Bio-Assay Guided Isolation and Structural Identification of Acetylcholinesterase Inhibitors from Sideroxylon obtusifolium (Roem. & Schult.) TD Penn.

Abstract:

In a search for potential acetylcholinesterase inhibitors (IAChE), the dichloromethane ex-tract from Sideroxylon obtusifolium leaves demonstrated a marked enzyme inhibition. A TLC bioautographic assay and Ellman’s reaction were used as bioassays to guide the isolation of IAChE. Three compounds were purified sufficiently to allow structural analysis and determination of their half inhibitory concentration (IC50). The structures of these compounds were elucidated by spectrometric methods including EIMS, 1H, 13C and 2D NMR experiments. Ursolic acid has been identified as the compound responsible for that inhibition. Two other molecules–the triterpernoids betulin and lupeol–were also isolated and characterized for the first time from S. obtusifolium. The IC50 value of ursolic acid was found to be 34.3 μM/mL.

Año de publicación:

2013

Keywords:

Fuente:

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