The boundary between medicine and food is not always clear in many ancient cultures. Many plants have traditionally been used in both culinary and healing practices. Herbs, in particular, have shown this dual functionality. Scientific information on herbal medicines has been limited to exotic plants, and only a few herbal plants native to, or grown in, Canada, such as American ginseng, Echinacea, St. John's wort and feverfew, have been studied. Thorough investigations have not been carried out, and there is a lack of information about native Canadian plants and their potential as medicinal plants, particularly in terms of their chemical composition, biological activity and potential use for disease prevention. Also, from the marketing point of view, many of the existing herbs have only a small niche in the marketplace, so over production and consequent price depression can easily happen, as seen in the ginseng industry. There is obviously a need for multidisciplinary collaboration among herbalists, botanists, chemists and other scientists, since introducing native plants into mass production requires knowledge of environmental impact, genetic variability and the effects of other factors on the bioactive components. This review is intended to introduce the needs, techniques and challenges of such an approach with an emphasis on chemical and biochemical characterizations.