Wortmannilactones I-L, new NADH-fumarate reductase inhibitors, induced by adding suberoylanilide hydroxamic acid to the culture medium of Talaromyces wortmannii

详细信息    查看全文

• 作者：Wen-Cai Liu^a ; Yi-Yu Wang^a ; Jun-Hui Liu^a ; Ai-Bing Ke^b ; Zhi-Hui Zheng^b ; Xin-Hua Lu^b ; Yu-Shi Luan^a ; Zhi-Long Xiu^a ; Yue-Sheng Dong^a ; ^{yshdong@dlut.edu.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Wortmannilactones ; Talaromyces wortmannii ; Epigenome manipulation ; Suberoylanilide hydroxamic acid ; NADH-fumarate reductase
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 November 2016
• 年：2016
• 卷：26
• 期：21
• 页码：5328-5333
• 全文大小：964 K

文摘

With the aim of finding more potential inhibitors against NADH-fumarate reductase (specific target for treating helminthiasis and cancer) from natural resources, Talaromyces wortmannii was treated with the epigenome regulatory agent suberoylanilide hydroxamic acid, which resulted in the isolation of four new wortmannilactones derivatives (wortmannilactones I–L, 1–4). The structures of these new compounds were elucidated based on IR, HRESIMS and NMR spectroscopic data analyses. These four new compounds showed potent inhibitory activity against NADH-fumarate reductase with the IC₅₀ values ranging from 0.84 to 1.35 μM.