Article
Biochemistry & Molecular Biology
Serena Montanari, Marco Allara, Laura Scalvini, Magdalena Kostrzewa, Federica Belluti, Silvia Gobbi, Marina Naldi, Silvia Rivara, Manuela Bartolini, Alessia Ligresti, Alessandra Bisi, Angela Rampa
Summary: Recent studies have revealed the connection between the endocannabinoid system (eCS) and neuroprotection, suggesting its involvement in regulating cognitive processes and the pathophysiology of Alzheimer's disease. Designed and synthesized coumarin-based compounds showed promising potential as multitarget agents for combating complex diseases like AD.
Review
Biochemistry & Molecular Biology
Jan Skubnik, Vladimira Pavlickova, Silvie Rimpelova
Summary: Cardiac glycosides have shown potential not just in treating cardiac diseases, but also as anticancer agents. They induce multiple signaling pathways to inhibit tumor growth, interact with immune cell death mechanisms, and modulate immune response genes, suggesting a wide range of potential applications in treating autoimmune and inflammatory diseases.
Article
Biochemistry & Molecular Biology
Haya Hussain, Shujaat Ahmad, Syed Wadood Ali Shah, Abid Ullah, Niaz Ali, Mazen Almehmadi, Manzoor Ahmad, Atif Ali Khan Khalil, Syed Babar Jamal, Hanif Ahmad, Mustafa Halawi
Summary: In this study, six curcumin analogs were synthesized and evaluated for their potential to inhibit cholinesterase. The synthesized compounds showed promising results in improving memory functions in mice models. Further research is needed to determine their exact mechanism of action.
Article
Pharmacology & Pharmacy
Radoslaw Wojcik, Marek R. Baranowski, Lukasz Markiewicz, Dorota Kubacka, Marcelina Bednarczyk, Natalia Baran, Anna Wojtczak, Pawel J. Sikorski, Joanna Zuberek, Joanna Kowalska, Jacek Jemielity
Summary: This passage discusses the utility of dinucleotide analogs of messenger RNA cap, particularly those with benzyl substitution at N7 position, for potential translational inhibition. The synthesis of novel Bn(7)GpppG analogs and their evaluation in terms of translation and translational inhibition are highlighted, showing promising results for N7-(4-halogenbenzyl) substitutions. Additionally, crystal structures of compounds with eIF4E were determined to gain more molecular insight into N7-benzylation of mRNA cap.
Article
Biochemistry & Molecular Biology
Wojciech Rogoz, Aleksandra Owczarzy, Karolina Kulig, Andrzej Zieba, Malgorzata Maciazek-Jurczyk
Summary: The study aimed to investigate new synthetic quinoline derivatives and their antioxidant properties, as well as their potential as modulators of Human Serum Albumin (HSA) antioxidant activity. Spectroscopic methods were used to analyze the interaction between the derivatives and HSA. Qui3 showed significant antioxidant potential and exhibited synergistic effects with HSA against DPPH, ABTS, and FRAP. Qui2 and Qui3 were identified as potential modulators of HSA antioxidant activity.
Article
Biochemistry & Molecular Biology
Vessela D. Kancheva, Maria Antonietta Dettori, Davide Fabbri, Petko Alov, Silvia E. Angelova, Adriana K. Slavova-Kazakova, Paola Carta, Valerii A. Menshov, Olga I. Yablonskaya, Aleksei V. Trofimov, Ivanka Tsakovska, Luciano Saso
Summary: Oxidative stress is caused by an increase in reactive oxygen species or a significant decrease in the effectiveness of antioxidant enzymes and nonenzymatic defense. A study compared the chain-breaking antioxidant activity of 40 phenolic antioxidants to investigate their role as modulators of oxidative stress. The research focused on the chemical reactions initiating free radicals and the effects of substituents in the phenolic structure.
Review
Biochemistry & Molecular Biology
Bianca Nitzsche, Michael Hoepfner, Bernhard Biersack
Summary: Heat shock protein 70 (Hsp70) and its interaction with Hsp90 play a significant role in cancer diseases. The Hsp70-Hsp40 axis, formed by the connection between Hsp70 and a smaller heat shock protein Hsp40, is a suitable target for designing anticancer drugs. This review discusses the current state and recent developments in the field of (semi-)synthetic small molecule inhibitors targeting Hsp70 and Hsp40, as well as their potential in medicinal chemistry and anticancer therapies.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Infectious Diseases
Javier Moreno-Morales, Salvador Guardiola, Clara Balleste-Delpierre, Ernest Giralt, Jordi Vila
Summary: In this study, we successfully synthesized PLP-3, a peptide with broad-spectrum antimicrobial activity, especially against A. baumannii, while maintaining low haemolysis and toxicity against human cells at antimicrobial concentrations.
