Anti-Alzheimer’s disease activity of compounds from the root bark of Morus alba L.
Kuk Eun-Bi, 조아라, Oh Seo-In, 손희숙, 성수희, Roy Anupom, 최재수, 정현아,
소속 상세정보
( Kuk Eun-Bi )
Chonbuk National University Department of Food Science and Human Nutrition
조아라 ( Jo A-Ra )
Chonbuk National University Department of Food Science and Human Nutrition
( Oh Seo-In )
Chonbuk National University Department of Food Science and Human Nutrition
손희숙 ( Sohn Hee-Sook )
Chonbuk National University Department of Food Science and Human Nutrition
성수희 ( Seong Su-Hui )
Pukyong National University Department of Food Science and Nutrition
( Roy Anupom )
Pukyong National University Department of Food Science and Nutrition
최재수 ( Choi Jae-Sue )
Pukyong National University Department of Food Science and Nutrition
정현아 ( Jung Hyun-Ah )
Chonbuk National University Department of Food Science and Human Nutrition
KMID : 0043320170400030338
Abstract
The inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE1) plays important roles in prevention and treatment of Alzheimer’s disease (AD). Among the individual parts of Morus alba L. including root bark, branches, leaves, and fruits, the root bark showed the most potent enzyme inhibitory activities. Therefore, the aim of this study was to evaluate the anti-AD activity of the M. alba root bark and its isolate compounds, including mulberrofuran G (1), albanol B (2), and kuwanon G (3) via inhibition of AChE, BChE, and BACE1. Compounds 1 and 2 showed strong AChE- and BChE-inhibitory activities; 1?3 showed significant BACE1 inhibitory activity. Based on the kinetic study with AChE and BChE, 2 and 3 showed noncompetitive-type inhibition; 1 showed mixed-type inhibition. Moreover, 1?3 showed mixed-type inhibition against BACE1. The molecular docking simulations of 1?3 demonstrated negative binding energies, indicating a high affinity to AChE and BACE1. The hydroxyl group of 1?3 formed hydrogen bond with the amino acid residues located at AChE and BACE1. Consequently, these results indicate that the root bark of M. alba and its active compounds might be promising candidates for preventive and therapeutic agents for AD.
키워드
Morus alba L.; Root bark; Acetylcholinesterase; Butyrylcholinesterase; BACE1; Alzheimer’s disease
원문 및 링크아웃 정보
등재저널 정보