1. Academic Validation
  2. Polyyne hybrid compounds from Notopterygium incisum with peroxisome proliferator-activated receptor gamma agonistic effects

Polyyne hybrid compounds from Notopterygium incisum with peroxisome proliferator-activated receptor gamma agonistic effects

  • J Nat Prod. 2014 Nov 26;77(11):2513-21. doi: 10.1021/np500605v.
Xin Liu 1 Olaf Kunert Martina Blunder Nanang Fakhrudin Stefan M Noha Clemens Malainer Andreas Schinkovitz Elke H Heiss Atanas G Atanasov Manfred Kollroser Daniela Schuster Verena M Dirsch Rudolf Bauer
Affiliations

Affiliation

  • 1 Department of Pharmacognosy, Institute of Pharmaceutical Sciences, Karl-Franzens-University Graz , Universitätsplatz 4/I, 8010 Graz, Austria.
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.

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