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
(2022)
Article
Chemistry, Medicinal
Elsamani I. Abdelfadiel, Rama Gunta, Bharath Kumar Villuri, Daniel K. Afosah, Nehru Viji Sankaranarayanan, Umesh R. Desai
Summary: Natural glycosaminoglycans (GAGs) are a diverse group of natural products that have not been fully utilized. Research has only led to the development of one GAG-like synthetic drug, highlighting the difficulty in working with GAGs. This Perspective aims to transform the negative perception of GAGs by highlighting recent advances in GAG mimetics, specifically in the design of synthetic sulfated small molecules as allosteric modulators of coagulation factors.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Anastasia A. Zabolotneva, Andrei M. Gaponov, Sergey A. Roumiantsev, Ilya Yu. Vasiliev, Tatiana V. Grigoryeva, Oleg I. Kit, Elena Yu. Zlatnik, Aleksey Yu. Maksimov, Anna S. Goncharova, Inna A. Novikova, Svetlana A. Appolonova, Pavel A. Markin, Aleksandr V. Shestopalov
Summary: Alkylresorcinols (ARs), polyphenolic compounds with diverse biological activities potentially involved in host metabolism regulation, were found to be produced by the human gut microbiota. Alterations in AR content and metabolic activity of the gut microbiota were observed in mice according to diet specifications and olivetol supplementation. The findings suggest that ARs may function as quorum-sensing molecules, influencing gut microbiota composition and host metabolism.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Behavioral Sciences
Anne S. Berry, Theresa M. Harrison
Summary: The basal forebrain cholinergic system (BFCS) has been associated with age-related cognitive changes and Alzheimer's disease (AD). Despite limitations in cholinergic interventions, there is a renewed interest in studying the BFCS using novel frameworks. This article outlines the structure and function of the BFCS, its role in cognition and emotion, and its vulnerability to aging and AD. It also explores the BFCS in relation to the amyloid hypothesis, selective vulnerability, pathology spread, and sleep health in AD research.
NEUROSCIENCE AND BIOBEHAVIORAL REVIEWS
(2023)
Article
Chemistry, Organic
Taiki Tsurusaki, Kazuki Sato, Takeshi Wada
Summary: In this study, a new method for the solution-phase synthesis of oligodeoxynucleotides (ODNs) was developed using nucleoside 3'-H-phosphonamidate derivatives as monomers. The H-phosphonamidate monomers reacted with alcohol under mild basic conditions to form an internucleotidic H-phosphonate diester, without the need for additives. The resultant internucleotidic linkage was then converted into a more stable linkage, such as an S-cyanoethyl phosphorothioate diester. This method reduces the number of reagents and simplifies the purification process.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Jun Liu, Jin-Song Hou, Yi-Qun Chang, Li-Jun Peng, Xiao-Yi Zhang, Zhi-Ying Miao, Ping-Hua Sun, Jing Lin, Wei-Min Chen
Summary: Development of new bacterial biofilm inhibitors as antibacterial synergists is an effective strategy to combat Pseudomonas aeruginosa resistance. Compound 20p was identified as a potential novel antibacterial synergist candidate for the treatment of P. aeruginosa infections, showing significant antibacterial synergy when combined with approved antibiotics for CF.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Neurosciences
Rita Bardoni
Summary: The role of 5-HT7 receptors in modulating pain perception has been explored through in vivo studies using different pain models. While most studies have reported an antinociceptive effect of 5-HT7 receptor activation, some researchers have suggested a pronociceptive action. The discrepancies in the results could be explained by differences in pain models, animal species and gender, receptor types, agonists, and route of administration. This mini-review summarizes the main findings and discusses the expression patterns, cellular mechanisms, alterations in receptor function, and the future perspectives of 5-HT7 receptors in the pain system.
