scholarly journals Acetylcholinesterase inhibition by medicinal plants: A Review

2017 ◽  
Vol 6 (06) ◽  
pp. 1640 ◽  
Author(s):  
Navi Ranjan* ◽  
Manorma Kumari
Keyword(s):  
Side Effects ◽  
Senile Dementia ◽  
Synaptic Cleft ◽  
Inhibitory Effect ◽  
Acetylcholinesterase Inhibition ◽  
Ache Inhibitors ◽  
Cholinergic Synapses ◽  
Ache Inhibitory Activity ◽  
Myastenia Gravis ◽  
The Brain

Acetylcholinesterase (AChE), the predominant cholinesterase in the brain, hydrolyzes ACh to choline and acetate, thereby terminating the effect of this neurotransmitter at cholinergic synapses. Therefore, AChE is the target of cholinesterase inhibitors used for addressing the cholinergic deficit in Alzheimer’s disease (AD) patients. Despite decades of research and advances in our understanding of its aetiology and pathogenesis, current pharmacotherapeutic options for AD are still very limited and represent an area of need that is currently unmet. The leading AD therapeutics involves AChE inhibitors, resulting in increased acetylcholine concentrations in the synaptic cleft and enhanced cholinergic transmission. Compounds showing an AChE inhibitory effect are also used for the treatment of senile dementia, myastenia gravis, Parkinson’s disease and ataxia. Taking into account that the inhibition of AChE has been one of the most used strategies for treating AD and that existing drugs are effective only against mild to moderate type of disease while presenting considerable side effects, the search for new sources of effective and selective anti acetylcholinesterase agents with fewer side effects is imperative. Various plants and phytochemical substances have demonstrated AChE inhibitory activity and thus could be beneficial in the treatment of neurodegenerative disorders such as AD.

New Galantamine Derivatives with Inhibitory Effect on Acetylcholinesterase Activity

2021 ◽  
Vol 83 (3) ◽  
pp. 1211-1220 ◽  
Author(s):  
Maria I. Lazarova ◽  
Daniela S. Tsekova ◽  
Lyubka P. Tancheva ◽  
Kiril T. Kirilov ◽  
Diamara N. Uzunova ◽  
...  
Keyword(s):  
Lipid Peroxidation ◽  
Memory Performance ◽  
Acetylcholinesterase Activity ◽  
Inhibitory Effect ◽  
Long Term Memory ◽  
Molegro Virtual Docker ◽  
Ache Inhibitors ◽  
Hybrid Molecules ◽  
Ache Inhibitory Activity ◽  
Biological Assessments

Background: Inhibitors of acetylcholinesterase (AChE) are used to treat many disorders, among which are neurodegenerative upsets, like Alzheimer’s disease (AD). One of the limited licensed AChE inhibitors (AChEIs) used as drugs is the natural compound galantamine (Gal). Objective: As Gal is a toxic compound, here we expose data about its four derivatives in hybrid peptide-norgalantamine molecules, which have shown 100 times lower toxicity. Methods: Four newly synthesized galantamine derivatives have been involved in docking analysis made by Molegro Virtual Docker. Biological assessments were performed on ICR male mice. The change in short and long-term memory performance was evaluated by passive avoidance test. AChE activity and levels of main oxidative stress parameters: lipid peroxidation, total glutathione (GSH), enzyme activities of catalase (CAT), superoxide dismutase, and glutathione peroxidase were measured in brain homogenates. Results: Our experimental data revealed that the new hybrid molecules did not impair memory performance in healthy mice. Two of the compounds demonstrated better than Gal AChE inhibitory activity in the brain. None of them changed the level of lipid peroxidation products, one of the compounds increased GSH levels, and all of them increased CAT enzyme activity. Conclusion: The new galantamine-peptide hybrids demonstrated a potential for inhibition of AChE and antioxidant activity and deserve further attention.

