Article
Chemistry, Multidisciplinary
Ryo Okamoto, Hiroyuki Shibata, Takahiro Yatsuzuka, Takuya Hanao, Yuta Maki, Kazuya Kabayama, Ayane Miura, Koichi Fukase, Yasuhiro Kajihara
Summary: This paper introduces a new peptide derivative called peptide-aminothiazoline, which plays a crucial role in sequential peptide coupling and demonstrates the convergent synthesis of circular proteins and homogeneous glycoproteins.
CHEMICAL COMMUNICATIONS
(2023)
Article
Pharmacology & Pharmacy
Hyeju Lee, Byeongkwon Kim, Minju Kim, Seoyeong Yoo, Jinkyeong Lee, Eunha Hwang, Yangmee Kim
Summary: The antimicrobial peptide T. ni cecropin demonstrated significant antibacterial and antibiofilm activities against colistin-resistant Escherichia coli. It targeted the outer membrane of E. coli and interacted strongly with lipopolysaccharide. Additionally, T. ni cecropin showed anti-inflammatory and anti-septic effects, suggesting its potential as a therapeutic agent.
Review
Biochemistry & Molecular Biology
Luis Uriel Gonzalez-Avila, Miguel Angel Loyola-Cruz, Cecilia Hernandez-Cortez, Juan Manuel Bello-Lopez, Graciela Castro-Escarpulli
Summary: The increased use of antimicrobials like colistin has led to the emergence of colistin-resistant Aeromonas strains. These strains have been found not only in clinical settings, but also in environmental and animal isolates, identified by detection of mcr genes. Different mcr variants have been detected in Aeromonas from various sources, including animals, environments, and human samples. This article provides an overview of colistin resistance in Aeromonas, along with general characteristics of the molecule and recommended methods for determining colistin resistance in certain Aeromonas species.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Engineering, Biomedical
Nhan D. T. Tram, Vanitha Selvarajan, Alister Boags, Devika Mukherjee, Jan K. Marzinek, Bernadette Cheng, Zi-Chen Jiang, Pascal Goh, Jun-Jie Koh, Jeanette W. P. Teo, Peter J. Bond, Pui Lai Rachel Ee
Summary: By examining the significance of the turn region of beta-hairpin peptides, valuable knowledge was presented for the design of novel antimicrobial peptides. The de novo designed synthetic peptides displayed selective activity against Gram-negative bacteria and potent activity against clinically relevant antibiotic-resistant strains. Our peptides showed robust bactericidal activity in challenging conditions and were non-cytotoxic against human cells.
ACTA BIOMATERIALIA
(2021)
Article
Chemistry, Organic
Shingo Takiguchi, Yuki Hirota-Takahata, Takahide Nishi
Summary: The absolute configuration of ogipeptins has been elucidated by the successful total synthesis of ogipeptin A.
Article
Agriculture, Multidisciplinary
Hong-hao Huang, Yi-xing Lu, Su-juan Wu, Zhen-bao Ma, Dong-ping Zeng, Zhen-ling Zeng
Summary: Carbapenem- and colistin-resistant Enterobacter strains harboring blaIMI were isolated from intestinal samples and the environment of a duck farm in China. The study demonstrated the diversity of carbapenemases in a duck farm and provided evidence for the transmission of bla(IMI) genes. Whole-genome sequencing and comparative genetic analysis revealed the presence of chromosomal and plasmid bla(IMI) and identified the horizontal transmission of bla(IMI)-carrying plasmids.
JOURNAL OF INTEGRATIVE AGRICULTURE
(2023)
Article
Engineering, Biomedical
Ziyi Lu, Yueming Wu, Zihao Cong, Yuxin Qian, Xue Wu, Ning Shao, Zhongqian Qiao, Haodong Zhang, Yunrui She, Kang Chen, Hengxue Xiang, Bin Sun, Qian Yu, Yuan Yuan, Haodong Lin, Meifang Zhu, Runhui Liu
Summary: The peptide polymer-modified thermoplastic polyurethane (TPU) surfaces exhibit broad-spectrum antibacterial properties and good biocompatibility, functioning through a contact-killing mechanism by disrupting the bacterial membrane.
BIOACTIVE MATERIALS
(2021)
Article
Pharmacology & Pharmacy
Sandra Patricia Rivera-Sanchez, Ivan Dario Ocampo-Ibanez, Yamil Liscano, Natalia Martinez, Isamar Munoz, Marcela Manrique-Moreno, Luis Martinez-Martinez, Jose Onate-Garzon
Summary: This study investigates the interaction between a cationic antimicrobial peptide (CAMP) derived from Cecropin D-like and bacterial-like model membranes of colistin-resistant Pseudomonas aeruginosa (CRPa) strains. The experimental analysis shows that the peptide interacts with the lipids of CRPa membranes, resulting in an increase in the phase transition temperature of the lipid systems and a transition in the peptide's secondary structure.
