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Showing papers on "Taspine published in 2006"


Journal ArticleDOI
TL;DR: A bioactivity-guided approach was taken to identify the acetylcholinesterase inhibitory agent in a Magnolia x soulangiana extract using a microplate enzyme assay with Ellman's reagent, and suggested ligand 1 to bind in an alternative binding orientation when compared to galanthamine.
Abstract: A bioactivity-guided approach was taken to identify the acetylcholinesterase (AChE, EC 3.1.1.7) inhibitory agent in a Magnolia x soulangiana extract using a microplate enzyme assay with Ellman's reagent. This permitted the isolation of the alkaloids taspine (1) and (−)-asimilobine (2), which were detected for the first time in this species. Compound 1 showed a significantly higher effect on AChE than the positive control galanthamine and selectively inhibited the enzyme in a long-lasting and concentration-dependent fashion with an IC50 value of 0.33 ± 0.07 μM. Extensive molecular docking studies were performed with human and Torpedo californica-AChE employing Gold software to rationalize the binding interaction. The results suggested ligand 1 to bind in an alternative binding orientation when compared to galanthamine. While this is located in close vicinity to the catalytic amino acid triad, the 1−AChE complex was found to be stabilized by (i) sandwich-like π-stacking interactions between the planar aroma...

58 citations


Patent
12 Jul 2006
TL;DR: In this article, a method for preparing for taspine alkali and the applied in preparing for the drug to treat tumor was described, which consisted of dissolving solution, dissolving the cohosh root base, adsorption stripping, preparing for eluent, cleaning, and concave condensation, recrystallizing and checking.
Abstract: The invention relates to a method for preparing for taspine alkali and the applied in preparing for the drug to treat tumor. The preparing method comprises: preparing for dissolving solution, dissolving the cohosh root base, adsorption stripping, preparing for eluent, cleaning, and concave condensation, recrystallizing and checking. The 222 test result expresses that it has the effect of depressing blood vessel formation.

1 citations