Article
Clinical Neurology
Nunzio Pomara, Davide Bruno, Chelsea Reichert Plaska, Anilkumar Pillai, Jaime Ramos-Cejudo, Ricardo Osorio, Bruno P. Imbimbo, Amanda Heslegrave, Henrik Zetterberg, Kaj Blennow
Summary: This study found that individuals with depression had lower levels of BChE in their cerebrospinal fluid, and lower BChE and AChE activities were associated with reduced markers of neuroinflammation. Additionally, there was an inverse relationship between peripheral inflammation markers and levels of BChE and AChE in the cerebrospinal fluid of patients with depression.
JOURNAL OF AFFECTIVE DISORDERS
(2021)
Article
Biochemistry & Molecular Biology
Alessandro Pesaresi, Doriano Lamba, Lyubomir Vezenkov, Daniela Tsekova, Valentin Lozanov
Summary: Complex neurological disorders, including Alzheimer's disease, require multitarget drugs for treatment. This study reports on the synthesis and activity profiles of seven multitarget anti-Alzheimer compounds, and investigates their mechanisms using molecular docking simulations and enzyme inhibition kinetics.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Article
Neurosciences
Saritha S. L. Silva, Luciane V. V. Tureck, Leonardo C. Souza, Joao V. V. Mello-Hortega, Ana Luiza Piumbini, Mayza D. Teixeira, Lupe Furtado-Alle, Maria A. B. F. Vital, Ricardo L. R. Souza
Summary: Alzheimer's disease (AD) is a complex disease and the understanding of its pathogenesis is still incomplete. The cholinergic system has been implicated in AD, with alterations in acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and acetyltransferase (ChAT) activities. A rat model of late onset AD (LOAD) induced by intra-cerebroventricular injection of streptozotocin (icv-STZ) was used to study the long-term effects on the cholinergic system. The results showed decreased AChE and BChE activities in the hippocampus of STZ-induced rats euthanized 30 and 120 days after icv-STZ, suggesting that the cholinergic system may not be compromised in the long term.
Review
Biochemistry & Molecular Biology
Anna Bubley, Alexaner Erofeev, Peter Gorelkin, Elena Beloglazkina, Alexander Majouga, Olga Krasnovskaya
Summary: Alzheimer's disease (AD) is a neurodegenerative disorder characterized by Aβ aggregation, tau hyperphosphorylation, and loss of cholinergic neurons. AD is also associated with oxidative stress, metal dyshomeostasis, inflammation, and cell cycle dysregulation. In this review, THA-based hybrids are summarized as potential anti-AD agents, highlighting strategies for drug design that have led to cognitive improvements and reduced hepatotoxicity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Jun-Cheng Su, Qianrong Pan, Xingyuan Xu, Xia Wei, Xueping Lei, Peng Zhang
Summary: Compound 8 was found to have remarkable anti-inflammatory activity and regulate the cholinergic anti-inflammatory pathway by increasing α7nAchR expression and inhibiting downstream signaling pathways.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Article
Pharmacology & Pharmacy
Ana Matosevic, Andreja Radman Kastelic, Ana Mikelic, Antonio Zandona, Maja Katalinic, Ines Primozic, Anita Bosak, Tomica Hrenar
Summary: The study confirmed that quinuclidinium carbamates are promising candidates for further development as CNS-active drugs, particularly for Alzheimer's disease treatment. The synthesized compounds showed good acetylcholinesterase and butyrylcholinesterase inhibitory activity, and were able to pass the blood-brain barrier.
Article
Biochemistry & Molecular Biology
Ana Mercia Silva Mascarenhas, Raquel Bianca Marchesine de Almeida, Moyses Fagundes de Araujo Neto, Gessica Oliveira Mendes, Jorddy Neves da Cruz, Cleydson Breno Rodrigues dos Santos, Mariana Borges Botura, Franco Henrique Andrade Leite
Summary: This study aimed to identify promising dual inhibitors against hAChE and hBuChE using in silico approaches. By constructing pharmacophore models and conducting molecular docking experiments, several potential dual inhibitors against both enzymes were identified.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2021)
Article
Biochemistry & Molecular Biology
Yingjie Xia, Qiyun Wu, Shinghung Mak, Etta Y. L. Liu, Brody Z. Y. Zheng, Tina T. X. Dong, Rongbiao Pi, Karl W. K. Tsim
Summary: This study explores the role of AChE in neuroinflammation and finds that AChE expression is upregulated during inflammation, while ACh or α7 nAChR agonists can suppress the production of pro-inflammatory cytokines and the phagocytosis of microglia.
