Article
Biology
Maqsood Ahmad Malik, Shroog ShdiedRoyji Albeladi, Saleh Mohammed Al-Maaqar, Abdulmohsen Ali Alshehri, Shaeel Ahmed Al-Thabaiti, Imran Khan, Majid Rasool Kamli
Summary: Bimetallic Ag-Cu nanoparticles with enhanced electronic, catalytic, and optical properties were synthesized from leaf extracts of sage. The nanoparticles showed antibacterial and antibiofilm effects against both Gram-positive and Gram-negative bacteria strains, suggesting their potential as novel antibacterial agents.
Article
Multidisciplinary Sciences
Jiong Zhang, Xiangxiang Zhao, John R. Cappiello, Yi Yang, Yunfei Cheng, Guang Liu, Wenjing Fang, Yinzhu Luo, Yu Zhang, Jiajia Dong, Lixin Zhang, K. Barry Sharpless
Summary: A series of arylfluorosulfates synthesized via SuFEx, including compounds 3, 81, and 101, showed potent antibacterial activity, the ability to overcome multidrug resistance, and a lack of susceptibility to resistance development. These compounds also demonstrated rapid bactericidal potency, selectivity against gram-positive bacteria, and the capability to disrupt bacterial biofilms and kill persisters. Additionally, compound 3 exhibited synergy with streptomycin and gentamicin, while their anti-MRSA activity was evaluated using the Caenorhabditis elegans model.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2021)
Article
Biochemistry & Molecular Biology
Jing Li, Ru Si, Qingqing Zhang, Yanchen Li, Jie Zhang, Yuanyuan Shan
Summary: Based on the scaffold hybridization strategy, twenty-four indole-guanidines were designed and synthesized. Most of these hybrids exhibited moderate to high anti-proliferative activity against various cancer cells, especially human hepatoma cell lines. Selectivity investigation showed that the hybrids had the best selectivity for the SMMC-7721 subtype in human hepatoma cells. Particularly, compound 22 demonstrated potent inhibition against SMMC-7721 cells, inducing apoptosis and cell cycle arrest in a dose-dependent manner, while down-regulating the expression of specific proteins.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Review
Pharmacology & Pharmacy
Michael A. Serwetnyk, Brian S. J. Blagg
Summary: Hsp90 is a crucial molecular chaperone with potential as a target for cancer therapy. In addition to known inhibitory mechanisms, alternative approaches for Hsp90 inhibition are being explored.
ACTA PHARMACEUTICA SINICA B
(2021)
Article
Agronomy
Jiao-Jiao Zhang, Yu-Mei Feng, Jun-Rong Zhang, Wan-Lin Xiao, Shuai-Shuai Liu, Xiang Zhou, Heng Zhang, Pei-Yi Wang, Li-Wei Liu, Song Yang
Summary: A series of simple triclosan derivatives containing isopropanolamine moiety were designed and assessed for their antibacterial behavior. Some compounds showed excellent bioactivity against three destructive bacteria. Compound C-8 displayed high bioactivities towards Xoo and Xac.
