scholarly journals Advances on plant extracts and phytocompounds with acetylcholinesterase inhibition activity for possible treatment of Alzheimer's disease

2021 ◽  
pp. 100184
Author(s):  
Rashid Taqui ◽  
Mithila Debnath ◽  
Safin Ahmed ◽  
Associate professor Ajit Ghosh
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Plant Extracts ◽  
Acetylcholinesterase Inhibition ◽  
Inhibition Activity

Main Plant Extracts’ Active Properties Effective on Scopolamine-Induced Memory Loss

2017 ◽  
Vol 32 (7) ◽  
pp. 418-428 ◽  
Author(s):  
Ioana-Miruna Balmus ◽  
Alin Ciobica
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Plant Extracts ◽  
Current Knowledge ◽  
Symptomatic Relief ◽  
Memory Loss ◽  
Current Treatment ◽  
General Effect ◽  
Function Loss ◽  
Theory Research

Alzheimer’s disease leads to progressive cognitive function loss, which may impair both intellectual capacities and psychosocial aspects. Although the current knowledge points to a multifactorial character of Alzheimer’s disease, the most issued pathological hypothesis remains the cholinergic theory. The main animal model used in cholinergic theory research is the scopolamine-induced memory loss model. Although, in some cases, a temporary symptomatic relief can be obtained through targeting the cholinergic or glutamatergic neurotransmitter systems, no current treatment is able to stop or slow cognitive impairment. Many potentially successful therapies are often blocked by the blood–brain barrier since it exhibits permeability only for several classes of active molecules. However, the plant extracts’ active molecules are extremely diverse and heterogeneous regarding the biochemical structure. In this way, many active compounds constituting the recently tested plant extracts may exhibit the same general effect on acetylcholine pathway, but on different molecular ground, which can be successfully used in Alzheimer’s disease adjuvant therapy.

scholarly journals Medicinal Plants from Northeastern Brazil against Alzheimer’s Disease

2017 ◽  
Vol 2017 ◽  
pp. 1-7 ◽  
Author(s):  
Alexandre Batista Penido ◽  
Selene Maia De Morais ◽  
Alan Bezerra Ribeiro ◽  
Daniela Ribeiro Alves ◽  
Ana Livya Moreira Rodrigues ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Antioxidant Activity ◽  
Phenolic Compounds ◽  
Antioxidant Activities ◽  
Mangifera Indica ◽  
Psidium Guajava ◽  
Northeastern Brazil ◽  
Acetylcholinesterase Inhibition ◽  
Copaifera Langsdorffii

Alzheimer’s disease (AD) has been linked with oxidative stress, acetylcholine deficiency in the brain, and inflammatory processes. In the northeast region of Brazil, various plants are used to treat several diseases associated with these processes; then an antioxidant test was performed with those plants in a previous work and twelve species with higher antioxidant activity were selected for AChE inhibition evaluation. The phenolic compounds content was determined by Folin–Ciocalteu test and flavonoid content with AlCl3reagent using UV-visible spectrophotometry. The antioxidant activity was assessed analyzing the inhibitory activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-azinobis-3-ethylbenzothiazoline-6-sulfonate (ABTS) and by theβ-carotene/linoleic acid system and acetylcholinesterase inhibition using qualitative and quantitative tests. The combination of better acetylcholinesterase inhibitory and antioxidant activities pointed out six species, in descending order, as the best potential sources of therapeutic agents against AD:Hancornia speciosa > Myracrodruon urundeuva > Copaifera langsdorffii > Stryphnodendron coriaceum > Psidium guajava > Mangifera indica. Besides, the phenolic compounds in the species probably contribute to these activities. However, further pharmacological studies to assess the specific applications of these plants against AD are required to confirm these results.

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 Pharmacokinetic and Pharmacodynamic Evaluation of Nasal Liposome and Nanoparticle Based Rivastigmine Formulations in Acute and Chronic Models of Alzheimer’s Disease

2021 ◽  
Author(s):  
Sampath Kumar L Rompicherla ◽  
Karthik Arumugam ◽  
Sree Lalitha Bojja ◽  
Nitesh Kumar ◽  
Mallikarjuna Rao Chamallamudi
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Memory Loss ◽  
Rapid Onset ◽  
Liposomal Formulation ◽  
Direct Access ◽  
Acetylcholinesterase Inhibition ◽  
Pharmacokinetic Parameters ◽  
Ageing Population ◽  
Onset Of Action

Abstract With the increasing ageing population and progressive nature of the disease, Alzheimer's disease (AD) poses to be an oncoming epidemic with limited therapeutic strategies. It is characterized by memory loss, behavioral instability, impaired cognitive function, predominantly, cognitive inability manifested due to the accumulation of β-amyloid, with malfunctioned cholinergic system. Rivastigmine, a reversible dual cholinesterase inhibitor is more tolerable and widely used choice of drug for AD. However, rivastigmine being hydrophilic and undergoing first pass metabolism, exhibits low CNS bioavailability. Nanoformulations including liposomes and PLGA nanoparticles can encapsulate hydrophilic drugs and deliver efficiently to brain. Besides, the nasal route is receiving considerable attention recently, due to its direct access to brain. Therefore, the present study attempts to evaluate the pharmacokinetic and pharmacodynamic properties of nasal liposomal and PLGA nanoparticle formulations of rivastigmine in scopolamine induced amnesia model and validate the best formulation by employing pharmacokinetic and pharmacodynamic (PK-PD) modelling. Nasal liposomal rivastigmine formulation showed the best pharmacokinetic features with rapid onset of action (Tmax=5 minutes), higher Cmax (1489.5 ± 620.71), enhanced systemic bioavailability (F=118.65 ± 23.54; AUC= 35921.75 ± 9559.46), increased half-life (30.92 ± 8.38 minutes), and reduced clearance rate (Kel (1/min) = 0.0224 ± 0.006) compared to oral rivastigmine (Tmax= 15 minutes; Cmax= 56.29 ± 27.05; F=4.39 ± 1.82; AUC=1663.79 ± 813.54; t1/2= 13.48 ± 5.79; Kel (1/min) =0.0514 ± 0.023). Further, the liposomal formulation significantly rescued the memory deficit induced by scopolamine superior to other formulations as assessed in Morris water maze and passive avoidance tasks. PK-PD modelling demonstrated strong correlation between the pharmacokinetic parameters and acetylcholinesterase inhibition of liposomal formulation.

Sign in / Sign up

Export Citation Format

Share Document