Article
Biochemistry & Molecular Biology
Selena P. Maxwell, Meghan K. Cash, Sultan Darvesh
Summary: A study found that some octogenarians and older adults maintain normal cognitive function despite a high prevalence of cognitive decline linked to neurodegeneration or aging. The preserved cholinergic neurotransmission in specific brain regions may contribute to their intact cognition.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Article
Chemistry, Medicinal
Ling Lv, Mireguli Maimaitiming, Yan Huang, Jichen Yang, Shuxia Chen, Yanfeng Sun, Xuetao Zhang, Xin Li, Changhu Xue, Pingyuan Wang, Chang-Yun Wang, Zhiqing Liu
Summary: A series of quinazolin-4(3H)-one derivatives with cholinesterase inhibition and anti-inflammatory activities were designed and synthesized. The compound MR2938 showed promising inhibitory activity against acetylcholinesterase and suppressed NO production. It also decreased the levels of pro-inflammatory cytokines and suppressed neuroinflammation through blocking certain signaling pathways. These results suggest that MR2938 could be developed as a potential lead compound for anti-AD drugs.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Physical
Samira Ansari, Milad Noori, Keyvan Pedrood, Maryam Mohammadi-Khanaposhtani, Ali Moazzam, Samanesadat Hosseini, Bagher Larijani, Hossein Adibi, Mahmood Biglar, Haleh Hamedifar, Hojjat Rahmani, Mohammad Mahdavi, Nastaran Sadeghian, Parham Taslimi
Summary: A series of new aryl(4-phenylpiperazin-1-yl)methanethione derivatives were designed, synthesized, and evaluated for their inhibitory activity against cholinesterases and alpha glucosidase. The synthesized compounds demonstrated higher potency than the standard inhibitor donepezil for cholinesterases and showed superior activity compared to donepezil for alpha glucosidase. Compound 4k exhibited the highest activity against cholinesterases and established significant interactions with the target enzyme residues. Druglikeness/ADME/Toxicity prediction suggested that these compounds have the potential to be drug candidates with suitable ADME and toxicity profiles.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Biochemistry & Molecular Biology
Junio G. Silva, Tatiane F. Borgati, Samuel M. G. Lopes, Niels Heise, Sophie Hoenke, Rene Csuk, Luiz C. A. Barbosa
Summary: A series of amides derived from (3aR)-(+)-sclareolide were synthesized and evaluated as inhibitors for AChE or BuChE. Five amides showed strong inhibition towards BuChE, outperforming the positive control galantamine, and exhibited favorable properties for drug development, including permeability across the blood brain barrier and adherence to Lipinski rules.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Sri Devi Sukumaran, Shah Bakhtiar Nasir, Jia Ti Tee, Michael J. C. Buckle, Rozana Othman, Noorsaadah Abd Rahman, Vannajan Sanghiran Lee, Syed Nasir Abbas Bukhari, Chin Fei Chee
Summary: A series of C4-substituted tertiary nitrogen-bearing 2 '-hydroxychalcones were synthesized and compound 4c showed the best inhibition against acetylcholinesterase with high selectivity over butyrylcholinesterase. Molecular docking studies and ADMET analysis support the therapeutic potential of compound 4c as a lead compound for Alzheimer's disease treatment.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Bushra Adalat, Fazal Rahim, Wajid Rehman, Zarshad Ali, Liaqat Rasheed, Yousaf Khan, Thoraya A. Farghaly, Sulaiman Shams, Muhammad Taha, Abdul Wadood, Syed A. A. Shah, Magda H. Abdellatif
Summary: Twenty-one analogs based on benzimidazole, incorporating a substituted benzaldehyde moiety (1-21), were synthesized and screened for their acetylcholinesterase and butyrylcholinesterase inhibition profiles. Compound 3 showed the most potent activity due to the presence of chloro groups at the 3 and 4 positions of the phenyl ring. Molecular dynamics simulations revealed that compound 3 formed the most stable complex with both acetylcholinestrase and butyrylcholinesterase, displaying higher binding affinities compared to the standard inhibitor donepezil.