PEST MANAGEMENT SCIENCE
(2023)
Article
Chemistry, Multidisciplinary
Zhennan Zhao, Huinan Li, Xuan Tao, Yanxuan Xie, Liang Yang, Zong-Wan Mao, Wei Xia
Summary: A novel ruthenium-based compound with dual functionality as a boronic acid-decorated photosensitizer and light-triggered nitric oxide releasing agent is reported in this study. The compound can selectively attach to bacterial membranes and biofilms, effectively eradicating Pseudomonas aeruginosa biofilms through simultaneous release of NO and ROS. It shows higher efficacy than the clinical antibiotic tobramycin, with excellent bacterial specificity and no significant cytotoxicity to human cells, suggesting potential applications in combatting bacterial biofilm infections.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Article
Chemistry, Multidisciplinary
Shuwen Guo, Qiaoxian Huang, Yuan Chen, Jianwen Wei, Jun Zheng, Leyong Wang, Yitao Wang, Ruibing Wang
Summary: A novel guanidinium-functionalized pillar[5]arene, GP5, was designed and synthesized to effectively combat bacterial biofilms. GP5 showed high antibacterial potency against Gram-negative and Gram-positive strains and successfully disrupted preformed biofilms by penetrating biofilm barriers and destroying biofilm-enclosed bacteria. Additionally, host-guest complexation between GP5 and cefazolin sodium exhibited synergistic disruption activity against biofilms, providing a novel supramolecular platform for biofilm eradication.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Chemistry, Medicinal
Yongzhi Chen, Hongxia Li, Jiayong Liu, Rongcui Zhong, Haizhou Li, Shanfang Fang, Shouping Liu, Shuimu Lin
Summary: The emergence of bacterial multidrug resistance and the lack of new antimicrobial agents have led to the urgent need for the discovery and development of novel antibacterials. Antimicrobial peptidomimetics have shown promise in overcoming antibiotic resistance and are effective in rapidly killing bacteria without inducing resistance. Specific compounds have demonstrated potent activity against Gram-positive bacteria, low toxicity to mammalian cells, good stability, and high efficacy in treating bacterial infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Microbiology
Jiya Singh, Viswanathan Vijayan, Saiema Ahmedi, Pradeep Pant, Nikhat Manzoor, Tej P. Singh, Pradeep Sharma, Sujata Sharma
Summary: The study demonstrates that lactosmart may serve as a promising new potent antimicrobial agent, showing better inhibitory effects against pathogenic microorganisms compared to native LF. The research findings highlight the tighter binding of LPS to lactosmart, indicating its potential as a targeted approach against pro-inflammatory responses caused by LPS exposure in bacterial infections.
FRONTIERS IN MICROBIOLOGY
(2021)
Article
Microbiology
Yu-Bin Bai, Meng-Yan Shi, Wei-Wei Wang, Ling-Yu Wu, Yu-Ting Bai, Bing Li, Xu-Zheng Zhou, Ji-Yu Zhang
Summary: A new antibacterial strategy based on inhibiting bacterial quorum sensing has been identified as a promising method to reduce bacterial pathogenicity and prevent antibiotic resistance. Echinatin (Ech) was screened as a highly effective anti-quorum sensing compound. The results showed that Ech interfered with quorum sensing phenotype and synergistically enhanced the antibacterial activity of marketed antibiotics against Escherichia coli.
FRONTIERS IN MICROBIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Petr Jaros, Elizaveta Timkina, Jana Michailidu, Dominik Marsik, Marketa Kulisova, Irena Kolouchova, Katerina Demnerova
Summary: Boswellic acids, derived from Boswellia sp. plants, have positive effects on human health, especially in treating inflammation, arthritis, or asthma. This study found that boswellic acids have antimicrobial and antibiofilm effects, and they synergize with commonly available antibiotics.
Article
Chemistry, Multidisciplinary
Andrei Diaconu, Tom Coenye, Mihail Barboiu, Stephane P. Vincent
Summary: Dynamic constitutional frameworks (DCFs) composed of trialdehyde core, diamine PEG connector, and various neutral, anionic, or cationic heads demonstrated effective biofilm inhibition or disruption. Among them, polycationic DCFs showed the best antibiofilm activity, with the nature of cationic heads playing a significant role. DCF3B exhibited the best antibiofilm activity, while DCF3C, with a guanidinium functional head, was superior in inhibiting biofilm growth in an advanced in vitro biofilm model of chronic wound infection.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Nanoscience & Nanotechnology
Dengyan Wu, Dong Wei, Maotao Du, Song Ming, Qian Ding, Ranjing Tan
Summary: In this study, novel chitosan and poly (D,L-lactide-co-glycolide) nanoparticles loaded with benzalkonium bromide (BZK) were developed for wound healing after MRSA infection. These nanoparticles exhibited significant antibacterial activity, anti-biofilm properties, and the ability to damage bacterial cell walls, indicating their potential in promoting skin wound healing. These findings suggest a new avenue for nanomedicine development in wound treatment.
