Combined magnetic ligand fishing and high-resolution inhibition profiling for identification of α-glucosidase inhibitory ligands: A new screening approach based on complimentary inhibition and affinity profiles

Summary

Plants are well-recognized sources of inhibitors for -glucosidase - a key target enzyme for
management of type 2 diabetes. Recently, two advanced bioactivity-profiling techniques, i.e., ligand
fishing and high-resolution inhibition profiling, have shown great promises for accelerating
identification of -glucosidase inhibitors from complex plant extracts. Non-specific affinities and
non-specific inhibitions are major sources of false positive hits from ligand fishing and highresolution
inhibition profiling, respectively. In an attempt to minimize such false positive hits, we
describe a new screening approach based on ligand fishing and high-resolution inhibition profiling
for detection of high-affinity ligands and assessment of inhibitory activity, respectively. The
complementary nature of ligand fishing and high-resolution inhibition profiling was explored to
Manuscript for Talanta
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identify-glucosidase inhibitory ligands from a complex mixture, and proof-of-concept was
demonstrated with crude ethyl acetate extract of Ginkgo biloba. In addition to magnetic beads with
a 3-carbon aliphatic linker, -glucosidase was immobilized on magnetic beads with a 21-carbon
aliphatic linker; and the two different types of magnetic beads were compared for their hydrolytic
activity and fishing efficiency.

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DOI : doi.org/10.1016/j.talanta.2019...
NVA : hdl.handle.net/11250/2593069