SIRT1 deacetylates and inhibits SREBP-1C activity in regulation of hepatic lipid metabolism

J Biol Chem. 2010 Oct 29;285(44):33959-70. doi: 10.1074/jbc.M110.122978. Epub 2010 Sep 3.

Abstract

The SIRT1 deacetylase inhibits fat synthesis and stimulates fat oxidation in response to fasting, but the underlying mechanisms remain unclear. Here we report that SREBP-1c, a key lipogenic activator, is an in vivo target of SIRT1. SIRT1 interaction with SREBP-1c was increased during fasting and decreased upon feeding, and consistently, SREBP-1c acetylation levels were decreased during fasting in mouse liver. Acetylated SREBP-1c levels were also increased in HepG2 cells treated with insulin and glucose to mimic feeding conditions, and down-regulation of p300 by siRNA decreased the acetylation. Depletion of hepatic SIRT1 by adenoviral siRNA increased acetylation of SREBP-1c with increased lipogenic gene expression. Tandem mass spectrometry and mutagenesis studies revealed that SREBP-1c is acetylated by p300 at Lys-289 and Lys-309. Mechanistic studies using acetylation-defective mutants showed that SIRT1 deacetylates and inhibits SREBP-1c transactivation by decreasing its stability and its occupancy at the lipogenic genes. Remarkably, SREBP-1c acetylation levels were elevated in diet-induced obese mice, and hepatic overexpression of SIRT1 or treatment with resveratrol, a SIRT1 activator, daily for 1 week decreased acetylated SREBP-1c levels with beneficial functional outcomes. These results demonstrate an intriguing connection between elevated SREBP-1c acetylation and increased lipogenic gene expression, suggesting that abnormally elevated SREBP-1c acetylation increases SREBP-1c lipogenic activity in obese mice. Reducing acetylation of SREBP-1c by targeting SIRT1 may be useful for treating metabolic disorders, including fatty liver, obesity, and type II diabetes.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • COS Cells
  • Chlorocebus aethiops
  • Gene Expression Regulation*
  • Humans
  • Insulin / metabolism
  • Lipids / chemistry*
  • Liver / metabolism*
  • Male
  • Mass Spectrometry / methods
  • Mice
  • Mice, Inbred BALB C
  • Sirtuin 1 / metabolism*
  • Sterol Regulatory Element Binding Protein 1 / metabolism*

Substances

  • Insulin
  • Lipids
  • Sterol Regulatory Element Binding Protein 1
  • SIRT1 protein, human
  • Sirt1 protein, mouse
  • Sirtuin 1