Abstract
Inhibitory activity of thirty-one ethanol extracts obtained from albedo, flavedo, seed and leaf parts of 17 cultivars of Citrus species from Turkey, the bark and leaves of Olea europaea L. from two locations (Turkey and Cyprus) as well as caffeic acid and hesperidin was tested against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), related to the pathogenesis of Alzheimer's disease, using ELISA microtiter assays at 500 µg/mL. Metal-chelating capacity of the extracts was also determined. BChE inhibitory effect of the Citrus sp. extracts was from (7.7±0.7) to (70.3±1.1) %, whereas they did not show any inhibition against AChE. Cholinesterase inhibitory activity of the leaf and bark ethanol extracts of O. europaea was very weak ((10.2±3.1) to (15.0±2.3) %). The extracts had either no or low metal-chelating capacity at 500 µg/mL. HPTLC fingerprinting of the extracts, which indicated a similar phytochemical pattern, was also done using the standards of caffeic acid and hesperidin with weak cholinesterase inhibition. Among the screened extracts, the albedo extract of C. limon 'Interdonato', the flavedo extracts of 'Kara Limon' and 'Cyprus' cultivars and the seed extract of C. maxima appear to be promising as natural BChE inhibitors.
Highlights
Alzheimer’s disease (AD) is a neurological disorder and the most common cause of dementia
Our findings indicate that it is possible to discriminate Citrus aurantium, C. deliciosa, C. limon, C. maxima/C. paradisi and C. sinensis/C. reticulata
A parallel fingerprint was observed for all extracts of C. paradisi cultivars that contained hesperidin, while the extracts obtained from C. reticulata and C. sinensis ‘Navelina’ resemble each other (Fig. 2)
Summary
Alzheimer’s disease (AD) is a neurological disorder and the most common cause of dementia. It is a slowly progressive and degenerative disease that leads to loss of memory, decline in thinking and language skills. ACh levels in addition to its possible action in the etiology and progression of the disease [3]. Inhibition of both AChE and BChE is an important target for the development of new anti-Alzheimer drugs. Dysregulation of some transition metals such as iron, aluminum or copper has been very important in formation of oxidative stress and cellular damage relevant to some neurodegenerative diseases including AD and Parkinson’s disease [5,6]. It is strategically advantageous to have a drug candidate with both cholinesterase inhibition and metal-chelating properties for the treatment of AD as the need for development of novel drugs remains
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