on polydopamine adhesive, have been developed to effectively reduce the transmission of microbial diseases. These transparent coatings can inactivate microbes within minutes, with high efficiency, making them essential for applications such as antimicrobial cell phone screens.
ACS APPLIED MATERIALS & INTERFACES
(2021)
Article
Biochemistry & Molecular Biology
Fahima Bekka-Hadji, Isabelle Bombarda, Ferhat Djoudi, Sofiane Bakour, Abdelaziz Touati
Summary: Essential oils extracted from M. pulegium and A. herba alba showed antibacterial activities that were potentiated by antibiotics, especially against the multi-drug-resistant bacteria strain IRAB S3310. Synergistic effects were observed with different combinations of essential oils and antibiotics, with the best results seen with A. herba alba essential oil in association with cefoxitin against MRSA S19, and with M. pulegium in association with amikacin against IRAB S3310.
Review
Chemistry, Medicinal
Kadja Luana Chagas Monteiro, Osmar Nascimento Silva, Igor Jose dos Santos Nascimento, Francisco Jaime Bezerra Mendonca Junior, Pedro Gregorio Vieira Aquino, Edeildo Ferreira da Silva-Junior, Thiago Mendonca de Aquino
Summary: The discovery of antibiotics revolutionized medicine by providing effective treatments for various bacterial infections. However, the indiscriminate use of antibiotics has led to the emergence of antibiotic-resistant strains. Recent advances in molecular biology and microbiology have opened new possibilities in drug design and development, allowing the generation of new drugs that are not affected by bacterial resistance mechanisms. Additionally, the combination of drugs with adjuvants shows promise in combating bacterial resistance. This manuscript aims to address the mechanisms of bacterial resistance from a medicinal chemistry perspective and discuss potential strategies for developing new antibiotics.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Lulu Liu, Wanfeng Wu, Yan Fang, Haoqiang Liu, Fei Chen, Minwei Zhang, Yanan Qin
Summary: Functionalized poly-ethylene glycol MoS2 nanoflowers with excellent photothermal conversion efficiency and stability were synthesized via a one-step hydrothermal method. These nanoflowers exhibited significant inhibition of antibiotic resistant bacteria under NIR laser irradiation, making them a promising solution for combating ARB.
Article
Biochemistry & Molecular Biology
Claudia Ardino, Filomena Sannio, Carolina Pasero, Lorenzo Botta, Elena Dreassi, Jean-Denis Docquier, Ilaria D'Agostino
Summary: Trifluoroacetic acid (TFA) is commonly used in synthetic strategies due to its strong acidity and low boiling point. However, residual amounts of TFA may affect the accuracy of cellular assays. This study evaluates the effect of different counterions on the biological activity of an antibacterial compound and optimizes the preparation methods.
MOLECULAR DIVERSITY
(2023)
Article
Chemistry, Physical
Naeem Asad, Davide Deodato, Sangram Gore, Timothy M. Dore
Summary: By functionalizing four derivatives, the release of tertiary amines via two-photon excitation (2PE) was studied. These derivatives exhibited good properties in biological settings and an optimized photoremovable protecting group (PPG) mediated the efficient photoactivation of various biological effectors.
Article
Biochemistry & Molecular Biology
Annalaura Brai, Federica Poggialini, Chiara Vagaggini, Claudia Pasqualini, Sauro Simoni, Valeria Francardi, Elena Dreassi
Summary: A novel, cheap and convenient toxicity model using Tenebrio molitor coleoptera (TMC) was developed for preliminary evaluation of drug safety and metabolite formation. The results demonstrate that TMC can be used as a preliminary toxicity model to assess the safety of experimental compounds and the formation of main metabolites, and to reduce the costs and number of rodents, according to 3R principles.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Loic Martinet, Aymeric Naome, Lucas C. D. Rezende, Deborah Tellatin, Bernard Pignon, Jean-Denis Docquier, Filomena Sannio, Dominique Baiwir, Gabriel Mazzucchelli, Michel Frederich, Sebastien Rigali
Summary: Streptomyces lunaelactis strains isolated from moonmilk deposits exhibit significant heterogeneity in the content of biosynthetic gene clusters (BGCs) for specialized metabolite production. Specifically, the cryptic BGC 28a is carried only by a subgroup of S. lunaelactis strains and is predicted to produce nonribosomal peptide antibiotics containing piperazic acid (Piz). Through metabolomics and peptidogenomics analysis, the cyclic hexapeptide lunaemycin A, with a unique amino acid sequence, was identified as the main compound synthesized by BGC 28a. Lunaemycins demonstrated potent bactericidal activity against Gram-positive bacteria, including multi-drug resistant clinical isolates. This study highlights the importance of accurate in silico analysis in elucidating the structure and bioactivity of cryptic BGCs.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Agriculture, Multidisciplinary
A. Brai, C. Vagaggini, C. Pasqualini, F. Poggialini, F. Tarchi, V. Francardi, E. Dreassi
Summary: This study demonstrates that distillery by-products contain abundant antioxidant compounds and beneficial fatty acids even after processing. Using them as feed for Tenebrio molitor larvae not only increases the average weight gain of the larvae but also has no effect on their survival rate. Furthermore, the use of these by-products can enhance the total antioxidant activity and improve the nutraceutical properties of the larvae.
