Article
Biochemistry & Molecular Biology
Angela Di Somma, Carolina Cane, Natalie Paola Rotondo, Maria Maddalena Cavalluzzi, Giovanni Lentini, Angela Duilio
Summary: Medicinal plants from the genus Berberis, containing berberine alkaloids, show potential as sources of drugs to combat antimicrobial resistance. Berberine is effective against both Gram-negative and Gram-positive bacteria, affecting various cellular processes. Recent studies have explored the interaction between berberine derivatives and the essential bacterial protein FtsZ. In this study, the inhibition mechanisms of different berberine analogues were investigated on the recombinant FtsZ of Escherichia coli. Results showed that these compounds inhibited FtsZ activity through various mechanisms, with the tertiary amine 1c exhibiting the strongest inhibitory effects and interaction with FtsZ.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Hang Sun, Shi-Yu Huang, Ponmani Jeyakkumar, Gui-Xin Cai, Bo Fang, Cheng-He Zhou
Summary: Natural berberine-derived azolyl ethanols were designed and synthesized as new structural antibacterial agents to combat bacterial resistance, with potent activity against multidrug-resistant Escherichia coli. These compounds could rapidly kill bacteria and eradicate biofilms, aiding in alleviating bacterial resistance development.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Cui-Cui Chen, Yi-Qi Zhang, Dong-Xiao Zhong, Xuan-He Huang, Yi-Han Zhang, Wen-Hao Jiang, Ming Li, Qian Chen, Wing-Leung Wong, Yu-Jing Lu
Summary: The study revealed that two 9,10-dihydroacridine derivatives have strong antibacterial activity against selected Gram-positive bacteria by promoting FtsZ polymerization and disrupting Z-ring formation, leading to bacterial cell division interruption and cell death.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2021)
Article
Materials Science, Multidisciplinary
Alicja Warowicka, Mikolaj Koscinski, Maciej Waszczyk, Anna Gozdzicka-Jozefiak
Summary: The combination of natural plant compounds with collagen confers anti-inflammatory, antimicrobial, and antiviral activities to the material, enabling broad-spectrum applications in biomedicine.
MRS COMMUNICATIONS
(2022)
Review
Infectious Diseases
Yorinobu Maeda, Teruo Murakami
Summary: Small intestinal bacterial overgrowth (SIBO) is characterized by an increase in the number and/or alteration in the type of bacteria in the upper gastrointestinal tract, causing various bowel symptoms. SIBO can be diagnosed using microbial culture or breath tests after carbohydrate ingestion. However, these methods have limitations and risks. Urinary excretion tests using bile acid conjugates have shown potential as diagnostic substrates for SIBO. PABA-UDCA disulfate offers a simple and rapid method for evaluating SIBO. Treatments for SIBO include antibiotics, probiotics, therapeutic diets, herbal medicines, and fecal microbiota transplantation.
Article
Biotechnology & Applied Microbiology
Sinosh Skariyachan, Dhrithi Deshpande, Anusha Joshi, Nischita Subramanya, Shreeya Kale, Rajeswari Narayanappa
Summary: The study revealed that the physicochemical, heavy metal, and microbiological qualities of water samples from Bellandur Lake exceeded the permissible limits set by standard authorities. Most isolates were found to be multidrug-resistant against 44 antibiotics. Two isolates showing the highest resistance were identified through 16S rRNA gene sequencing. Treatment with isolated bacteriophages resulted in a 99.99% reduction in viable bacterial count in the lake water samples.
ENVIRONMENTAL TECHNOLOGY & INNOVATION
(2021)
Article
Materials Science, Multidisciplinary
Muhammad Abubaker Khan, Yangwei Wang, Muhammad Hamza, Ghulam Yasin, Mohammad Tabish, Chuangshi Feng, Waheed Qamar Khan, Tahir Ahmad, Wei-Bing Liao, Mohamed A. Afifi
Summary: High strain rate compression results in the growth and overlap of precipitates in the Al alloy, affecting its properties. With increasing strain rates, coarse precipitates are no longer effective in hindering dislocation motion, leading to a decrease in yield strength.
