Progress in clinical, pharmacological, chemical and structural biological studies of huperzine A: a drug of traditional chinese medicine origin for the treatment of Alzheimer's disease.
HupA is a potent, reversible AChEI, which crosses the blood-brain barrier smoothly, and shows high specificity for AChE with a prolonged biological half-life. It has been approved as the drug for the treatment of AD in China, and marketed in USA as a dietary supplement. HupA has been the subject of investigations by an ever-increasing number of researchers since 1980's. In the last four years, HupA has been further studied in many aspects such as the chemical synthesis, structural modification, structure-activity relationship, various biological effects, and mechanisms of action. A number of papers dealing with the computational modeling and X-ray crystallographic studies of HupA-AChE complex have also been published. This review represents a comprehensive documentation of the progress in the studies on HupA during the period of 1999-2002.
Jiang
Hualiang
H
Drug Discovery and Design Center, and State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Zhangjiang Hi-Tech Park, Shanghai 201203, China.
Luo
Xiaomin
X
Bai
Donglu
D
D000470:Alkaloids; D000818:Animals; D002986:Clinical Trials as Topic; D018360:Crystallography, X-Ray; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D018696:Neuroprotective Agents / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D012717:Sesquiterpenes / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D000470:Alkaloids; D018696:Neuroprotective Agents; D012717:Sesquiterpenes; C050426:huperzine A