Article
Pharmacology & Pharmacy
Syed Mohammad Danish, Anshul Gupta, Urooj Ahmad Khan, Nazeer Hasan, Farhan Jalees Ahmad, Musarrat Husain Warsi, Ahmed M. Abdelhaleem Ali, Ameeduzzafar Zafar, Gaurav Kumar Jain
Summary: Intranasal cerium oxide nanoparticles (CNPs) have the potential to improve cognitive function in Alzheimer's disease (AD) through their antioxidant effect.
Article
Biochemistry & Molecular Biology
Jagadeesh Dhamodharan, Ganthimathy Sekhar, Arunachalam Muthuraman
Summary: This study aimed to explore the ameliorative potential of gefitinib (GE) in Alzheimer's disease (AD) mice. The results showed that GE significantly improved AD-associated behavioral, biochemical, and histopathological changes by inhibiting EGFR kinase activation and having antioxidant and antilipid peroxidative effects against A beta(1-42) oligomer-induced neurotoxicity.
Article
Biochemistry & Molecular Biology
Lih-Geeng Chen, Shyr-Yi Lin, Yi-Shan Lee, Ching-Chiung Wang, Wen-Chi Hou
Summary: Agricultural waste from water caltrop hulls was extracted and shown to have AChE inhibitory activities, free radical scavenging activities, and anti-non-enzymatic protein glycation effects. Several compounds with strong AChE inhibitory activities and anti-amyloid 13 peptide aggregation effects were identified. Additionally, treatment with the extracted compounds or water caltrop hull extracts improved learning behavior in mice with induced amnesia.
Article
Chemistry, Multidisciplinary
Nasiara Karim, Inbisat Khan, Imran Khan, Sobia Ahsan Halim, Asaad Khalid, Ashraf N. Abdalla, Najeeb Ur Rehman, Ajmal Khan, Ahmed Al-Harrasi
Summary: This study explored newly synthesized phthalimide derivatives (compounds 1-3) for their potential in improving memory impairment associated with Alzheimer's disease. The compounds exhibited significant inhibition of acetylcholinesterase and butyrylcholinesterase, as well as excellent antioxidant potential. In vivo studies showed that the compounds reversed scopolamine-induced amnesia, indicating their potential as novel therapeutics for Alzheimer's disease.
Article
Biochemistry & Molecular Biology
Khian Giap Lim, Rajavel Varatharajan, Arunachalam Muthuraman
Summary: This study investigated the beneficial effects of beta-carotene on diabetes-associated vascular dementia and its antioxidative actions. Beta-carotene treatment improved cognitive function and reduced oxidative stress markers in rats with diabetic vascular dementia.
Article
Neurosciences
Keyvan Mehri, Zohreh Zavvari Oskuye, Ehsan Nassireslami, Esmail Karami, Mohammad Reza Parvizi
Summary: This study investigated the effects of Botulinum toxin on spatial memory and biochemical and histological parameters in the hippocampus of male rats. Results showed that Botox significantly impaired memory performance and led to a decrease in acetylcholine levels, increase in acetylcholinesterase activity, and morphological damage in the hippocampus. Administration of Rivastigmine partially alleviated these effects and could serve as a protective approach.
Article
Food Science & Technology
Chi Heung Cho, Young Sung Jung, Jong Min Kim, Tae Gyu Nam, Sang-Hoon Lee, Hye Sung Cho, Myoung Chong Song, Ho Jin Heo, Dae-Ok Kim
Summary: The Actinidia eriantha cv. Bidan extract (AEE) showed neuroprotective effects by reducing reactive oxygen species levels and suppressing apoptotic cell death, resulting in improvements in learning and spatial memory in Aβ1-42-treated mice. AEE also increased endogenous antioxidant systems in mouse brain tissue and contained caffeic acid derivatives, suggesting its potential to improve cognitive function as a source of antioxidant phenolics.
JOURNAL OF FUNCTIONAL FOODS
(2021)
Article
Behavioral Sciences
Ewa Zwierzynska, Boguslawa Pietrzak
Summary: Lacosamide does not impair memory and learning processes, with temporary disruption of emotional memory observed only after a single high dose administration.
