Nutraceuticals and Human Health

The Food-to-supplement Paradigm

Paul A Spagnuolo, Alejandro G Marangoni

• Publisher: Royal Society of Chemistry
• Year: 2020
• ISBN:
  9781839160585
• Edition: 1
• Topic: Medicine
• Subtopic: Nutrition, Dietics & Bariatrics

Nutraceuticals is a broad umbrella term used to describe any product derived from food sources with extra health benefits in addition to the basic nutritional value found in foods. This book is a comprehensive look at two themes in the area: technical and biological considerations. Technical considerations include an in-depth look at the process of bioactive identification and extraction and factors controlling bioactive concentrations in food. It also includes details of how these products are regulated and the steps necessary to utilize these products in human populations. Biological considerations include looking at how these products can be used in the prevention and treatment of chronic diseases, and a discussion on the process of formulations and how these influence bioavailability.

This will be the first book to comprehensively examinethe entire process of nutraceutical development from food to supplement creation and all the important considerations in between. This serves as an excellent and up-to-date reference for food scientists, food chemists, researchers in nutraceuticals and human nutrition.

CHAPTER 1

Nutraceuticals

PAUL A. SPAGNUOLO

Department of Food Science, University of Guelph50 Stone Rd., Guelph Ontario, Canada N1G2W1

Email: [email protected]

1.1 Introduction

Food-derived bioactive compounds are commonly referred to as nutraceuticals (in Canada) or dietary supplements (in the United States (US)). They are defined primarily by two features: (1) their ability to impart cellular or physiological effects and (2) their form, which is independent of the conventional product in which they are found (i.e., as a powder or pill). In the US, dietary supplements are classified as foods and regulated by the Dietary Supplements Health and Education Act (DSHEA); while in Canada, they are defined under the umbrella of natural health products (NHPs) and are regulated as a subset of drugs under the Natural and Non-prescription Health Products Directorate (NNHPD). They are recognized as self-care products, making them available over-the-counter and considered safe for use without direct oversight of a health care practitioner. With this accessibility and consumers’ desire to improve their own health care, patients frequently consume these products.

Nutraceutical was a term first coined in 1989 and is a hybrid word derived from nutrition, which is the science of food and nutrient effects on the body, and pharmaceutical, which is a compound manufactured for medical purposes. Health Canada defines nutraceuticals as “a product isolated or purified from food that is sold in a medicinal form that is not associated with food and is demonstrated to have a physiological protective effect against chronic disease”.¹ Interestingly, this definition omits the utility of these products as potential therapeutics for disease. While the debate rages over the quality of the scientific evidence, which is commonly misinterpreted by media and overstated by corporations that market these products, undoubtedly there is a place for “bioactive molecules with demonstrated physiological benefit” (i.e., words directly extracted from Health Canada's definition) for use as disease therapeutics. The medical research and/or regulations simply need to catch up with consumer demand for these compounds.

1.2 Nutraceuticals for Deficiency

The National Institutes of Health (NIH) recommends that if you do not eat a variety of nutritious foods, then “some supplements might help you get adequate amounts of essential nutrients”.² They further state, before recommending following the food guide, that “supplements can't take the place of the variety of foods that are important to a healthy diet”. Indeed, a general belief exists that supplementation is only useful in periods of deficiency and, historically, there is no denying this observation. Vitamins C or D to prevent scurvy or rickets, respectively, are classic examples of the utility of nutrition to prevent disease. Similarly, folic acid supplementation to prevent spina bifida has been implemented with great success; however, it should be noted that supplementation recommendations are implemented because fewer than 1 in 3 women of child-bearing age consume the recommended dose.³ These are clear examples of how supplementation can prevent diseases in vulnerable populations, but can bioactive molecules be used to prevent or treat chronic disease in populations that are not vulnerable? Does an invulnerable population actually exist?

1.3 Why are Nutraceuticals Needed?

Humans require food to survive and our evolutionary history is filled with agricultural advancements that have resulted in the stable production of food free from harmful pathogens. These successes, however, have paradoxically come at a cost of these processed foods being of lower nutritional quality. For example, whole grains such as wheat and rice contain three layers: bran, endosperm and germ. The bran layer is comprised of minerals and B-vitamins, which are important enzymatic co-factors, and fiber-rich materials, which provide physiological benefits ranging from improving digestion, regulation of cholesterol and glucose absorption. The germ layer consists of phytochemicals, B-vitamins and vitamin E whereas the endosperm consists primarily of carbohydrates and proteins. With the advancement of agriculture, development of new preparation and storage techniques, and the advent of the industrial revolution, whole grains became highly processed. Milling separates the bran and germ leaving behind only the endosperm. Further refinement results in a powder (i.e., flour) that is suitable for long-term storage and can, in-turn, be used to create a wide range of products. However, during that process, all of the fiber is lost and between 70 and 80% of the vitamins are also lost.⁴ This drastic reduction in nutritional quality has resulted in flour being fortified with B-vitamins;⁵ calcium and iron may also be added as a means of increasing the nutritional value of flour-based products. This classic example demonstrates how processing alters nutritional quality and has directly resulted in the need to re-introduce bioactive food compounds. While fortification has become the solution to maintain the nutritional value of wheat, other products that undergo similar processing may not be as fortunate. Moreover, highly processed and foods of convenience, which make up nearly half of our daily total caloric intake, further add to the diminished quality of the food supply.⁶ Couple processing with the drastic alterations in the diversity of our food supply that has favored, instead of more nutritional varieties, cultivars resistant to fluctuations in growing conditions and that better survive harvesting, storage and transport, and the overall quality of our food supply is diminished.

