Healthy Cholesterol and Metabolic Syndrome

  • CLINICAL STUDY 1
  • CLINICAL STUDY 2
  • CLINICAL STUDY 3
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  • CLINICAL STUDY 5

Bergamot polyphenolic fraction enhances rosuvastatin-induced effect on LDLcholesterol, LOX-1 expression and Protein Kinase B
phosphorylation in patients with hyperlipidemia

International Journal of Cardiology November 14, 2013
Micaela Gliozzi, Ross Walker, Saverio Muscoli, Cristiana Vitale, Santo Gratteri, Cristina Carresi,
Vincenzo Musolino, Vanessa Russo, Elzbjeta Janda, Salvatore Ragusa, Antonio Aloe, Ernesto
Palma, Carolina Muscoli, Franco Romeo and, Vincenzo Mollace

Statins are the most commonly prescribed drugs to reduce cardiometabolic risk. Besides the well-known efficacy of such compounds in both preventing and treating cardiometabolic disorders, some patients experience statin-induced side effects. We hypothesize that the use of natural bergamot-derived polyphenols may allow patients undergoing statin treatment to reduce effective doses while achieving target lipid values. The aim of the present study is to investigate the occurrence of an enhanced effect of bergamot-derived polyphenolic fraction (BPF) on rosuvastatin-induced hypolipidemic and vasoprotective response in patients with mixed hyperlipidemia.

Methods: A prospective, open-label, parallel group, placebo-controlled study on 77 patients with elevated serum LDL-C and triglycerides was designed. Patients were randomly assigned to a control group receiving placebo (n = 15), two groups receiving orally administered rosuvastatin (10 and 20 mg/daily for 30 days; n = 16 for each group), a group receiving BPF alone orally (1000 mg/daily for 30 days; n = 15) and a group receiving BPF (1000 mg/daily given orally) plus rosuvastatin (10 mg/daily for 30 days; n = 15).

Results: Both doses of rosuvastatin and BPF reduced total cholesterol, LDL-C, the LDL-C/HDL-C ratio and urinary mevalonate in hyperlipidemic patients, compared to control group. The cholesterol lowering effect was accompanied by reductions of malondialdehyde, oxyLDL receptor LOX-1 and phosphoPKB, which are all biomarkers of oxidative vascular damage, in peripheral polymorphonuclear cells.

Conclusions: Addition of BPF to rosuvastatin significantly enhanced rosuvastatin-induced effect on serum lipemic profile compared to rosuvastatin alone. This lipid-lowering effect was associated with significant reductions of biomarkers used for detecting oxidative vascular damage, suggesting a multi-action enhanced potential for BPF in patients on statin therapy.

HYPOLIPEMIC AND HYPOGLYCAEMIC ACTIVITY OF BERGAMOT POLYPHENOLS: FROM ANIMAL MODELS TO HUMAN STUDIES

Fitoterapia Volume 82, Issue 3, April 2011, Pages 309-316 Vincenzo Mollace, Iolanda Sacco, Elzbieta Janda, Claudio Malara, Domenica Ventrice, Carmen Colica, Valeria Visalli, Saverio Muscoli, Salvatore Ragusa, Carolina Muscoli, Domenicantonio Rotiroti, Franco Romeo

Bergamot juice produces hypolipemic activity in rats though the mechanism remains unclear. Here we investigated on the effect of bergamot extract (BPF) in diet-induced hyperlipemia in Wistar rats and in 237 patients suffering from hyperlipemia either associated or not with hyperglycaemia. BPF, given orally for 30 days to both rats and patients, reduces total and LDL cholesterol levels (an effect accompanied by elevation of cHDL), triglyceride levels and by a significant decrease in blood glucose. Moreover, BPF inhibited HMG-CoA reductase activity and enhanced reactive vasodilation thus representing an efficient phytotherapeutic approach in combating hyperlipemic and hyperglycaemic disorders.

Bergamot Polyphenols: Pleiotropic Players in the Treatment of Metabolic Syndrome

Journal of Metabolic Syndrome May 2014. Micaela Gliozzi, Ross Walker and Vincenzo Mollace

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Clinical application of bergamot (Citrus bergamia) for reducing high cholesterol and cardiovascular disease markers

Integr Food Nutr Metab. Feb 2019. Mirielle C Nauman and Jeremy J Johnson

The bergamot is a citrus fruit native to southern Italy with traditional uses that include improving immune response and cardiovascular function. There are a variety of phytochemicals that have been found in the bergamot including brutieridin and melitidin as well as other flavonoids, flavones O-glucosides and C-glucosides. Multiple clinical trials have provided evidence that different forms of orally administered bergamot can reduce total cholesterol and low-density lipoprotein cholesterol. In vitro mechanistic studies have provided evidence that polyphenols from the bergamot can alter the function of AMPK and pancreatic cholesterol ester hydrolase (pCEH). The use of bergamot in multiple clinical trials has consistently shown that it is well tolerated in studies ranging from 30 days to 12 weeks. This mini-review reports on the clinical studies performed with different forms of bergamot along with their effectiveness in reducing total cholesterol and LDL cholesterol in patients with hypercholesterolemia.

The effect of bergamot polyphenolic fraction on lipid transfer protein system and vascular oxidative stress in a rat model of hyperlipemia

Lipids in Health and Disease (2019) 18:115. Vincenzo Musolino, Micaela Gliozzi, Saverio Nucera, Cristina Carresi, Jessica Maiuolo, Rocco Mollace, Sara Paone, Francesca Bosco, Federica Scarano, Miriam Scicchitano, Stefano Ruga, Maria Caterina Zito, Carmen Colica, Roberta Macrì, Ernesto Palma, Salvatore Ragusa, Carolina Muscoli and Vincenzo Mollace

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