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The identification of novel modulators for the SIRT‐6 protein
Author(s) -
Moaddel Ruin,
Singh Nagendra,
Ravichandran Sarangan,
Norton Darrell D.,
Fugmann Sebastian
Publication year - 2013
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.27.1_supplement.890.8
Subject(s) - vitexin , trigonella , chemistry , quercetin , ligand (biochemistry) , identification (biology) , biological activity , biochemistry , pharmacology , traditional medicine , biology , flavonoid , medicine , in vitro , botany , receptor , antioxidant
Objective SIRT6 has been proposed as a potential therapeutic target for metabolic disorders and the prevention of age‐associated diseases. The aim of this study was to develop a screening method for the identification of novel modulators of SIRT6 from a natural plant extract. Methods SIRT6 was immobilized onto the surface of magnetic beads (SIRT6‐MB), and the enzymatic activity was measured. Subsequently, SIRT6 was immobilized onto the surface of an open tubular capillary and characterized by frontal chromatography. Results The identification of quercetin, vitexin as inhibitors from Trigonella foenum‐graecum was carried out. Structurally related flavonoids were then tested for their activity on SIRT6. In addition to obtaining their binding activity, they were also ranked based on their ability to displace quercetin. Further, preliminary results with ligand fishing experiments using the SIRT6‐MB suggest the identification of additional compounds from fenugreek seed extract with activity at the SIRT6‐protein. Conclusion The SIRT6‐MBs were successfully used for the identification of an active ligand from a botanical matrix, which sets the basis for identification of SIRT6 modulators from plant extracts.