EPILEPSY & BEHAVIOR
(2021)
Article
Endocrinology & Metabolism
Maryam Sajjadi, Ehsan Oskoueian, Ehsan Karimi, Mahdi Ebrahimi
Summary: The root extract of Amygdalus spinosissima plant contains bioactive phenolic and flavonoid compounds with antioxidant and anti-inflammatory properties, improving learning and memory function in mice. This extract shows promising potential in retarding the development of neurodegenerative diseases such as Alzheimer's disease.
METABOLIC BRAIN DISEASE
(2021)
Article
Biochemistry & Molecular Biology
Derya Osmaniye, Iqrar Ahmad, Begum Nurpelin Saglik, Serkan Levent, Harun M. Patel, Yusuf Ozkay, Zafer Asim Kaplancikli
Summary: Alzheimer's disease is a progressive and fatal neurodegenerative disease that affects the elderly and is characterized by memory and cognitive impairments. In this study, new compounds were synthesized and their inhibitory potentials against AChE and BChE were evaluated. Two compounds showed significant activity against AChE. Further analysis revealed their interactions with the enzyme active site similar to a reference drug.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Bishwajit Das, Durjoy Majumder
Summary: Nerve agent poisoning remains a threat to civilization. This study uses molecular docking to compare the toxicity of different nerve agents and the effectiveness of different antidote drugs, finding that VX is the most harmful nerve agent and HI-6 is the best drug for prevention.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Chemistry, Multidisciplinary
Shraddha Manish Gupta, Ashok Behera, Neetesh K. Jain, Avanish Tripathi, Dinesh Rishipathak, Siddharth Singh, Nafees Ahemad, Meryem Erol, Devendra Kumar
Summary: The main pathological markers of Alzheimer's disease (AD) are Acetylcholinesterase (AChE), Butyrylcholinesterase (BuChE), Amyloid beta (Aβ), and reactive oxygen species (ROS). IND-30, a lead molecule, was found to have selective inhibition on AChE (selectivity ratio: 22.92) compared to BuChE and exhibited maximum inhibition potential on human AChE (IC50: 4.16±0.063 μM). IND-30 was safe on the SH-SY5Y cell line up to a dose of 30 mM. Furthermore, IND-30 also showed the ability to inhibit AChE-induced Aβ aggregation at doses of 0.5, 10, and 20 μM, inhibiting approximately 50% of AChE-induced Aβ aggregation. Thus, IND-30 exhibits multitargeting properties for AD.
Article
Biochemistry & Molecular Biology
Evelyn Munoz-Nunez, Soledad Quiroz-Carreno, Edgar Pastene-Navarrete, David S. Seigler, Carlos Cespedes-Acuna, Ignacio Martinez Valenzuela, Martina Oppliger Munoz, Alexis Salas-Burgos, Julio Alarcon-Enos
Summary: The inhibitory capacity of ceanothanes triterpenes isolated from Chilean Rhamnaceae on acetylcholinesterase and butyrylcholinesterase enzymes was determined in this study. Compound 3 showed a strong inhibitory effect on acetylcholinesterase, with competitive and reversible inhibition mechanism. The interaction with the peripheral anionic site of acetylcholinesterase was suggested to be the cause of its inhibitory effect.
Article
Medicine, Research & Experimental
Karina Sierra, Jean Paulo de Andrade, Luciana R. Tallini, Edison H. Osorio, Osvaldo Yanez, Manuel Isaias Osorio, Nora H. Oleas, Olimpo Garcia-Beltran, Warley de S. Borges, Jaume Bastida, Edison Osorio, Natalie Cortes
Summary: This study isolated and described the alkaloids of Zephyranthes carinata Herb., finding galanthine as the main component with significant inhibitory activity against acetylcholinesterase. Molecular dynamics analysis revealed that galanthine interacts with the peripheral anionic binding site of the enzyme, preventing the entrance and exit of molecules from the active site. This research provides important information for the search of new cholinesterase inhibitors by identifying unknown bio-interactions between bioactive compounds and biological targets.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Chemistry, Physical
Erlon Ferreira Martin, Luiz Antonio Escorteganha Pollo, Layzon Antonio Lemos da Silva, Maique Weber Biavatti, Louis Pergaud Sandjo
Summary: Alzheimer's disease is a prevalent neurodegenerative disease, and a compound family called pyranochromenes has shown potential as inhibitors of acetylcholinesterase, making them promising candidates for the development of new drugs against Alzheimer's disease.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Medicinal
Ilcim Ceyhun, Sevval Karaca, Derya Osmaniye, Begum N. Saglik, Serkan Levent, Yusuf Ozkay, Zafer A. Kaplancikli
Summary: According to the cholinergic hypothesis, an increase in acetylcholine levels in Alzheimer's disease patients can slow down symptoms. A study focused on designing and synthesizing 12 new chalcones, with compounds 2d, 2f, 2j, and 2l showing significant inhibitory activity against AChE.Further research is needed to understand the potential of these compounds in treating Alzheimer's disease.
