Review
Neurosciences
Federico Emanuele Pozzi, Elisa Conti, Ildebrando Appollonio, Carlo Ferrarese, Lucio Tremolizzo
Summary: This study conducted a systematic review of the predictors of response to acetylcholinesterase inhibitors (AChEI) in neurodegenerative dementias. The results showed heterogeneity in duration, drug dosage, and diagnostic criteria. Factors associated with cholinergic deficit and preserved cholinergic neurons were found to be potential predictors of response. Other factors related to drug availability and genetic variations were also identified. The study highlights the importance of considering these predictors when using AChEI therapy in neurodegenerative dementias.
FRONTIERS IN NEUROSCIENCE
(2022)
Review
Biochemistry & Molecular Biology
Fatimah K. Khalaf, Jacob Connolly, Bella Khatib-Shahidi, Abdulsahib Albehadili, Iman Tassavvor, Meghana Ranabothu, Noha Eid, Prabhatchandra Dube, Samer J. Khouri, Deepak Malhotra, Steven T. Haller, David J. Kennedy
Summary: Paraoxonase enzymes are an important redox system that protect cells against oxidative stress. The PON enzymes family, consisting of PON-1, PON-2, and PON-3, play a role in preventing cardiovascular disease and are associated with neurological disorders and neurodegenerative diseases. This review summarizes the evidence on the role of PONs in these diseases and their ability to modify risk factors for neurological disorders, focusing on Alzheimer's disease, Parkinson's disease, and other neurodegenerative and neurological diseases.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Raquel B. M. de Almeida, Deyse B. B. Barbosa, Mayra R. R. do Bomfim, Jessika A. O. Amparo, Bruno S. S. Andrade, Silvia L. L. Costa, Joaquin M. Campos, Jorddy N. Cruz, Cleydson B. R. Santos, Franco H. A. Leite, Mariana B. B. Botura
Summary: The compound ZINC390718 was found to exhibit inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), and showed low cytotoxicity in vitro. Molecular dynamics (MD) simulation revealed that ZINC390718 interacted with the catalytic residue sites of both enzymes. These findings suggest that ZINC390718 could be a potential chemotype for the development of new dual cholinesterase inhibitors.
Article
Chemistry, Medicinal
Thierno Moussa Ndongo, Marieta L. C. Passos, Fernando Duraes, Diana I. S. P. Resende, Madalena Pinto, Emilia Sousa, Maria Lucia M. F. S. Saraiva
Summary: A miniaturized microsequential injection/lab-on-valve (mu SIA-LOV) system has been developed as a useful alternative for inhibitory studies on acetylcholinesterase, showing potential inhibitory effects higher than clinical agents at lower costs and reagent consumption. The system is robust, rapid, reliable, and easy to use.
ARCHIV DER PHARMAZIE
(2021)
Article
Biochemistry & Molecular Biology
Mehrdad Sadafi Kohnehshahri, Gholamabbas Chehardoli, Masoomeh Bahiraei, Tahmineh Akbarzadeh, Akram Ranjbar, Arezoo Rastegari, Zahra Najafi
Summary: The newly designed quinolotacrine hybrids showed promising inhibitory effects on AChE, with one compound exhibiting the best inhibitory activity. Additionally, these compounds demonstrated significant neuroprotective effects in in vitro experiments.
