Researchers have made a new compound aspirin that promises to provide the same pain relief as aspirin, but without stomach ache or the risk of kidney damage. The compound described in tomorrow Science , can also help reduce the risk of certain cancers and Alzheimer's disease.
This new "superaspirin" is one of a dozen new compounds under development that soothe joint pain by blocking the activity of an enzyme called COX-2, which promotes the inflammation, pain and fever. The problem with aspirin and nonsteroidal anti-inflammatory drugs (NSAIDs) is that they also interfere with the activity of the COX-1 enzyme, which protects the walls of the stomach and kidneys. Thus, pharmaceutical companies have been eager to find drugs that target only COX-2, especially since epidemiologic and laboratory studies now indicate the long-term use of these drugs may protect against cancer colon and Alzheimer's disease.
At least two companies, Monsanto Corp. in St. Louis, Missouri, and Merck and Co., based in Whitehouse Station, New Jersey, tested COX-2 inhibitors in people and hope to be marketing their new superaspirin next year. "Finally, all these [NSAID] marketing molecules become dinosaurs," predicts Philip Portoghese, a medicinal chemist at the University of Minnesota in Minneapolis.
So far, however, all new inhibitors COX-2 pain relief for only as long as they were attached to the COX-2. But now biochemist Lawrence Marnett at Vanderbilt University school of Medicine in Nashville, Tennessee, and colleagues describe one that works much like aspirin and chemically modifies COX-2, permanently blocking the production of hormones until the body makes more enzyme COX-2.
to build the next generation of these selective inhibitors, Amit and Kalgutkar Vanderbilt Marnett made a molecule which retains original side group acetylated aspirin, aspirin which transfers to the COX-2 enzyme to destroy it. This new molecule also has a carbon ring attached to a sulfur atom, and short chain of carbon atoms which hang sulfur. They found that it could reduce the activity of COX-2 by as much as temporary COX-2 inhibitors exist. Marnett, whose university has patented this class of COX-2 inhibitors permanent, hopes to partner with a pharmaceutical company to come up with a more efficient version of the new superaspirin.
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