title: Polyyne hybrid compounds from Notopterygium incisum with peroxisome proliferator-activated receptor gamma agonistic effects.
abstract: In the search for peroxisome proliferator-activated receptor gamma (PPARγ) active constituents from the roots and rhizomes of Notopterygium incisum, 11 new polyacetylene derivatives (1-11) were isolated. Their structures were elucidated by NMR and HRESIMS as new polyyne hybrid molecules of falcarindiol with sesquiterpenoid or phenylpropanoid moieties, named notoethers A-H (1-8) and notoincisols A-C (9-11), respectively. Notoincisol B (10) and notoincisol C (11) represent two new carbon skeletons. When tested for PPARγ activation in a luciferase reporter assay with HEK-293 cells, notoethers A-C (1-3), notoincisol A (9), and notoincisol B (10) showed promising agonistic activity (EC50 values of 1.7 to 2.3 μM). In addition, notoincisol A (9) exhibited inhibitory activity on NO production of stimulated RAW 264.7 macrophages.
authors.affiliation: Department of Pharmacognosy, Institute of Pharmaceutical Sciences, Karl-Franzens-University Graz , Universitätsplatz 4/I, 8010 Graz, Austria.
authors.forename: Xin
authors.initials: X
authors.lastname: Liu
authors.forename: Olaf
authors.initials: O
authors.lastname: Kunert
authors.forename: Martina
authors.initials: M
authors.lastname: Blunder
authors.forename: Nanang
authors.initials: N
authors.lastname: Fakhrudin
authors.forename: Stefan M
authors.initials: SM
authors.lastname: Noha
authors.forename: Clemens
authors.initials: C
authors.lastname: Malainer
authors.forename: Andreas
authors.initials: A
authors.lastname: Schinkovitz
authors.forename: Elke H
authors.initials: EH
authors.lastname: Heiss
authors.forename: Atanas G
authors.initials: AG
authors.lastname: Atanasov
authors.forename: Manfred
authors.initials: M
authors.lastname: Kollroser
authors.forename: Daniela
authors.initials: D
authors.lastname: Schuster
authors.forename: Verena M
authors.initials: VM
authors.lastname: Dirsch
authors.forename: Rudolf
authors.initials: R
authors.lastname: Bauer
mesh_terms: D000818:Animals; D019661:Apiaceae / Q000737:chemistry*; D053280:Diynes / Q000494:pharmacology; D005233:Fatty Alcohols / Q000494:pharmacology; D057809:HEK293 Cells; D006801:Humans; D008070:Lipopolysaccharides / Q000494:pharmacology; D008156:Luciferases / Q000378:metabolism; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D015394:Molecular Structure; D009569:Nitric Oxide / Q000096:biosynthesis; D047495:PPAR gamma / Q000187:drug effects*; D018517:Plant Roots / Q000737:chemistry; D053279:Polyynes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D027343:Rhizome / Q000737:chemistry
chemical_list: D053280:Diynes; D005233:Fatty Alcohols; D008070:Lipopolysaccharides; D047495:PPAR gamma; C000599240:notoincisol B; D053279:Polyynes; D009569:Nitric Oxide; C034379:falcarindiol; D008156:Luciferases