ARCHIV DER PHARMAZIE
(2022)
Article
Biochemistry & Molecular Biology
Derya Osmaniye, Iqrar Ahmad, Begum Nurpelin Saglik, Serkan Levent, Harun M. Patel, Yusuf Ozkay, Zafer Asim Kaplancikli
Summary: Alzheimer's disease is a progressive and fatal neurodegenerative disease that affects the elderly and is characterized by memory and cognitive impairments. In this study, new compounds were synthesized and their inhibitory potentials against AChE and BChE were evaluated. Two compounds showed significant activity against AChE. Further analysis revealed their interactions with the enzyme active site similar to a reference drug.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Chemistry, Multidisciplinary
Asaf Evrim Evren, Abdullah Burak Karaduman, Begum Nurpelin Saglik, Yusuf Ozkay, Leyla Yurttas
Summary: In order to find new chemotherapeutics for infectious diseases, we designed, synthesized, and tested 14 new quinoline derivatives. Compound 4m showed the most potent antifungal activity with low cytotoxicity and fewer side effects, while compounds 4j and 4l can be used for special patients suffering from fungal infections in addition to the primary disease.
Article
Biochemistry & Molecular Biology
Taha Almarsoomi, Derya Osmaniye, Begum Nurpelin Saglik, Serkan Levent, Usman Ghani, Yusuf Ozkay, Zafer Asim Kaplancikli
Summary: In this study, ten thiazole derivative compounds were synthesized and analyzed by NMR methods. The inhibitory effect of these compounds on COX enzymes was investigated, and compounds 5a, 5b, and 5c were found to be the most potent against COX-2 isoenzyme.
JOURNAL OF MOLECULAR RECOGNITION
(2023)
Article
Chemistry, Multidisciplinary
Derya Osmaniye, Begum Nurpelin Saglik, Narmin Khalilova, Serkan Levent, Gizem Bayazit, Ulkuye Dudu Gul, Yusuf Ozkay, Zafer Asim Kaplancikli
Summary: Cancer is a prevalent and progressive disease, and its incidence is increasing globally. The development of novel drugs is necessary due to the side effects and resistance of existing drugs. Additionally, cancer patients are susceptible to bacterial and fungal infections. In this study, new naphthalene-chalcone derivatives were synthesized and their anticancer-antibacterial-antifungal properties were evaluated. Compound 2j exhibited anticancer activity against the A549 cell line with IC50 = 7.835 +/- 0.598 mu M, as well as antibacterial and antifungal activities. It also demonstrated apoptotic potential and inhibited VEGFR-2 enzyme.
Article
Biochemistry & Molecular Biology
Nazli Turan Yucel, Ummuhan Kandemir, Umut Irfan Ucel, Umide Demir Ozkay, Ozgur Devrim Can
Summary: The therapeutic potential of vortioxetine on mechanical hyperalgesia/allodynia was investigated in rats with streptozotocin-induced diabetes, and its possible mechanism of action was elucidated in this study. The findings demonstrated that vortioxetine administration significantly improved diabetes-induced hyperalgesia and allodynia responses in the rats without affecting their motor coordination. The involvement of the catecholaminergic system, alpha(2)- and beta(2)-adrenoceptors, D-2/3 dopaminergic receptors and cholinergic muscarinic receptors in the exhibited pharmacological activity was suggested.
Article
Biochemistry & Molecular Biology
Neslihan Conger, Derya Osmaniye, Begum Nurpelin Saglik, Serkan Levent, Yusuf Ozkay, Zafer Asim Kaplancikli
Summary: Compound 3a, among the 12 synthesized compounds, showed the strongest inhibitory potential against AChE enzyme and exhibited important interactions. Molecular dynamics studies demonstrated its stability in vivo.