INTERNATIONAL JOURNAL OF NANOMEDICINE
(2021)
Correction
Chemistry, Multidisciplinary
Zhangyong Si, Wenbin Zhong, Dicky Prananty, Jianghua Li, Chong Hui Koh, En-Tang Kang, Kevin Pethe, Mary B. Chan-Park
Summary: This article reviews the research progress of polymers as advanced antibacterial and antibiofilm agents for direct and combination therapies. By modulating the physicochemical properties and functional modifications of materials, polymers have demonstrated excellent antibacterial and antibiofilm activities and have shown broad prospects for application.
Article
Polymer Science
Xuanyu Shentu, Yong Guan, Lili Wang, Jin Pan, Anna Zheng, Dafu Wei, Xiang Xu
Summary: A novel antimicrobial agent PPMG was successfully prepared and grafted onto down fibers through melt polycondensation, resulting in modified down fibers with efficient and durable antimicrobial properties against Escherichia coli and Staphylococcus aureus even after multiple washings.
POLYMERS FOR ADVANCED TECHNOLOGIES
(2021)
Article
Ophthalmology
Parthasarathi Kalaiselvan, Muhammad Yasir, Ajay Kumar Vijay, Mark D. P. Willcox, Shyam Tummanapalli
Summary: This study evaluated the persistence of disinfection of three different hand sanitizers. The results showed that hand sanitizers containing capric acid or alcohol had better microbial inhibitory effects, which could help reduce the spread of microbes.
CLINICAL AND EXPERIMENTAL OPTOMETRY
(2023)
Article
Biochemistry & Molecular Biology
Emma-Lucille Blayney, Milna Chennath, Charles G. Cranfield, Ronald J. Clarke
Summary: The Na+, K+-ATPase is an integral membrane protein that uses ATP hydrolysis to transport Na+ and K+ ions across the plasma membrane. It has essential roles in various physiological processes and is regulated through phosphorylation by protein kinase C (PKC) and Src kinase families. The study used the mirror tree method to analyze the coevolution between these kinases and Na+, K+-ATPase. The results suggested that the theta and eta isoforms of PKC and Src kinase are the most likely to interact with Na+, K+-ATPase. These findings will guide future experimental studies.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Michael Chhor, Esra Tulpar, Tara Nguyen, Charles G. Cranfield, Catherine A. Gorrie, Yik Lung Chan, Hui Chen, Brian G. Oliver, Lana McClements, Kristine C. McGrath
Summary: Cardiovascular disease (CVD) is a leading cause of death globally, with smoking being a major risk factor. Quitting smoking is challenging due to nicotine addiction and withdrawal symptoms. Electronic cigarettes (e-Cigs) have emerged as an alternative, but their cardiovascular effects are unclear.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Infectious Diseases
Rajesh Kuppusamy, Muhammad Yasir, Tsz Tin Yu, Florida Voli, Orazio Vittorio, Michael J. Miller, Peter Lewis, David StC Black, Mark Willcox, Naresh Kumar
Summary: There is an urgent need for new antimicrobial agents to address the global increase in antibiotic resistance. This study focused on producing short amphiphilic antibacterial and antibiofilm agents by modifying the hydrophobic and cationic groups of anthranilamide peptidomimetics. The addition of a lysine cationic group at the tail position significantly enhanced activity against E. coli and reduced cytotoxicity against mammalian cells. These compounds demonstrated notable disruption of preformed biofilms of S. aureus at micromolar concentrations.
Article
Nanoscience & Nanotechnology
Upeksha Mirissa Lankage, Stephen A. Holt, Samara Bridge, Bruce Cornell, Charles G. Cranfield
Summary: This study introduces a sparsely tethered triglyceride substrate for the impedance sensing of lipase activity in real time. The substrate can form an anchored bilayer off the gold electrode, allowing for ion transport through membrane defects caused by enzymatic hydrolysis. The rapid and reliable detection method has potential applications in disease studies, monitoring of lipase production, and point-of-care diagnostics.