Protective influence of coded amino acids on the development of liver tissue culture in the presence of cytostatic

2020 ◽  
pp. 48-53
Author(s):  
N. I. Chalisova ◽  
V. K. Kozlov ◽  
A. B. Mulik ◽  
E. P. Zatsepin ◽  
T. A. Kostrova
Keyword(s):  
Amino Acids ◽  
Tissue Culture ◽  
Side Effects ◽  
Liver Tissue ◽  
Organotypic Culture ◽  
Growth Zone ◽  
Inhibitory Effect ◽  
Cytostatic Drugs ◽  
Urgent Problem ◽  
Combined Exposure

An urgent problem is the search for substances that can provide a protective effect in cases of DNA synthesis and repair disorders that arise as a result of side effects of cytostatic drugs used in the treatment of cancer. The aim of this work was to study the effect of 20 encoded amino acids in the presence of Cyclophosphane on the development of organotypic culture of rat liver tissue. The results obtained indicate that Cyclophosphane; which simulates the action of such cytostatic substances; inhibits cell proliferation in the liver tissue. It was also found that the encoded amino acids: asparagine; arginine; and glutamic acid; eliminate the inhibitory effect of Cyclophosphane in liver tissue culture. The growth zone of explants after combined exposure to Cyclophosphane (whose isolated action suppressed the growth zone) and these amino acids increased significantly and reached control values. Thus; the experimental data create the basis for the development of methods for the therapeutic use of the three studied amino acids for the removal of side effects in the treatment with cytostatic drugs.

Liposomes: Novel Drug Delivery Approach for Targeting Parkinson’s Disease

2020 ◽  
Vol 26 (37) ◽  
pp. 4721-4737 ◽  
Author(s):  
Bhumika Kumar ◽  
Mukesh Pandey ◽  
Faheem H. Pottoo ◽  
Faizana Fayaz ◽  
Anjali Sharma ◽  
...  
Keyword(s):  
Parkinson’S Disease ◽  
Drug Delivery ◽  
Parkinson's Disease ◽  
Side Effects ◽  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Brain Targeting ◽  
Neural Cells ◽  
Blood Brain ◽  
The Brain

Parkinson’s disease is one of the most severe progressive neurodegenerative disorders, having a mortifying effect on the health of millions of people around the globe. The neural cells producing dopamine in the substantia nigra of the brain die out. This leads to symptoms like hypokinesia, rigidity, bradykinesia, and rest tremor. Parkinsonism cannot be cured, but the symptoms can be reduced with the intervention of medicinal drugs, surgical treatments, and physical therapies. Delivering drugs to the brain for treating Parkinson’s disease is very challenging. The blood-brain barrier acts as a highly selective semi-permeable barrier, which refrains the drug from reaching the brain. Conventional drug delivery systems used for Parkinson’s disease do not readily cross the blood barrier and further lead to several side-effects. Recent advancements in drug delivery technologies have facilitated drug delivery to the brain without flooding the bloodstream and by directly targeting the neurons. In the era of Nanotherapeutics, liposomes are an efficient drug delivery option for brain targeting. Liposomes facilitate the passage of drugs across the blood-brain barrier, enhances the efficacy of the drugs, and minimize the side effects related to it. The review aims at providing a broad updated view of the liposomes, which can be used for targeting Parkinson’s disease.

scholarly journals Importance of Nanoparticles for the Delivery of Antiparkinsonian Drugs

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 508
Author(s):  
Sara Silva ◽  
António J. Almeida ◽  
Nuno Vale
Keyword(s):  
Side Effects ◽  
Dopaminergic Neurons ◽  
Lewy Bodies ◽  
Pharmacokinetic Profile ◽  
The Elderly ◽  
Motor Symptoms ◽  
Administration Routes ◽  
Pharmaceutical Therapy ◽  
Drug Pharmacokinetic ◽  
The Brain

Parkinson’s disease (PD) affects around ten million people worldwide and is considered the second most prevalent neurodegenerative disease after Alzheimer’s disease. In addition, there is a higher risk incidence in the elderly population. The main PD hallmarks include the loss of dopaminergic neurons and the development of Lewy bodies. Unfortunately, motor symptoms only start to appear when around 50–70% of dopaminergic neurons have already been lost. This particularly poses a huge challenge for early diagnosis and therapeutic effectiveness. Actually, pharmaceutical therapy is able to relief motor symptoms, but as the disease progresses motor complications and severe side-effects start to appear. In this review, we explore the research conducted so far in order to repurpose drugs for PD with the use of nanodelivery systems, alternative administration routes, and nanotheranostics. Overall, studies have demonstrated great potential for these nanosystems to target the brain, improve drug pharmacokinetic profile, and decrease side-effects.

