Plants have developed an enormous diversity of secondary products and most of them have evolved to exhibit a certain biological activity, which is useful for survival of the individual plant or species. Since 1000 bc, the Chinese and Indian literatures have described the medicinal use of plants and many recipes are still in use (1-9). Such information from traditional medicine has been used for decades to isolate medicinally active secondary products. These efforts have been very successful and a number of drugs are on the market as a result of this strategy, including plant-derived anticancer compounds such as taxol, docetaxel, and camptothecin. However, despite these successes, the advent of combinatorial chemistry led to decreased interest in natural products. Recently, this trend has changed again, and natural products, including those from plant sources, are now being used as a general source of chemical diversity, which may well complement the chemical structures amenable to total organic synthesis. As by far most plant species have not yet been studied for biologically active secondary products, there is great potential to discover new drugs or lead structures for further development. In addition, modification of secondary product formation by
*Current affiliation'. Graffinity Pharmaceuticals AG, Heidelberg, Germany.
molecular techniques and more extensive use of cell culture technologies may further increase the chances for successful drug discovery from plants.
There are in principle two approaches for drug discovery from plant sources: (1) sourcing using various strategies followed by "random" screening and (2) use of information from traditional medicine on biologically active plant extracts and isolation of the active secondary product(s). As strategy 2 is quite straightforward when the information is available, this chapter focuses on random screening approaches. As an introduction, current industrial strategies and paradigms used for drug discovery in general are described. The reader is referred not only to published papers but also to the Web sites of specialized companies in the particular fields. In addition, several databases, e.g., NAPRALERT, are available for on-line searches (or references) regarding all aspects of natural products.
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