Discovering Active Food & Nutraceutical Ingredients

Systematic screening may lead to the discovery of new food and nutraceutical actives and indications.

By Joerg Gruenwald

The food and nutraceutical markets are hungry for new active ingredients with proven efficacy, be they from known food sources or from newly discovered ethnic foods or traditional herbal remedies. Some of the challenges include finding these new active ingredients and then isolating, characterizing and patenting them for international marketing. This requires an adequate discovery platform capable of fractionizing and screening large amounts of material.

Historically, most active food ingredients were established after discovering their physiological effects, e.g. the health-promoting effects of soy in Asia were well-described before the effects of isoflavones and soy proteins were discovered in great detail. In the area of herbal medicine, many effects of medicinal plants were described thousands of years ago, and only during the last several decades have active ingredients been discovered, described and characterized. Today it is also commonplace for consumers to use supplements, herbal medicines or functional foods to support their general health, mental state and immune system, or to reduce cholesterol or protect the body from free radicals, which is why the search for new active ingredients derived from natural products is of high interest to many companies worldwide.

Systematic Screening

The pharmaceutical industry has been using a systematic screening approach for years. In fact, several new pharmaceutical compounds from botanical origins have been found in the large biodiversity of the plant kingdom worldwide. Until recently, however, this systematic research platform has never been used to actively search for new active food and nutraceutical ingredients. By combining creativity and strategic business, one major pharmaceutical company has created a new opportunity using a systemic screening platform.

Like many other pharmaceutical companies, Bayer used to possess a large natural products research unit that collected and screened thousands of plants from around the world for the purpose of identifying pharmaceutical targets that could be developed into synthetic drugs. Today, InterMed Discovery GmbH (IMD) is a privately held company, which originated as a Management Buy Out from Bayer HealthCare AG. This company uses its expertise to create new business models and innovative products based on its screening database, research platform and knowledgebase.

The team at IMD, which is based in Dortmund, Germany, is now actively working with food and food ingredient companies, in addition to cosmetic and cosmetic ingredient companies.

The most attractive aspect of this company is its ability to create intellectual property (IP), which is very difficulty to do in the natural products arena. For one thing, for most natural product sources—whether this includes fruits/vegetables, fungi or other plants with some known effects—numerous publications, textbooks, original literature describing the pharmacological or physiological activities of these sources and their ingredients already exist. So none of these effects can be subject of a patent claim. While technological patents can be applied, they are much weaker than a specific use patent for a specific application, compound and usage for a defined plant species.

By combining IMD’s technology platform and already existing data for thousands of plants and other biological sources, several fractions and compounds have undergone intensive screening to determine their biological activities (BIO-PROFILING) in order to discover new health effects that could then be selected and optimally IP-protected.

IMD maintains a unique natural product source collection that allows it to supply ready-to-screen NP test samples either as pure fully characterized compounds (“NatPure” library), almost pure yet non-characterized compounds (“prefrac”) or pre-purified samples (“advanced extracts”) with maximized structural diversity. In this way, known food sources such as cherry, cacao, lemon and grapefruit, etc., can be tested for new indications and usages, yielding their active ingredients as pure substance.

Further, it is possible to uncover new plants or foodstuffs that have certain weight loss, calming or immuno-stimulant properties. This screening system has the capability to deliver new, patentable food plants with those desired effects, including active ingredients as pure substance. In these cases, it is highly probable that an indication patent for the plant in question can be filed.

One can also search for known ingredients (i.e., caffeine) in new plant sources. Such a search will yield new patentable sources for desired ingredients, including the respective active ingredient as a pure substance in totally new plants nobody has looked at until now. Here, too, new indication patents for plants are possible.

In the area of obesity, some 12,000 substances from different biological sources were screened in a sophisticated multi-purpose assay system in order to isolate active components. Five well-defined but structurally different substances were isolated, each of them derived from different plant species, and each being patented already. In vivo investigations have now confirmed the anti-obesity effects of these new food ingredients.

This is just the start of a new area of food research. Many will jump on the bandwagon and use or copy this approach, as it offers a fast and readily protected way to discover new food ingredients.

For the future, expect to see many new IP-protected food and nutraceutical actives coming to a market near you. NW