Medicinal Plants with Acetylcholinesterase Inhibitory Activity: Therapeutic Potential of Brazilian Plants for the Treatment of Alzheimer's Disease

2021 ◽  
Vol 13 (26) ◽  
pp. 45-49
Author(s):  
Fernanda Granja da Silva Oliveira ◽  
Bruno de Oliveira Veras ◽  
Juliane Maria Dos Santos Silva ◽  
Deyzi Caroline da Silva Barbosa ◽  
Tayane de Cássia Dias Mendes Silva ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Medicinal Plants ◽  
Inhibitory Activity ◽  
Therapeutic Potential ◽  
Acetylcholinesterase Inhibitory Activity

SEMI-SYNTHESIS AND EVALUATION OF HESPERETIN DERIVATIVES AS ACETYLCHOLINESTERASE INHIBITORS7

2018 ◽  
Vol 8 (4) ◽  
pp. 7-12
Author(s):  
Huan Tran The ◽  
Dao Tran Thanh
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Key Words ◽  
Inhibitory Activity ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Ic50 Value ◽  
Ellman’S Method ◽  
Further Development ◽  
Derivatives Of

Background: Inhibition of acetylcholinesterase are regarded as one of promising approach to treat Alzheimer’s disease. Hesperetin is a potential flavonoid for further development in this direction. Objectives: Semi-synthesized and assayed for hesperetin derivatives’s acetylcholinesterase inhibitory activity in vitro. Materials and methods: Ester and ether derivatives of hesperetin were semi-synthesized. The semi-synthesis compounds were tested for acetylcholinesterase inhibitory activity in vitro according to the Ellman’s method. Results: Hesperetin is obtained by hydrolysing hesperidin. Then, two ester and two ether derivatives were semi-synthesized from hesperetin. The results showed that some of the semi-synthesis hesperetin derivatives displayed stronger acetylcholinesterase inhibitory activity than hesperetin. Among them, derivative 1 has the best activity with an IC50 value of 43.50 μM. Conclusions: Four hesperetin derivatives were semi-synthesized and investigated their acetylcholinesterase inhibitory activity, some of which showed improvement in activity. Key words: Hesperetin, semi-synthesis, inhibit, enzyme, acetylcholinesterase

Potential Ayurvedic Herbs for Neurodegenerative Diseases: A review

2021 ◽  
pp. 69-74
Author(s):  
Dipsundar Sahu ◽  
Shakti Bhushan ◽  
Debajyoti Das ◽  
Saroj Kumar Debnath ◽  
Laxmidhar Barik ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Medicinal Plants ◽  
Cognitive Abilities ◽  
Therapeutic Potential ◽  
Conventional Medicine ◽  
Acetylcholinesterase Activity ◽  
Medical Studies ◽  
Hyperactivity Disorder ◽  
Biochemical Effects

In herbal medicine, there is a substantial amount of variety of plants have been used to treat neurodegenerative disorders including Alzheimer's (AD)as well as other memory-related issues. Dementia is a neurological condition characterised by a progressive loss in emotional and cognitive abilities. Dementia is linked to a number of conditions like inadequate cerebral blood flow, poison toxicity, and other risk factors and conditions mitochondrial dysfunction, oxidative injury, and, in certain cases coexistence with other diseases like Alzheimer's disease (AD), Huntington's disease, Parkinson's syndrome (PD) and Attention Deficit Hyperactivity Disorder (ADHD).Despite the fact that there are well-established semi-synthetic medications for the treatment of AD and AD-related dementia, the majority of them have a number of side effects. As a result, conventional medicine offers a variety of plant-derived lead molecules that may be valuable in future medical studies. In this paper, we look at how ayurvedic plants are used to treat neurodegenerative disease around the world. Plants are also neuroprotective against proinflammatory cytokines including IL-6, IL-1b, TNF-a and it was reported that Antioxidant activity was increased, oxidant levels were reduced, and acetylcholinesterase activity was inhibited in the nervous system by these medicinal plants. We've highlighted the most essential ayurvedic medicinal plants as well as their biochemical effects. As a result, the effects of the above medicinals plants and their active constituents strengthened neurodegenerative conditions, indicating their therapeutic potential in ailments like Alzheimer's disease. and depression that are linked to neuroinflammation and neurotransmitter dysfunction.

