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, ProfessorDebra
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, Moriarity, and Lawton and the Natural Products Drug Discovery
Group have been studying tropical plants for over ten years---rainforest
plants from Costa
Rica as well as tropical Australia.
The Group currently has field laboratories located in Monteverde, Costa
Rica, and Paluma, North Queensland, Australia.
The UAH Natural Products Drug Discovery Group has been looking for new anticancer drugs, new antibacterial agents, and new antivirals. 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:
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Plant
materials, leaves or bark, are then chopped and dried:
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The
dried plant materials are extracted with organic solvents:
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The
crude plant extracts are brought back to UAH for biological screening (for
antimicrobial, antiviral, and antitumor activity):
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Active
extracts are subjected to bioactivity-directed chromatography to isolate
the active components:
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The
biologically active materials are purified and identified using spectroscopic
or crystallographic techniques. X-ray
crystallographic studies are carried out in collaboration with theLaboratory
for Structural Biology at UAH.
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If you would like
to participate in this exciting area of research, contact Dr.
Setzer.
Clickhere if you are interested in learning more about field research in Monteverde, Costa Rica.
Return
to William Setzer's Home Page
August,
2000