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

Nguyen Tuan Hiep, Yun Hyeok Choi, Nahyun Kim, Seong Su Hong, Seung Beom Hong, Bang Yeon Hwang, Hak Ju Lee, Sung-Joon Lee, Dae Sik Jang, Dongho Lee

Research output: Contribution to journalArticle

21 Citations (Scopus)

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)-γ with EC50 values of 1.15 and 11.05 μM, respectively. The expression of PPAR-γ 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-γ agonist and a possible therapeutic candidate for treatment of diabetes.

Original languageEnglish
Pages (from-to)784-788
Number of pages5
JournalJournal of Natural Products
Volume75
Issue number4
DOIs
Publication statusPublished - 2012 Apr 27

ASJC Scopus subject areas

  • Complementary and alternative medicine
  • Molecular Medicine
  • Organic Chemistry
  • Analytical Chemistry
  • Pharmaceutical Science
  • Pharmacology
  • Drug Discovery

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