Abstract

As total life expectancy increases, the prevalence of age-related diseases such as Alzheimer’s is also increasing. Many hypotheses about Alzheimer’s disease have been developed, including cholinergic neuron damage. Acetylcholine is a major neurotransmitter in the brain and cholinergic deficits leads to cognitive dysfunction and decline. 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. In abnormal activation of AChE, acetylcholine will degrade rapidly, especially in the brain and this is associated with Alzheimer’s disease (AD). It has been shown that theraphy with essential oils from medicinal plants can improve cognitive performance in Alzheimer’s disease patients. Eugenol from these essential oils is reported to inhibit acetylcholinesterase, both in vitro and in vivo. This paper is set to Determine inhibitory/stimulatory effect of tested extracts on acetylcholine esterase (AChE) activity. The sampled out plant extracts include Thymus vulgaris, Berberis vulgaris and Calluna vulgaris with which inhibition or activation by different chemical catalysts is performed to establish their effects in the tested natural extracts. Experimental design is used where the reagents are determined and chemical reactions performed in the procedures as outlined in the methodology section. The results of the cholinergic/ anti-cholinergic effect of tested natural extracts are then recorded. This study reflects that most of the extracts inhibited AChE activity with berberis vulgaris showing highest inhibitory effect.

Highlights

  • Inhibition of Cholinesterases, mainly Acetylcholinesterase (AChE) and prevention of acetylcholine degradation in synapses of cholinergic system is one of the most accepted palliative therapy opportunities for Alzheimer’s disease (AD) today

  • Since the introduction of the first cholinesterase inhibitor in 1997, most clinicians would consider the cholinergic drugs, donepezil, rivastigmine and galantamine to be the first line pharmacotherapy for mild and moderate AD. These compounds have been reported to have their adverse effects including gastrointestinal disturbances and problems associated with bioavailability, high cost, and short half-life [2] which necessitates the interest in finding better acetylcholine esterase (AChE) inhibitors from natural resources

  • Considering the importance of sufficient knowledge base for accurate recommendations on the use of plant extracts, this study found the main functional component alkaloids such as which is the main active ingredient of Berberis vulgaris

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Summary

Introduction

Inhibition of Cholinesterases, mainly Acetylcholinesterase (AChE) and prevention of acetylcholine degradation in synapses of cholinergic system is one of the most accepted palliative therapy opportunities for Alzheimer’s disease (AD) today. Since the introduction of the first cholinesterase inhibitor in 1997, most clinicians would consider the cholinergic drugs, donepezil, rivastigmine and galantamine to be the first line pharmacotherapy for mild and moderate AD. These compounds have been reported to have their adverse effects including gastrointestinal disturbances and problems associated with bioavailability, high cost, and short half-life [2] which necessitates the interest in finding better AChE inhibitors from natural resources. Desirable properties of botanical extracts or natural product based compounds include a comparatively better penetration of the blood–brain barrier better than the pharmaceutical options and better specificity for human type AChE. Plant-derived essential oils exhibit pharmacological properties traceable to the presence of various structurally diverse bioactive chemical

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