Article
Microbiology
Do-Hoon Lee, Ju-Hee Cha, Dae-Wi Kim, Kihyun Lee, Yong-Seok Kim, Hyo-Young Oh, You-Hee Cho, Chang-Jun Cha
Summary: A novel colistin resistance mechanism via enzymatic inactivation of the drug was discovered and its clinical importance in microbial communities during polymicrobial infections was proposed.
Article
Biochemistry & Molecular Biology
Rani Maharani, Hasna Noer Agus Yayat, Ace Tatang Hidayat, Jamaludin Al Anshori, Dadan Sumiarsa, Kindi Farabi, Tri Mayanti, Desi Nurlelasari, Desi Harneti, Unang Supratman
Summary: Cyclopurpuracin was successfully synthesized using a combination of solid- and solution-phase synthetic methods. The precursor compounds were cyclised using the PyBOP/NaCl method, resulting in a cyclic product with similar NMR profiles to the natural product. The antimicrobial activity of cyclopurpuracin was evaluated, showing weak activity for the synthetic products and higher activity for the reversed cyclopurpuracin.
Article
Infectious Diseases
Michael Timmermans, Pierre Wattiau, Olivier Denis, Cecile Boland
Summary: This study identified a reservoir of mobile colistin resistance genes (mcr-1 to -5) in commensal Escherichia coli isolated from healthy pigs, cattle and poultry in Belgium over at least 5 years (2012-2016), highlighting the ongoing presence of colistin resistance genes in these animal populations.
INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS
(2021)
Review
Microbiology
Madubuike Umunna Anyanwu, Ishmael Festus Jaja, Obichukwu Chisom Nwobi, Anthony Christian Mgbeahuruike, Chinaza Nnenna Ikpendu, Nnenna Audrey Okafor, James Wabwire Oguttu
Summary: Mobile colistin resistance genes pose a threat to the treatment of infections caused by drug-resistant bacteria. The use of colistin in horses without sensitivity testing facilitates the acquisition of these resistance genes. The dissemination of these genes among horse populations is non-clonal and may involve other resistance genes.
Article
Chemistry, Medicinal
Cornelis J. Slingerland, Charlotte M. J. Wesseling, Paolo Innocenti, Koen G. C. Westphal, Rosalinde Masereeuw, Nathaniel I. Martin
Summary: Polymyxins are potent and specific anti-infective agents against Gram-negative bacteria. The synthesis and evaluation of novel polymyxin analogues with reduced nephrotoxic effects were described in this study.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Microbiology
Sarah E. Turbett, Ryan A. Bronson, Colin J. Worby, Graham E. G. McGrath, Emily Hodgkins, Margaret Becker, Barbara Belford, Lucyna Kogut, Elizabeth Oliver, Edward T. Ryan, Regina C. LaRocque, Ashlee M. Earl, Virginia M. Pierce
Summary: A bacterial species is considered to be intrinsically resistant to an antimicrobial when nearly all of the wild-type isolates exhibit sufficiently high MIC values, making susceptibility testing unnecessary and the antimicrobial unsuitable for therapy. In this study, we found that Hafnia spp. are intrinsically resistant to colistin. This recognition of phenotype will inform rational approaches to antimicrobial susceptibility testing and therapy for infections caused by Hafnia spp.
JOURNAL OF CLINICAL MICROBIOLOGY
(2023)
Article
Multidisciplinary Sciences
Qi Zhang, Runming Wang, Chunjiao Liu, Minji Wang, Mohamad Koohi-Moghadam, Pak-Leung Ho, Hongyan Li, Haibo Wang, Robert Bonomo, Hongzhe Sun
Summary: The study found that silver (Ag+), including silver nanoparticles, can restore the efficacy of colistin against mcr-positive bacteria by inhibiting the activity of the MCR-1 enzyme and slowing down the development of resistance. The combined use of Ag+ and colistin can relieve dermonecrotic lesions and reduce the bacterial load of mice infected with mcr-1-carrying pathogens. This suggests the potential of Ag+ as a broad-spectrum inhibitor for treating mcr-positive bacterial infections.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2022)
Review
Biochemistry & Molecular Biology
Beatriz G. G. de la Torre, Fernando Albericio
Summary: While the world was battling with the COVID-19 Omicron wave at the end of 2021, except for China, most countries ended 2022 with COVID-19 being treated like the flu. As a result, the U.S. Food and Drug Administration (FDA) only authorized 37 new drugs this year, compared to an average of 52 in the previous four years. This marks the second lowest number of drug approvals in the last six years, even though it may change in the future. The decrease in FDA approvals mainly applies to small molecule drugs, while biologics and TIDES have remained relatively constant.
