Review
Pharmacology & Pharmacy
Miguel A. A. Lasuncion, Javier Martinez-Botas, Covadonga Martin-Sanchez, Rebeca Busto, Diego Gomez-Coronado
Summary: The mevalonate pathway is essential for the synthesis of isoprenoids, including sterols, and plays a crucial role in cell division and cell cycle progression.
BIOCHEMICAL PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Lukasz Swiatek, Elwira Sieniawska, Kouadio Ibrahime Sinan, Gokhan Zengin, Anastazja Boguszewska, Benita Hryc, Kouadio Bene, Malgorzata Polz-Dacewicz, Stefano Dall'Acqua
Summary: This study investigated the chemical profiles and biological properties of Justicia secunda extracts obtained using different solvents. Over 50 compounds, including flavonoids, phenolic acids, and alkaloids, were identified using LC-MS. The methanol and water extracts showed higher phenolic and flavonoid contents and stronger antioxidant abilities. The dichloromethane and ethyl acetate extracts exhibited greater activity against alpha-amylase and alpha-glucosidase. The aqueous extracts demonstrated selective anticancer properties and the methanolic extract decreased the infectious titer and viral load of human herpesvirus type-1. Overall, J. secunda could be used as a multifunctional bioactive raw material for managing diseases related to oxidative stress.
Article
Chemistry, Physical
Basavarajaiah Suliphuldevara Mathada, Sasidhar B. Somappa
Summary: Prevention, accurate diagnosis, and effective treatment of infections are crucial in managing infectious diseases. Indoles, a class of important compounds, have diverse therapeutic applications. This review discusses the natural sources, drugs, and biological activities of indole, including antibacterial and antifungal properties. The structure-activity relationships of indole derivatives are also presented.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Biochemistry & Molecular Biology
Manvendra Kumar, Gaurav Joshi, Sahil Arora, Tashvinder Singh, Sajal Biswas, Nisha Sharma, Zahid Rafiq Bhat, Kulbhushan Tikoo, Sandeep Singh, Raj Kumar
Summary: A series of non-covalent imidazo[1,2-a]quinoxaline-based inhibitors of EGFR were designed and synthesized, with compounds 6b, 7h, 7j, 9a, and 9c showing potent inhibitory effects. Compound 6b demonstrated significant inhibitory potential against gefitinib-resistant H1975 cells.
Review
Oncology
Tatiana Shorstova, William D. Foulkes, Michael Witcher
Summary: Transcriptional upregulation of oncogenes drives tumor progression, and targeting BET proteins with inhibitors has shown promise in suppressing oncogenic networks in tumors. Understanding the biology of BET proteins, designing better BET inhibitors, and incorporating BET inhibitors into combination therapies can enhance their efficacy in clinical settings.
BRITISH JOURNAL OF CANCER
(2021)
Article
Chemistry, Multidisciplinary
Dan Wan, Feng-Qin Wang, Jiang Xie, Lin Chen, Xian-Li Zhou
Summary: In this study, multifunctional hybrid compounds were obtained by connecting benzylpiperidine with phenylethylamine. Compound 3 exhibited excellent acetylcholinesterase inhibitory activity and neuroprotective effects. Molecular docking research indicated that the square amide group formed strong interactions with the target protein. Therefore, square amide could be an interesting construction unit in anti-Alzheimer’s disease agents.
Article
Chemistry, Medicinal
Daniil V. Spector, Kirill G. Pavlov, Roman A. Akasov, Alexander N. Vaneev, Alexander S. Erofeev, Petr V. Gorelkin, Vita N. Nikitina, Elena V. Lopatukhina, Alevtina S. Semkina, Kseniya Yu. Vlasova, Dmitrii A. Skvortsov, Vitaly A. Roznyatovsky, Nikolay V. Ul'yanovskiy, Ilya I. Pikovskoi, Sergey A. Sypalov, Anastasiia S. Garanina, Stepan S. Vodopyanov, Maxim A. Abakumov, Yulia L. Volodina, Alina A. Markova, Albina S. Petrova, Dmitrii M. Mazur, Dmitry A. Sakharov, Nikolay V. Zyk, Elena K. Beloglazkina, Alexander G. Majouga, Olga O. Krasnovskaya
Summary: In this study, a series of novel Pt(IV) prodrugs with nonsteroidal anti-inflammatory drugs were designed and synthesized. By tuning the drug lipophilicity via variation of the axial ligands, the most potent Pt(IV) prodrug was obtained, showing enhanced cellular accumulation and cytotoxicity. The prodrugs exhibited superior antiproliferative activity compared to cisplatin and overcame tumor cell line resistance.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Maria Chiara Proto, Donatella Fiore, Chiara Piscopo, Cristina Pagano, Mario Galgani, Sara Bruzzaniti, Chiara Laezza, Patrizia Gazzerro, Maurizio Bifulco
Summary: Efficient strategies are still needed to counteract viral infections despite progress made, with Lipid metabolism and targeting the mevalonate pathway showing potential in mitigating viral infections, including the SARS-CoV-2 pandemic.
