The effect of bergamot polyphenolic fraction on lipid transfer protein system and vascular oxidative stress in a rat model of hyperlipemia (original) (raw)
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Hypolipemic and hypoglycaemic activity of bergamot polyphenols: From animal models to human studies
Fitoterapia, 2011
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.
Effect of bergamot on lipid profile in humans: A systematic review
Critical Reviews in Food Science and Nutrition, 2019
Dyslipidemia is a well-established modifiable cardiovascular risk. Although statins can reduce LDLc by 50-60%, less than 20% of patients with high risk of CVD achieve LDL targets. The aim of this systematic review is to evaluate the effect of the nutraceutical, bergamot (Citrus bergamia), on lipid parameters in humans. PubMed, Embase, Cochrane Library, and Google Scholar databases were searched for interventional and observational studies investigating the effect of bergamot on lipid profile in humans. This systematic review retrieved a total of 442 studies of which 12 articles fulfilled the eligibility criteria and were included in the qualitative synthesis. Based on data, 75% of studies showed a significant decrease in total cholesterol, triglycerides and LDLc. The decrease in total cholesterol varied from 12.3% to 31.3%, from 7.6% to 40.8% in LDLc and from 11.5% to 39.5% in triglycerides. Eight trials reported HDLc increase after intervention with bergamot. Overall, a dose-dependent and possible synergistic effect when administering with statins can be deducted from these trials. It is essential to point out that studies had heterogeneous designs and scientific quality of studies was quite limited. Promising findings reveal an alternative therapeutic option in dyslipidemia management with bergamot supplementation, especially in subjects with statins intolerance.
Frontiers in pharmacology, 2015
Some patients experience statin-induced side effects or prefer nutraceutical approaches for the treatment of dyslipidemia. This has led to a search for alternative therapeutic approaches for dyslipidemia management. In recent studies Citrus bergamia (known as Bergamot) juice was able to reduce serum levels of lipids. Such benefit may be attributed to high amounts of flavonoids contained in Bergamot fruit juice (neoeriocitrin, neohesperidin, naringin). The aim of the present study was to fully investigate the effects of a Bergamot extract on cardio-metabolic parameters, including plasma lipids, atherogenic lipoproteins and subclinical atherosclerosis. Eighty subjects (42 men and 38 women, mean age: 55 ± 13 years) with moderate hypercholesterolemia [e.g., with plasma LDL-cholesterol concentrations between 160 and 190 mg/dl (between 4.1 and 4.9 mmol/l)] were included. A Bergamot-derived extract (Bergavit R(®)) was given at a fixed dose daily (150 mg of flavonoids, with 16% of neoerioci...
Effect of Bergamot Polyphenolic Fraction on level of HDL-C & LDL-C
International Journal of Scientific Research in Science and Technology, 2023
A well-established modifiable cardiovascular risk component is low density lipoprotein (LDL-C). Although statins can lessen LDL-c through 50–60%, less than 20% of patients with excessive risk of CVD acquire LDL targets. The purpose of this systematic review is to assess the impact of the nutraceutical, bergamot (Citrus bergamia), on lipid parameters in humans. Based on data, 75% of studies confirmed a significant lower in overall cholesterol, triglycerides and LDL-c. The lower in overall cholesterol varied from 12.3% to 31.3%, from 7.6% to 40.8% in LDL-c and from 11.5% to 39.5% in triglycerides. The incidence of metabolic syndrome (MS) represents an independent risk factor for developing cardiovascular disorder states in patients affected by type 2 diabetes mellitus. Moreover, both the size of LDL particles and liver disorder recognized as non- alcoholic steato-hepatitis (NASH) constitute essential biomarkers for the improvement of cardiometabolic risk in patients with MS. Recent evidence indicates that bergamot polyphenolic fraction (BPF) in patients with MS and NASH induces a significant decrease of fasting plasma glucose, serum LDL cholesterol and triglycerides along with an increase of HDL cholesterol. In addition, a significant reduction of both ultrasonographic, TC scans and metabolic biomarkers of NASH in addition to a significant reduction of small dense LDL particles have been determined after BPF treatment suggesting a useful impact of bergamot-extract in patients with MS and NASH. In this regards, emerging evidence indicates a capability protecting function of bergamot extracts, specially bergamot flavonoids, in the control of various features of MetS (metabolic syndrome), because of their pleiotropic anti-oxidative, anti-inflammatory and lipid- reducing results. The purpose of this review is to discuss the beneficial effects of bergamot polyphenols providing a brand-new therapeutic method in the treatment of cholesterol.
