University of Hertfordshire

Natural chalcones as dual inhibitors of HDACs and NF-κB

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Natural chalcones as dual inhibitors of HDACs and NF-κB. / Orlikova, B.; Schnekenburger, M.; Zloh, Mire; Golais, F.; Diederich, M.; Tasdemir, D.

In: Oncology Reports, Vol. 28, No. 3, 2012, p. 797-805.

Research output: Contribution to journalArticlepeer-review

Harvard

Orlikova, B, Schnekenburger, M, Zloh, M, Golais, F, Diederich, M & Tasdemir, D 2012, 'Natural chalcones as dual inhibitors of HDACs and NF-κB', Oncology Reports, vol. 28, no. 3, pp. 797-805. https://doi.org/10.3892/or.2012.1870

APA

Orlikova, B., Schnekenburger, M., Zloh, M., Golais, F., Diederich, M., & Tasdemir, D. (2012). Natural chalcones as dual inhibitors of HDACs and NF-κB. Oncology Reports, 28(3), 797-805. https://doi.org/10.3892/or.2012.1870

Vancouver

Orlikova B, Schnekenburger M, Zloh M, Golais F, Diederich M, Tasdemir D. Natural chalcones as dual inhibitors of HDACs and NF-κB. Oncology Reports. 2012;28(3):797-805. https://doi.org/10.3892/or.2012.1870

Author

Orlikova, B. ; Schnekenburger, M. ; Zloh, Mire ; Golais, F. ; Diederich, M. ; Tasdemir, D. / Natural chalcones as dual inhibitors of HDACs and NF-κB. In: Oncology Reports. 2012 ; Vol. 28, No. 3. pp. 797-805.

Bibtex

@article{a25d4bf781584110b6d40e4b305cdd85,
title = "Natural chalcones as dual inhibitors of HDACs and NF-κB",
abstract = "Histone deacetylase enzymes (HDACs) are emerging as a promising biological target for cancer and inflammation. Using a fluorescence assay, we tested the in vitro HDAC inhibitory activity of twenty-one natural chalcones, a widespread group of natural products with well-known anti-inflammatory and antitumor effects. Since HDACs regulate the expression of the transcription factor NF-κB, we also evaluated the inhibitory potential of the compounds on NF-κB activation. Only four chalcones, isoliquiritigenin (no. 10), butein (no. 12), homobutein (no. 15) and the glycoside marein (no. 21) showed HDAC inhibitory activity with IC50 values of 60-190 µM, whereas a number of compounds inhibited TNFα-induced NF-κB activation with IC50 values in the range of 8-41 µM. Interestingly, three chalcones (nos. 10, 12 and 15) inhibited both TNFα-induced NF-κB activity and total HDAC activity of classes I, II and IV. Molecular modeling and docking studies were performed to shed light into dual activity and to draw structure-activity relationships among chalcones (nos. 1-21). To the best of our knowledge this is the first study that provides evidence for HDACs as potential drug targets for natural chalcones. The dual inhibitory potential of the selected chalcones on NF-κB and HDACs was investigated for the first time. This study demonstrates that chalcones can serve as lead compounds in the development of dual inhibitors against both targets in the treatment of inflammation and cancer.",
author = "B. Orlikova and M. Schnekenburger and Mire Zloh and F. Golais and M. Diederich and D. Tasdemir",
note = "Article available on open access at http://dx.doi.org/10.3892/or.2012.1870",
year = "2012",
doi = "10.3892/or.2012.1870",
language = "English",
volume = "28",
pages = "797--805",
journal = "Oncology Reports",
issn = "1021-335x",
publisher = "Spandidos Publications",
number = "3",

}

RIS

TY - JOUR

T1 - Natural chalcones as dual inhibitors of HDACs and NF-κB

AU - Orlikova, B.

AU - Schnekenburger, M.

AU - Zloh, Mire

AU - Golais, F.

AU - Diederich, M.

AU - Tasdemir, D.

N1 - Article available on open access at http://dx.doi.org/10.3892/or.2012.1870

PY - 2012

Y1 - 2012

N2 - Histone deacetylase enzymes (HDACs) are emerging as a promising biological target for cancer and inflammation. Using a fluorescence assay, we tested the in vitro HDAC inhibitory activity of twenty-one natural chalcones, a widespread group of natural products with well-known anti-inflammatory and antitumor effects. Since HDACs regulate the expression of the transcription factor NF-κB, we also evaluated the inhibitory potential of the compounds on NF-κB activation. Only four chalcones, isoliquiritigenin (no. 10), butein (no. 12), homobutein (no. 15) and the glycoside marein (no. 21) showed HDAC inhibitory activity with IC50 values of 60-190 µM, whereas a number of compounds inhibited TNFα-induced NF-κB activation with IC50 values in the range of 8-41 µM. Interestingly, three chalcones (nos. 10, 12 and 15) inhibited both TNFα-induced NF-κB activity and total HDAC activity of classes I, II and IV. Molecular modeling and docking studies were performed to shed light into dual activity and to draw structure-activity relationships among chalcones (nos. 1-21). To the best of our knowledge this is the first study that provides evidence for HDACs as potential drug targets for natural chalcones. The dual inhibitory potential of the selected chalcones on NF-κB and HDACs was investigated for the first time. This study demonstrates that chalcones can serve as lead compounds in the development of dual inhibitors against both targets in the treatment of inflammation and cancer.

AB - Histone deacetylase enzymes (HDACs) are emerging as a promising biological target for cancer and inflammation. Using a fluorescence assay, we tested the in vitro HDAC inhibitory activity of twenty-one natural chalcones, a widespread group of natural products with well-known anti-inflammatory and antitumor effects. Since HDACs regulate the expression of the transcription factor NF-κB, we also evaluated the inhibitory potential of the compounds on NF-κB activation. Only four chalcones, isoliquiritigenin (no. 10), butein (no. 12), homobutein (no. 15) and the glycoside marein (no. 21) showed HDAC inhibitory activity with IC50 values of 60-190 µM, whereas a number of compounds inhibited TNFα-induced NF-κB activation with IC50 values in the range of 8-41 µM. Interestingly, three chalcones (nos. 10, 12 and 15) inhibited both TNFα-induced NF-κB activity and total HDAC activity of classes I, II and IV. Molecular modeling and docking studies were performed to shed light into dual activity and to draw structure-activity relationships among chalcones (nos. 1-21). To the best of our knowledge this is the first study that provides evidence for HDACs as potential drug targets for natural chalcones. The dual inhibitory potential of the selected chalcones on NF-κB and HDACs was investigated for the first time. This study demonstrates that chalcones can serve as lead compounds in the development of dual inhibitors against both targets in the treatment of inflammation and cancer.

U2 - 10.3892/or.2012.1870

DO - 10.3892/or.2012.1870

M3 - Article

C2 - 22710558

VL - 28

SP - 797

EP - 805

JO - Oncology Reports

JF - Oncology Reports

SN - 1021-335x

IS - 3

ER -