4.4 Article

Tamarixetin Abrogates Adipogenesis Through Inhibiting p300/CBP-Associated Factor Acetyltransferase Activity in 3T3-L1 Preadipocyte Cells

Journal

JOURNAL OF MEDICINAL FOOD
Volume 25, Issue 3, Pages 272-280

Publisher

MARY ANN LIEBERT, INC
DOI: 10.1089/jmf.2021.K.0126

Keywords

adipogenesis; histone acetyltransferase; p300; CBP-associated factor; tamarixetin

Funding

  1. Main Research Program of the Korea Food Research Institute (KFRI)
  2. Ministry of Science, ICT

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Tamarixetin (TX) derived from natural products is a potent antilipogenic agent that reduces lipid accumulation and inhibits the expression and activity of p300/CBP-associated factor (pCAF), thereby decreasing lipogenesis-related gene expression.
Tamarixetin (TX) is an O-methylated flavonoid naturally derived from quercetin. TX has bioactive properties; however, whether it shows antilipogenic activity remains unknown. Therefore, in the present study, we aimed to determine the antilipogenic effects of TX using 3T3-L1 adipocytes. The 3T3-L1 adipocytes were cultured in a differentiation medium with or without TX. Lipid accumulation was diminished and the mRNA expression of lipogenesis-related genes was decreased following TX treatment. We found that TX exhibited antilipogenic effects by inhibiting the expression of p300/CBP-associated factor (pCAF), a histone acetyltransferase, as confirmed by pCAF knockdown. Furthermore, TX inhibited both pCAF expression and its activity, thereby reducing the total acetylation level of nonhistone and histone proteins. Finally, TX decreased the expression of CCAAT/enhancer-binding protein alpha and beta (CEBP alpha and CEBP beta), and peroxisome proliferator-activated receptor gamma along with pCAF expression during adipogenesis of 3T3-L1 cells in a time-dependent manner. Collectively, our findings suggest that TX is a potent antilipogenic agent derived from natural products and may be used as a pCAF inhibitor.

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