Researchers at the Georgia Institute of Technology, in collaboration with colleagues at Mercer University, have developed what are believed to be the first orally active selenium-based antihypertensive compounds.
Beyond their potential value in treating high blood pressure, the phenylaminoalkyl selenide compounds could also point the way toward other selenium-based therapeutic agents -- and help expand knowledge of the role this trace element plays in human health.
Development and testing of the patented compounds, which have been studied so far only in animals, are reported in the November issue of The Journal of Pharmacology and Experimental Therapeutics.
"We think our antihypertensive compounds are the first in which biological activity is a consequence of the unique chemistry and biochemistry of selenium," explained Dr. Sheldon W. May, Regents' Professor in Georgia Tech's School of Chemistry and Biochemistry. "We look at this as a paradigm for understanding selenium's chemistry and biochemistry and using that knowledge to incorporate selenium into rationally designed molecules that could have therapeutic potential for many different applications."
Researchers Use Rational Drug Design Techniques
Using rational design techniques, the research team developed a series of derivatives based on their original selenium-based antihypertensive compound. The derivatives were designed to minimize absorption into the central nervous system and to resist damage from enzymes in the gastrointestinal tract.
The biochemistry and pharmacology of selenium are subjects of
intense current interest because of evidence that a deficiency of the
trace nutrient may play a role in diseases as diverse as cancer, heart
disease, arthritis and AIDS. Selenium is an
Contact: John Toon
Georgia Institute of Technology Research News