Choroidal metastases: case report and review

2020 ◽  
pp. 1-7
Author(s):  
Victor Duque ◽  
Carolina de la Pinta ◽  
Ciriaco Corral ◽  
Carmen Vallejo ◽  
Margarita Martin ◽  
...  
Keyword(s):  
Visual Acuity ◽  
Side Effects ◽  
External Beam Radiotherapy ◽  
Choroidal Metastasis ◽  
Good Visual Acuity ◽  
Good Local Control ◽  
Radiological Response ◽  
The Right ◽  
The Brain

Abstract Introduction: Choroidal metastases are the most frequent intraocular secondary tumours, with a prevalence of 2–7% according to the literature. Our aim was to review a clinical case of choroidal metastasis. We present a case of a 63-year-old male patient diagnosed in 2018 with lung adenocarcinoma cT4N0M1. The patient had three metastases in the brain, which were successfully treated with radiosurgery (RS). The patient was treated with chemotherapy with pemetrexed–cisplatin schedule. Five months after diagnosis, the patient presented with decreased vision in the right eye. After ophthalmologic evaluation, he was diagnosed with a right choroidal metastasis, which was treated with external beam radiotherapy with 20 Gy in five fractions, resulting in improved visual acuity and a complete clinical and radiological response. The patient took part in a clinical trial that continued with systemic chemotherapy. Twenty-two months after radiotherapy to the eye, the patient has good visual acuity without any side effects. Conclusions: Choroidal metastasis treated with radiotherapy achieves good local control, with limited side effects, allowing an improvement in visual acuity and consequently, an improvement in the patient´s quality of life.

In vivo exploration of brain phosphorus 31 metabolism in patients with senile dementia of Alzheimer type

1994 ◽  
Vol 9 (2) ◽  
pp. 105-109
Author(s):  
G Mecheri ◽  
Y Bissuel ◽  
J Dalery ◽  
JL Terra ◽  
G Balvay ◽  
...  
Keyword(s):  
Statistical Analysis ◽  
Senile Dementia ◽  
Phospholipid Metabolism ◽  
Alzheimer Type ◽  
Dementia Of Alzheimer Type ◽  
Non Invasive ◽  
Significant Difference ◽  
The Brain

SummaryIn vivo NMR 31p spectroscopy is a non invasive, non ionizing method of exploration of energy and phospholipid metabolism in the brain. This study consisted of comparing 31p spectra in five patients with Senile Dementia of Alzheimer Type (SDAT) with those of four controls of similar ages. Abnormal phosphonionocsters (PME) concentrations, either high or low, were found in the patients, but statistical analysis did not elicit any significant difference relative to controls.

Fluoxetine Efficacy vs Comparative Drugs: An Overview

1988 ◽  
Vol 153 (S3) ◽  
pp. 51-58 ◽  
Author(s):  
Malcolm Lader
Keyword(s):  
Side Effects ◽  
Tricyclic Antidepressants ◽  
Antipsychotic Agents ◽  
Synaptic Cleft ◽  
Endogenous Depression ◽  
Acute Effects ◽  
Anticholinergic Effects ◽  
The Past ◽  
Chronic Effects ◽  
Clinical Action

The tricyclic antidepressants (TCAs) were discovered accidentally by pharmaceutical chemists seeking first, better antihistamines and then antipsychotic agents. Careful clinical assessment revealed the antidepressant properties and suggested that the closer the patient resembled the classical textbook description of ‘endogenous’ depression, the more likely was an adequate clinical response to occur (Kuhn, 1958). However, it was quickly realised that the TCAs possess a plethora of side-effects, particularly sedation and symptoms related to their anticholinergic effects.Despite much research over the past 25 years, it is unclear how TCAs effect clinical improvement. The two main neurotransmitters involved in some way are noradrenaline (Schildkraut, 1965) and 5-hydroxytryptamine (5-HT; serotonin; Van Praag, 1977). It was proposed that TCAs acted by blocking the reuptake of one or other or both of these neurotransmitters, thereby increasing their concentration in the synaptic cleft. However, as well as these acute effects, chronic effects, such as a decrease in the number of central beta-adrenoceptors (‘down-regulation’) occur, and these are probably more relevant to the clinical action.

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