Multi-target screening mines hesperidin as a multi-potent inhibitor: Implication in Alzheimer's disease therapeutics

2016 ◽  
Vol 121 ◽  
pp. 810-822 ◽  
Author(s):  
Sandipan Chakraborty ◽  
Jaya Bandyopadhyay ◽  
Sourav Chakraborty ◽  
Soumalee Basu
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Potent Inhibitor ◽  
Target Screening

Multi-functional neuroprotective activity of neohesperidin dihydrochalcone: a novel scaffold for Alzheimer's disease therapeutics identified via drug repurposing screening

2018 ◽  
Vol 42 (14) ◽  
pp. 11755-11769 ◽  
Author(s):  
Sandipan Chakraborty ◽  
Jyotirmoy Rakshit ◽  
Jaya Bandyopadhyay ◽  
Soumalee Basu
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Antioxidant Activity ◽  
Drug Repurposing ◽  
Neuroprotective Activity ◽  
Amyloid Aggregation ◽  
Aggregation Inhibition ◽  
Target Screening ◽  
Novel Scaffold

Multi-target screening identifies neohesperidin dihydrochalcone for Alzheimer's disease therapeutics, which exhibits strong BACE1 and amyloid aggregation inhibition along with antioxidant activity.

scholarly journals The Therapeutic Potential of Berberis darwinii Stem-Bark: Quantification of Berberine and In Vitro Evidence for Alzheimer's Disease Therapy

2011 ◽  
Vol 6 (8) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Solomon Habtemariam
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Charles Darwin ◽  
Potent Inhibitor ◽  
Methanolic Extract ◽  
Therapeutic Potential ◽  
Stem Bark ◽  
Acetylcholinesterase Inhibition ◽  
Disease Therapy

Berberis darwinii is native to South America but has been widely distributed in Europe and other continents following its discovery by Charles Darwin. Herewith, the therapeutic potential of stem-bark of the plant for treating Alzheimer's disease was studied using an in vitro acetylcholinesterase inhibition assay. It was found that the methanolic extract of the stem-bark was a potent inhibitor of the enzyme with an IC50 value of 1.23 ± 0.05 μg/mL. An HPLC-based berberine quantification study revealed an astonishing 38% yield of the dried methanolic extract.

scholarly journals Bioactivity-guided Separation of the Active Compounds in Acacia Pennata Responsible for the Prevention of Alzheimer's Disease

2015 ◽  
Vol 10 (8) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Pattamapan Lomarat ◽  
Sirirat Chancharunee ◽  
Natthinee Anantachoke ◽  
Worawan Kitphati ◽  
Kittisak Sripha ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Carboxylic Acid ◽  
Spectroscopic Analysis ◽  
Potent Inhibitor ◽  
Health Benefits ◽  
Biological Testing ◽  
Amyloid Aggregation ◽  
Active Compounds ◽  
Β Amyloid

The objective of this study was to evaluate the health benefits of plants used in Thai food, specifically Acacia pennata Willd., in Alzheimer's prevention. A. pennata twigs strongly inhibited β-amyloid aggregation. Bioactivity-guided separation of the active fractions yielded six known compounds, tetracosane (1), 1-(heptyloxy)-octadecane (2), methyl tridecanoate (3), arborinone (4), confertamide A (5) and 4-hydroxy-1-methyl-pyrrolidin-2-carboxylic acid (6). The structures were determined by spectroscopic analysis. Biological testing revealed that tetracosane (1) was the most potent inhibitor of β-amyloid aggregation, followed by 1-(heptyloxy)-octadecane (2) with IC50 values of 0.4 and 12.3 μM. Methyl tridecanoate (3), arborinone (4) and 4-hydroxy-1-methyl-pyrrolidin-2-carboxylic acid (6) moderately inhibited β-amyloid aggregation. In addition, tetracosane (1) and methyl tridecanoate (3) weakly inhibited acetylcholinesterase (AChE). These results suggested that the effect of A pennata on Alzheimer's disease was likely due to the inhibition of β-amyloid aggregation. Thus A. pennata may be beneficial for Alzheimer's prevention.

scholarly journals Therapeutic Potential of Multifunctional Tacrine Analogues

2019 ◽  
Vol 17 (5) ◽  
pp. 472-490 ◽  
Author(s):  
Maja Przybyłowska ◽  
Szymon Kowalski ◽  
Krystyna Dzierzbicka ◽  
Iwona Inkielewicz-Stepniak
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Liver Toxicity ◽  
Potent Inhibitor ◽  
Therapeutic Potential ◽  
Treatment Strategies ◽  
Biological Properties ◽  
New Paradigm ◽  
Experimental Systems