PROGRESS IN LIPID RESEARCH
(2021)
Article
Plant Sciences
Julia Langeder, Kristin Doering, Hannes Schmietendorf, Ulrike Grienke, Michaela Schmidtke, Judith M. Rollinger
Summary: MDAAs derived from the white mulberry tree have been discovered as dual inhibitors of influenza viruses and pneumococci. The study aimed to identify the most prolific natural source of MDAAs, develop a protocol to maximize their content in Morus alba extracts, unravel constituents with high anti-infective potential, and select a hit extract as a candidate for further studies. Analysis revealed that root bark was the best starting material and pressurized liquid extraction was the optimum technique for extraction. The hit extract showed good tolerance by lung cells and potent in vitro activities against influenza viruses, S. pneumoniae, S. aureus, and inflammation.
JOURNAL OF NATURAL PRODUCTS
(2022)
Article
Medicine, Research & Experimental
Wenjun Mao, Yun Cai, Danrong Chen, Guanyu Jiang, Yongrui Xu, Ruo Chen, Fengxu Wang, Xuehai Wang, Mingfeng Zheng, Xinyuan Zhao, Jie Mei
Summary: ICB therapy has achieved breakthroughs in treating advanced NSCLC, but the presence of immuno-cold tumors limits its efficacy. Targeting cholesterol synthesis can improve the treatment of immuno-cold tumors. Statin can inhibit the aggressiveness of lung cancer and enhance the response to ICB therapy.
Article
Multidisciplinary Sciences
Jenna E. van Leeuwen, Wail Ba-Alawi, Emily Branchard, Jennifer Cruickshank, Wiebke Schormann, Joseph Longo, Jennifer Silvester, Peter L. Gross, David W. Andrews, David W. Cescon, Benjamin Haibe-Kains, Linda Z. Penn, Deena M. A. Gendoo
Summary: The study shows that dipyridamole can enhance statin-induced cancer cell death. To identify similar compounds, an integrative pharmacogenomics pipeline is developed based on drug structure, cell sensitivity, and molecular perturbation. The effectiveness of nelfinavir and honokiol is validated, and low expression of E-cadherin is found to be associated with statin-compound synergy.
NATURE COMMUNICATIONS
(2022)
Review
Biochemistry & Molecular Biology
Ainur D. D. Sharapov, Ramil F. F. Fatykhov, Igor A. A. Khalymbadzha, Grigory V. V. Zyryanov, Oleg N. N. Chupakhin, Mikhail V. V. Tsurkan
Summary: This review summarizes the literature on the anti-HIV activity of plant coumarins. It highlights the isolation and mechanism of their antiviral action, demonstrating that plant-derived coumarins can act through different mechanisms to inhibit HIV replication. The review also discusses the resistance of some coumarins to HIV mutations and presents the research conducted in the past two decades on the anti-HIV activity of naturally occurring coumarins.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Chemistry, Organic
Shweta Mishra, Pradip Jana
Summary: After the COVID-19 pandemic, it is a reminder from global health agencies that tuberculosis is the deadliest infectious disease worldwide, with approximately ten million new cases each year. Despite efforts to discover effective management of this disease, treatment success remains low and there is a high rate of drug treatment failure and resistance. Therefore, there is an urgent need to develop new chemical entities as antituberculosis agents. Chalcone and its derivatives have been found to possess anti-inflammatory and antituberculosis activities, making them potential drug candidates for treating tuberculosis.
POLYCYCLIC AROMATIC COMPOUNDS
(2023)
Editorial Material
Biotechnology & Applied Microbiology
Tacieli Fagundes da Rosa, Vitoria Segabinazzi Foletto, Marissa Bolson Serafin, Angelita Bottega, Rosmari Horner
Summary: Infectious diseases are a major cause of morbidity and mortality, highlighting the need for new drug options and combat strategies. Proton pump inhibitors (PPIs) have emerged as potential candidates for anti-infective properties, showing activities against bacterial, fungal, parasitic, and viral agents in studies.
