Linked Life Data

18249473

Source:http://linkedlifedata.com/resource/pubmed/id/18249473

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
8
pubmed:dateCreated
2008-8-4
pubmed:abstractText
Inhibition of cytochrome P450 (CYP) is a major cause of drug-drug interactions. In this work, inhibitory potentials of 33 curcumin analogues, i.e. 2,6-dibenzylidenecyclohexanone (A series), 2,5-dibenzylidenecyclopentanone (B series) and 1,4-pentadiene-3-one (C series) substituted analogues of curcumin towards recombinant human CYP1A2, CYP3A4, CYP2B6, CYP2C9 and CYP2D6, all important for drug metabolism, were studied in vitro. Fluorescence plate reader and high performance liquid chromatography (HPLC) assays were used to evaluate CYP-inhibitory activities. MOE-based Quantitative structure-activity relationship (QSAR) analysis suggested that electrostatic and hydrophobic interactions and lipophilicity are important factors for CYP inhibition. Apart from insights in important molecular properties for CYP inhibition, the present results may also guide further design of curcumin analogues with less susceptibility to drug-drug interactions.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
0223-5234
pubmed:author
pubmed:issnType
Print
pubmed:volume
43
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1621-31
pubmed:meshHeading
pubmed:year
2008
pubmed:articleTitle
Structure-activity relationships for the inhibition of recombinant human cytochromes P450 by curcumin analogues.
pubmed:affiliation
Divisions of Molecular Toxicology, Leiden/Amsterdam Center for Drug Research, Department of Pharmacochemistry, Vrije Universiteit, De Boelelaan 1083, 1081 HV, Amsterdam, The Netherlands.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't