Research Strategies Developed for the Treatment of Alzheimer’s Disease. Reversible and Pseudo-Irreversible Inhibitors of Acetylcholinesterase: Structure-Activity Relationships and Drug Design

Palafox, M. Alcolea; Posada-Moreno, Paloma; Ortuño-Soriano, Ismael; Pacheco-del-Cerro, José L.; Martínez-Rincón, Carmen; Rodríguez-Martínez, Dolores; Pacheco-Cuevas, Lara

doi:10.1016/b978-0-12-803959-5.50008-8

Cited by 9 publications

(10 citation statements)

References 140 publications

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“…The currently available U. S. Food and Drug Administration approved drugs in the market for AD include cholinesterase inhibitors (rivastigmine, galantamine, and donepezil) and N-methyl-D-aspartate receptor antagonist (memantine) [21]. Tacrine has been the first approved drug (1993) as a reversible inhibitor of AChE later on abandoned in 2013 due to its hepatotoxicity, short half-life, and cholinergic side effects [22]. Huperzin A obtained from Huperzia serrata (Thunb.)…”

Section: Introductionmentioning

confidence: 99%

Essential Oils as Treatment Strategy for Alzheimerʼs Disease: Current and Future Perspectives

Benny

Thomas

2018

Planta Med

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Alzheimerʼs disease is a multifarious neurodegenerative disease that causes cognitive impairment and gradual memory loss. Several hypotheses have been put forward to postulate its pathophysiology. Currently, few drugs are available for the management of Alzheimerʼs disease and the treatment provides only symptomatic relief. Our aim is to review the relevant in vitro, in vivo, and clinical studies focused toward the potential uses of essential oils in the treatment of Alzheimerʼs disease. Scientific databases such as PubMed, ScienceDirect, Scopus, and Google Scholar from April 1998 to June 2018 were explored to collect data. We have conducted wide search on various essential oils used in different models of Alzheimerʼs disease. Out of 55 essential oils identified for Alzheimerʼs intervention, 28 have been included in the present review. A short description of in vivo studies of 13 essential oils together with clinical trial data of Salvia officinalis, Salvia lavandulifolia, Melissa officinalis, Lavandula angustifolia, and Rosmarinus officinalis have been highlighted. In vitro studies of remaining essential oils that possess antioxidant and anticholinesterase potential are also mentioned. Our literary survey revealed encouraging results regarding the various essential oils being studied in preclinical and clinical studies of Alzheimerʼs disease with significant effects in modulating the pathology through anti-amyloid, antioxidants, anticholinesterase, and memory-enhancement activity.

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Section: Introductionmentioning

confidence: 99%

Essential Oils as Treatment Strategy for Alzheimerʼs Disease: Current and Future Perspectives

Benny

Thomas

2018

Planta Med

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“…Currently, three cholinesterase inhibitors (rivistagmine, donepezil and galantamine) are being used for AD treatment. Rivastigmine selectively inhibits both cortical AChE in the central nervous system and butyrylcholinesterase (BuChE), which is documented as the predominant cholinesterase in many key regions affected in AD, including the hippocampus, thalamic nuclei and the amygdala [51]. Donepezil is a reversible and highly selective inhibitor of AChE which has also been found to be effective in treating cognitive impairment in patients with mild to moderate AD [52].…”

Section: Cholinesterase Inhibitorsmentioning

confidence: 99%

Impact of New Drugs for Therapeutic Intervention in Alzheimer’s Disease

Olloquequi¹,

Ettcheto²,

Cano³

et al. 2022

Front. Biosci. (Landmark Ed)

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The increases in population ageing and growth are leading to a boosting in the number of people living with dementia, Alzheimer's disease (AD) being the most common cause. In spite of decades of intensive research, no cure for AD has been found yet. However, some treatments that may change disease progression and help control symptoms have been proposed. Beyond the classical hypotheses of AD etiopathogenesis, i.e., amyloid beta peptide (Aβ) accumulation and tau hyperphosphorylation, a trend in attributing a key role to other molecular mechanisms is prompting the study of different therapeutic targets. Hence, drugs designed to modulate inflammation, insulin resistance, synapses, neurogenesis, cardiovascular factors and dysbiosis are shaping a new horizon in AD treatment. Within this frame, an increase in the number of candidate drugs for disease modification treatments is expected, as well as a focus on potential combinatory multidrug strategies.The present review summarizes the latest advances in drugs targeting Aβ and tau as major contributors to AD pathophysiology. In addition, it introduces the most important drugs in clinical studies targeting alternative mechanisms thought to be involved in AD's neurodegenerative process.

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Section: Introductionmentioning

confidence: 99%

“…A non-communicable disease, Alzheimer's, is the most prevailing progressive and irreversible neurological brain disorder among the elderly community; it causes short-term memory loss leading to difficulties associated with the daily routine of patients [16,17] . Although the precise cause of Alzheimer's is uncertain, cholinergic hypothesis-based Alzheimer's management is focused on the inhibition of one of the overactivated key enzymes in neurotransmission, AChE [17,18] . The oxidative stress hypothesisbased management of Alzheimer's disease is emphasized on the inhibition of generation and existence of oxidative stress products which cause neurofibrillary tangles and consequently, brain neuronal cell destruction and memory loss [19,20] .…”

Section: Introductionmentioning

confidence: 99%

Phytochemical Analysis, Antioxidant and Acetylcholinesterase Inhibitory Activities of Fruit Pulps of Selected Banana Varieties

2022

JJC

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This study focused on qualitative and quantitative analysis of phytochemicals and the study of antioxidant and acetylcholinesterase (AChE) inhibitory activities of fruit pulps of three abundant banana varieties grown in Sri Lanka. Aqueous, ethanol, ethyl acetate and hexane extracts of nearly three-month-old fruit pulps of Musa accuminata AAA, Musa accuminata AAB and Musa balbisiana ABB were prepared by shaking fresh, chopped banana pulps in the above-mentioned solvents separately. The standard spectrophotometric methods were used to quantify the alkaloids, flavonoids, condensed tannins and phenolic compounds contents of four solvent extracts of each banana variety. Among them, the ethanol extract of M. accuminata AAB possessed the highest total alkaloid content, while the ethanol extract of M. balbisiana ABB exhibited the highest total flavonoid content, total condensed tannin content and total phenolic content. The antioxidant and AChE inhibitory activities of each banana variety were determined using standard 2,2-diphenyl-1-picrylhydrazyl (DPPH) and Ellman’s colorimetric assays, respectively. The ethanol extracts of M. accuminata AAB and M. balbisiana ABB demonstrated the highest antioxidant activity and AChE inhibitory activity, respectively. This reporting study revealed that M. balbisiana ABB and M. accuminata AAB could be recommended as promising sources of edible natural antioxidants and AChE inhibitors, respectively.

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Research Strategies Developed for the Treatment of Alzheimer’s Disease. Reversible and Pseudo-Irreversible Inhibitors of Acetylcholinesterase: Structure-Activity Relationships and Drug Design

Cited by 9 publications

References 140 publications

Essential Oils as Treatment Strategy for Alzheimerʼs Disease: Current and Future Perspectives

Essential Oils as Treatment Strategy for Alzheimerʼs Disease: Current and Future Perspectives

Impact of New Drugs for Therapeutic Intervention in Alzheimer’s Disease

Phytochemical Analysis, Antioxidant and Acetylcholinesterase Inhibitory Activities of Fruit Pulps of Selected Banana Varieties

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