ACS APPLIED MATERIALS & INTERFACES
(2023)
Article
Biochemistry & Molecular Biology
Katrina Browne, Rajesh Kuppusamy, William R. Walsh, David StC Black, Mark D. P. Willcox, Naresh Kumar, Renxun Chen
Summary: Antibiotic resistance is a global challenge, and combination therapies using antibiotics and antimicrobial peptidomimetics can mitigate the development of resistance in bacteria. This strategy demonstrates synergistic activity against both Gram-positive and Gram-negative bacteria and has significant potential in clinical applications.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Pharmacology & Pharmacy
Anuja Dahal, Kamal Shrestha, Rashmi Karki, Saraswati Bhattarai, Shiva Aryal, Satish Kumar Deo, Balmukunda Regmi, Mark Willcox, Shyam Kumar Mishra
Summary: This study analyzed the antibiotic sensitivity and biofilm-forming ability of urinary tract infection strains from renal disease patients. The results showed that the most common uropathogens in renal disease patients were Escherichia coli, Klebsiella pneumoniae, and Enterococcus spp. Some antibiotics such as amikacin, meropenem, and cefoperazone-sulbactam were effective against Gram-negative bacteria, while doxycycline, nitrofurantoin, and tetracycline were effective against Gram-positive bacteria. Additionally, most strains were capable of forming biofilms, and 70.8% were multidrug-resistant. Therefore, aminoglycoside, carbapenem, beta-lactam combination agents, and nitrofuran group of antibiotics may be the optimal first-line empirical therapies for uropathogens in hospitalized renal disease patients. Regular surveillance of resistance patterns and the study of biofilm formation in uropathogens are important for effective management of the patients.
JOURNAL OF CLINICAL PHARMACY AND THERAPEUTICS
(2023)
Article
Chemistry, Physical
Sudip Chakraborty, Georgio Katsifis, Iman Roohani, Cyrille Boyer, David McKenzie, Mark D. P. Willcox, Renxun Chen, Naresh Kumar
Summary: This study demonstrates the efficacy of an antibacterial polymer as a coating material for hydroxyapatite and glass surfaces, which are widely used in orthopedics and biomedical sciences. Both physical and covalent attachment modes of the polymer to the material surfaces were explored. The modified surfaces showed significant antibacterial activity against Gram-negative bacterium E. coli, and the activity persisted for a prolonged period on the covalently modified materials' surfaces.
Article
Biochemistry & Molecular Biology
Floriana Cappiello, Sudhir Verma, Xiao Lin, Isabel Y. Moreno, Bruno Casciaro, Debarun Dutta, Alison M. McDermott, Mark Willcox, Vivien J. Coulson-Thomas, Maria Luisa Mangoni
Summary: The corneal epithelium is essential for both vision and immune defense. Corneal abrasion can lead to severe eye infections, but recent research has discovered peptides that not only treat keratitis but also promote corneal wound healing, which could have potential clinical applications.
Article
Infectious Diseases
Sahil Shandil, Tsz Tin Yu, Shekh Sabir, David StC. Black, Naresh Kumar
Summary: As bacteria develop resistance against antimicrobials, alternative methods to tackle this issue must be developed. In this study, quinazolinone inhibitors were designed using molecular docking to target the pqs system in P. aeruginosa. Compound 6b showed the highest pqs inhibitory activity and no bacterial growth inhibition.
Review
Infectious Diseases
Shakeel Shahzad, Mark D. P. Willcox, Binod Rayamajhee
Summary: The global rise in antibiotic resistance in bacteria has become a major challenge in treating infectious diseases. This literature review aims to decipher the evolving mechanisms of resistance to polymyxins among clinically significant pathogens. Understanding these mechanisms may help develop suitable methods for detecting polymyxin resistance determinants and the development of novel antimicrobial molecules.
