LA JOLLA, CA January 18, 2011 Using chemical compounds found in a Japanese plant as a lead and the clever application of ultraviolet light, a Scripps Research Institute team has created a unique library of dozens of synthetic compounds to test for biomedical potential. Already, one of the compounds has shown great promise in inhibiting replication of HIV particles and fighting inflammation.
With the report of their work scheduled to appear in the online Early Edition of Proceedings of the National Academy of Sciences this week, the researchers now plan to optimize the compound's pharmaceutical potential so that it can be pursued as a drug candidate.
The plant Hypericum chinense, known in Japan as biyouyanagi, produces beautiful yellow flowers and, as it happens, potent chemical compounds known as biyouyanagins that have already shown promising anti-HIV and anti-tumor activity. That got the attention of K.C. Nicolaou, who holds the titles chair of the Department of Chemistry, Aline W. and L.S. Skaggs Professor of Chemical Biology, and Darlene Shiley Chair in Chemistry at Scripps Research. Nicolaou's interest was also piqued because the plant is from the same family that produces St. John's wort, and the biyouyanagins possess an intriguing molecular architecture.
"It was the perfect recipe for convincing a synthetic chemist to get into the game," said Nicolaou, who spearheaded the project in collaboration with a number of Scripps Research colleagues. "It seemed like there was so much to be discovered."
Best of Both Worlds
Within the biomedical field there are some researchers that argue natural products are the best route to new drug discovery. Others laud the potential of designing completely synthetic drugs. "I belong to both camps," says Nicolaou, because he prefers to start with natural products and then modify them in a variety of ways to create new synthetic products with improved potential. "The po
|Contact: Mika Ono|
Scripps Research Institute