Reported May 25, 2011
The Natural Pain Killer
(Ivanhoe Newswire) – For the first time scientists have accomplished a laboratory synthesis of a rare natural product isolated from the bark of a plant widely employed in traditional medicine. This advance may provide the scientific foundation to develop an effective alternative to commonly prescribed narcotic pain treatments.
The study defines a chemical means to access meaningful quantities of the rare natural product conolidine. Based on data from mouse models, the study also suggests that synthetic conolidine is a potent analgesic as effective as morphine in alleviating inflammatory and acute pain, with few, if any, side effects.
In recent years, there has been significant interest in developing alternatives to opiate-based pain medications such as morphine. While widely prescribed for pain, morphine has a number of adverse side effects that range from the unpleasant to the lethal, including nausea, chronic constipation, addiction, and breathing depression.
Once the synthesis was complete, research shifted to pharmacology for evaluation. The pharmacological assessment, performed in the laboratory of Scripps Florida Associate Professor Laura Bohn, showed that the new synthetic compound has surprisingly potent analgesic properties.
"Her pharmacological studies confirmed that while it's not an opiate, it's nearly as potent as morphine," Glenn Micalizio, an associate professor in the Department of Chemistry, who initiated and directed the study, was quoted as saying.
In various models of pain, the new synthetic compound performed spectacularly, suppressing acute pain and inflammatory-derived pain, two key measures of efficacy. Not only that, but the new compound passed easily through the blood-brain barrier, and was present in the brain and blood at relatively high concentrations up to four hours after injection.
"While the pain-relieving properties are encouraging, we are still challenged with elucidating the mechanism of action," Bohn said. "After pursuing more than 50 probable cellular targets, we are still left without a primary mechanism."
"The lack of side effects makes it a very good candidate for development," Bohn said. "On the other hand, if there were side effects, they might provide additional clues as to how the compound works at the molecular level."
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SOURCE: Nature Chemistry, May 23, 2011
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