Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
11
pubmed:dateCreated
2010-5-21
pubmed:abstractText
In our consecutive research on an anti-AD remedy derived from maritime plants, the BACE1 inhibitory activities of Eisenia bicyclis and its isolated phlorotannins were evaluated. The E. bicyclis extract and its fractions exhibited predominant BACE1 inhibition. With the exception of phloroglucinol (1), all test phlorotannins isolated from the most active EtOAc soluble fraction, showed significant and non-competitive inhibition against BACE1:dioxinodehydroeckol (2, IC(50)=5.35 microM; K(i)=8.0); eckol (3, IC(50)=12.20 microM; K(i)=13.9); phlorofurofucoeckol-A (4, IC(50)=2.13muM; K(i)=1.3); dieckol (5, IC(50)=2.21 microM; K(i)=1.5); triphloroethol A (6, IC(50)=11.68 microM; K(i)=12.1); 7-phloroethol (7, IC(50)=8.59 microM; K(i)=7.2). In addition, plausible protein-ligand interactions of 3, 4, and 5 were similar and may occur primarily through the TYR132 and THR133 of BACE1 via molecular docking simulations (autodock 4.0 and fred 2.0 programs). As a result, the E. bicyclis extract and the phlorotannins contained therein would clearly have beneficial use in the development of therapeutic and preventive agents for AD and suggest potential guidelines for the design of BACE-selective inhibitors.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
1464-3405
pubmed:author
pubmed:copyrightInfo
Copyright 2010 Elsevier Ltd. All rights reserved.
pubmed:issnType
Electronic
pubmed:day
1
pubmed:volume
20
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
3211-5
pubmed:meshHeading
pubmed:year
2010
pubmed:articleTitle
Molecular docking studies of phlorotannins from Eisenia bicyclis with BACE1 inhibitory activity.
pubmed:affiliation
Division of Food Science and Biotechnology, Pukyong National University, Busan 608-737, Republic of Korea.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't