Review
Chemistry, Multidisciplinary
Narges Hosseini Nasab, Fereshteh Azimian, Hendrik G. Kruger, Song Ja Kim
Summary: Coumarins, heterocyclic compounds with a benzo-a-pyrone structure, are widely used in pharmacology, cosmetics, chemical, and medicinal industries. Various methods and reactions have been employed to synthesize coumarin derivatives. This review covers the reactions of 3-acetylcoumarin with different reagents and provides an overview of various reactions of 3-acetylcoumarin, including multicomponent, cycloaddition, α-halogenation, aldol condensation, reduction, and 1,2-addition reactions. The synthesis of different compounds starting from 3-acetylcoumarins and their biological activities are presented. This review serves as a valuable resource for researchers in this field.
ARABIAN JOURNAL OF CHEMISTRY
(2023)
Article
Chemistry, Organic
Srinivas Ambala, Kimberleigh B. Govender, Kamal K. Rajbongshi, Thavendran Govender, Hendrik G. Kruger, Tricia Naicker, Per I. Arvidsson
Summary: Here, an effective and efficient transition metal-free method for the N-arylation of primary sulfonimidamides was reported. The benzyne intermediates generated from silyl aryl triflates successfully coupled with the primary sulfonimidamides, resulting in good to excellent yields. In addition, by adding 18-crown-6, the scope of this method was extended to tertiary sulfonimidamides with moderate to low yields.
TETRAHEDRON LETTERS
(2023)
Article
Chemistry, Medicinal
Byron K. Peters, Nakita Reddy, Mbongeni Shungube, Letisha Girdhari, Sooraj Baijnath, Sipho Mdanda, Lloyd Chetty, Thandokuhle Ntombela, Thilona Arumugam, Linda A. Bester, Sanil D. Singh, Anil Chuturgoon, Per I. Arvidsson, Glenn E. M. Maguire, Hendrik G. Kruger, Tricia Naicker, Thavendran Govender
Summary: Fi-lactams are the most commonly prescribed antibiotics due to their potent antimicrobial activities, but their efficacy is threatened by the alarming rates of antimicrobial resistance, particularly in carbapenem-resistant Enterobacterales expressing metallo-fi-lactamases (MBLs). In this study, a cyclic zinc chelator called BP1 was developed, which restored the efficacy of meropenem against MBL-expressing bacteria and showed no toxicity to human cells. The study also demonstrated the therapeutic potential of BP1 in reducing bacterial load in infected mice. These findings propose a promising strategy to combat antimicrobial resistance.
ACS INFECTIOUS DISEASES
(2023)
Article
Chemistry, Physical
Nkululeko E. Damoyi, Holger B. Friedrich, Gert H. Kruger, David J. Willock
Summary: Supported vanadium oxides are widely used catalysts for the selective oxidative dehydrogenation of alkanes to alkenes. The activity of these catalysts is influenced by the different oxygen species involved, with singly coordinated vanadyl V(V)=O being the most reactive. Understanding the relative activity of different oxygen species can help improve catalyst design and enhance productivity and selectivity in the reaction.
MOLECULAR CATALYSIS
(2023)
Article
Infectious Diseases
Nakita Reddy, Letisha Girdhari, Mbongeni Shungube, Arnoldus C. Gouws, Byron K. Peters, Kamal K. Rajbongshi, Sooraj Baijnath, Sipho Mdanda, Thandokuhle Ntombela, Thilona Arumugam, Linda A. Bester, Sanil D. Singh, Anil Chuturgoon, Per I. Arvidsson, Glenn E. M. Maguire, Hendrik G. Kruger, Thavendran Govender, Tricia Naicker
Summary: This study evaluated the use of a novel beta-lactamase inhibitor, BP2, in combination with meropenem to overcome resistance in hard-to-treat infectious diseases caused by virulent bacteria expressing beta-lactamases. The results showed that BP2 enhanced the activity of meropenem, exhibiting bactericidal effects with a MIC of <= 1 mg/L and was safe to use at the tested concentrations. BP2 also demonstrated strong inhibitory activity against NDM-1 and VIM-2, specifically targeting MBLs. In a murine infection model, the combination of BP2 and meropenem showed significant efficacy. These promising pre-clinical results make BP2 a suitable candidate for further research and development as a metallo-beta-lactamase inhibitor (MBLI).
