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Liu, X; Kunert, O; Blunder, M; Fakhrudin, N; Noha, SM; Malainer, C; Schinkovitz, A; Heiss, EH; Atanasov, AG; Kollroser, M; Schuster, D; Dirsch, VM; Bauer, R.
Polyyne hybrid compounds from Notopterygium incisum with peroxisome proliferator-activated receptor gamma agonistic effects.
J Nat Prod. 2014; 77(11):2513-2521
Doi: 10.1021/np500605v
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- Co-authors Med Uni Graz
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Kollroser Manfred
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- Abstract:
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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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