UAH

Natural Products Drug Discovery

 The UAH Natural Products Drug Discovery Group is a collaboration between faculty members in the Departments of Chemistry and Biological Sciences. The group is interested in tropical rainforest plants as sources of new drugs. The group consists of Dr. William Setzer, a phytochemist and Professor of Chemistry, Professor Bernhard Vogler, a phytochemist and NMR spectroscopists, Professor Debra Moriarity, a biochemist in the Biological Sciences Department, and Professor Robert Lawton, a tropical rainforest ecologist in the Biology Department.

With funds from the National Institutes of Health, members of the group are using their experience in plant biochemistry and ecology to find and harvest medicines from tropical rainforest plants. Drs. Setzer, Vogler, Moriarity, and Lawton and the Natural Products Drug Discovery Group have been studying tropical plants for over ten years – rainforest plants from Costa Rica, tropical Australia, and Abaco Island, Bahamas. The Group currently has field laboratories located in Monteverde, Costa Rica, and Marsh Harbour, Abaco, Bahamas.  In addition, the Group collaborates with investigators from the University of Ibadan, Nigeria, and National University of Science and Technology, Bulawayo, Zimbabwe.

The UAH Natural Products Drug Discovery Group has been looking for new anticancer drugs, new antimicrobial agents, and new antiparasitics. They have recorded a “hit rate” of over 30% (a hit being the discovery of a plant that appears to have interesting biological properties).  Extracts that show potential medicinal utility are subjected to bioactivity-directed fractionation and isolation. The structures of the active components are then elucidated using spectroscopic and crystallographic techniques.

In earlier times, all drugs and medicinal agents were derived from natural substances, and most of these remedies were obtained from higher plants. Today, many new chemotherapeutic agents are synthetically derived, based on “rational” drug design. The study of natural products has advantages over synthetic drug design in that it leads optimally to materials having new structural features with novel biological activity. Not only do higher plants continue to serve as important sources of new drugs, but phytochemicals derived from them are also extremely useful as lead structures for synthetic modification and optimization of bioactivity. The starting materials for about one-half of the medicines we use today come from natural sources. Virtually every pharmacological class of drugs includes a natural product prototype. The future of higher plants as sources of medicinal agents for use in investigation, prevention, and treatment of diseases is very promising.

 

The group must travel to exotic tropical locations around the world (such as Costa Rica, Australia, Bahamas) to collect plant materials:

rainforest1   rainforest2


Plant materials, leaves or bark, are then chopped and dried:

girls-working   drying


The dried plant materials are extracted with organic solvents:

extracting


The crude plant extracts are brought back to UAH for biological screening (for antimicrobial, antiviral, and antitumor activity):

screening

micro1   micro2


Active extracts are subjected to bioactivity-directed chromatography to isolate the active components:

chroma1   chroma2


The biologically active materials are purified and identified using spectroscopic or crystallographic techniques.  NMR studies are carried out in collaboration with the UAH Biomolecular NMR Laboratory; X-ray crystallographic studies are carried out in collaboration with the Laboratory for Structural Biology at UAH.

lab1   lab2


If you would like to participate in this exciting area of research, contact Dr. Setzer.

Click here if you are interested in learning more about field research in Monteverde, Costa Rica.