MOLECULAR DIVERSITY
(2022)
Article
Biochemistry & Molecular Biology
Kamila Czarnecka, Malgorzata Girek, Pawel Krecisz, Robert Skibinski, Kamil Latka, Jakub Jonczyk, Marek Bajda, Piotr Szymczyk, Grzegorz Galita, Jacek Kabzinski, Ireneusz Majsterek, Alba Espargaro, Raimon Sabate, Pawel Szymanski
Summary: Alzheimer's disease (AD) is a progressive neurodegenerative brain disease and current drugs are not entirely effective in its treatment. This study evaluated eight derivatives as candidates for stronger anti-AD potential with fewer side effects. Compound 3e displayed moderate inhibition of cholinesterase and significant inhibition of A beta aggregation, indicating promise as a potential new anti-AD drug.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Somaia S. Abd El-Karim, Manal M. Anwar, Nesreen S. Ahmed, Yasmin M. Syam, Samia A. Elseginy, Hanan F. Aly, Eman A. Younis, Wagdy K. B. Khalil, Kawkab A. Ahmed, Faten F. Mohammed, Maha Rizk
Summary: A series of novel benzofuran-based compounds were synthesized and investigated as acetylcholinesterase inhibitors. Compound 7c showed promising inhibitory activity and antioxidant activity, making it a potential candidate for the treatment of Alzheimer's disease.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Neurosciences
Jose Maria Garcia-Alberca, Esther Gris, Paz de la Guia, Silvia Mendoza, Maria Lopez de la Rica
Summary: This study examined the effectiveness of combining Souvenaid with cholinesterase inhibitors in treating mild Alzheimer's disease. The results showed that the combination therapy significantly improved cognitive and behavioral outcomes compared to cholinesterase inhibitors alone. Therefore, the use of Souvenaid in combination with antidementia drugs could be an effective treatment approach.
JOURNAL OF ALZHEIMERS DISEASE
(2023)
Review
Biochemistry & Molecular Biology
Marta Perez-Gomez Moreta, Natalia Burgos-Alonso, Maria Torrecilla, Jose Marco-Contelles, Cristina Bruzos-Cidon
Summary: The study confirmed a low efficacy of AChEI in improving cognitive symptoms of patients with mild to moderate AD, especially in cognitive aspects. However, AChEI showed better effects in improving the global state, with donepezil being the most effective treatment. Nonetheless, there was no evidence of improvement in behavioral disturbances with the use of AChEI.
Article
Biochemistry & Molecular Biology
Blazej Grodner, Mariola Napiorkowska, Dariusz Maciej Pisklak
Summary: This study evaluated the inhibition efficacy of four aminoalkanol derivatives on acetylcholinesterase in vitro. The results showed that the inhibitory potency of the derivatives varied depending on the nature of the substituents, with isopropylamine and/or methyl substituents being the most effective. Docking studies suggested that the compounds bind to the peripheral anionic site rather than entering the catalytic pocket.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Chemistry, Multidisciplinary
Nicolas Navarro Martinez, Jorge Toledo Hernandez, Javier O. Morales
Summary: Alzheimer's disease (AD) is a common neurodegenerative disease among the elderly, characterized by oxidative stress and the deposition of neurofibrillary tangles and A beta plaques. Natural antioxidants or ROS scavengers may prevent the formation of these aggregates, while A beta-degrading/anti-aggregating molecules could slow down AD progression. Traditional drugs for AD have limitations in crossing the blood-brain barrier. Nanocarrier conjugation of these drugs could enhance brain targeting and delivery, potentially delaying neurodegeneration in AD.
NANOTECHNOLOGY REVIEWS
(2023)
Article
Biochemistry & Molecular Biology
Prabhat Tiwari, Nicholas S. Tolwinski
Summary: A dementia case is diagnosed every three seconds worldwide, with 50-60% of cases being caused by Alzheimer's disease (AD). The deposition of amyloid beta (Aβ) is believed to be correlated with the onset of dementia, although it remains unclear whether Aβ is causative. Optogenetic techniques provide a precise way to regulate cellular dynamics and could offer a better understanding of the etiology of AD.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Bhupinder Kumar, Ashish Ranjan Dwivedi, Tania Arora, Khadga Raj, Vikash Prashar, Vijay Kumar, Shamsher Singh, Jyoti Prakash, Vinod Kumar
Summary: This study reports a series of N-propargyl-substituted diphenylpyrimidine derivatives with potential inhibitory activity against AChE and MAO-B, as well as neuroprotective effects and improvement of cognitive function.
ACS CHEMICAL NEUROSCIENCE
(2022)
Article
Pharmacology & Pharmacy
G. Lombardi, N. Lombardi, A. Bettiol, G. Crescioli, C. Ferrari, G. Lucidi, C. Polito, V Berti, V Bessi, S. Bagnoli, B. Nacmias, A. Vannacci, S. Sorbi
Summary: The study aimed to assess the impact of long-term use of commonly prescribed drugs in Alzheimer's disease on its clinical course and identify factors associated with a delay in disease progression. The results showed that long-term use of memantine, either alone or in combination with acetylcholinesterase inhibitors, was associated with a significantly lower risk of disease progression.
EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Natalia Smyrska-Wieleba, Tomasz Mroczek
Summary: This article provides an updated description and comparison of natural inhibitors of cholinesterases (IChEs), namely, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), based on data from the last 15 years. It also highlights the potential impact of compound structures on the therapeutic effects of cholinesterase inhibitors. The findings suggest that natural sources are still promising for the discovery of new compounds with significant pharmacological activity, and further research is needed to understand the mechanisms of action and structure-activity correlation of cholinesterase inhibitors for medical applications.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Gastroenterology & Hepatology
Miroslaw Drozdz, Joanna Gdula-Argasinska, Grazyna Biesiada, Artur Jurczyszyn, William Perucki, Pawel Wolkow, Agnieszka Borys, Katarzyna Sroczynska, Anna Zajac, Tadeusz Librowski, Aleksander Garlicki, Jacek Czepiel
EUROPEAN JOURNAL OF GASTROENTEROLOGY & HEPATOLOGY
(2020)
Article
Medicine, General & Internal
Kinga Kowalska-Duplaga, Przemyslaw Kapusta, Tomasz Gosiewski, Agnieszka Sroka-Oleksiak, Agnieszka H. Ludwig-Slomczynska, Pawel P. Wolkow, Krzysztof Fyderek
JOURNAL OF CLINICAL MEDICINE
(2020)
Article
Medicine, Research & Experimental
Ewa Dziewiecka, Justyna Toton-Zuranska, Pawel Wolkow, Maria Kolton-Wroz, Ewelina Pitera, Sylwia Wisniowska-Smialek, Lusine Khachatryan, Aleksandra Karabinowska, Maria Szymonowicz, Piotr Podolec, Pawel Rubis
ADVANCES IN CLINICAL AND EXPERIMENTAL MEDICINE
(2020)
Article
Microbiology
Jacek Czepiel, Grazyna Biesiada, Ewelina Pitera, Pawel P. Wolkow, Mateusz Michalak, Aleksander Garlicki
Article
Biochemistry & Molecular Biology
Przemyslaw Kapusta, Joanna Dulinska-Litewka, Justyna Toton-Zuranska, Agnieszka Borys, Pawel S. Konieczny, Pawel P. Wolkow, Michal T. Seweryn
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2020)
Article
Biochemistry & Molecular Biology
Agnieszka H. Ludwig-Slomczynska, Michal T. Seweryn, Przemyslaw Kapusta, Ewelina Pitera, Urszula Mantaj, Katarzyna Cyganek, Pawel Gutaj, Lucja Dobrucka, Ewa Wender-Ozegowska, Maciej T. Malecki, Pawel P. Wolkow
Summary: The study identified genes and genetic variants influencing both BMI and gestational weight gain (GWG) in general population and type 1 diabetes (T1DM) cohorts through TWAS (PrediXcan) and variant association analysis, indicating a potential impact of BMI related loci on GWG and vice versa. The findings suggest a connection between both phenotypes and insulin signaling, glucose homeostasis, mitochondrial metabolism, ubiquitinoylation, and inflammatory responses.
MOLECULAR MEDICINE
(2021)
Article
Microbiology
Agnieszka Sroka-Oleksiak, Tomasz Gosiewski, Wojciech Pabian, Artur Gurgul, Przemyslaw Kapusta, Agnieszka H. Ludwig-Slomczynska, Pawel P. Wolkow, Monika Brzychczy-Wloch
Article
Microbiology
Sandra Mrozinska, Przemyslaw Kapusta, Tomasz Gosiewski, Agnieszka Sroka-Oleksiak, Agnieszka H. Ludwig-Slomczynska, Bartlomiej Matejko, Beata Kiec-Wilk, Malgorzata Bulanda, Maciej T. Malecki, Pawel P. Wolkow, Tomasz Klupa
Summary: Several studies have explored the associations between type 1 diabetes and microbiota, with this study focusing on the colonic microbiota structure in T1DM patients treated with insulin pumps. The study found that there were differences in microbial composition and metabolic pathways between patients with good and poor metabolic control, indicating the potential impact of insulin therapy on colonic flora. Further research is needed to fully understand the implications of these findings.
