An epigenetic modifier enhances the production of anti-diabetic and anti-inflammatory sesquiterpenoids from Aspergillus sydowii

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• 作者：Yu-Ming Chung^a ; Chien-Kei Wei^a ; Da-Wei Chuang^a ; Mohamed El-Shazly^a ; ^b ; Chi-Ting Hsieh^a ; Teigo Asai^c ; Yoshiteru Oshima^c ; Tusty-Jiuan Hsieh^d ; Tsong-Long Hwang^e ; Yang-Chang Wu^a ; ^f ; ^g ; ^h ; ^{yachwu@mail.cmu.edu.tw} ; Fang-Rong Chang^a ; ^{aaronfrc@kmu.edu.tw}
• 关键词：Epigenetic ; Aspergillus sydowii ; Bisabolane-type ; Anti-diabetic ; Anti-inflammatory
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2013
• 出版时间：1 July, 2013
• 年：2013
• 卷：21
• 期：13
• 页码：3866-3872
• 全文大小：785 K

文摘

The addition of a DNA methyltransferase inhibitor, 5-azacytidine, to Aspergillus sydowii fungus culture broth changed its secondary metabolites profile. Analysis of the culture broth extract led to the isolation of three new bisabolane-type sesquiterpenoids: (7S)-(+)-7-O-methylsydonol (class=""boldFont"">1), (7S,11S)-(+)-12-hydroxysydonic acid (class=""boldFont"">2) and 7-deoxy-7,14-didehydrosydonol (class=""boldFont"">3), along with eight known compounds. The isolated compounds were evaluated for their anti-diabetic and anti-inflammatory activities. Among the isolates, (S)-(+)-sydonol (class=""boldFont"">4) did not only potentiate insulin-stimulated glucose consumption but also prevented lipid accumulation in 3T3-L1 adipocytes. Additionally, (S)-(+)-sydonol (class=""boldFont"">4) exhibited significant anti-inflammatory activity through inhibiting superoxide anion generation and elastase release by fMLP/CB-induced human neutrophils. This is the first report on isolating a secondary metabolite with anti-diabetic and anti-inflammatory activities from microorganisms.