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United States Department of Agriculture

Agricultural Research Service

Title: Strategies for the Discovery of Bioactive Phytochemicals

Authors
item Duke, Stephen
item Rimando, Agnes
item Dayan, Franck
item Canel, Camilo
item Wedge, David
item Tellez, Mario
item Schrader, Kevin
item Smillie, Troy - UNIV. OF MS
item Paul Jr, Rex
item Duke, Mary

Submitted to: Book Chapter
Publication Type: Book / Chapter
Publication Acceptance Date: December 1, 1999
Publication Date: N/A

Interpretive Summary: This book chapter describes modern strategies for discovery of bioactive pytochemicals that can be used in agriculture or medicine. The use of ethnobotanical, chemical ecological, and anatomical approaches to identify likely plant species sources of compounds is detailed. How informatics, microbioassays, and modern chemical instrumentation are used to identify specific chemical compounds is described.** Leslie A. Weston from Cornell University is author #8.

Technical Abstract: Plants synthesize a wide diversity of secondary products, many,if not most, of which have yet to be identified. Although massive effort has been expended on chemical elucidation of these compounds, there has been comparatively little research to determine their biological activities. Discovery of those compounds with useful biological activities can be approached as a random walk through the chemistry of the plant kingdom, or strategies can be employed to maximize research efforts. Ecological and ethnobotanical clues have been very useful in identifying plant species as likely sources of phytochemicals, as well as in suggesting medicinal and agricultural uses. After a species is identified, anatomical clues can be helpful in determining the location of compounds of interest within the plant. Many bioactive secondary compounds are secreted or sequestered within specialized structures or cells to protect the producing plant from autotoxic injury. Examinaton of the compounds secreted by the plant into the soil, its resin canals, or onto plant surfaces can accelerate the discovery of bioactive molecules. Similarly, highly bioactive compounds often accumulate in trichomes and trichome-like structures. Examples of anatomical localization of bioactive compounds by plants discussed in this chapter include sorgoleone and its analogues from Sorghum species, artemisiniin from Artemisia annua, and hypericin from various Hypericum species. Anatomical localization may also sometimes suggest the type of biological activities compounds may have.Perhaps the most costly aspect of natural product discovery has been the wasted effort in the rediscovery of known compounds.Use of informatics and modern analytical instrumentation such as LC-MS/MS and LC-NMR can minimize this aspect of dereplication.

Last Modified: 7/28/2014
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