Huperzine A, A Potential Therapeutic Agent for Treatment of Alzheimer's Disease

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 Alzheimer s disease.

Cholinergic Treatments with Emphasis on M1 Muscarinic Agonists as Potential Disease-Modifying Agents for Alzheimer's Disease

“…33 In addition to the Food and Drug Administration-approved AChE-Is, several other such inhibitors at various stages of research and development have been reported. These include compounds such as: phenserine, 34,35 CHF2819, 36 TAK147, 37 TV3326, 38 huperzine A and analogs, 39 NP-61, 40 and Memoquin. 41 Preclinical studies showed that some of these newer AChE-Is may have additional properties versus the existent AChE-Is prescribed drugs that may enhance their putative therapeutic value in AD treatment.…”

A Current Understanding of Alzheimers Disease and the Prospects of Phytopharmacological Intervention as a Management Strategy

“…It has been shown to contain an extract Huperzine A (HupA). It is known to be a selective inhibitor of acetylcholine esterase with significant pharmacodynamics and kinetic properties in the brain demonstrated in animal studies [65]. It has long half-life and tolerance with few cholinergic side effects [65].…”

Study of the interaction of Huperzia saururus Lycopodium alkaloids with the acetylcholinesterase enzyme

“…However, the order of the binding energies was the same as that expected on the basis of the experimental values of IC 50 . [83] a Experimental values of IC 50 are informed in M. These values were determined according to the Ellman method, [50] with some modifications, as described in the experimental section.…”