Cholesterol Control: Bergamot, Berberine, and Amla May Help

June 5, 2013

Imbalanced blood fat levels—including elevated total and LDL cholesterol—continue to plague westernized civilizations as well as those increasingly adopting western dietary practices. As we know, these are significant risk factors for coronary heart disease, heart attack, and stroke.

High LDL cholesterol levels are a major risk factor for atherosclerosis because LDL cholesterol molecules are highly prone to oxidation. Oxidation causes molecules to structurally modify and become more likely to stick to the walls of blood vessels, particularly those of the heart and brain, contributing to the formation of plaque. This plaque can cause the narrowing of arteries, while also making them less flexible. In this event, circulating clots are more likely to get stuck in these narrowed blood vessels, leading to heart attack and stroke.

According to 2011 Centers for Disease Control and Prevention (CDC) estimates, more than one in three American adults has elevated LDL cholesterol, while nearly 14% of Americans have high total cholesterol, putting them at a doubled risk of heart disease compared with those individuals with optimal cholesterol levels.

Primary treatment with statin medications has served to effectively address elevated total cholesterol and LDL levels in many individuals; however, statin therapy is not without its risks. Recent studies point to factors such as increased blood sugar levels and possibly type 2 diabetes, particularly in women using statin drugs (Journal of the American College of Cardiology, 2012). Moreover, there are a number of treated patients who are statin intolerant for various reasons, including because of risks associated with nutritional deficiencies caused by or aggravated by statin drugs (Journal of Postgraduate Medicine, 2011). Beyond this, individuals with metabolic syndrome often are unable to achieve their lipid reduction goals with statins alone (The American Journal of Cardiology, 2008).

With the continued prevalence of cholesterol imbalances and the problems associated with statin use in many individuals, it’s fortunate that there are viable alternatives in the realm of therapeutic nutrition that are effective and inherently have a high level of safety. Recent studies in this area have shown promising results with a number of novel botanical extracts that have long been used in traditional systems of medicine. This research shows impressive benefits for lowering total cholesterol and LDL cholesterol levels, along with significantly improving several other heart health parameters.

Bergamot Polyphenols

The Bergamot orange (Citrus bergamia) is a yellow-colored citrus fruit the size of a lemon mainly grown in the southern Calabria region of Italy. It is distinct from other citrus fruits based on its unique profile and high concentration of flavonoids and flavonoid glycosides. Preliminary cell-based and animal research studies have shown several of these flavonoids to possess anti-atherosclerotic properties, including the ability to inhibit LDL oxidation. Some also have structural similarity to the natural substrate of the HMG-CoA reductase enzyme, which is the major target of statin drugs. Inhibiting this enzyme’s function serves to decrease cholesterol synthesis.

A recent study by Vincenzo Mollace and colleagues in Italy (Fitoterapia, 2011) investigated the effect of bergamot extract high in polyphenols, in both rats and humans. In rats with diet-induced hyperlipidemia, 10 and 20 mg/kg of bergamot polyphenols orally administered daily for 30 days led to significant reductions in total cholesterol, LDL, and triglycerides, with moderate elevations in HDL cholesterol levels seen compared to rats fed the hypercholesterolemic diet alone.

The human study was conducted as a randomized, double-blind, placebo-controlled trial consisting of 237 patients with high cholesterol levels (104 patients with isolated hypercholesterolemia/LDL levels greater than 130 mg/dL) (Group A); 42 patients with elevated cholesterol and triglycerides (Group B); 59 patients with high cholesterol, triglycerides, and blood sugar (Group C); and a final group of 32 patients classified as post–statin therapy who had stopped simvastatin due to musculoskeletal and liver adverse effects (Group D). Each of the above groups was divided into three subgroups. One subgroup received 500 mg of bergamot polyphenols per day; the second received 1000 mg/day; the third group received placebo. The post–statin therapy group received 1500 mg of bergamot polyphenols per day after a 60-day statin washout period. All patients were treated for 30 days.

In aggregate, groups A, B, and C showed an average reduction in total cholesterol of 21.8% and LDL cholesterol of 24.1% and an increase in HDL levels of 22.3% with 500 mg/day. The group taking 1000 mg/day of bergamot polyphenols saw reductions of 29.4% and 36.0% in total cholesterol and LDL, respectively, while achieving an increase in HDL levels of 40.1%. All parameters in the placebo group were essentially unchanged from baseline. In the post-statin group, there was a 25.0% reduction in total cholesterol, 27.6% decrease in LDL levels, and a 23.8% increase in HDL—with none of the side effects seen earlier with statin therapy in this group. Based on these results, the bergamot polyphenols proved to be an effective therapeutic intervention for elevated cholesterol levels as well as a safe and beneficial alternative for individuals intolerant to statin drugs.