Choi, Yongsoo Jung, Yujung Kim, Su-Nam 2024-01-20T06:32:43Z 2024-01-20T06:32:43Z 2021-09-04 2015-08 1420-3049 https://pubs.kist.re.kr/handle/201004/125199 Peroxisome proliferator-activated receptors (PPARs) are key nuclear receptors and therapeutic targets for the treatment of metabolic diseases through the regulation of insulin resistance, diabetes, and dyslipidemia. Although a few drugs that target PPARs have been approved, more diverse and novel PPAR ligands are necessary to improve the safety and efficacy of available drugs. To expedite the search for new natural agonists of PPARs, we developed a screening assay based on ultrafiltration liquid chromatography-mass spectrometry (LC-MS) that is compatible with complex samples such as dietary foods or botanical extracts. The known PPAR and/or PPAR ligands resveratrol and rosiglitazone were used as positive controls to validate the developed method. When applied to the screening of an Artemisia argyi extract, eupatilin was identified as a selective PPAR ligand. A PPAR competitive binding assay based on FRET detection also confirmed eupatilin as a selective PPAR agonist exhibiting a binding affinity of 1.18 M (IC50). Furthermore, eupatilin activation of the transcriptional activity of PPAR was confirmed using a cell-based transactivation assay. Thus, ultrafiltration LC-MS is a suitable assay for the identification of PPAR ligands in complex matrixes such as extracts of dietary foods and botanicals. English MDPI GAMMA-AGONIST ANTIINFLAMMATORY ACTIVITIES MASS-SPECTROMETRY SCREENING ASSAY L. ANTICANCER LIGANDS EXTRACT FRET Identification of Eupatilin from Artemisia argyi as a Selective PPAR alpha Agonist Using Affinity Selection Ultrafiltration LC-MS Article 10.3390/molecules200813753 1 MOLECULES, v.20, no.8, pp.13753 - 13763 MOLECULES 20 8 13753 13763 scie scopus 000361375400017 2-s2.0-84941578409 Biochemistry & Molecular Biology Chemistry, Multidisciplinary Biochemistry & Molecular Biology Chemistry Article GAMMA-AGONIST ANTIINFLAMMATORY ACTIVITIES MASS-SPECTROMETRY SCREENING ASSAY L. ANTICANCER LIGANDS EXTRACT FRET PPAR eupatilin Artemisia argyi ultrafiltration LC-MS