Food guides are created by governments with the intention of improving population health and minimizing disease. Offering guidance on appropriate food selection choices, these documents are common across the globe (Table 1.1). However, whether the population believes in or follows the guide is debatable. A 2019 Canadian survey showed that only 49% of people believe that the food guide is an important document and 52.4% say that they face barriers, including economic and cultural, in following the guide. This calls into question whether these expert recommendations are practiced, which can greatly impact the overall health of the population. While increases in chronic disease burden is not the ideal indicator to link disease onset with a lack of adherence to a food guide, it certainly speaks to the health, or lack thereof, of the global population.

Table 1.1 Global distribution of countries with a food guide.

Continent	Countries with a food guide (%)
North America	87
South America	67
Africa	11
Europe	61
Australia and Oceania	14
Asia	35

Together, these examples show that a diminished quality of the food supply and general non-compliance with expert recommendations of following food guides are contributing factors leading to poor population health that likely drive consumers toward the use of supplements.

1.4 Supplement Use

According to a recent survey, nutraceuticals are consumed mainly to “improve” or “maintain” health.⁷ Whether this is: (1) to combat the reduced quality of the processed food supply, (2) a result of a more health-conscious consumer, (3) a result of a booming global billion-dollar supplement industry, or (4) a combination of all three, nutraceuticals are popular compounds consumed by 70–75% of the population. Moreover, and far more concerning, is the alarming statistic that up to 69% of prescription drug users did not report dietary supplement use to their physician.⁸ As such, regardless of your position on the value of these products, they are readily available and consumed with great frequency.

Nutraceuticals fall under the broader category of NHPs, which is a global industry estimated to grow to over $360 billion (USD) by 2020. Natural products, which have contributed greatly to medicine, are derived from various sources including microbes, marine organisms, food and terrestrial plants. From 1981 to 2014, approximately 51% of all Food and Drug Administration (FDA)-approved drugs were natural products or their derivatives. Morphine was originally isolated from opium resin and quinine from the chincona tree. Indeed, acetylsalicylic acid (ASA), better known as aspirin, is a chemical modification of salicin, which was originally derived from the bark of the willow tree. Among the 141 approved anti-bacterial agents, 73% are derived from natural products.^9,10 Further, 83% of the FDA-approved chemotherapeutics are from natural sources.⁹ Among these are paclitaxel and irinotecan, which are the cornerstones of many solid tumor drug regimens and were originally isolated from the bark of the Pacific yew and trees of the Camptotheca genus, respectively. In addition, nucleoside analogues such as cytarabine and decitabine, which are used to treat hematological malignancies, are synthesized to mimic structures found in marine sponges. Natural products also influence the discovery of new molecular entities (NMEs), making up 38% of the FDA-approved NMEs and 22% of approved drugs in 2014.^9,10 It is evident that research on natural products has been and continues to be essential in drug discovery, a fact typically overlooked by critics of natural product research.

1.5 Product Development Considerations

Up to this point, we have focused mainly on the finished product. However, in the process of nutraceutical development (Figure 1.1), there are many steps that can drastically change the nature and quality of the final product. While the final product dictates the clinical findings that determine the overall value and claims that can be made, final product variability is dependent on several factors. The nature and quality of the starting material (see Chapter 3), the nature of the extraction process (see Chapter 4) and methods used to formulate (or encapsulate) the product (see Chapter 6), all together determine the concentration and structural integrity of the bioactive within the final product. Without taking these factors into consideration, questions about quality as they pertain to standardization, dosing, stability, bioaccessibility and bioavailability of the bioactive can easily be overlooked. As outlined within several chapters of this book, all of these factors must be first considered when determining the value of the final product, as each can impact the safety and efficacy of the nutraceutical.

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Table of contents

• Cover
• Title
• Copyright
• Preface
• Dedication
• Contents
• Chapter 1 Nutraceuticals
• Chapter 2 Regulation of Nutraceuticals in Canada and the United States
• Chapter 3 Effects of Growing Conditions on Plant Medicinal Bioactives
• Chapter 4 Extraction Technologies for Plant-derived Nutraceuticals and Natural Health Products
• Chapter 5 Analytical Approaches for Characterization of Bioactives in Plant-based Natural Health and Food Products
• Chapter 6 Encapsulation of Nutraceuticals
• Chapter 7 Coffee and Solid Tumors
• Chapter 8 Nutraceuticals in Hematological Malignancies
• Chapter 9 Nutraceuticals as Metabolic Modulators for the Treatment of Obesity and Associated Diseases
• Chapter 10 Nutraceuticals in Neurodegenerative Diseases
• Chapter 11 Probiotic Supplements – Basic Concepts of the Gut Microbiome and the Role of Probiotics to Sustain Health
• Chapter 12 Clinically-relevant Herb–Drug Interactions: Current Status and Practical Considerations
• Subject Index