Huperzine A, A Potential Therapeutic Agent for Treatment of Alzheimers Disease

D.   L.   Bai; X.   C.   Tang; X.   C.   He

Abstract

HupA is a potent, reversible and selective inhibitor of AChE with a rapid absorption and penetration into the brain in animal tests. It exhibits memory-enhancing activities in animal and clinical trials. Compared to tacrine and donepezil, HupA possesses a longer duration of action and higher therapeutic index, and the peripheral cholinergic side effects are minimal at therapeutic doses. This review article deals with a comprehensive survey of the progress in chemical and pharmacological studies of HupA including the isolation and structure elucidation, pharmacological actions, total synthesis, SAR studies and the future development of HupA. Recently, it has been reported that HupA could reduce neuronal cell death caused by glutamate. The dual bio-activities of HupA would further enhance its value and potentiality as the therapeutic agent for Alzheimers disease.

Keywords: huperzine A, inhibitor of AChE, revesibile inhibitors if AChE, lycopoduim, HupA, Huperzia serrata, alzheimer s disease, glutamate, dual bio activities, neuronal cell death, structure elucidation, pharmacological actions, total synthesis, SAR studies, donepezil, brain receptor, learning, memory, cyvlohexanedione mono ethylene ketal 10, keto ester, pyridine derivatives, dimethyl 4 oxopimelate, recemic HupA, stereiselective michael aldok reaction, diastereomeric separation, chiral catalyst, natura HupA, enantioselective palladium catalyzed bicycloannulation, structure activity relationships, the anti AChE activities, zusammen together, entgegen, lithium aluminium hydride, enantiomer excess, tetramethylguanidine, rectus, sinister left