Article
Plant Sciences
Jing Li, Guangyi Yang, Wenfeng Shi, Xiaoping Fang, Lintao Han, Yan Cao
Summary: This study screened and identified potential anti-Alzheimer's disease (AD) active components from Hedyotis diffusa. Through in vivo experiments, one of these components, quercetin-3-O-sophoroside (QS), was confirmed as an effective anti-AD agent. These findings provide a molecular basis for the potential applications of Hedyotis diffusa in the medical industry.
JOURNAL OF ETHNOPHARMACOLOGY
(2022)
Article
Electrochemistry
Miroslav Pohanka
Summary: The quartz crystal microbalance biosensor was developed for the simple measurement of HSP60 levels, showing high sensitivity, rapid detection, and resistance to interference. The assay results were highly correlated with standard ELISA, making it a reliable tool for HSP60 detection.
INTERNATIONAL JOURNAL OF ELECTROCHEMICAL SCIENCE
(2021)
Review
Biochemistry & Molecular Biology
Miroslav Pohanka
Summary: Melatonin is a hormone produced naturally by the human body, which regulates the circadian rhythm and has antioxidative and cell cycle regulating properties. It is currently used as a medication for sleep disorders and shows potential for preventing chemical exposure and treating other diseases.
CURRENT MEDICINAL CHEMISTRY
(2022)
Review
Electrochemistry
Miroslav Pohanka
Summary: Biosensors are important analytical devices, and aptamers as a new biorecognition element play a significant role in them. Aptamers are short sequences of DNA, RNA, and peptides with high affinity similar to antibodies. Aptasensors with immobilized aptamers serve as an alternative to biosensors based on antibodies and other bioreceptor molecules.
INTERNATIONAL JOURNAL OF ELECTROCHEMICAL SCIENCE
(2022)
Review
Chemistry, Medicinal
Miroslav Pohanka
Summary: Caffeine, an abundant compound found in coffee, food, and drugs, primarily interacts with adenosine receptors but also influences other physiological pathways. Long-term intake of caffeine-containing products can have a significant impact, while acute and chronic toxicity of caffeine is low. Recent research suggests that caffeine may play a role in the progression of certain neurodegenerative diseases. This review article presents the latest findings on the impact of caffeine on neurodegenerative diseases and describes important facts about its effects.
MINI-REVIEWS IN MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Analytical
Miroslav Pohanka, Jitka Zakova
Summary: This paper presents a colorimetric biosensor constructed using 3D-printed multiwell pads treated with indoxylacetate as a chromogenic substrate and gold nanoparticles with the immobilized enzyme butyrylcholinesterase. The biosensor exhibits good sensitivity to neurotoxic compounds and can detect carbofuran and paraoxon ethyl with low limits of detection. It offers advantages of low cost, simplicity, and portability, and can fully replace standard spectroscopic methods.
INTERNATIONAL JOURNAL OF ANALYTICAL CHEMISTRY
(2022)
Review
Chemistry, Analytical
Miroslav Pohanka
Summary: C-reactive protein is an important component of the immune system's response to pathological impulses and can be used for diagnosing various pathological states. The current methods for CRP diagnosis have limitations, but research on biosensors and bioassay devices is providing more sensitive and suitable tools.
Review
Chemistry, Multidisciplinary
Ondrej Kerestes, M. Pohanka
Summary: This review article provides an introduction to enzyme-based biosensors and presents selected examples of pesticide detection using these biosensors. While cholinesterases are commonly used for pesticide analysis, the importance of alternative enzymes is also highlighted. The article presents the current status of enzyme-based biosensors for pesticide analysis in the environment and discusses the potential of using open source electronics as a promising interface for wireless biosensing.
