Inhibition of SREBP by a small molecule, betulin, improves hyperlipidemia and insulin resistance and reduces atherosclerotic plaques. | CureHunter

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Inhibition of SREBP by a small molecule, betulin, improves hyperlipidemia and insulin resistance and reduces atherosclerotic plaques.

Abstract	Sterol regulatory element-binding proteins (SREBPs) are major transcription factors activating the expression of genes involved in biosynthesis of cholesterol, fatty acid and triglyceride. In this study, we identified a small molecule, betulin, that specifically inhibited the maturation of SREBP by inducing interaction of SREBP cleavage activating protein (SCAP) and Insig. Inhibition of SREBP by betulin decreased the biosynthesis of cholesterol and fatty acid. In vivo, betulin ameliorated diet-induced obesity, decreased the lipid contents in serum and tissues, and increased insulin sensitivity. Furthermore, betulin reduced the size and improved the stability of atherosclerotic plaques. Our study demonstrates that inhibition SREBP pathway can be employed as a therapeutic strategy to treat metabolic diseases including type II diabetes and atherosclerosis. Betulin, which is abundant in birch bark, could be a leading compound for development of drugs for hyperlipidemia.
Authors	Jing-Jie Tang, Jia-Gui Li, Wei Qi, Wen-Wei Qiu, Pei-Shan Li, Bo-Liang Li, Bao-Liang Song
Journal	Cell metabolism (Cell Metab) Vol. 13 Issue 1 Pg. 44-56 (Jan 05 2011) ISSN: 1932-7420 [Electronic] United States
PMID	21195348 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Copyright	Copyright Â© 2011 Elsevier Inc. All rights reserved.
Chemical References	Fatty Acids Intracellular Signaling Peptides and Proteins Membrane Proteins SREBP cleavage-activating protein Sterol Regulatory Element Binding Proteins Triterpenes betulin Cholesterol
Topics	Animals Cholesterol (biosynthesis, genetics) Down-Regulation Energy Metabolism (drug effects) Fatty Acids (biosynthesis) Humans Hyperlipidemias (drug therapy, genetics, metabolism) Insulin Resistance (physiology) Intracellular Signaling Peptides and Proteins (metabolism) Lipid Metabolism Male Membrane Proteins (metabolism) Mice Mice, Inbred C57BL Mice, Knockout Obesity (drug therapy) Plaque, Atherosclerotic (drug therapy, genetics, metabolism) Sterol Regulatory Element Binding Proteins (antagonists & inhibitors, genetics, metabolism) Triterpenes (analysis, chemistry, pharmacology)

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