Huperzine A

Abstract

Huperzine A is obtained from Huperzia serrata, which is a highly effective and selective reversible inhibitor of acetylcholinesterase. It shows ability to improve learning and memory and was approved for treatment in Alzheimer's disease (AD) in China in 1996. The low efficiency (only about six ten thousandths) of extraction of huperzine A from Huperzia serrata and the complexity of the full synthesis and structure modification of huperzine A limit its large-scale development and utilization. ZT-1, a derivative of huperzine A, was found to be with similar AChE inhibitory activity and lower butyrylcholinesterase inhibitory activity and toxicity compared with huperzine A. It can go through the blood-brain barrier, and its oral bioavailability and duration of action are comparable with huperzine A. ZT-1 is a promising anti-AD drug and has approved patents in China, America, Japan, and Europe.