Wortmannilactones I–L, new NADH-fumarate reductase inhibitors, induced by adding suberoylanilide hydroxamic acid to the culture medium of Talaromyces wortmannii. Issue 21 (1st November 2016)

• Record Type: Journal Article
• Authors: Liu, Wen-Cai; Wang, Yi-Yu; Liu, Jun-Hui; Ke, Ai-Bing; Zheng, Zhi-Hui; Lu, Xin-Hua; Luan, Yu-Shi; Xiu, Zhi-Long; Dong, Yue-Sheng
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 21(2016)
• Page Start: 5328
• Page End: 5333
• Publication Date: 2016-11-01
• Subjects: Wortmannilactones -- Talaromyces wortmannii -- Epigenome manipulation -- Suberoylanilide hydroxamic acid -- NADH-fumarate reductase; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.09.032
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: 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.