Zenger, Katharina and Dutta, Subhajit and Wolff, Horst and Genton, Marc G. and Kraus, Birgit (2015) In vitro structure-toxicity relationship of chalcones in human hepatic stellate cells. TOXICOLOGY, 336. pp. 26-33. ISSN 0300-483X,
Full text not available from this repository. (Request a copy)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. (C) 2015 Elsevier Ireland Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | HOPS HUMULUS-LUPULUS; HUMAN LIVER-MICROSOMES; KAPPA-B P65; ANTIOXIDATIVE ACTIVITY; PRENYLATED FLAVONOIDS; XANTHOHUMOL; MITOCHONDRIA; CYTOTOXICITY; METABOLISM; APOPTOSIS; Chalcones; Structure activity relationship; Xanthohumol; Hepatic stellate cell |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 16 May 2019 12:55 |
| Last Modified: | 16 May 2019 12:55 |
| URI: | https://pred.uni-regensburg.de/id/eprint/4643 |
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