Dhamodharan, G Mohan, C Gopi
Published in
Molecular diversity
Multi-target directed ligand-based 2D-QSAR models were developed using different N-benzyl piperidine derivatives showing inhibitory activity toward acetylcholinesterase (AChE) and β-Site amyloid precursor protein cleaving enzyme (BACE1). Five different classes of molecular descriptors belonging to spatial, structural, thermodynamics, electro-topolo...
Ganeshpurkar, Ankit Singh, Ravi Shivhare, Shalini Divya, Kumar, Devendra Gutti, Gopichand Singh, Ravibhushan Kumar, Ashok Singh, Sushil Kumar
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Molecular diversity
Structure-based drug design (SBDD) is an important in silico technique, used for the identification of enzyme inhibitors. Acetylcholinesterase (AChE), obtained from Electrophorus electricus (ee), is widely used for the screening of AChE inhibitors. It shares structural homology with the AChE of human and other organisms. Till date, the three-dimens...
Mundy, Paige C Mendieta, Rosalia Lein, Pamela J
Diisopropylfluorophosphate (DFP) is an organophosphate (OP) that is commonly used as a surrogate of OP nerve agents to study the neurotoxic effects of acute OP intoxication. In preliminary studies, we discovered abnormally high incidence of deaths in DMSO control zebrafish larvae housed in the same 96-well plate as DFP-exposed larvae and hypothesiz...
Firdaus, Zeba Singh, Neha Prajapati, Santosh Kumar Krishnamurthy, Sairam Singh, Tryambak Deo
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Drug and chemical toxicology
Chronic D-galactose (D-gal) administration causes cognitive impairment and is used widely in animal models for anti-aging studies. Centella asiatica (CA), a traditional herbal medicine, has been used as a brain tonic to enhance memory. This study evaluates the neuroprotective role of an ethanolic extract of Centella asiatica (CAE) against D-gal-ind...
Ogidigo, Joyce Oloaigbe Anosike, Chioma Assumpta Joshua, Parker Elijah Ibeji, Collins U Nwanguma, Bennett C Nwodo, Okwesili Fred Chiletugo
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Toxicology mechanisms and methods
Toxic metals such as aluminum accumulation in the brain have been associated with the pathophysiology of several neurodegenerative disorders. Bryophyllum pinnatum leaves contain a vast array of polyphenols, particularly flavonoids, that may play a role in the prevention of toxic and degenerative effects in the brain. This study assessed the neuro-r...
Puopolo, Tess Liu, Chang Ma, Hang Seeram, Navindra P.
Published in
Medical Cannabis and Cannabinoids
Introduction Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are two cholinergic enzymes catalyzing the reaction of cleaving acetylcholine into acetate and choline at the neuromuscular junction. Abnormal hyperactivity of AChE and BChE can lead to cholinergic deficiency, which is associated with several neurological disorders including ...
Moreira, Natália Chermont dos Santos Lima, Jéssica Ellen Barbosa de Freitas Marchiori, Marcelo Fiori Carvalho, Ivone Sakamoto-Hojo, Elza Tiemi
Published in
Journal of Alzheimer's Disease Reports
Alzheimer’s disease (AD) is a slowly progressive neurodegenerative disease conceptualized as a continuous process, ranging from mild cognitive impairment (MCI), to the mild, moderate, and severe clinical stages of AD dementia. AD is considered a complex multifactorial disease. Currently, the use of cholinesterase inhibitors (ChEI), such as tacrine,...
Rajkumar, Manickam Sakthivel, Murugesan Senthilkumar, Kottaisamy Thangaraj, Ramasundaram Kannan, Soundarapandian
Published in
Current Research in Pharmacology and Drug Discovery
• Hydrogel-based drug treatment normalized cognitive deficit sin ICV-STZ rats with AD. • Hydrogel-based drug treatment enhanced behavioral and biochemical activities in AD-induced rats. • Hydrogel-based drug treatment increased memory performance and neuronal growth in rats with AD. • Antioxidant potential of hydrogel-tethered Gal blocked apoptosis...
Güleç, Özcan Türkeş, Cüneyt Arslan, Mustafa Demir, Yeliz Yeni, Yeşim Hacımüftüoğlu, Ahmet Ereminsoy, Ergün Küfrevioğlu, Ömer İrfan Beydemir, Şükrü
Published in
Molecular diversity
The acetylcholinesterase and carbonic anhydrase inhibitors (AChEIs and hCAIs) remain key therapeutic agents for many bioactivities such as anti-Alzheimer and antiobesity antiepileptic, anticancer, antiinfective, antiglaucoma, and diuretic effects. Here, it has been attempted to discover novel multi-target AChEIs and hCAIs that are highly potent, or...
Oyeleke, Mosunmola Busayo Oni, Heritage Tolulope Arokoyo, Oluwatamilore Lois Owoyele, Bamidele Victor
Published in
Heliyon
Bacopa floribunda (BF), an African traditional plant and its species have been widely used as brain tonic for memory enhancement. It has also been reported to help relieve anxiety and some psychological disorders. This study aimed to investigate the mechanisms of action of BF on Amyloid beta (Aβ) 1-42 peptides induced cognitive deficit in male Wist...