Exploration of Acetylcholinesterase Inhibitors from Flavonoids and Flavonoid Glycosides
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XPERIMENTAL ARTICLES
Exploration of Acetylcholinesterase Inhibitors from Flavonoids and Flavonoid Glycosides Peng Zhoua, 1 and Fang Huab, c, 1 aSchool of Integrated Chinese and Western Medicine, Anhui University of Chinese Medicine; Institute of Integrated Chinese and Western Medicine, Anhui Academy of Chinese Medicine; Anhui Province Key Laboratory of Chinese Medicinal Formula, Hefei, 230012 People’s Republic of China b Pharmacy School, Anhui Xinhua University, Hefei, 230088 People’s Republic of China c Natural Products Laboratory, International Joint Lab of Tea Chemistry and Health Effects, State Key Laboratory of Tea Plant Biology and Utilization, Anhui Agricultural University, Hefei, 230036 People’s Republic of China
Received February 16, 2020; revised March 27, 2020; accepted April 17, 2020
Abstract—A few organic synthetic drugs, such as donepezil, rivastigmine and tacrine, are used for inhibition of acetylcholinesterase (AChE) can provide palliative treatment without generally affecting the progression of the disease, however, sometimes at the cost of severe side effects. Flavonoids and flavonoid glycosides are the potential natural compounds from plants and foods for the treatment of Alzheimer’s disease (AD). In this study, the affinity of nine kaempferol and its glycosides on AChE were evaluated, and their interactions with flavonoids by molecular docking were predicted. Results indicated that Kaempferol exhibited the highest affinity to inhibit the activity of AChE. Besides, kaempferol-3-O-rhamnoside showed good AChE affinity among kaempferol monoglycosides. Kaempferol-3-O-glucorhamnoside and kaempferol-3-O-gentiobioside showed some AChE affinity among kaempferol diglycosides. We can conclude that these compounds are a promising class of AChE inhibitors for the treatment of AD and deserve further study. Keywords: acetylcholinesterase inhibitors, flavonoids, flavonoid glycosides, molecular docking DOI: 10.1134/S1819712420030137
INTRODUCTION Alzheimer’s disease (AD) is the most common neurodegenerative disease in the elderly, which is characterized by two biomarkers: neuritic plaques and neurofibrillary tangles [1–3]. In addition, AD is accompanied by cholinergic dysfunction of the central nervous system [4]. At present, there are many hypotheses related to the pathogenesis of AD. Most relevant therapies for AD patients are based on the inhibition of acetylcholinesterase activity [5, 6]. Cholinergic neurotransmission in AD is the basis of the well-known cholinergic hypothesis, and AD is connected with the reduced level of acetylcholine (Ach) and loss of cholinergic neurons in the brain [7]. Therefore, AChE is considered to be the most promising therapeutic target, and AChE inhibitors are considered to be the most promising drugs for AD. Nowadays, a few organic synthetic drugs are used for inhibition of AChE, such as donepezil, rivastig1 Corresponding
author; address: School of Integrated Chinese and Western Medicine, Anhui University of Chinese Medicine; Institute of Integrated Chinese and Western Medicin
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