Medicinal plants with acetylcholinesterase inhibitory activity

2018 ◽  
Vol 29 (5) ◽  
pp. 491-529 ◽  
Author(s):  
Sita Sharan Patel ◽  
Ramsaneh Raghuwanshi ◽  
Misha Masood ◽  
Ashish Acharya ◽  
Surendra Kumar Jain
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Medicinal Plants ◽  
Neurological Disorders ◽  
Ache Activity ◽  
Therapeutic Potential ◽  
Brain Regions ◽  
Special Focus ◽  
Distinct Region ◽  
Traditional System

AbstractAlzheimer’s disease, a progressive neurodegenerative disease, is characterised by hypofunction of acetylcholine (ACh) neurotransmitter in the distinct region of brain. Acetylcholinesterase (AChE) is an enzyme that metabolises the ACh at synaptic cleft resulting in Alzheimer’s disease. Medicinal plants have been used to treat numerous ailments and improve human health from ancient time. A traditional system of medicine is long recognised for its effective management of neurological disorders. The present review confers the scope of some common medicinal plants with a special focus on AChE-mediated central nervous system complications especially Alzheimer’s disease. Literature suggests that medicinal plants reduce neuronal dysfunctions by reducing AChE activity in different brain regions. In some instances, activation of AChE activity by medicinal plants also showed therapeutic potential. In conclusion, medicinal plants have a wide scope and possess therapeutic potential to efficiently manage neurological disorders associated with AChE dysregulation.

Neuroprotective Effects of Ellagic Acid in Alzheimer's Disease: Focus on Underlying Molecular Mechanisms of Therapeutic Potential

2020 ◽  
Vol 26 ◽  
Author(s):  
Nimra Javaid ◽  
Muhammad Ajmal Shah ◽  
Azhar Rasul ◽  
Zunera Chauhdary ◽  
Uzma Saleem ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Ellagic Acid ◽  
Molecular Mechanisms ◽  
Neurodegenerative Disorder ◽  
Therapeutic Potential ◽  
Neuronal Cell Death ◽  
Neuronal Cell ◽  
Acetylcholinesterase Activity ◽  
Neuroprotective Effects

: Neurodegeneration is a multifactorial process involved the different cytotoxic pathways that lead towards neuronal cell death. Alzheimer’s disease (AD) is a persistent neurodegenerative disorder that normally has a steady onset yet later on it worsens. The documented evidence of AD neuropathology manifested the neuro-inflammation, increased reactive oxygen, nitrogen species and decreased antioxidant protective process; mitochondrial dysfunction as well as increased level of acetylcholinesterase activity. Moreover, enhanced action of proteins leads towards neural apoptosis which have a vital role in the degeneration of neurons. The inability of commercial therapeutic options to treat AD with targeting single mechanism leads the attraction towards organic drugs. Ellagic acid is a dimer of gallic acid, latest studies expressed that ellagic acid can initiate the numerous cell signaling transmission and decrease the progression of disorders, involved in the degeneration of neurons. The influential property of ellagic acid to protect the neurons in neurodegenerative disorders is due to its antioxidant effect, iron chelating and mitochondrial protective effect. The main goal of this review is to critically analyze the molecular mode of action of ellagic acid against neurodegeneration.

The Therapeutic Potential of Purinergic Receptors in Alzheimer’s Disease and Promising Therapeutic Modulators

2020 ◽  
Vol 20 ◽  
Author(s):  
Lili Pan ◽  
Yu Ma ◽  
Yunchun Li ◽  
Haoxing Wu ◽  
Rui Huang ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Purinergic Receptors ◽  
Therapeutic Potential ◽  
Purinergic Signaling ◽  
Memory Loss ◽  
Related Research ◽  
Central Nervous System Disorders ◽  
G Protein Coupled

Abstract:: Recent studies have proven that the purinergic signaling pathway plays a key role in neurotransmission and neuromodulation, and is involved in various neurodegenerative diseases and psychiatric disorders. With the characterization of the subtypes of receptors in purinergic signaling, i.e. the P1 (adenosine), P2X (ion channel) and P2Y (G protein-coupled), more attentions were paid to the pathophysiology and therapeutic potential of purinergic signaling in central nervous system disorders. Alzheimer’s disease (AD) is a progressive and deadly neurodegenerative disease that is characterized by memory loss, cognitive impairment and dementia. However, as drug development aimed to prevent or control AD follows a series of failures in recent years, more researchers focused on the neuroprotection-related mechanisms such as purinergic signaling in AD patients to find a potential cure. This article reviews the recent discoveries of purinergic signaling in AD, summaries the potential agents as modulators for the receptors of purinergic signaling in AD related research and treatments. Thus, our paper provided an insight for purinergic signaling in the development of anti-AD therapies.