JOURNAL OF INSECTS AS FOOD AND FEED
(2023)
Article
Agriculture, Multidisciplinary
A. Brai, F. Poggialini, C. I. Trivisani, C. Vagaggini, F. Tarchi, V. Francardi, E. Dreassi
Summary: Circular economy principles combined with the search for novel sustainable functional foods can transform agricultural waste into feed supplements, creating benefits for the environment, industries, and consumers. The study found that using tomato peels and seeds, olive and mastic leaves as feed supplements efficiently supported the growth of Tenebrio molitor larvae, increased antioxidant activities, and improved fatty acid composition.
JOURNAL OF INSECTS AS FOOD AND FEED
(2023)
Article
Chemistry, Medicinal
Maria Grazia Martina, Federica Giammarino, Ilaria Vicenti, Elisabetta Groaz, Jef Rozenski, Matteo Incerti, Filomena Sannio, Jean Denis Docquier, Maurizio Zazzi, Marco Radi
Summary: The increasing number of viral outbreaks in recent years calls for the development of novel broad-spectrum antivirals. Non-natural nucleosides have shown to be successful in treating infectious diseases and new base-modified nucleosides were developed for potential antimicrobial activity against different viruses and bacteria.
Review
Biochemistry & Molecular Biology
Annalaura Brai, Federica Poggialini, Claudia Pasqualini, Claudia Immacolata Trivisani, Chiara Vagaggini, Elena Dreassi
Summary: Vaccines are crucial for preventing pathogen diffusion and cancer. The addition of adjuvants enhances the immune response to antigens, improving the effectiveness and duration of protection. The search for new adjuvants has increased in recent decades, uncovering novel classes and mechanisms of action, but there is still much to learn.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Chiara Dalla Torre, Filomena Sannio, Mattia Battistella, Jean-Denis Docquier, Marta De Zotti
Summary: New classes of antibacterial drugs, such as cationic trichogin analogs, show strong activity against clinically relevant bacterial species, including antibiotic-resistant strains. These modified natural peptides provide potential therapeutic options for addressing antibiotic resistance and developing improved antibacterial agents.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Marialuigia Fantacuzzi, Ilaria D'Agostino, Simone Carradori, Francesco Liguori, Fabrizio Carta, Mariangela Agamennone, Andrea Angeli, Filomena Sannio, Jean-Denis Docquier, Clemente Capasso, Claudiu T. Supuran
Summary: Vibrio cholerae, a pathogen responsible for life-threatening infections in low-income countries, has developed resistance to antibacterial drugs. Researchers have identified carbonic anhydrases (CAs) encoded by V. cholerae as potential pharmacological targets. They have developed a large library of CAs inhibitors with different flexibility degrees and found compounds with strong inhibition against Vch alpha CA. Computational studies have provided insights into the inhibitory activity and isoform selectivity of these compounds.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Lorenzo Jacopo Ilic Balestri, Claudia Immacolata Trivisani, Francesco Orofino, Diego Fiorucci, Giuseppina Ivana Truglio, Ilaria D'Agostino, Federica Poggialini, Lorenzo Botta, Jean-Denis Docquier, Elena Dreassi
Summary: Our research group has been studying the development of macrocyclic amidinoureas (MCAs) as antifungal agents. Through in silico target fishing study, we identified chitinases as one of their potential targets. Compound 3f emerged as a promising inhibitor of acidic mammalian chitinase (AMCase) with improved potency and selectivity.
ACS MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Chemistry, Analytical
Chiara Vagaggini, Annalaura Brai, Denise Bonente, Jessica Lombardi, Federica Poggialini, Claudia Pasqualini, Virginia Barone, Claudio Nicoletti, Eugenio Bertelli, Elena Dreassi
Summary: In this study, a sensitive and reproducible LC-MS/MS method was developed and validated for the quantification of short-chain fatty acids (SCFAs) in human, rat, and mouse plasma. The method showed good performance in terms of recovery (> 80%), precision (RSD <14%), accuracy (RE < ± 10%), and sensitivity (LOQ of 0.01 μM for acetic, butyric, propionic, and isobutyric acid). The results highlighted the correlation between plasma concentrations of SCFAs and age, emphasizing the importance of developing a reliable method for their quantification to study their biological role.
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
(2023)
Article
Biochemistry & Molecular Biology
Marisanna Centini, Isabel Martinez-Sanudo, Marco Biagi, Elena Dreassi, Luca Mazzon, Laura Marri
Summary: In recent years, the use of bacteria for carotenoid production has gained attention as a sustainable alternative to expensive and technically challenging chemical synthesis. This study reports the isolation of an orange-pigmented bacterium from the gut of adult olive flies, contributing to the repertoire of carotenogenic bacteria. The isolated bacterium, designated as M3d10, was found to be a derivative of hydroxylated astaxanthin through preliminary characterization.
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)