Wortmannilactones I-L, new NADH-fumarate reductase inhibitors, induced by adding suberoylanilide hydroxamic acid to the culture medium of Talaromyces wortmannii.
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 IC50values ranging from 0.84 to 1.35μM.
School of Life Science and Biotechnology, Dalian University of Technology, Linggong Road 2, Dalian 116024, Liaoning, PR China.
Wen-Cai
WC
Liu
School of Life Science and Biotechnology, Dalian University of Technology, Linggong Road 2, Dalian 116024, Liaoning, PR China.
Yi-Yu
YY
Wang
School of Life Science and Biotechnology, Dalian University of Technology, Linggong Road 2, Dalian 116024, Liaoning, PR China.
Jun-Hui
JH
Liu
New Drug Research and Development Center, North China Pharmaceutical Group Corporation and National Microbial Medicine Engineering and Research Center, Shijiazhuang 050015, PR China.
Ai-Bing
AB
Ke
New Drug Research and Development Center, North China Pharmaceutical Group Corporation and National Microbial Medicine Engineering and Research Center, Shijiazhuang 050015, PR China.
Zhi-Hui
ZH
Zheng
New Drug Research and Development Center, North China Pharmaceutical Group Corporation and National Microbial Medicine Engineering and Research Center, Shijiazhuang 050015, PR China.
Xin-Hua
XH
Lu
School of Life Science and Biotechnology, Dalian University of Technology, Linggong Road 2, Dalian 116024, Liaoning, PR China.
Yu-Shi
YS
Luan
School of Life Science and Biotechnology, Dalian University of Technology, Linggong Road 2, Dalian 116024, Liaoning, PR China.
Zhi-Long
ZL
Xiu
School of Life Science and Biotechnology, Dalian University of Technology, Linggong Road 2, Dalian 116024, Liaoning, PR China. Electronic address: yshdong@dlut.edu.cn.
Yue-Sheng
YS
Dong
D003470:Culture Media; D006877:Hydroxamic Acids / Q000494:pharmacology*; D018942:Macrolides / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D044925:Oxidoreductases Acting on CH-CH Group Donors / Q000037:antagonists & inhibitors*; D013057:Spectrum Analysis / Q000379:methods; D032901:Talaromyces / Q000737:chemistry*; D000077337:Vorinostat
D003470:Culture Media; D006877:Hydroxamic Acids; D018942:Macrolides; D000077337:Vorinostat; D044925:Oxidoreductases Acting on CH-CH Group Donors; C020155:fumarate reductase (NADH)
Epigenome manipulation; NADH-fumarate reductase; Suberoylanilide hydroxamic acid; Talaromyces wortmannii; Wortmannilactones