INTERNATIONAL MICROBIOLOGY
(2022)
Article
Infectious Diseases
Jakob Hofmann, Sabrina Klingele, Uwe Haberkorn, Gerhard Schmidmaier, Tobias Grossner
Summary: The study evaluated the effects of antibiotics and antifungal agents on the differentiation of mesenchymal stem cells into osteoblast-like cells and synthesis of hydroxyapatite. Results showed that all anti-infective agents had cytotoxic effects on mesenchymal stem cells, but at certain doses, they also had a positive impact on osteogenesis.
Article
Chemistry, Medicinal
Eleonora Diamanti, Mostafa M. Hamed, Antoine Lacour, Patricia Bravo, Boris Illarionov, Markus Fischer, Matthias Rottmann, Matthias Witschel, Anna K. H. Hirsch
Summary: The MEP pathway enzymes are crucial for synthesizing isoprenoids and are potential drug targets. A high-throughput screening approach led to the discovery of a novel fragment hit against PfIspD, and a systematic SAR investigation identified a new compound for structure-guided optimization. A putative binding mode for the inhibitors was proposed using a homology model of PfIspD.
Article
Biochemical Research Methods
Marina Creydt, Silke Lautner, Joerg Fromm, Markus Fischer
Summary: A non-targeted metabolomics-based approach using liquid chromatography high-resolution mass spectrometry was used to differentiate spruce wood from different geographic source areas. Despite the small distance (250 km) between the two sample sites in Germany, a distinction between the sample groups was achieved based on non-polar data sets using supervised multivariate methods. Major metabolites contributing to differentiation were identified through MS/MS experiments.
JOURNAL OF CHROMATOGRAPHY A
(2022)
Article
Biochemistry & Molecular Biology
Soeren Wenck, Marina Creydt, Jule Hansen, Florian Gaerber, Markus Fischer, Stephan Seifert
Summary: This study demonstrates the importance of using random forest methods and surrogate minimal depth methods for analyzing metabolomics data. The selection of important features and evaluation of their impact on multi-level classification reveals meaningful biological relationships.
Article
Food Science & Technology
Kristian von Wuthenau, Torben Segelke, Marie-Sophie Mueller, Hardy Behlok, Markus Fischer
Summary: The study successfully used isotopolomic fingerprinting to distinguish the origin of almonds, preventing food fraud, and found that the respective harvest year and almond variety had no significant effect on origin discrimination.
Article
Agriculture, Multidisciplinary
Anja Devenie Riegel, Hidehiko Wakabayashi, Motoko Wakabayashi, Marketa Rynesova, Viktoriia Dudko, Wolfgang Eisenreich, Karl-Heinz Engel
Summary: Through studying the stereoisomers of two 1,3-oxathianes, it was found that the positions and spatial orientations of substituents have a significant impact on their sensory properties. Different stereoisomers have different odor thresholds and odor qualities.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2022)
Article
Biotechnology & Applied Microbiology
Marion Ringel, Nicole Dimos, Stephanie Himpich, Martina Haack, Claudia Huber, Wolfgang Eisenreich, Gerhard Schenk, Bernhard Loll, Thomas Brueck
Summary: This study identified two novel terpene synthases from the wood rotting fungus Coniophora puteana, which can catalyze the production of a potentially new bioactive compound, (+)-delta-cadinol. Mutagenesis studies revealed that the catalytic cycle of these enzymes may involve different conformational changes, suggesting a more complex role of tertiary structure elements in terpene synthase reactions. These findings may contribute to the sustainable production of bioactive compounds and serve as a model system for further mechanistic studies of terpenoid catalysis.
MICROBIAL CELL FACTORIES
(2022)
Article
Chemistry, Multidisciplinary
Ani Ozcelik, Daniel Aranda, Raquel Pereira-Cameselle, Maria Talavera, Berta Covelo, Fabrizio Santoro, Angeles Pena-Gallego, J. Lorenzo Alonso-Gomez
Summary: This study demonstrates the control of spiroconjugation and its effect on the chemical and photophysical properties of spirobifluorenes through peripheral functionalization, which is of significant importance in the field of organic electronics.
Article
Biotechnology & Applied Microbiology
Michael Paper, Matthias Glemser, Martina Haack, Jan Lorenzen, Norbert Mehlmer, Tobias Fuchs, Gerhard Schenk, Daniel Garbe, Dirk Weuster-Botz, Wolfgang Eisenreich, Michael Lakatos, Thomas B. Brueck
Summary: This study demonstrates that the marine chlorophyte Picochlorum sp. can efficiently grow under green light illumination and produce unknown pigments. Green light illumination can enhance biomass production and trigger the formation of new metabolites.
