Huperzine A, a compound isolated from the Chinese Medicinal Herb Qian Ceng Ta, has shown good efficacy in improving the memory in patients suffering from Alzheimer’s Disease. However, despite these promising results, Huperzine A has not been developed as a drug in the West due to scarcity of the natural source, a complicated molecular structure, and the lack of intellectual property protection for this material.
But Virginia Tech researcher Paul R. Carlier, an associate professor of chemistry, has come up with a novel solution to these problems. Working in collaboration with researchers at the Hong Kong University of Science and Technology (HKUST) and the Mayo Clinic, Carlier found that a highly simplified fragment of the Huperzine A molecule could be easily synthesized from cheap, commercially available chemicals.
“Remarkably, the optimum drug obtained by this approach, known as Huperzine A Fragment Dimer, is more than twice as potent as Huperzine A itself,” he reports. “The enhanced potency observed is due to two-point attachment of the dimeric drug to acetylcholinesterase,” he says.
Carlier stresses that all of the tests have been in animals, including a behavioral assay in rats that establishes improved memory. “No work has been done in humans and even if the compounds prove effective in humans, it will be as a treatment of the memory loss in the early stages of the disease,” he says. “This approach could never cure Alzheimer’s and after the disease progresses to a certain point, these drugs could not restore mental function.”
Carlier will present his research at the 220th national meeting of the American Chemical Society Aug. 20-24 in Washington, D.C.