Article
Infectious Diseases
Umme Laila Urmi, Samuel Attard, Ajay Kumar Vijay, Mark D. P. Willcox, Naresh Kumar, Salequl Islam, Rajesh Kuppusamy
Summary: The development of potent antiviral agents is crucial for combating viral infections worldwide. In this study, the antiviral potential of 17 peptidomimetic compounds was evaluated against MHV-1 and HSV-1. Compounds 11 and 14 showed the most potent inhibitory effects, and they were found to directly influence the viral envelope. These findings suggest that peptidomimetic compounds could offer a new approach for the development of potent antiviral agents.
Meeting Abstract
Biophysics
Ronald J. Clarke, Bogdan Lev, Milna Chennath, Toby W. Allen, Charles G. Cranfield, Emma-Lucille Blayney, Flemming Cornelius
BIOPHYSICAL JOURNAL
(2023)
Article
Chemistry, Organic
Faiza Diaba, Gisela Trenchs
Summary: The first violet light-mediated synthesis of gamma- and delta-lactams from N-alkenyl trichloroacetamides is reported in this paper. The reactions are conducted in tetrahydrofuran or 2-methyltetrahydrofuran as the sole solvent without catalysts or additives, under non-anhydrous conditions in an air atmosphere where the solvent serves as the radical initiator.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Feroze Hussain, Sajjad Ahmed, Ashiq Hussain Padder, Qazi Naveed Ahmed
Summary: This study reports a novel and efficient one-pot synthesis method for mixed phosphorotrithioates, which does not require supplementary additives and shows broad applicability.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Hyunjin Oh, Ikyon Kim
Summary: A new 1,2,4-triazole-pyrrolo[1,2-a]pyrazine hybrid system, 6-acylpyrrolo[1,2-a][1,2,4]triazolo[5,1-c]pyrazine, was synthesized using a catalyst-free method. This method involved sequential exposure of pyrrole-2-carbonitrile-derived substrates to DMF-DMA and acyl hydrazide, resulting in the formation of acylated pyrazine and 1,2,4-triazole rings, enabling the installation of various substituents at specific positions on the core skeleton.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Ming Yan, Si-fan Wang, Yong-po Zhang, Jin-zhong Zhao, Zhuo Tang, Guang-xun Li
Summary: Here we developed an efficient photocatalytic approach for the convenient preparation of sulfinamides. The reaction allows for the gram-scale preparation of sulfinamides and the one-pot synthesis of various sulfonyl amides.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Farzaneh Bandehali-Naeini, Zahra Tanbakouchian, Noushin Farajinia-Lehi, Nicolas Mayer, Morteza Shiri, Martin Breugst
Summary: Two tandem catalytic systems were developed for the synthesis of novel 3,4-disubstituted maleimides using the same Ugi adducts. Different maleimide structures can be synthesized using either Pd or Cu catalysis.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Tanya Raghava, Anjan Chattopadhyay, Subhadeep Banerjee, Nivedita Sarkar
Summary: Amine substitution of two ortho fluorine atoms of tetrafluoroterephthalonitrile through SNAr chemistry is easily achievable. But further fluorine substitution is only possible under forcing conditions, yielding valuable fluorophores for bioimaging.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Review
Chemistry, Organic
Anju Chadha, Santosh Kumar Padhi, Selvaraj Stella, Sowmyalakshmi Venkataraman, Thangavelu Saravanan
Summary: Alcohol dehydrogenases are enzymes that use cofactors for oxidation or reduction reactions of alcohols or carbonyl compounds. They are utilized in green chemistry and have applications in the production of pharmaceuticals. Recombinant enzymes have solved the challenge of producing purified enzymes in large quantities. Engineered alcohol dehydrogenases have been used in asymmetric synthesis in industry. Various methods have been established for regenerating expensive cofactors to make the enzymatic process more efficient and economically viable.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)