Structural activity relationship of flavonoids with estrogen-related receptor gamma

FEBS Letters
Zhiyan HuangChi-Wai Wong

Abstract

In this study, we investigated the structural activity relationships (SARs) of flavonoids with estrogen-related receptor gamma (ERRgamma) and its coactivator peroxisome proliferators-activated receptor gamma coactivator-1alpha (PGC-1alpha). Isoflavones (genistein and daidzein) and flavanones (naringenin and hesperetin) did not significantly affect ERRgamma activity. Flavone apigenin and flavonol kaempferol directly suppressed the interaction between ERRgamma and PGC-1alpha functioning as inverse agonists. In contrast, flavone luteolin suppressed PGC-1alpha activity in part through promoting the degradation of PGC-1alpha leading to suppressed ERRgamma activity. Therefore, these flavones and flavonols utilize alternative mechanisms to influence the transcriptional activities of ERRgamma and PGC-1alpha.

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Citations

Apr 30, 2013·Bioorganic & Medicinal Chemistry·Dana AtrahimovichSoliman Khatib
Nov 12, 2013·Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy·Harshita SinghRakesh Maurya
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Apr 19, 2019·Antioxidants·Meenakshi SudhakaranAndrea I Doseff
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Jul 25, 2019·BMC Genomics·Dana AtrahimovichEli Reuveni
Oct 18, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mai KhaterHelen M I Osborn

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