Bio-Guided Screening of Terrestrial Natural Products for the Treatment of Parasitic Diseases

Plasmodium falciparum (Malaria) and Trypanosoma brucei brucei (African Trypanosomiasis) are life-threatening diseases that affect half of the world’s population.  These protozoans are very infectious because they are effectively transmitted by insect vectors.  Current drug protocols are administered for extended time periods and patients do not complete them.  These clinical factors along with random parasitic mutations lead to drug resistance. In search of identifying new leads to treat these diseases, we are working on a drug discovery program that utilizes Native American traditional medicinal plants.  In a bio-guided screening assay, fractionated extracts from terrestrial natural products were tested against these parasites.  Biologically active fractions were purified and characterized utilizing column chromatography, UPLC-MS, and NMR techniques. Promising leads as well as our efforts for future structure activity relationship studies will be discussed.