Article
Biochemistry & Molecular Biology
Milosz Pietrus, Michal Seweryn, Przemyslaw Kapusta, Pawel Wolkow, Kazimierz Pitynski, Gracjan Wator
Summary: Endometrial cancer (EC) is treated based on stage and prognostic risk factors. Differences between grades can be distinguished through miRNA profiling, with miR-375 and miR190b being markers that best distinguish high-grade EC from low-grade EC. One possible mechanism for high-grade EC is virus modulation of host morphology or physiology.
Article
Nutrition & Dietetics
Wojciech Czogala, Malgorzata Czogala, Wojciech Strojny, Gracjan Wator, Pawel Wolkow, Malgorzata Wojcik, Miroslaw Bik Multanowski, Przemyslaw Tomasik, Andrzej Wedrychowicz, Wojciech Kowalczyk, Karol Miklusiak, Agnieszka Lazarczyk, Przemyslaw Halubiec, Szymon Skoczen
Summary: The study revealed that increased expression of the FTO gene is associated with obesity in children and insulin resistance, while higher expression of the PLAG1 gene is linked to a higher body fat percentage. This suggests that the FTO gene may play a significant role in childhood adiposity and glucose-lipid metabolism impairment.
Article
Chemistry, Medicinal
Katarzyna Nazimek, Eugenio Bustos-Moran, Noelia Blas-Rus, Bernadeta Nowak, Justyna Toton-Zuranska, Michal T. Seweryn, Pawel Wolkow, Olga Woznicka, Rafal Szatanek, Maciej Siedlar, Philip W. Askenase, Francisco Sanchez-Madrid, Krzysztof Bryniarski
Summary: This study demonstrates that suppressor T cell-derived EVs carrying miRNA-150 can antigen-specifically downregulate mouse delayed-type hypersensitivity. Pre-incubation with antigen-specific antibodies enhances the inhibitory effect of macrophage-released EVs on effector T cells. The specific binding of EVs to MHC class II-expressing EVs promotes their aggregation and significantly increases their suppressive activity in vivo, potentially offering therapeutic benefits.
Article
Medicine, Research & Experimental
Jaroslaw Szymon Swirta, Gracjan Wator, Michal Seweryn, Przemyslaw Kapusta, Marcin Barczynski, Pawel Wolkow
Summary: Using next-generation sequencing and polymerase chain reaction, this study found that the overexpression of hsa-miR-146b-5p and hsa-miR-146b-3p, as well as the downregulation of hsa-miR-195-3p, could be potential biomarkers to distinguish between follicular adenoma (FA) and well-differentiated thyroid cancer (WDTC) in patients with suspicious for follicular neoplasm (SFN) classification.
ADVANCES IN CLINICAL AND EXPERIMENTAL MEDICINE
(2023)
Article
Biochemistry & Molecular Biology
Agnieszka H. Ludwig-Slomczynska, Michal T. Seweryn, Jerzy Wiater, Agnieszka Borys, Anna Ledwon, Magdalena Druszczynska, Magdalena Labieniec-Watala, Grzegorz J. Lis, Pawel P. Wolkow
Summary: By analyzing the transcriptome of db/db mice, we identified significant changes in gene expression in the liver tissue, which is closely related to immune response and mitochondrial signaling pathways.
Meeting Abstract
Hematology
Maciej Szydlowski, Michal Pawlak, Filip Garbicz, Patryk Gorniak, Justyna Zuranska, Magdalena Krol, Bartlomiej Taciak, Maciej Bialasek, Anna Szumera-Cieckiewicz, Kamil Sokol, Monika Stanczak, Daria Owczarek, Monika Prochorec-Sobieszek, Anna Polak, Emilia Bialopiotrowicz, Michal Kurlapski, Jan Zaucha, Pawel Wolkow, Przemyslaw Juszczynski
Article
Endocrinology & Metabolism
Joanna Gastol, Przemyslaw Kapusta, Anna Polus, Ewelina Pitera, Maria Biela, Pawel Wolkow, Lukasz Pawlinski, Beata Kiec-Wilk
