Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
SHR Neuro Krebs Kardio Lipid Stoffw Microb
Scharinger, B; Messner, B; Türkcan, A; Schuster, D; Vuorinen, A; Pitterl, F; Heinz, K; Arnhard, K; Laufer, G; Grimm, M; Stuppner, H; Oberacher, H; Eller, P; Ritsch, A; Bernhard, D.
Leoligin, the major lignan from Edelweiss, inhibits 3-hydroxy-3-methyl-glutaryl-CoA reductase and reduces cholesterol levels in ApoE-/- mice.
J Mol Cell Cardiol. 2016; 99(7):35-46
Doi: 10.1016/j.yjmcc.2016.08.003
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- Co-Autor*innen der Med Uni Graz
- Eller Philipp
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- Abstract:
- The health benefit through the control of lipid levels in hyperlipidaemic individuals is evident from a large number of studies. The pharmacological options to achieve this goal shall be as specific and personalized as the reasons for and co-factors of hyperlipidaemia. It was the goal of this study to reveal the impact of leoligin on cholesterol levels and to define its mechanism of action. Oral application of leoligin in ApoE-/- mice led to significantly reduced total serum cholesterol levels and a reduction in postprandial blood glucose peak levels. In the absence of biochemical signs of toxicity, leoligin treatment resulted in reduced weight gain in mice. The effects of leoligin on serum cholesterol levels may be due to a direct inhibition of 3-hydroxy-3-methyl-glutaryl-CoA reductase (HMGCR) by a unique, non-statin-like binding mode. Postprandial serum glucose peaks may be reduced by a mild peroxisome proliferator-activated receptor-gamma (PPAR-γ) agonistic activity of leoligin. No effect on atherosclerotic plaque size was observed. As a non-toxic, cholesterol-, peak glucose-, and weight gain-lowering compound, leoligin continues to fulfil characteristics of a potential agent for the treatment of cardiovascular disease (CVD). The counterregulatory overexpression of hepatic HMGCR in leoligin treated animals possibly explains the missing permanent anti-atherosclerotic effect. Copyright © 2016 The Authors. Published by Elsevier Ltd.. All rights reserved.
- Find related publications in this database (using NLM MeSH Indexing)
- Animals -
- Apolipoproteins E - deficiency
- Cholesterol - blood
- Cholesterol - metabolism
- Female -
- Glucose - metabolism
- Hydrogen Bonding -
- Hydroxymethylglutaryl CoA Reductases - chemistry
- Hydroxymethylglutaryl CoA Reductases - metabolism
- Hydroxymethylglutaryl-CoA Reductase Inhibitors - administration & dosage
- Hydroxymethylglutaryl-CoA Reductase Inhibitors - chemistry
- Hydroxymethylglutaryl-CoA Reductase Inhibitors - pharmacology
- Lignans - administration & dosage
- Lignans - chemistry
- Lignans - pharmacology
- Liver - drug effects
- Liver - metabolism
- Mice -
- Mice, Knockout -
- Models, Molecular -
- Molecular Conformation -
- PPAR gamma - agonists
- PPAR gamma - chemistry
- Plant Extracts - administration & dosage
- Plant Extracts - chemistry
- Plant Extracts - pharmacology
- Protein Binding -
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- Structure-Activity Relationship -
- Time Factors -
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- Cholesterol
- HMGCR inhibitor
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