Polyyne hybrid compounds from Notopterygium incisum with peroxisome proliferator-activated receptor gamma agonistic effects.
- 2014-10-21
- Journal of natural products 77(11)
- Xin Liu
- 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
- PubMed: 25333853
- DOI: 10.1021/np500605v
Study Design
- Methods
- Isolation and structural elucidation of 11 new polyacetylene derivatives, tested for PPARγ activation in luciferase reporter assay with HEK-293 cells and NO production inhibition in RAW 264.7 macrophages
- Funding
- Unclear
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.