BACE1 and cholinesterase inhibitory activities of Nelumbo nucifera embryos

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• 作者：Hyun Ah Jung ; Subash Karki ; Ji Hye Kim ; Jae Sue Choi
• 关键词：Alzheimer’s disease ; Cholinesterase inhibition ; BACE1 ; Nelumbo nucifera ; Embryos ; Alkaloids
• 刊名：Archives of Pharmacal Research
• 出版年：2015
• 出版时间：June 2015
• 年：2015
• 卷：38
• 期：6
• 页码：1178-1187
• 全文大小：590 KB
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• 作者单位：Hyun Ah Jung (1)
  Subash Karki (2)
  Ji Hye Kim (2)
  Jae Sue Choi (2)
  
  1. Department of Food Science and Human Nutrition, Chonbuk National University, Jeonju, 561-756, Republic of Korea
  2. Department of Food Science and Nutrition, Pukyong National University, Busan, 608-737, Republic of Korea
  
• 刊物主题：Pharmacy; Pharmacology/Toxicology;
• 出版者：Springer Netherlands
• ISSN：1976-3786

文摘

The aim of the present study was to evaluate the comparative anti-Alzheimer’s disease (AD) activities of different parts of Nelumbo nucifera (leaves, de-embryo seeds, embryos, rhizomes, and stamens) in order to determine the selectivity and efficient use of its individual components. Anti-AD activities of different parts of N. nucifera were evaluated via inhibitory activities on acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein-cleaving enzyme 1 (BACE1) along with scavenging activity on peroxynitrite (ONOO?/sup>). Among the evaluated parts of N. nucifera, the embryo extract exhibited significant inhibitory potential against BACE1 and BChE as well as scavenging activity against ONOO?/sup>. Thus, the embryo extract was selected for detailed investigation on anti-AD activity using BACE1- and ChEs-inhibitory assays. Among the different solvent-soluble fractions, the dichloromethane (CH2Cl2), ethyl acetate (EtOAc), and n-butanol (n-BuOH) fractions showed promising ChEs and BACE1 inhibitory activities. Repeated column chromatography of the CH2Cl2, EtOAc and n-BuOH fractions yielded compounds 1-, which were neferine (1), liensinine (2), vitexin (3), quercetin 3-O-glucoside (4) and northalifoline (5). Compound 2 exhibited potent inhibitory activities on BACE1, AChE, and BChE with respective IC50 values of 6.37?±?0.13, 0.34?±?0.02, and 9.96?±?0.47?μM. Likewise, compound 1 showed potent inhibitory activities on BACE1, AChE, and BChE with IC50 values of 28.51?±?4.04, 14.19?±?1.46, and 37.18?±?0.59?μM, respectively; the IC50 values of 3 were 19.25?±?3.03, 16.62?±?1.43, and 11.53?±?2.21?μM, respectively. In conclusion, we identified potent ChEs- and BACE1-inhibitory activities of N. nucifera as well as its isolated constituents, which may be further explored to develop therapeutic and preventive agents for AD and oxidative stress related diseases.