In a new study published in the International Journal of Cardiology, a team of researchers found that bergamot polyphenolic extract, when taken with the popular cholesterol-lowering statin - rosuvastatin, enhanced the potency of the statin therapy. Previous data showed that Bergamonte extract, rich in brutieridine and melitidine has the ability to inhibit HMG-CoA reductase, which catalyzes the rate-limiting step in mevalonate biosynthesis, a key intermediate in cholesterol metabolism.
"For millions of adults living with elevated cholesterol levels (hyperlipidemia), statins are the pharmaceutical protocol to try to lower those levels into healthy ranges," explains Annie Eng, CEO of HP Ingredients. "However, patients with diabetes and metabolic syndrome do not achieve the recommended cholesterol target with statins alone.”
Based on previous research of bergamot, the researchers investigated the occurrence of an enhanced effect of bergamot extract on rosuvastatin-induced hypolipidemic and vasoprotective response in patients with mixed hyperlipidemia.
The 30-day, open-label, parallel group, placebo-controlled study on 77 patients with elevated serum LDL-C and triglycerides was designed. Patients were randomized to either a placebo (control) group, two groups taking rosuvastatin (10 and 20 mg/daily for 30 days), a group receiving Bergamonte extact alone orally (1000 mg/daily for 30 days;) and a group receiving Bergamonte extract (1000 mg/daily given orally) plus rosuvastatin (10 mg/daily for 30 days).
The researchers found that doses of rosuvastatin and Bergamonte reduced total cholesterol, LDL-C, the LDL-C/ HDL-C ratio and urinary mevalonate in hyperlipidemic patients, compared to control group. 1000mg of Bergamonte and 10mg of rosuvastatin has the same effects in reducing total cholesterol and LDL-C. 1000mg of Bergamonte extract showed much better result compared to 10mg of rovustatin in improving HDL-C and reducing triglycerides.
According to the researchers, the addition of 1000mg of Bergamonte extract to 10mg of rosuvastatin significantly enhanced rosuvastatin-induced effects on serum lipid profile compared to 20mg of rosuvastatin alone. This lipid-lowering effect was associated with significant reductions in trigycerides and increase in HDL-C.
In addition, the cholesterol lowering effect was accompanied by reductions of malondialdehyde, and oxyLDL receptor LOX-1, which correlates to the vasoprotective properties in patients with cardiometabolic risk. The effect of Bergamonte extract in combination with rosuvastatin also resulted in an enhanced expression of PKB levels in PMNs of hyperlipemic patients. These suggest a multi-action enhanced potential of Bergamonte extract in patients on statin therapy.
The authors concluded, "These data are in accordance with previous evidence showing that Bergamonte extract possess antilipidemic and vasoprotective effects both in rat models of hyperlipidemia and vascular disease and in hyperlipidemic patients. In addition, there is a significant additive effect of Bergamonte extract with rosuvastatin, an effect consistent with the further reduction seen in urinary MVA as detected in patients after treatment with both Bergamonte extract and lower doses of rosuvastatin."
These findings reflect those of a previous study, in which Bergamonte extract was found to improve lipid profiles through reduction of LDL, trigyclerides and total cholesterol, increasing HDL-C, and reducing blood glucose in 238 patients in 30 days of daily supplementation.
Reference: M. Gliozzi, et al, "Bergamot polyphenolic fraction enhances rosuvastatin-induced effect on LDL-cholesterol, LOX-1 expression and Protein Kinase B phosphorylation in patients with hyperlipidemia" Int J Cardiology, 2013