Linked Life Data

16500106

Source:http://linkedlifedata.com/resource/pubmed/id/16500106

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
12
pubmed:dateCreated
2006-5-8
pubmed:abstractText
Lipoxygenases (LO) have been implicated in asthma, immune disorders, and various cancers and as a consequence, there is great interest in isolating selective LO isozyme inhibitors. Currently, there is much use of baicalein as a selective human platelet 12-LO (12-hLO) inhibitor, however, our current steady-state inhibition data indicate that baicalein is not selective against 12-hLO versus human reticulocyte 15-LO-1 (15-hLO-1) (15/12=1.3), in vitro. However, in the presence of detergents baicalein is slightly more selective (15/12=7) as seen by the steady-state inhibition kinetics, which may imply greater selectivity in a cell-based assay but has yet to be proven. The mechanism of baicalein inhibition of 15-hLO-1 is reductive, which molecular modeling suggests is through direct binding of the catecholic moiety of baicalein to the iron. A structurally related flavonoid, apigenin, is not reductive, however, molecular modeling suggests a hydrogen bond with Thr591 may account for its inhibitor potency.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0968-0896
pubmed:author
pubmed:issnType
Print
pubmed:day
15
pubmed:volume
14
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
4295-301
pubmed:dateRevised
2010-11-18
pubmed:meshHeading
pubmed:year
2006
pubmed:articleTitle
Baicalein is a potent in vitro inhibitor against both reticulocyte 15-human and platelet 12-human lipoxygenases.
pubmed:affiliation
Department of Chemistry and Biochemistry, University of California, Santa Cruz, CA 95064, USA.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't, Research Support, N.I.H., Extramural