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Synthesis and Biological Evaluation of a New Series of Berberine Derivatives as Dual Inhibitors of Acetylcholinesterase and Butyrylcholinesterase by Ling Huang; Zonghua Luo; Feng He; Jing Lu; Xingshu Li is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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A series of novel berberine derivatives were designed, synthesized, and biologically evaluated as inhibitors of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Among these derivatives, compound 48a, berberine linked with 3-methylpyridinium by a 2-carbon spacer, was found to be a potent inhibitor of AChE, with an IC 50 value of 0.048 lM and compound 40c, berberine linked with 2thionaphthol by a 4-carbon spacer, acted as the most potent inhibitor for BuChE with an IC 50 value of 0.078 lM. Kinetic studies and molecular modeling simulations of the AChE-inhibitor complex indicated that a mixed-competitive binding mode existed for these berberine derivatives.

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Author

Ling Huang; Zonghua Luo; Feng He; Jing Lu; Xingshu Li

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2010

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)