JOURNAL OF MOLECULAR RECOGNITION
(2023)
Article
Biochemistry & Molecular Biology
Delal Erzurum, Derya Osmaniye, Begum Nurpelin Saglik, Serkan Levent, Yusuf Ozkay, Zafer Asim Kaplancikli
Summary: Carbonic anhydrase (CA) enzymes are common catalytic enzymes in many organisms and play important physiological roles. This study synthesized 10 sulfonamide derivatives and evaluated their inhibition effects on CA enzymes through experimental and analytical methods. The results showed that compound 2e exhibited the strongest interaction with the active sites of CA enzymes.
ZEITSCHRIFT FUR NATURFORSCHUNG SECTION C-A JOURNAL OF BIOSCIENCES
(2023)
Article
Chemistry, Multidisciplinary
Derya Osmaniye, Nurnehir Baltaci Bozkurt, Serkan Levent, Gamze Benli Yardimci, Begum Nurpelin Saglik, Yusuf Ozkay, Zafer Asim Kaplancikli
Summary: In this study, 17 new triazole derivative compounds were synthesized and their structures were determined by spectroscopic analysis methods. The antifungal effects of these compounds on Candida strains were evaluated in vitro. Compound 5d showed promising activity against Candida glabrata and Candida krusei with higher activity than fluconazole. Molecular docking and molecular dynamics simulations further supported the activity of compound 5d.
Article
Chemistry, Multidisciplinary
Berkant Kurban, Begum Nurpelin Saglik, Derya Osmaniye, Serkan Levent, Yusuf Ozkay, Zafer Asim Kaplancikli
Summary: Lung cancer, a common cancer with high mortality rates, can be treated with promising EGFR inhibitors. In this study, new EGFR inhibitor candidates containing thiadiazole and pyrazole rings were developed and evaluated. Compounds 6d, 6g, and 6j showed inhibitory activity against A549 cell line, with IC50 values of 5.176±0.164, 1.537±0.097, and 8.493±0.667 μM, respectively. Compound 6g also exhibited significant inhibition of mitochondrial membrane potential and EGFR enzyme with IC50 values of 0.024±0.002 μM.
Article
Chemistry, Multidisciplinary
Nurdan Ebru Irmak, Begum Nurpelin Saglik, Ismail Celik, Hasan Tahsin Sen, Yusuf Ozkay, Guelgun Ayhan-Kilcigil
Summary: A novel class of benzimidazole-thiazole compounds were designed as potential inhibitors of cyclooxygenase. In vitro studies showed dose-dependent inhibitory effects on COX-1, with reduced effectiveness at lower concentrations. Among the compounds tested, 7b, 7c, 8b, and 8c exhibited the most promising activity against COX-2. Molecular docking and molecular dynamics simulations supported the potential of these compounds to act as potent and selective COX-2 inhibitors.
NEW JOURNAL OF CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Derya Osmaniye, Serkan Levent, Begum Nurpelin Saglik, Sennur Gorgulu, Yusuf Ozkay, Zafer Asim Kaplancikli
Summary: New imidazole-2,3-dihydrothiazole derivatives were synthesized and their antifungal activities were evaluated in this study. Compound 2d exhibited activity against the C. parapsilosis strain and was the most potent derivative in the series. Moreover, compound 2d inhibited the biosynthesis of ergosterol. The results of molecular docking and molecular dynamics simulations were consistent with the activity studies.
NEW JOURNAL OF CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Derya Osmaniye, Serkan Levent, Begum Nurpelin Saglik, Sennur Gorgulu, Yusuf Ozkay, Zafer Asim Kaplancikli
Summary: In this study, new imidazole-2,3-dihydrothiazole derivatives were synthesized and characterized. The compounds' antifungal activities and their inhibition on ergosterol biosynthesis were evaluated. Compound 2d showed the highest antifungal activity and significant inhibition on ergosterol biosynthesis.
NEW JOURNAL OF CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Derya Osmaniye, Serkan Levent, Begum Nurpelin Saglik, Abdullah Burak Karaduman, Yusuf Ozkay, Zafer Asim Kaplancikli
Summary: In this study, new aromatase-MAO-B dual inhibitors were developed to fight against breast cancer. These inhibitors can alleviate the side effects of aromatase inhibitors and prevent their impact on dopaminergic neurons.
NEW JOURNAL OF CHEMISTRY
(2022)
