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Pure Appl. Chem., 2007, Vol. 79, No. 12, pp. 2269-2276

Glutathione S-transferase- and acetylcholinesterase-inhibiting natural products from medicinally important plants*

Athar Ata, Stephanie A. Van Den Bosch, Drew J. Harwanik and Grant E. Pidwinski

Department of Chemistry, The University of Winnipeg, 515 Portage Ave., Winnipeg, MB R3B 2E9, Canada

Abstract: Naturally occurring enzyme inhibitors play an important role in a drug discovery program. Glutathione S-transferases (GSTs) play a significant role in the detoxification and metabolism of many xenobiotic and endobiotic compounds. GSTs are considered to be responsible for decreasing the effectiveness of anticancer/antiparasitic agents used for the treatment of cancer and parasitic diseases. The effectiveness of these biomedical agents may be improved by using GST inhibitors as an adjuvant during chemotherapy. Acetylcholinesterase (AChE) inhibitors have potential applications in curing cardiac problems and Alzheimer's disease. This article describes the identification of natural products exhibiting GST and AChE inhibitory activities, from medicinally important plants. Results obtained from the structure-activity relationship (SAR) studies of some of these newly discovered enzyme inhibitors are also discussed.
*Invited contribution to a collection of papers for the IUPAC project 2005-042-1-300 "Chemistry for Biology". Other contributions to the project are published in this issue, pp. 2179-2366.