Anti-Alzheimer and Antioxidant Activities of Coptidis Rhizoma Alkaloids

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概要

• 論文の詳細を見る

• Coptidis Rhizoma and its isolated alkaloids are reported to possess a variety of activities, including neuroprotective and antioxidant effects. Thus, the anti-Alzheimer and antioxidant effects of six protoberberine alkaloids (berberine, palmatine, jateorrhizine, epiberberine, coptisine, and groenlandicine) and one aporphine alkaloid (magnoflorine) from Coptidis Rhizoma were evaluated via β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) assays, along with peroxynitrite (ONOO−) scavenging and total reactive oxygen species (ROS) inhibitory assays. Six protoberberine alkaloids exhibited predominant cholinesterases (ChEs) inhibitory effects with IC50 values ranging between 0.44—1.07 μM for AChE and 3.32—6.84 μM for BChE; only epiberberine (Ki=10.0) and groenlandicine (Ki=21.2) exerted good, non-competitive BACE1 inhibitory activities with IC50 values of 8.55 and 19.68 μM, respectively. In two antioxidant assays, jateorrhizine and groenlandicine exhibited significant ONOO− scavenging activities with IC50 values of 0.78 and 0.84 μM, respectively; coptisine and groenlandicine exhibited moderate total ROS inhibitory activities with IC50 values of 48.93 and 51.78 μM, respectively. These results indicate that Coptidis Rhizoma alkaloids have a strong potential of inhibition and prevention of Alzheimers disease (AD) mainly through both ChEs and β-amyloids pathways, and additionally through antioxidant capacities. In particular, groenlandicine may be a promising anti-AD agent due to its potent inhibitory activity of both ChEs and β-amyloids formation, as well as marked ONOO− scavenging and good ROS inhibitory capacities. As a result, Coptidis Rhizoma and the alkaloids contained therein would clearly have beneficial uses in the development of therapeutic and preventive agents for AD and oxidative stress-related disease.

• 日本薬学会の論文

著者

• Yokozawa Takako

  Institute of Natural Medicine, University of Toyama

• JUNG Hyun

  Division of Applied Plant Sciences, Sangji University

• Min Byung-sun

  Coll. Of Pharmacy Catholic Univ. Of Daegu

• Min Byung

  Institute Of Natural Medicine Toyama Medical And Pharmaceutical University

• Kim Yeong

  Department Of Mathematics And Center For Applied Mathematics Korea Advanced Institute Of Science And

• Min Byung-sun

  College Of Pharmacy Catholic University Of Daegu

• Yokozawa Takako

  Institute Of Natural Medicine Toyama Medical And Pharmaceutical University

• Lee Je-Hyun

  College of Oriental Medicine, Dongguk University

• Choi Jae

  Division of Food Science and Biotechnology, Pukyong National University

• Min Byung-sun

  Laboratory Of Immunomodulator Korea Research Institute Of Bioscience And Biotechnology

• Lee Je-hyun

  College Of Oriental Medicine Dongguk University

• Choi Jae

  Division Of Food Science And Biotechnology Pukyong National University

• Min Byung-Sun

  College of Pharmacy, Catholic University of Daegu

• JUNG Hyun

  Division of Food Science and Biotechnology, Pukyong National University

• Kim Yeong

  Department of Pharmaceutical Sciences, College of Pharmacy, Seoul National University

• Choi Jae

  Division of Cardiology, Department of Internal Medicine, Kangnam St. Mary's Hospital, The Catholic University of Korea

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