Hypocholesterolaemic activity of 3-hydroxy-3-methyl-glutaryl flavanones enriched fraction from bergamot fruit (Citrus bergamia): "In vivo" studies

Statins are the pharmacological inhibitors of cholesterol biosynthesis, acting on key enzyme 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR). They are the most effective class of drugs used to treat cardiovascular disease, the main cause of mortality in western- ized countries. Our major goal was to investigate the hypocholesterolaemic effects of the 3-hydroxy-3-methyl-glutaryl flavanones enriched fraction (HMGF), extracted from berga- mot fruit, in comparison with one of the most used statins, i.e. simvastatin, in a rat model. HMGF and simvastatin reduced the total cholesterol (TC), triacylglycerols (TG), very low- density lipoproteins (VLDL) and low-density lipoproteins (LDL) levels, whereas an increase of the high-density lipoproteins (HDL) content was observed exclusively in the HMGF trea- ted rats. Additionally, an appreciable increase of HMGR, LDL receptor (LDLR) and fatty acid synthase (FASN) was evidenced, at mRNA and protein levels. HMGF did not exhibit geno- toxic effects and was cytotoxic only at elevated concentrations. The daily supplementation of HMGF in the diet could be very effective for the treatment of hypercholesterolaemia.

Statins are the pharmacological inhibitors of cholesterol biosynthesis, acting on key enzyme 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR). They are the most effective class of drugs used to treat cardiovascular disease, the main cause of mortality in westernized countries. Our major goal was to investigate the hypocholesterolaemic effects of the 3-hydroxy-3-methyl-glutaryl flavanones enriched fraction (HMGF), extracted from bergamot fruit, in comparison with one of the most used statins, i.e. simvastatin, in a rat model. HMGF and simvastatin reduced the total cholesterol (TC), triacylglycerols (TG), very low-density lipoproteins (VLDL) and low-density lipoproteins (LDL) levels, whereas an increase of the high-density lipoproteins (HDL) content was observed exclusively in the HMGF treated rats. Additionally, an appreciable increase of HMGR, LDL receptor (LDLR) and fatty acid synthase (FASN) was evidenced, at mRNA and protein levels. HMGF did not exhibit genotoxic effects and was cytotoxic only at elevated concentrations. The daily supplementation of HMGF in the diet could be very effective for the treatment of hypercholesterolaemia. (C) 2013 Elsevier Ltd. All rights reserved.