MATERIALS CHARACTERIZATION
(2021)
Article
Engineering, Chemical
Leo Desbois, Pierre Tchoreloff, Vincent Mazel
Summary: This study focuses on the influence of viscoplasticity on powder behavior and tablet properties. Experimental results show that viscoplasticity is not constant during compaction and transient phenomena and stress relaxation occur.
Article
Chemistry, Medicinal
Guilherme F. S. Fernandes, Debora L. Campos, Isabel C. Da Silva, Joao L. B. Prates, Aline R. Pavan, Fernando R. Pavan, Jean L. Dos Santos
Summary: This study synthesized and evaluated 23 new compounds against drug-resistant strains of M. tuberculosis, with compound 5 b standing out for its effectiveness against all multi-drug resistant strains, suggesting a potential different mechanism of action. Benzofuroxan compounds like 5 b show promising potency against replicating and drug-resistant strains of M. tuberculosis.
Article
Chemistry, Physical
Satyaveni Malasala, Anusha Polomoni, Md. Naiyaz Ahmad, Manjulika Shukla, Grace Kaul, Arunav Dasgupta, Sidharth Chopra, Srinivas Nanduri
Summary: TrmD, a tRNA-(N(1)G37) methyltransferase, is essential for the growth of various bacteria including Staphylococcus aureus, Pseudomonas aeruginosa, Mycobacterium tuberculosis, and Mycobacterium abscessus. In this study, a library of around 200 structurally diverse thienopyrimidines was designed, synthesized, and evaluated for their inhibitory activities against multiple pathogens. Several compounds showed promising inhibitory effects against M. tuberculosis and S. aureus, with compound 18f demonstrating selectivity against the latter. Further studies were conducted to understand the mechanism of action and physico-chemical properties of the selected compounds.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Biochemistry & Molecular Biology
Jose B. de Araujo-Neto, Maria M. C. da Silva, Cicera D. de M. Oliveira-Tintino, Ieda M. Begnini, Ricardo A. Rebelo, Luiz E. da Silva, Sandro L. Mireski, Michele C. Nasato, Maria I. L. Krautler, Jaime Ribeiro-Filho, Abolghasem Siyadatpanah, Polrat Wilairatana, Henrique D. M. Coutinho, Saulo R. Tintino
Summary: This study evaluated the antibacterial and antibiotic-modulating activities of 1,8-naphthyridine derivatives against multi-resistant bacterial strains. While the compounds themselves had no direct antibacterial activity, they were able to potentiate the activity of fluoroquinolone antibiotics, indicating a potential for synergism in combating multidrug resistant bacterial infections.
Article
Environmental Sciences
Haijie Li, Ruihua Mu, Yanhui He, Zihe Deng, Xiaocheng Liu, Wu Zhansheng
Summary: The study revealed that adding commercial microbial agents can significantly increase the cellulose degradation rate and seed germination index in spent mushroom substrate composting, promote organic matter decomposition, and enhance the quality of mature compost.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2022)
Article
Microbiology
Qian Wang, Juan Song, Jinlian Zhang, Xiaojuan Qin, Yihao Kang, Shilv Huang, Shengmao Zhou, Tingsu Chen
Summary: This study investigated the influence of microbial agents on the rhizosphere microbiota of ginger, providing novel technologies for preventing and controlling ginger wilt disease. The results showed that treating continuous cropping soil and newly planted ginger with microbial agents significantly increased yields and reduced ginger wilt disease. Additionally, changes in soil properties played a crucial role in shaping the bacterial community structure.
FRONTIERS IN MICROBIOLOGY
(2023)
Review
Infectious Diseases
Bharat Kumar Reddy Sanapalli, Akram Ashames, Dilep Kumar Sigalapalli, Afzal B. Shaik, Richie R. Bhandare, Vidyasrilekha Yele
Summary: Fused pyridines have diverse pharmacological activities and are widely used in medicinal chemistry. Imidazopyridines are important fused heterocycles with more diverse profiles. Researchers explore strategies for preparing other imidazopyridines and focus on the antibacterial profile and structure-activity relationship of synthesized derivatives, providing a foundation for creating novel antibacterial agents.
