Chemistry Reference
In-Depth Information
THE OVERVIEW OF STUDIES
ON HUPERZINE A: A NATURAL
DRUG FOR THE TREATMENT
OF ALZHEIMER'S DISEASE
D
A
-Y
UAN
Z
HU
,C
HANG
-H
ENG
T
AN
,
AND
Y
I
-M
ING
L
I
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica,
Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai, China
4.1
INTRODUCTION
4.1.1
Powerful AChEI Originated From Traditional Chinese Medicine
Traditional Chinese medicine (TCM) has a long history of serving people, which
tends to raise the natural defenses of the organism instead of trying to restore its nat-
ural functions. The accumulated clinical experience inspired the search for new drugs
in modern times. Huperzine A (HA, 1) is one successful example of this continuum.
HA is a natural-occurring alkaloid that was isolated from Chinese medicinal
herbs, Qian Ceng Ta [Huperzia serrata (Thunb.) Trev.
¼
Lycopodium serratum]
and its related genera by Chinese scientists in the early 1980s.
1,2
Pharmacological
studies in vitro and in vivo demonstrated that HA was a potent, selective, and rever-
sible acetylcholinesterase inhibitor (AChEI), which crosses the blood-brain barrier
smoothly and shows high specificity for AChE with a prolonged biological half-
life.
3-5
It has been approved as a drug for the treatment of Alzheimer's disease
(AD) in China. Because the isolation and use of HA was released without patent
protection, it is sold in the United States as a dietary supplement. Several review
articles for the research progress in the chemistry, pharmacology, structural biology,
and clinical trials of HA have been published within the last 10 years.
4-10
This
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