scholarly journals Potential Drug Candidates to Treat TRPC6 Channel Deficiencies in the Pathophysiology of Alzheimer’s Disease and Brain Ischemia

Cells ◽  
2020 ◽  
Vol 9 (11) ◽  
pp. 2351 ◽  
Author(s):  
Veronika Prikhodko ◽  
Daria Chernyuk ◽  
Yurii Sysoev ◽  
Nikita Zernov ◽  
Sergey Okovityi ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cerebral Ischemia ◽  
Brain Ischemia ◽  
In Vivo Studies ◽  
Potential Drug ◽  
Drug Candidates ◽  
Chemical Structures ◽  
Trpc6 Channel

Alzheimer’s disease and cerebral ischemia are among the many causative neurodegenerative diseases that lead to disabilities in the middle-aged and elderly population. There are no effective disease-preventing therapies for these pathologies. Recent in vitro and in vivo studies have revealed the TRPC6 channel to be a promising molecular target for the development of neuroprotective agents. TRPC6 channel is a non-selective cation plasma membrane channel that is permeable to Ca2+. Its Ca2+-dependent pharmacological effect is associated with the stabilization and protection of excitatory synapses. Downregulation as well as upregulation of TRPC6 channel functions have been observed in Alzheimer’s disease and brain ischemia models. Thus, in order to protect neurons from Alzheimer’s disease and cerebral ischemia, proper TRPC6 channels modulators have to be used. TRPC6 channels modulators are an emerging research field. New chemical structures modulating the activity of TRPC6 channels are being currently discovered. The recent publication of the cryo-EM structure of TRPC6 channels should speed up the discovery process even more. This review summarizes the currently available information about potential drug candidates that may be used as basic structures to develop selective, highly potent TRPC6 channel modulators to treat neurodegenerative disorders, such as Alzheimer’s disease and cerebral ischemia.

Electromagnetic field in Alzheimer’s disease: a literature review of recent preclinical and clinical studies

2020 ◽  
Vol 17 ◽  
Author(s):  
Reem Habib Mohamad Ali Ahmad ◽  
Marc Fakhoury ◽  
Nada Lawand
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Neurodegenerative Disorder ◽  
In Vivo Studies ◽  
Key Factors ◽  
Potential Benefits ◽  
Preclinical And Clinical Studies ◽  
The Brain

: Alzheimer’s disease (AD) is a neurodegenerative disorder characterized by the progressive loss of neurons leading to cognitive and memory decay. The main signs of AD include the irregular extracellular accumulation of amyloidbeta (Aβ) protein in the brain and the hyper-phosphorylation of tau protein inside neurons. Changes in Aβ expression or aggregation are considered key factors in the pathophysiology of sporadic and early-onset AD and correlate with the cognitive decline seen in patients with AD. Despite decades of research, current approaches in the treatment of AD are only symptomatic in nature and are not effective in slowing or reversing the course of the disease. Encouragingly, recent evidence revealed that exposure to electromagnetic fields (EMF) can delay the development of AD and improve memory. This review paper discusses findings from in vitro and in vivo studies that investigate the link between EMF and AD at the cellular and behavioural level, and highlights the potential benefits of EMF as an innovative approach for the treatment of AD.

Neuroprotective effects of bergenin in Alzheimer’s disease: Investigation through molecular docking, in vitro and in vivo studies

2019 ◽  
Vol 356 ◽  
pp. 18-40 ◽  
Author(s):  
Priyal Barai ◽  
Nisith Raval ◽  
Sanjeev Acharya ◽  
Ankit Borisa ◽  
Hardik Bhatt ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Molecular Docking ◽  
In Vivo Studies ◽  
Neuroprotective Effects

scholarly journals Olive-Oil-Derived Oleocanthal Enhances β-Amyloid Clearance as a Potential Neuroprotective Mechanism against Alzheimer’s Disease: In Vitro and in Vivo Studies

2013 ◽  
Vol 4 (6) ◽  
pp. 973-982 ◽  
Author(s):  
Alaa H. Abuznait ◽  
Hisham Qosa ◽  
Belnaser A. Busnena ◽  
Khalid A. El Sayed ◽  
Amal Kaddoumi
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Olive Oil ◽  
In Vivo Studies ◽  
Β Amyloid

An Upcoming Approach to Alzheimer's Disease: Ethnopharmacological Potential of Plant Bioactive Molecules

2020 ◽  
Vol 27 (26) ◽  
pp. 4344-4371 ◽  
Author(s):  
Natália Martins ◽  
Sandrina A. Heleno ◽  
Isabel C.F.R. Ferreira
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Present Report ◽  
Symptomatic Treatment ◽  
The Elderly ◽  
Bioactive Molecules ◽  
In Vivo Studies ◽  
Limited Effectiveness

Background:: Neurodegenerative disorders have achieved epidemic levels in the last decades; not only the elderly but also adult individuals have been increasingly affected. Among them, Alzheimer’s disease is one of the most prevalent and crippling diseases, associated with high rates of multi-morbidities and dependency. Despite the existence of a wide variety of drugs used as the symptomatic treatment, they have some side effects and toxicity, apart from their limited effectiveness. Botanical preparations have a secular use, being widely recommended for a multitude of purposes, such as for the improvement of brain health. Objective: The aim of the present report is to systematize the knowledge on plant-food derived bioactive molecules with promising in vitro enzymatic inhibitory activities. Results: Alkaloids, phenolic compounds and terpenes are the most studied phytochemicals, both derived from natural and commercial sources. In spite of their efficient activity as enzymatic inhibitors, the number of in vivo studies and even clinical trials have confirmed that their real bioactive potential remains scarce. Conclusions: Thus, it is of the utmost importance to deepen knowledge in this area, once those relevant and informative tools can significantly contribute to the promising advances in the field of Alzheimer’s disease treatment.

scholarly journals Korean Thistle (Cirsium japonicum var. maackii (Maxim.) Matsum.): A Potential Dietary Supplement against Diabetes and Alzheimer’s Disease

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 649 ◽  
Author(s):  
Aditi Wagle ◽  
Su Hui Seong ◽  
Srijan Shrestha ◽  
Hyun Ah Jung ◽  
Jae Sue Choi
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Dietary Supplement ◽  
Competitive Inhibition ◽  
Hydrophobic Interactions ◽  
Docking Studies ◽  
In Vivo Studies ◽  
Strong Hydrogen Bond ◽  
Cirsium Japonicum

In the search for natural products having a dual inhibitory action on diabetes and Alzheimer’s disease, this study investigated the activity of different parts of Korean thistle (Cirsium japonicum var. maackii (Maxim.) Matsum), and its fractional constituents by in vitro enzymatic and in silico molecular docking studies. Cirsium maackii has been used as a traditional medicine for the treatment of several diseases. The ethyl acetate and dichloromethane fractions of a leaf extract showed α-glucosidase and BACE1 inhibitory activity, respectively. Furthermore, the isolated compound, luteolin, exhibited concentration-dependent non-competitive inhibition against both α-glucosidase and BACE1 (IC50 = 51.27 ± 1.23 and 13.75 ± 0.26 μM; Ki value = 52.04 and 14.76 μM, respectively). Moreover, docking studies showed that luteolin formed a strong hydrogen bond with the peripheral binding amino acid residues, and hydrophobic interactions with the α-glucosidase and BACE1 enzymes. Therefore, Korean thistle may act as an important dietary supplement against diabetes and Alzheimer’s disease, especially the leaves, because of the preponderance of the active component, luteolin, making Korean thistle a promising candidate for more detailed in vitro and in vivo studies.

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