Article
Chemistry, Inorganic & Nuclear
Natalia Busto, Gloria Vigueras, Natalia Cutillas, Begona Garcia, Jose Ruiz
Summary: This study found that a new series of heteroleptic iridium(III) complexes showed remarkable effectiveness against Gram positive strains, especially Ir1 and Ir2, which were even 10 times more active than the fluoroquinolone antibiotic norfioxacin. The antimicrobial activity of these complexes is achieved by inducing ROS generation.
DALTON TRANSACTIONS
(2022)
Article
Chemistry, Medicinal
Kendall Carrasco, Camille Montersino, Carine Derviaux, Magali Saez-Ayala, Laurent Hoffer, Audrey Restouin, Remy Castellano, Justine Casassa, Philippe Roche, Eddy Pasquier, Sebastien Combes, Xavier Morelli, Yves Collette, Stephane Betzi
Summary: A BDII-selective compound was discovered through screening the Fr-PPIChem chemical library, showing low activity in cell-based assays but the ability to modulate anti-leukemic activity in combination with various drugs in a cell- and context-dependent differential manner.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Joelle Mesmar, Rola Abdallah, Adnan Badran, Marc Maresca, Abdullah Shaito, Elias Baydoun
Summary: This study summarizes the medicinal characteristics of Ziziphus nummularia, including its phytochemical contents and pharmacological activities in the treatment of various diseases. Ziziphus nummularia is rich in bioactive compounds and has demonstrated anti-inflammatory, antioxidant, antimicrobial, anthelmintic, antidiabetic, anticancer, analgesic, gastrointestinal activities, as well as anti-drought and anti-thermal characteristics.
Article
Chemistry, Medicinal
Elina Buitrago, Clarisse Faure, Marcello Carotti, Elisabetta Bergantino, Renaud Hardre, Marc Maresca, Christian Philouze, Nicolas Vanthuyne, Ahcene Boumendjel, Luigi Bubacco, Amaury du Moulinet d'Hardemare, Helene Jamet, Marius Reglier, Catherine Belle
Summary: In this study, the inhibition activities of 2-Hydroxypyridine-N-oxide analogs (HOPNO) on tyrosinase were enhanced by the combination with a reference inhibitor or a natural substrate. The (S) enantiomer of the racemic amino acid HOPNO-AA showed the strongest inhibitory effect.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Brayan Roulier, Inbal Rush, Leticia M. Lazinski, Basile Peres, Hamza Olleik, Guy Royal, Ayelet Fishman, Marc Maresca, Romain Haudecoeur
Summary: Considering the crucial role of human tyrosinase (hsTYR) in melanogenesis, finding new hsTYR inhibitors is essential for targeted pharmacological and dermocosmetic applications. Despite the abundance of mushroom tyrosinase (abTYR) inhibitors, the structural differences between these enzymes necessitate the development of true hsTYR inhibitors. In this study, researchers synthesized 38 derivatives and found two compounds that showed excellent inhibition values in hsTYR assays and demonstrated promising improvement in whole cell experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Sadegh Rajabi, Huda Fatima Rajani, Niloufar Mohammadkhani, Andres Alexis Ramirez-Coronel, Mahsa Maleki, Marc Maresca, Homa Hajimehdipoor
Summary: Metastasis is a multi-step process that leads to the spread of cancer cells to distant organs. Long non-coding RNAs (LncRNAs) are regulatory RNA molecules that modulate gene expression and have been implicated in various stages of cancer development, including metastasis. Phytochemical compounds derived from plants have shown potential in targeting LncRNAs to inhibit cancer metastasis. This review article provides an overview of metastasis steps, discusses well-established LncRNAs involved in metastasis, and highlights the role of phytochemicals in targeting LncRNAs to suppress cancer metastasis.
