Combinations of botanical extracts for promoting cardiovascular health

Highlights

With societal changes in diet and lifestyle, metabolic diseases in humans have developed rapidly in the last two decades and continue to grow. Similar situations have occurred in companion animals. Although drugs have been developed to manage and treat these emerging problems, side effects (sometimes severe) and efficacy have long been a challenge.

Natural health products are being increasingly considered as an excellent alternative to drugs for the prevention, management and treatment of these metabolic diseases.

The patented technology includes a combination of natural bioactive botanical extracts that provide commercial opportunities for functional foods and nutraceuticals for humans and natural ingredients for pet foods.

The combination results in a dramatic improvement of the blood lipid profile compared to individual extracts provided alone and without the serious side effects associated with some pharmaceutical treatments.

Technology transfer

This technology is available for licensing, or for further development through a collaborative research agreement with NRC. The business opportunity may be referred to by its NRC ID: 11720.

Market applications

  • Functional foods and/or nutraceuticals for humans
  • Functional foods for pet animals.

Abstract

Cardiovascular disease (CVD) is a leading cause of death. Hyperlipidaemia, specifically elevated circulating cholesterol levels, in particular low-density-lipoprotein cholesterol (LDL-cholesterol) levels and high levels of circulating triglycerides, have been established as major risk factors. The present technology includes a combination of natural bioactive botanical extracts which results in a dramatic improvement in the blood lipid profile compared to the individual extracts administered alone, without the serious side effects associated with some pharmaceutical treatments.

Hyperlipidaemia can occur alone but often associate with obesity and diabetes. Accordingly, reversing hyperlipidaemia is highly recommended to patients with one or more of these metabolic disorders. It is projected that by 2020 heart disease and stroke will affect more than 20 million people per year. Global pharmaceutical sales for cardiovascular disease and stroke are estimated at $70B per year. Statin drugs, the leading pharmaceutical product to reduce blood cholesterol, act through suppressing the activity of HMG-CoA reductase. The major drawback of statin or statin-like compounds is the inhibition of the synthesis of an important mitochondrial enzyme called Q10. This is thought to underlie the cause of a number of statin-associated muscle-related myopathies and may underlie other side effects that are dependent on the presence of normal physiological levels of coenzyme Q10. Moreover, there is a significant portion of subjects who respond poorly to statin treatment and need efficacious alternatives to manage their lipid profiles.

The global market for Natural Health Products (NHPs) and Functional Foods (FIs) continues to grow, with sales projected to double from $215B in 2005 to $426B by 2015. In Canada, industry sales have reached $7.6B, fuelled by health-conscious consumers demanding safe and efficacious products. Plant sterols/stanols and their various analogues can also reduce circulating blood cholesterol concentration by inhibiting dietary and biliary cholesterol absorption in the intestine, but the efficacy of sterols/stanols alone is not comparable to statin drugs. Moreover, plant sterols and their analogues have not previously been shown to have any significant effect in reducing serum triglyceride levels.

Berberine, a recently discovered botanical bioactive compound lowers cholesterol levels through increasing cholesterol clearance and/or decreased absorption.

Both plant sterols/stanols and berberine have been studied independently and shown to have good safety profiles in human trials.

The present technology includes a combination of berberine and plant sterols/stanols which act in a synergistic manner to result in dramatic reductions in both cholesterol and triacylglycerols. In vivo trials in hamsters and rats have demonstrated a 42-43% reduction in total cholesterol, 63-66% reduction in non- HDL (including LDL) cholesterol and 37-50% reduction in triglycerides compared to controls, without side effects.

The combination of compounds has also been shown to aid in weight management, reduce liver lipids and weight, offers benefits to diabetes, fatty liver, blood pressure, and liver and kidney functions. The combination could be developed into a natural product for the management of metabolic disorders in humans and companion animals.

The patents have been issued in EU, Canada, and in the USA.

Benefits

  • Lower both blood cholesterol and triacylglycerols
  • Lower blood glucose and improve insulin sensitivity, and protect the liver and kidneys from diabetic related damages
  • Weight and body composition management
  • Prevent or reverse fatty liver
  • A promising NHP product for lipid-lowering, and/or metabolic syndrome

Patents

  • NRC file 11720: Patents issued in Canada, the United States, and Europe.

Contact

Paul Neima
Business Advisor
Telephone: 902-566-7444
Email: Paul.Neima@nrc-cnrc.gc.ca

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