Polyhydroxylated macrolides from Seimatosporium discosioides and their effects on the activation of peroxisome proliferator-activated receptor gamma.

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Hiep NT, Choi YH, Kim N, Hong SS, Hong SB, Hwang BY, Lee HJ, Lee SJ, Jang DS, Lee D

Polyhydroxylated macrolides from Seimatosporium discosioides and their effects on the activation of peroxisome proliferator-activated receptor gamma.

J Nat Prod. 2012 Apr 27;75(4):784-8. doi: 10.1021/np200955z. Epub 2012 Mar 16.

PubMed ID
22424300 [ View in PubMed
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Abstract

Two new polyhydroxylated macrolides, seimatopolides A (1) and B (2), were isolated from an EtOAc extract of Seimatosporium discosioides culture medium. The structures of the new compounds were established on the basis of spectroscopic analysis, including 1D and 2D NMR, and their absolute configurations were determined using the modified Mosher's method. Seimatopolides A (1) and B (2) activated peroxisome proliferator-activated receptor (PPAR)-gamma with EC(50) values of 1.15 and 11.05 muM, respectively. The expression of PPAR-gamma target genes in HepG2 hepatocytes was significantly altered; in particular, expression of the gluconeogenic genes glucose-6-phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK) was reduced upon stimulation with 1, supporting the proposal that compound 1 is both a PPAR-gamma agonist and a possible therapeutic candidate for treatment of diabetes.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
TroglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)440N/AN/ADetails