CURRENT NEUROPHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Marta Ximenis, Jose Mulet, Salvador Sala, Francisco Sala, Manuel Criado, Rosario Gonzalez-Muniz, Maria Jesus Perez de Vega
Summary: This study evaluated a range of natural products and synthetic compounds, finding that phloretin, demethoxycurcumin, and bis-demethoxicurcuming act as positive allosteric modulators (PAMs) of α7 nAChR; and some new curcumin derivatives have the ability to enhance ACh-evoked signal, with tetrahydrocurcuminoid analog 23 showing particularly promising activity values.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Agriculture, Multidisciplinary
E. Jesser, C. Yeguerman, N. Stefanazzi, R. Gomez, A. P. Murray, A. A. Ferrero, J. O. Werdin-Gonzalez
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2020)
Article
Chemistry, Multidisciplinary
Emiliano Jesser, Cristhian Yeguerman, Valeria Gili, Graciela Santillan, Ana Paula Murray, Claudia Domini, Jorge Omar Werdin-Gonzalez
ACS SUSTAINABLE CHEMISTRY & ENGINEERING
(2020)
Article
Biochemistry & Molecular Biology
Jose L. Borioni, Valeria Cavallaro, Adriana B. Pierini, Ana P. Murray, Alicia B. Penenory, Marcelo Puiatti, Manuela E. Garcia
JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN
(2020)
Article
Neurosciences
Brunella Biscussi, Victoria Richmond, Carlos Javier Baier, Pau Arroyo Manez, Ana Paula Murray
CNS & NEUROLOGICAL DISORDERS-DRUG TARGETS
(2020)
Article
Biotechnology & Applied Microbiology
I. L. Cibanal, L. A. Fernandez, A. P. Murray, C. N. Pellegrini, L. M. Gallez
Summary: The study evaluated the antifungal activity of propolis extract and oregano essential oil against Penicillium allii, finding a strong synergistic effect between the two natural products. This suggests their potential use as a non-conventional strategy for controlling blue mould disease in garlic seed-cloves.
JOURNAL OF APPLIED MICROBIOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Jose L. Borioni, Valeria Cavallaro, Ana P. Murray, Alicia B. Penenory, Marcelo Puiatti, Manuela E. Garcia
Summary: Alzheimer's disease is the most alarming neurodegenerative disorder globally, with cholinesterase inhibitors commonly used in clinical treatments. The strategy of synthesizing hybrid cholinesterase inhibitors has shown improved inhibitory activity and enhanced interactions at multiple sites in the enzyme cavity. This approach should be further explored and exploited in this field.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Physical
Brunella Biscussi, Maria Alejandra Sequeira, Victoria Richmond, Pau Arroyo Manez, Ana Paula Murray
Summary: In this study, a series of azoderivatives were designed and synthesized as AChE inhibitors, with one compound showing high enzymatic response and stable photostationary state, serving as an efficient photo probe for remote control of AChE activity. Molecular modelling analysis revealed the compound's affinity for the peripheral anionic site of AChE, contributing to the development of promising agents for photopharmacological treatment of Alzheimer's disease.
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY A-CHEMISTRY
(2021)
Article
Environmental Sciences
Cristhian A. Yeguerman, Rodrigo Urrutia, Emiliano N. Jesser, Manlio Massiris, Claudio A. Delrieux, Ana P. Murray, Jorge O. Werdin Gonzalez
Summary: This paper introduces the lethal, sublethal, and ecotoxic effects of peppermint and palmarosa essential oils and their polymeric nanoparticles. The results demonstrate that the nanoparticles enhance the lethal activity and repellent effects of the oils, resulting in beneficial effects against pests. However, the nanoparticles have slight toxicity to certain aquatic organisms and no toxicity to terrestrial organisms.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2022)
Article
Food Science & Technology
E. Jesser, L. Castillo, Y. Alonso, R. Urrutia, A. P. Murray, C. Domini, J. O. Werdin-Gonzalez
Summary: Plodia interpunctella Hubner is a common moth pest of stored products, with its larvae being effective packaging penetrators. This study developed chitosan-based films incorporated with geranium and peppermint essential oils, which showed strong repellent and penetration inhibiting effects against P. interpunctella larvae. The films containing 0.5% w/w of geranium and peppermint EO exhibited the best results. Additionally, the mechanical properties of the control films were preserved after incorporation of the essential oils.
FOOD PACKAGING AND SHELF LIFE
(2022)
Article
Agronomy
Emiliano Jesser, Cristhian Alan Yeguerman, Rodrigo Inaki Urrutia, Ana Paula Murray, Claudia Domini, Jorge Omar Werdin-Gonzalez
Summary: This study elaborated and evaluated the toxicological effects of nanoemulsions (NEs) containing peppermint or palmarosa essential oils (EOs) combined with beta-cypermethrin (beta-CP) using ultrasound technique. The results showed that NEs peppermint/beta-CP and NEs palmarosa/beta-CP enhanced pyrethroid bioactivity and maintained high insecticidal activities, making them highly promising formulations for the development of new insecticides.
PEST MANAGEMENT SCIENCE
(2023)
Article
Chemistry, Multidisciplinary
Viktor S. Camara, Ana Julia Soares, Brunella Biscussi, Ana Paula Murray, Isabella A. Guedes, Laurent E. Dardenne, Thais C. Ruaro, Aline R. Zimmer, Marco A. Ceschi
Summary: This study developed a series of bis(n)-lophine analogues as potential new selective BuChE inhibitors for treating chronic Alzheimer's disease. These compounds showed strong selectivity to BuChE and exhibited potent inhibitory activity, while also demonstrating no cytotoxic effects in vitro studies.
JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY
(2021)