In vitro structure-toxicity relationship of chalcones in human hepatic stellate cells

Handle URI:
http://hdl.handle.net/10754/561140
Title:
In vitro structure-toxicity relationship of chalcones in human hepatic stellate cells
Authors:
Zenger, Katharina; Dutta, Subhajit; Wolff, Horst; Genton, Marc G. ( 0000-0001-6467-2998 ) ; Kraus, Birgit
Abstract:
Xanthohumol (XN), the major prenylated chalcone from hops (Humulus lupulus L.), has received much attention within the last years, due to its multiple pharmacological activities including anti-proliferative, anti-inflammatory, antioxidant, pro-apoptotic, anti-bacterial and anti-adhesive effects. However, there exists a huge number of metabolites and structurally-related chalcones, which can be expected, or are already known, to exhibit various effects on cells. We have therefore analyzed the effects of XN and 18 other chalcones in a panel, consisting of multiple cell-based assays. Readouts of these assays addressed distinct aspects of cell-toxicity, like proliferation, mitochondrial health, cell cycle and other cellular features. Besides known active structural elements of chalcones, like the Michael system, we have identified several moieties that seem to have an impact on specific effects and toxicity in human liver cells in vitro. Based on these observations, we present a structure-toxicity model, which will be crucial to understand the molecular mechanisms of wanted effects and unwanted side-effects of chalcones.
KAUST Department:
Computer, Electrical and Mathematical Sciences and Engineering (CEMSE) Division
Citation:
In vitro structure-toxicity relationship of chalcones in human hepatic stellate cells 2015 Toxicology
Journal:
Toxicology
Issue Date:
19-Jul-2015
DOI:
10.1016/j.tox.2015.07.012
Type:
Article
ISSN:
0300483X
Additional Links:
http://linkinghub.elsevier.com/retrieve/pii/S0300483X15300184
Appears in Collections:
Articles; Computer, Electrical and Mathematical Sciences and Engineering (CEMSE) Division

Full metadata record

DC FieldValue Language
dc.contributor.authorZenger, Katharinaen
dc.contributor.authorDutta, Subhajiten
dc.contributor.authorWolff, Horsten
dc.contributor.authorGenton, Marc G.en
dc.contributor.authorKraus, Birgiten
dc.date.accessioned2015-07-28T13:01:12Zen
dc.date.available2015-07-28T13:01:12Zen
dc.date.issued2015-07-19en
dc.identifier.citationIn vitro structure-toxicity relationship of chalcones in human hepatic stellate cells 2015 Toxicologyen
dc.identifier.issn0300483Xen
dc.identifier.doi10.1016/j.tox.2015.07.012en
dc.identifier.urihttp://hdl.handle.net/10754/561140en
dc.description.abstractXanthohumol (XN), the major prenylated chalcone from hops (Humulus lupulus L.), has received much attention within the last years, due to its multiple pharmacological activities including anti-proliferative, anti-inflammatory, antioxidant, pro-apoptotic, anti-bacterial and anti-adhesive effects. However, there exists a huge number of metabolites and structurally-related chalcones, which can be expected, or are already known, to exhibit various effects on cells. We have therefore analyzed the effects of XN and 18 other chalcones in a panel, consisting of multiple cell-based assays. Readouts of these assays addressed distinct aspects of cell-toxicity, like proliferation, mitochondrial health, cell cycle and other cellular features. Besides known active structural elements of chalcones, like the Michael system, we have identified several moieties that seem to have an impact on specific effects and toxicity in human liver cells in vitro. Based on these observations, we present a structure-toxicity model, which will be crucial to understand the molecular mechanisms of wanted effects and unwanted side-effects of chalcones.en
dc.relation.urlhttp://linkinghub.elsevier.com/retrieve/pii/S0300483X15300184en
dc.rightsNOTICE: this is the author’s version of a work that was accepted for publication in Toxicology. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be reflected in this document. Changes may have been made to this work since it was submitted for publication. A definitive version was subsequently published in Toxicology, 19 July 2015. DOI: 10.1016/j.tox.2015.07.012en
dc.subjectchalconesen
dc.subjectstructure activity relationshipen
dc.subjectxanthohumolen
dc.subjecthepatic stellate cellen
dc.titleIn vitro structure-toxicity relationship of chalcones in human hepatic stellate cellsen
dc.typeArticleen
dc.contributor.departmentComputer, Electrical and Mathematical Sciences and Engineering (CEMSE) Divisionen
dc.identifier.journalToxicologyen
dc.eprint.versionPost-printen
dc.contributor.institutionPharmaceutical Biology, Institute of Pharmacy, University of Regensburg, Regensburg, Germanyen
dc.contributor.institutionCarl Zeiss Microscopy GmbH, Göttingen, Germanyen
kaust.authorDutta, Subhajiten
kaust.authorGenton, Marc G.en
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