Yale researchers synthesize Alzheimer’s compound

By James M. Connolly  Source: MassHightech

Researchers at Yale University report that they have developed the first practical method to synthesize a compound that has been used to treat Alzheimer’s disease and may also be used to combat the effects of chemical warfare agents.

Huperzine A is an enzyme inhibitor that can be extracted from a species of moss found in China. It has been used to treat Alzheimer’s in China since the late 1990s, and has been sold in the U.S. as a dietary supplement to help maintain memory.

According to a report from Yale, the compound can be extracted from the Huperzia serrata plant or can be synthesized in the lab using cumbersome methods. Now, Yale researchers say they can synthesize huperzine A with a simpler eight-step process that produces a yield of 40 percent, compared with only 2 percent yields using earlier methods.

“Being able to synthesize large amounts of huperzine A in the lab is crucial because the plant itself, which has been used in Chinese folk medicine for centuries, takes decades to grow and is nearing extinction due to overharvesting,” said Seth Herzon, the Yale chemist who led the research. The Yale research is described in the Aug. 25 issue of the journal Chemical Science.

Noting that huperzine A can cost up to $1,000 per milligram, Herzon said his team produced several grams of the compound, and that they believe they will be able to drive the cost down to just 50 cents per milligram. A typical dose is expected to be about one milligram per day.

The researchers have partnered with an unidentified industrial firm to produce the compound and to it on a larger scale  and to evaluate the therapeutic potential of huperzine A by conducting clinical trials for several neurological disorders. The Herzon lab and the firm are working with the U.S. Army, which is interested in huperzine A’s potential in blocking the effects of chemical warfare agents, he said, adding that the compound has been shown to protect primates against chemical warfare agents.

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