Advances in Biological Chemistry, 2014
The occurrence of Metabolic Syndrome (MS) represents an independent risk factor for developing cardiovascular disease states in patients suffering from type 2 diabetes mellitus. Moreover, both the size of LDL particles and liver dysfunction identified as non alcoholic fatty liver disease (NAFLD) represent important biomarkers for the development of cardiometabolic risk in patients with MS. Here we studied the effect of bergamot polyphenolic fraction (BPF) in patients with MS and NAFLD. 107 patients were enrolled at the San Raffaele IRCCS (Rome). All of them showed ultrasonografic evidences of NAFLD and at least three out of five previous identified criteria for the diagnosis of MS. Patients were divided into two groups: one receiving placebo and the second receiving BPF 650 mg twice a day for 120 consecutive days. In the group receiving BPF 650 mg twice a day, a significant reduction of fasting plasma glucose, serum LDL cholesterol and triglycerides alongside with an increase of HDL cholesterol was found. This effect was accompanied by significant reduction of both ultrasonographic and metabolic biomarkers of NAFLD. Moreover, a significant reduction of small dense LDL particles, as detected via proton NMR Spectroscopy, was found * Corresponding author. M. Gliozzi et al. 130 after BPF treatment. In conclusion, our data confirm the beneficial effect of bergamot-extract in patients with MS an effect highlighted by significant reduction of small dense LDL particles and by improvement of NAFLD biomarkers. This suggests a potential preventive role of bergamot derivatives in reducing cardiometabolic risk.
Nutrients
Elevated serum cholesterol levels, either associated or not with increased triglycerides, represent a risk of developing vascular injury, mostly leading to atherothrombosis-related diseases including myocardial infarction and stroke. Natural products have been investigated in the last few decades as they are seen to offer an alternative solution to counteract cardiometabolic risk, due to the occurrence of side effects with the use of statins, the leading drugs for treating hyperlipidemias. Red yeast rice (RYR), a monacolin K-rich natural extract, has been found to be effective in counteracting high cholesterol, being its use accompanied by consistent warnings by regulatory authorities based on the potential detrimental responses accompanying its statin-like chemical charcateristics. Here we compared the effects of RYR with those produced by bergamot polyphenolic fraction (BPF), a well-known natural extract proven to be effective in lowering both serum cholesterol and triglycerides i...
Evaluation of lipid and cholesterol-lowering effect of bioflavonoids from bergamot extract
Natural Product Research, 2020
Several natural products have been reported to be involved in the suppression of adipogenesis. In this study, we reveal that a bergamot extract (BE) decreased the accumulation of intracellular lipids in murine pre-adipocytes 3T3-L1 cells during adipogenic differentiation. Both the inhibition of HMG-CoA reductase activity and the differentiation and proliferation of adipocytes could be used as a strategy for the treatment and prevention of obesity. The results of this study show a reduction of HMG-CoA activity and of lipid droplet accumulation in the presence of the BE, suggesting the potential of BE as an antiadipogenic agent to lower the content of cholesterol and body fat and prevent a gain in body weight. Moreover, BE as the result of high percentages of flavonoid compounds such as neoriocitrin, naringin and neohesperidin, the main flavonoids contained in BE, led to a significant inhibition of DPPH free radical, demonstrating a strong radical scavenging activity.
Nutrients, 2020
Metabolic syndrome (MetS) represents a set of clinical findings that include visceral adiposity, insulin-resistance, high triglycerides (TG), low high-density lipoprotein cholesterol (HDL-C) levels and hypertension, which is linked to an increased risk of developing type 2 diabetes mellitus (T2DM) and atherosclerotic cardiovascular disease (ASCVD). The pathogenesis of MetS involves both genetic and acquired factors triggering oxidative stress, cellular dysfunction and systemic inflammation process mainly responsible for the pathophysiological mechanism. In recent years, MetS has gained importance due to the exponential increase in obesity worldwide. However, at present, it remains underdiagnosed and undertreated. The present review will summarize the pathogenesis of MetS and the existing pharmacological therapies currently used and focus attention on the beneficial effects of natural compounds to reduce the risk and progression of MetS. In this regard, emerging evidence suggests a p...
2013
Background: Statins are the most commonly prescribed drugs to reduce cardiometabolic risk. Besides the wellknown 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.
Scientific Reports, 2020
There is a need for continued drug development for nonalcoholic steatohepatitis (NASH). Bergamot is a plant whose fruit juice is enriched with flavonoids and phenolic compounds which improves dyslipidemia and markers of systemic inflammation in patients with Metabolic Syndrome. The aim of this study was to perform a preclinical “proof of concept” study of Bergamot polyphenolic formulation (BPF99) for the treatment of NASH. A disease reversal study was performed in the diet-induced animal model of NAFLD (DIAMOND). Groups of 8 weeks old mice were randomly assigned to receive chow diet, high fat diet with sugar in drinking water (Western diet- WD). Mice on WD were further randomized to continue on WD gavaged with vehicle or continue on WD with additional gavage of BPF99 (50 mg/kg) after 16 weeks of diet. Mice were euthanized after 11 additional weeks. The primary endpoint was resolution of NASH. Secondary endpoints included changes in individual histological features, body weight, live...