Article
Chemistry, Multidisciplinary
K. P. Nandhini, Mahama Alhassan, Clinton G. L. Veale, Fernando Albericio, Beatriz G. de la Torre
Summary: The solid-phase synthesis of Met-containing peptides often leads to the formation of impurities, Met(O) and sulfonium salt, due to oxidation and S-alkylation reactions. These reactions occur during the final acidolytic cleavage step. In this study, two new cleavage solutions were developed to eliminate oxidation and reduce S-alkylation. The optimal mixture for Cys-containing peptides was TFA-anisole-TMSCl-Me2S-TIS with triphenyl phosphine, while TIS was not required for other peptides. Both cleavage solutions were effective for sensitive amino acids like Cys and Trp. The sulfonium salt was successfully reversed to free Met-containing peptide by heating with acetic acid.
Review
Biochemistry & Molecular Biology
Alexander C. Martins, Fernando Albericio, Beatriz G. de la Torre
Summary: The year 2022 saw the successful control of the COVID-19 pandemic in most countries through social and hygiene measures and vaccination campaigns. However, there was a decrease in total drug approvals by the FDA, particularly for small molecules. The Biologics class, on the other hand, maintained its figures with the authorization of 15 novel molecules.
Article
Biochemistry & Molecular Biology
Babita Kushwaha, Sinenhlanhla N. Mthembu, Anamika Sharma, Fernando Albericio, Beatriz G. de la Torre
Summary: We have synthesized disulfide-reducing agents DPDT and DMPDT from serinol and methyl serinol, respectively. DPDT demonstrated higher stability than DMPDT. The reducing capacity of DPDT was found to be comparable to that of DTT, and its effectiveness was evaluated in both liquid and solid phases.
Article
Chemistry, Multidisciplinary
Narges Hosseini Nasab, Hussain Raza, Young Seok Eom, Mubashir Hassan, Andrzej Kloczkowski, Lloyd Christopher Chetty, Hendrik Gert Kruger, Song Ja Kim
Summary: A series of 1,3,4-thiadiazole-thiazolidinone derivatives (7a-j) were synthesized and evaluated as carbonic anhydrase inhibitors. Compound 7i showed higher inhibitory activity (IC50 = 0.402 +/- 0.017 mu M) compared to the standard reference acetazolamide (IC50 = 0.998 +/- 0.046 mu M). Kinetic analysis revealed that compound 7i binds competitively to the target enzyme. Compound 7i also exhibited good conformational state and hydrogen bond interactions in the receptor binding pocket, according to molecular docking studies.
NEW JOURNAL OF CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Mbongeni Shungube, Ayanda K. Hlophe, Letisha Girdhari, Victor T. Sabe, Byron B. Peters, Nakita Reddy, Kehinde F. Omolabi, Lloyd Chetty, Thilona Arumugam, Anil Chuturgoon, Hendrik G. Kruger, Per I. Arvidsson, Hua-Li Qin, Tricia Naicker, Thavendran Govender
Summary: Beta-lactamases deactivate beta-lactam antibiotics through hydrolysis mechanism. This study developed 11 potential MBL inhibitors that successfully restored the effectiveness of meropenem against NDM-producing Klebsiella pneumoniae infections.
Article
Microbiology
Kehinde F. Omolabi, Nakita Reddy, Sipho Mdanda, Sphamandla Ntshangase, Sanil D. Singh, Hendrik G. Kruger, Tricia Naicker, Thavendran Govender, Sooraj Bajinath
Summary: The recent surge in beta-lactamase resistance has led to the emergence of superbugs, posing a significant threat to public healthcare. This study evaluated the potential of 1,4,7-triazacyclononane-1,4,7 triacetic acid (NOTA) as a metallo-beta-lactamase (MBL) inhibitor in combination with meropenem against MBL producing bacteria. The results showed that NOTA restored the efficacy of meropenem and significantly decreased the colony-forming units of carbapenem-resistant Klebsiella pneumoniae in a murine infection model.
FEMS MICROBIOLOGY LETTERS
(2023)
Review
Chemistry, Multidisciplinary
K. P. Nandhini, Danah Al Shaer, Fernando Albericio, Beatriz G. G. de la Torre
Summary: Peptide Nucleic Acids (PNAs) are important mimics of DNA/RNA that can effectively bind with high affinity and specificity. Due to their metabolic stability, PNAs have broad applications in various fields. However, PNA synthesis faces challenges such as difficulties in preparing monomers and their solubility, as well as obstacles related to intra/inter chain aggregation and side reactions. Different protecting group strategies can be employed to overcome these hurdles and optimize the synthesis process.
CHEMICAL SOCIETY REVIEWS
(2023)
Article
Chemistry, Organic
K. P. Nandhini, Sikabwe Noki, Edikarlos Brasil, Fernando Albericio, Beatriz G. de la Torre
Summary: Peptide Nucleic Acids (PNAs) are a class of synthetic biomolecules with great potential in medicine. A new PNA SPS strategy based on a safety-catch protecting group scheme has been developed, allowing the synthesis of PNAs using Boc as a temporal protecting group.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2023)