Tacrine is a potent inhibitor of cholinesterases (acetylcholinesterase and butyrylcholinesterase) that shows limiting clinical application by liver toxicity. In spite of this, analogues of tacrine are considered as a model inhibitor of cholinesterases in the therapy of Alzheimer’s disease. The interest in these compounds is mainly related to a high variety of their structure and biological properties. In the present review, we have described the role of cholinergic transmission and treatment strategies in Alzheimer’s disease as well as the synthesis and biological activity of several recently developed classes of multifunctional tacrine analogues and hybrids, which consist of a new paradigm to treat Alzheimer’s disease. We have also reported potential of these analogues in the treatment of Alzheimer’s diseases in various experimental systems.

scholarly journals Target screening of miR126 in pathological process of Alzheimer's disease

IBRO Reports ◽  
2019 ◽  
Vol 6 ◽  
pp. S99
Author(s):  
Seohoe Song ◽  
Haneul Noh ◽  
Kai C. Sonntag ◽  
Hyemyung Seo
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Pathological Process ◽  
Target Screening

scholarly journals Acetyl cholinesterase: a potential target for Alzheimer’s disease intervention

2020 ◽  
Vol 7 (2) ◽  
pp. 95-97
Author(s):  
Sandhya Khadka ◽  
Rajesh Basnet ◽  
Sandeep Shrestha ◽  
Yuchun Wang ◽  
Radheshyam Gupta
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cholinesterase Activity ◽  
Potent Inhibitor ◽  
Memory Loss ◽  
Brain Cells ◽  
Economic Aspects ◽  
Acetyl Cholinesterase ◽  
Ache Inhibitors

Alzheimer's disease is a neurological disorder in which the death of brain cells causes memory loss and cognitive decline. The role of treatment is not limited to pharmacology, but also involves many factors, such as the psychological, social, and economic aspects of the patient and family. It is important to consider the use of AChe inhibitors in patients with mild to moderate AD, despite cost issues and in the absence of any other immediate progression. Although there are allots of currently available inhibitor for acetyl cholinesterase but there is no selective potent inhibitor for AD. so, there is an urgent need discover of compounds that are active against Acetyl cholinesterase, along  with there is need of molecular modeling for  identifying functional groups that may be important for inhibiting Acetyl cholinesterase activity.

Cognitive control constrains memory attributions

2019 ◽  
Vol 42 ◽  
Author(s):  
Colleen M. Kelley ◽  
Larry L. Jacoby
Keyword(s):  
Alzheimer’S Disease ◽  
Older Adults ◽  
Alzheimer's Disease ◽  
Traumatic Brain Injury ◽  
Brain Injury ◽  
Cognitive Control

Abstract Cognitive control constrains retrieval processing and so restricts what comes to mind as input to the attribution system. We review evidence that older adults, patients with Alzheimer's disease, and people with traumatic brain injury exert less cognitive control during retrieval, and so are susceptible to memory misattributions in the form of dramatic levels of false remembering.

Formation of paired helical filaments in Alzheimer's disease

1984 ◽  
Vol 42 ◽  
pp. 302-303
Author(s):  
J. Metuzals ◽  
D. F. Clapin ◽  
V. Montpetit
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Frontal Lobe ◽  
Giant Axon ◽  
Paired Helical Filaments ◽  
Normal Brain ◽  
Protein Assemblies ◽  
Electron Microscopic ◽  
Helical Symmetry ◽  
Structural Levels

Information on the conformation of paired helical filaments (PHF) and the neurofilamentous (NF) network is essential for an understanding of the mechanisms involved in the formation of the primary lesions of Alzheimer's disease (AD): tangles and plaques. The structural and chemical relationships between the NF and the PHF have to be clarified in order to discover the etiological factors of this disease. We are investigating by stereo electron microscopic and biochemical techniques frontal lobe biopsies from patients with AD and squid giant axon preparations. The helical nature of the lesion in AD is related to pathological alterations of basic properties of the nervous system due to the helical symmetry that exists at all hierarchic structural levels in the normal brain. Because of this helical symmetry of NF protein assemblies and PHF, the employment of structure reconstruction techniques to determine the conformation, particularly the handedness of these structures, is most promising. Figs. 1-3 are frontal lobe biopsies.

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