FRONTIERS IN BIOENGINEERING AND BIOTECHNOLOGY
(2022)
Review
Immunology
Wolfgang Eisenreich, Thomas Rudel, Juergen Heesemann, Werner Goebel
Summary: Both antibiotic persistence and antibiotic resistance are phenotypes in which bacteria become insensitive to antibiotics, but they have different molecular bases. Antibiotic resistance is genetically determined and stable, while antibiotic persistence is a transient physiological state triggered by various stress conditions. Persisters are randomly formed in bacterial populations and their numbers depend on the culture conditions. We hypothesize that persistence is caused by an inability to initiate DNA replication, and in this state, bacteria become more susceptible to mutation-based antibiotic resistance if they have error-prone DNA repair functions.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2022)
Article
Chemistry, Inorganic & Nuclear
Maria Talavera, Raquel Pereira-Cameselle, Angeles Pena-Gallego, Irene Vazquez-Carballo, Inmaculada Prieto, J. Lorenzo Alonso-Gomez, Sandra Bolano
Summary: This article describes the synthesis and characterization of three new spirobifluorene iridaaromatic compounds with different substituents. The study shows that these novel systems exhibit high stability, low energy gap values, significant redshift, and high first hyperpolarizabilities, making them potential candidates for optoelectronic applications.
DALTON TRANSACTIONS
(2023)
Article
Microbiology
Thomas Steiner, Marie Zachary, Susanne Bauer, Martin J. Mueller, Markus Krischke, Sandra Radziej, Maximilian Klepsch, Bruno Huettel, Wolfgang Eisenreich, Thomas Rudel, Dagmar Beier
Summary: Through transcriptome and metabolome analysis, we have demonstrated the significant role of the sibling sRNAs NgncR_162/163 in the regulation of metabolic pathways, particularly in the biosynthesis of amino acids and nucleotides.
Article
Chemistry, Multidisciplinary
Ran Li, Wolfgang Eisenreich, Lei Lei, Johann Plan
Summary: This study investigated the role of polycarboxylate superplasticizers in a low carbon alkali-activated slag (AAS) system. Two series of PCEs with different anionicities were synthesized and characterized. The results showed that the synthesized HPEG PCEs exhibited superior dispersing performance over APEG PCEs, especially at high anionicity. The dispersing power of the PCEs increased with their anionicity as a result of stronger adsorption on slag. 13C NMR spectroscopy was used to identify specific structural motifs in the PCE copolymers.
ACS SUSTAINABLE CHEMISTRY & ENGINEERING
(2022)
Review
Chemistry, Medicinal
Julia Portela-Pino, Maria Talavera, Stefano Chiussi, Sandra Bolano, Angeles Pena-Gallego, J. Lorenzo Alonso-Gomez
Summary: Chiroptical responses are valuable for determining the structure of dissymmetric molecules, and the development of everyday applications based on chiroptical systems is still in progress. This article presents the contributions made in constructing robust chiroptical systems through the use of axially chiral allenes and chiral spirobifluorenes.
Article
Chemistry, Multidisciplinary
Philippe Diederich, Alexander Ruf, Thomas Geisberger, Leopold Weidner, Christian Seitz, Wolfgang Eisenreich, Claudia Huber, Philippe Schmitt-Kopplin
Summary: Chemical complexity is crucial for the origin of life and biological evolution. The chemical evolution of a complex prebiotic mixture containing acetylene, carbon monoxide, and nickel sulfide has been analyzed using mass spectrometry. Isotopic labeling reveals the presence of diverse compounds within the reaction mixture. Different degrees of labeling enable robust characterization of functional groups. The study also reveals a characteristic addition pattern and a high diversity of sulfur-containing compounds. The temporal analysis provides insights into the role of sulfur in the origin of life.
COMMUNICATIONS CHEMISTRY
(2023)
Review
Veterinary Sciences
Shereen Basiouni, Guillermo Tellez-Isaias, Juan D. Latorre, Brittany D. Graham, Victor M. Petrone-Garcia, Hesham R. El-Seedi, Sakine Yalcin, Amr Abd El-Wahab, Christian Visscher, Helen L. May-Simera, Claudia Huber, Wolfgang Eisenreich, Awad A. Shehata
Summary: Chronic stress and inflammation have detrimental impacts on the health and performance of animals, including poultry. This review discusses the mechanistic pathways of oxidative stress and inflammation associated with the main stressors in poultry, such as heat stress, dysbiosis, leaky gut syndrome, and mycotoxins. The use of phytogenic bioactive substances to mitigate oxidative stress and inflammation in poultry is also explored.
VETERINARY SCIENCES
(2023)