Article
Infectious Diseases
Magali Casanova, Hamza Olleik, Slim Hdiouech, Clarisse Roblin, Jean-Francois Cavalier, Vanessa Point, Katy Jeannot, Baptiste Caron, Josette Perrier, Simeon Charriau, Mickael Lafond, Yohann Guillaneuf, Stephane Canaan, Catherine Lefay, Marc Maresca
Summary: Cystic fibrosis (CF) is a disease associated with repeated lung bacterial infection, often leading to therapeutic failure and death. In this study, methacrylate-based copolymers were evaluated for their antibacterial activity against CF-associated bacterial strains. The results showed that certain copolymers possessed strong antibacterial activity, rapid membranolytic effect, and prevention of biofilm formation, making them potential alternatives to conventional antibiotics in the treatment of CF-associated bacterial infection.
Article
Chemistry, Medicinal
Laurent Hoffer, Manon Garcia, Raphael Leblanc, Mikael Feracci, Stephane Betzi, Khaoula Ben Yaala, Avais M. Daulat, Pascale Zimmermann, Philippe Roche, Karine Barral, Xavier Morelli
Summary: To address the challenge of early hit identification and optimization in drug discovery, we created a strategy called DOTS, which combines molecular dynamic simulations, computer-based library design with encoded medicinal chemistry reactions, constrained docking, and automated compound evaluation. We successfully applied the DOTS strategy to a challenging oncology target, syntenin, and created a best-in-class sub-micromolar small molecule inhibitor validated in cancer cell assays. The key to the success of our DOTS approach was the integration of protein conformational sampling during hit identification and synthetic feasibility ranking of the designed compounds during the optimization process. This approach can be widely used for other protein targets with known 3D structures to rapidly identify and optimize compounds as chemical probes and therapeutic candidates.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Alice Shi Ming Li, Serah Kimani, Brian Wilson, Mahmoud Noureldin, Hector Gonzalez-Alvarez, Ahmed Mamai, Laurent Hoffer, John P. Guilinger, Ying Zhang, Moritz von Rechenberg, Jeremy S. Disch, Christopher J. Mulhern, Belinda L. Slakman, John W. Cuozzo, Aiping Dong, Gennady Poda, Mohammed Mohammed, Punit Saraon, Manish Mittal, Prati k Modh, Vaibhavi Rathod, Bhashant Patel, Suzanne Ackloo, Vijayaratnam Santhakumar, Magdalena M. Szewczyk, Dalia Barsyte-Lovejoy, Cheryl H. Arrowsmith, Richard Marcellus, Marie-Aude Guie, Anthony D. Keefe, Peter J. Brown, Levon Halabelian, Rima Al-awar, Masoud Vedadi
Summary: DCAF1 is a substrate receptor for two E3 ligases and has critical physiological role in protein degradation, making it a potential drug target for cancer and viral treatments. By screening a large compound library and conducting hit optimization, a compound called OICR-8268 was discovered as a tool compound for the development of DCAF1 ligands for cancer therapeutics. OICR-8268 showed strong target engagement and can be used for further investigation of DCAF1 functions and the development of DCAF1-based PROTACs.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Environmental Sciences
Renato Bruno, Celine Boidin-Wichlacz, Oleg Melnyk, Daniela Zeppilli, Celine Landon, Frederic Thomas, Marie-Anne Cambon, Mickael Lafond, Kamel Mabrouk, Francois Massol, Stephane Hourdez, Marc Maresca, Didier Jollivet, Aurelie Tasiemski
Summary: Antimicrobial peptides (AMPs), such as Alvinellacin (ALV), arenicin (ARE) and polaricin (POL), play a crucial role in the external immunity of animals and provide a model for studying the impact of the environment on the diversification and evolution of immune effectors. These AMPs possess a conserved BRICHOS domain in their precursor molecule, despite significant structural and amino acid diversification in the C-terminal portion. The study demonstrates that the bactericidal activity of these AMPs is optimal against bacteria found in their respective habitats, and the presence of disulfide bridges enhances their effectiveness in fluctuating environmental conditions.