Review
Electrochemistry
Miroslav Pohanka
Summary: Biological warfare agents are infectious microorganisms and toxins with lethal potential for military or terrorist use. Early and reliable detection of these agents at the sites of use is crucial, and the ideal analytical devices should be hand-held or pocket-sized to cover all possible scenarios. However, current handheld analyzers have limitations such as size, weight, and sensitivity. Biosensors, combining a physical sensor with a recognition part, offer a platform for high-sensitivity detection with a simple design. This review focuses on electrochemical biosensors for the detection of biological warfare agents and discusses the progress in this field.
INTERNATIONAL JOURNAL OF ELECTROCHEMICAL SCIENCE
(2022)
Review
Chemistry, Analytical
Miroslav Pohanka
Summary: Point-of-care tests, especially lateral flow immunoassays, have proven to be valuable tools for early diagnosis of COVID-19. Biosensors, composed of selective molecules and sensor platforms, offer an advanced alternative to current diagnostic tests and laboratory methods.
Review
Electrochemistry
Miroslav Pohanka
Summary: Butyrylcholinesterase (BChE) biosensors are analytical devices that utilize BChE as a biorecognition element for specific interaction with analytes. They are particularly useful in detecting organophosphate and carbamate neurotoxins. Compared to acetylcholinesterase (AChE) biosensors, BChE biosensors are less sensitive to natural toxin inhibition and can work with multiple enzymatic substrates. Recent advancements in materials and analytical methods have expanded the applications of BChE biosensors. This review compares BChE biosensors with other analytical devices for neurotoxic compound assays, explains the assay principles, and introduces relevant recent papers.
INTERNATIONAL JOURNAL OF ELECTROCHEMICAL SCIENCE
(2022)
Article
Chemistry, Analytical
Miroslav Pohanka
Summary: In this study, a simple biosensor based on a QCM piezoelectric sensor and a conjugate of gold nanoparticles-antibodies conjugate was developed for procalcitonin assay suitable for point-of-care tests. The biosensor showed a strong correlation with the standard ELISA method and was free from false positive or negative results and interferences. The practical relevance of the biosensor was supported by the findings and the potential application of the assay principle for the development of biosensors for other markers is inferred.
Review
Chemistry, Analytical
Miroslav Pohanka
Summary: An immunosensor is a biosensor used for detecting hazardous substances like aflatoxin, botulinum toxin, ricin, and Shiga toxin. It has various applications including outdoor assays, point-of-care tests, and laboratory use. Some immunosensors have been successfully commercialized as tools for toxin assays, and new devices and advanced materials and techniques are being developed to enhance their competitiveness in this field. This review summarizes current applications and new trends of immunosensors based on recent papers in this area.
Article
Chemistry, Analytical
Ondrej Kerestes, Miroslav Pohanka
Summary: Excessive use of pesticides can harm the environment and human beings. This study presents a prototype of a photometer tested with cholinesterase to detect pesticides in the environment. The open-source portable photodetection platform using RGB LED and TSL230R sensor is equivalent to commercial photometry.
Article
Electrochemistry
Miroslav Pohanka
Summary: Low-molecular-weight antioxidants are chemical compounds that protect against oxidative damage. They have important biological functions and can be used as food or material preservatives, as well as in pharmacology. Chemical identification of antioxidants is possible but time-consuming and expensive. Optical assays such as FRAP, DPPH, and ABTS are commonly used to measure antioxidant capacity. Voltammetry provides an alternative method with some advantages over optical assays. This review describes and discusses basic optical and voltammetric assays for determining antioxidant capacity.
INTERNATIONAL JOURNAL OF ELECTROCHEMICAL SCIENCE
(2023)
Review
Medicine, General & Internal
Pavla Valkova, Miroslav Pohanka
Summary: Diabetes mellitus is a global health problem and a lifelong chronic disease that affects millions of people worldwide. The new types of biosensors offer new opportunities for diabetic patient care and improve current methods.
BRATISLAVA MEDICAL JOURNAL-BRATISLAVSKE LEKARSKE LISTY
(2022)