Dehydroepiandrosterone (DHEA) and its Sulphate (DHEAS) in Alzheimer’s Disease

2020 ◽  
Vol 17 (2) ◽  
pp. 141-157 ◽  
Author(s):  
Dubravka S. Strac ◽  
Marcela Konjevod ◽  
Matea N. Perkovic ◽  
Lucija Tudor ◽  
Gordana N. Erjavec ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Large Scale ◽  
Therapeutic Potential ◽  
Relevant Literature ◽  
Comprehensive Overview ◽  
Brain Functions ◽  
Specific Effects ◽  
And Behavior

Background: Neurosteroids Dehydroepiandrosterone (DHEA) and Dehydroepiandrosterone Sulphate (DHEAS) are involved in many important brain functions, including neuronal plasticity and survival, cognition and behavior, demonstrating preventive and therapeutic potential in different neuropsychiatric and neurodegenerative disorders, including Alzheimer’s disease. Objective: The aim of the article was to provide a comprehensive overview of the literature on the involvement of DHEA and DHEAS in Alzheimer’s disease. Method: PubMed and MEDLINE databases were searched for relevant literature. The articles were selected considering their titles and abstracts. In the selected full texts, lists of references were searched manually for additional articles. Results: We performed a systematic review of the studies investigating the role of DHEA and DHEAS in various in vitro and animal models, as well as in patients with Alzheimer’s disease, and provided a comprehensive discussion on their potential preventive and therapeutic applications. Conclusion: Despite mixed results, the findings of various preclinical studies are generally supportive of the involvement of DHEA and DHEAS in the pathophysiology of Alzheimer’s disease, showing some promise for potential benefits of these neurosteroids in the prevention and treatment. However, so far small clinical trials brought little evidence to support their therapy in AD. Therefore, large-scale human studies are needed to elucidate the specific effects of DHEA and DHEAS and their mechanisms of action, prior to their applications in clinical practice.

scholarly journals A novel orally active HDAC6 inhibitor T-518 shows a therapeutic potential for Alzheimer’s disease and tauopathy in mice

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Tomohiro Onishi ◽  
Ryouta Maeda ◽  
Michiko Terada ◽  
Sho Sato ◽  
Takahiro Fujii ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Therapeutic Potential ◽  
Drug Candidate ◽  
Histone Deacetylase 6 ◽  
Cellular Assays ◽  
Age Related ◽  
Acetylation State ◽  
Hdac6 Inhibitor ◽  
Orally Active

AbstractAccumulation of tau protein is a key pathology of age-related neurodegenerative diseases such as Alzheimer's disease and progressive supranuclear palsy. Those diseases are collectively termed tauopathies. Tau pathology is associated with axonal degeneration because tau binds to microtubules (MTs), a component of axon and regulates their stability. The acetylation state of MTs contributes to stability and histone deacetylase 6 (HDAC6) is a major regulator of MT acetylation status, suggesting that pharmacological HDAC6 inhibition could improve axonal function and may slow the progression of tauopathy. Here we characterize N-[(1R,2R)-2-{3-[5-(difluoromethyl)-1,3,4-oxadiazol-2-yl]-5-oxo-5H,6H,7H-pyrrolo[3,4-b]pyridin-6-yl}cyclohexyl]-2,2,3,3,3-pentafluoropropanamide (T-518), a novel, potent, highly selective HDAC6 inhibitor with clinically favorable pharmacodynamics. T-518 shows potent inhibitory activity against HDAC6 and superior selectivity over other HDACs compared with the known HDAC6 inhibitors in the enzyme and cellular assays. T-518 showed brain penetration in an oral dose and blocked HDAC6-dependent tubulin deacetylation at Lys40 in mouse hippocampus. A 2-week treatment restored impaired axonal transport and novel object recognition in the P301S tau Tg mouse, tauopathy model, while a 3-month treatment also decreased RIPA-insoluble tau accumulation. Pharmaceutical inhibition of HDAC6 is a potential therapeutic strategy for tauopathy, and T-518 is a particularly promising drug candidate.

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