SCIENCE OF THE TOTAL ENVIRONMENT
(2023)
Article
Nutrition & Dietetics
Homa Hajimehdipoor, Zahra Tahmasvand, Fatemeh Ghorban Nejad, Marc Maresca, Sadegh Rajabi
Summary: This study investigated the effects of rutin on the proliferation, metastasis, and angiogenesis of breast cancer cells. Rutin was found to stimulate the proliferation and migration of MDA-MB-231 and MCF-7 cells. It also modulated the expression of genes involved in cell adhesion and angiogenesis.
Article
Pharmacology & Pharmacy
Ziad Chebaro, Rola Abdallah, Adnan Badran, Kamar Hamade, Akram Hijazi, Marc Maresca, Joelle Edward Mesmar, Elias Baydoun
Summary: Pancreatic cancer is a highly aggressive malignancy with increasing incidence and mortality rates. Effective screening approaches are lacking, contributing to its poor prognosis. This study investigated the potential anticancer effects of Anchusa strigosa extracts and found that they may be a new resource for the design of novel drugs against pancreatic cancer.
FRONTIERS IN PHARMACOLOGY
(2023)
Review
Agronomy
Ghosoon Albahri, Amal A. Alyamani, Adnan Badran, Akram Hijazi, Mohamad Nasser, Marc Maresca, Elias Baydoun
Summary: A key concern in agriculture is to feed the expanding population and protect the environment from climate change. Innovative approaches are required to increase agricultural productivity and meet the rising demand for food. This review focuses on boosting yields of important grains through molecular technology, genetics, and other strategies.
Article
Multidisciplinary Sciences
Lama Shamseddine, Clarisse Roblin, Iris Veyrier, Christian Basset, Lisa De Macedo, Anne Boyeldieu, Marc Maresca, Cendrine Nicoletti, Gael Brasseur, Sylvie Kieffer-Jaquinod, Elise Courvoisier-Dezord, Agnes Amouric, Philippe Carpentier, Nathalie Campo, Mathieu Berge, Patrice Polard, Josette Perrier, Victor Duarte, Mickael Lafond
Summary: In the context where discovering new molecules to combat antibiotic resistance is important for public health, ribosomally synthesized and post-translationally modified peptides, known as sactipeptides, show promise as an alternative. In this study, the gut symbiont Ruminococcus gnavus E1 was found to produce five sactipeptides, named Ruminococcins C1 to C5 (RumC1-C5), along with two maturases. The antibacterial activities of the mature forms of RumC2-5 were evaluated and variations in efficacy and synergy with conventional antibiotics were observed.
Correction
Multidisciplinary Sciences
Clarisse Roblin, Steve Chiumento, Olivier Bornet, Matthieu Nouailler, Christina S. Mueller, Katy Jeannot, Christian Basset, Sylvie Kieffer-Jaquinod, Yohann Coute, Stephane Torelli, Laurent Le Pape, Volker Schuenemann, Hamza Olleik, Bruno De La Villeon, Philippe Sockeel, Eric Di Pasquale, Cendrine Nicoletti, Nicolas Vidal, Leonora Poljak, Olga Iranzo, Thierry Giardina, Michel Fons, Estelle Devillard, Patrice Polard, Marc Maresca, Josette Perrier, Mohamed Atta, Francoise Guerlesquin, Mickael Lafond, Victor Duarte
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2023)
Article
Chemistry, Multidisciplinary
Nicolas Giacoletto, Marie Le Dot, Hizia Cherif, Fabrice Morlet-Savary, Bernadette Graff, Valerie Monnier, Didier Gigmes, Frederic Dumur, Hamza Olleik, Marc Maresca, Pierre Gerard, Malek Nechab, Jacques Lalevee
Summary: In this study, a series of bio-based captodative ligands were designed and synthesized to replace controversial phosphine oxides commonly used in the polymerization of Elium, successfully reducing the curing time. The investigation of the redox properties of manganese(iii) complexes revealed the impact of captodative ligands on the reduction potential.