Polyhydroxylated Macrolides from Seimatosporium discosioides and Their Effects on the Activation of Peroxisome Proliferator-Activated Receptor Gamma
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- 作者：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
- 刊名：Journal of Natural Products
- 出版年：2012
- 出版时间：April 27, 2012
- 年：2012
- 卷：75
- 期：4
- 页码：784-788
- 全文大小：255K
- 年卷期：v.75,no.4(April 27, 2012)
- ISSN：1520-6025
文摘
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鈥檚 method. Seimatopolides A (1) and B (2) activated peroxisome proliferator-activated receptor (PPAR)-纬 with EC50 values of 1.15 and 11.05 渭M, respectively. The expression of PPAR-纬 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-纬 agonist and a possible therapeutic candidate for treatment of diabetes.