Bisabolane Sesquiterpenoids from the Plant Endophytic Fungus Paraconiothyrium brasiliense----中国科学院微生物研究所

科研成果

论文题目:	Bisabolane Sesquiterpenoids from the Plant Endophytic Fungus Paraconiothyrium brasiliense
作者:	Ling Liu, Xiaoyan Chen, Dong Li, Yang Zhang, Li Li, Liangdong Guo, Ya* Cao, and Yongsheng* Che.
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刊物名称:	J Nat Prod
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年份:	2015
影响因子:	3.404
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摘要:	Brasilamides E-J (1-6), the bisabolane sesquiterpenoids with the 3-cyclohexylfuran (1 and 2) and 3-cyclohexylfuranone (3-6) skeletons, were isolated from the scale-up fermentation cultures of the plant endophytic fungus Paraconiothynium brasiliense Verkley. Although brasilamide E (1) is a known metabolite, its structure elucidation has yet to be described. The structures of 1-6 were elucidated primarily by NMR experiments. Compounds 3-6 were found to be racemic, and 3 was further separated into enantiomers 3a and 3b on a chiral HPLC column. The absolute configurations of 3a and 3b were assigned by electronic circular dichroism calculations. Compound 1 selectively inhibited the proliferation of the breast (MCF-7) and gastric (MGC) cancer cell lines, with IC50 values of 8.4 and 14.7 muM, respectively. Initial mechanistic investigation revealed that compound 1 inhibited the expression of a key energy metabolic enzyme, hexokinase II (HK2), in MCF-7 cells, which resulted in dysfunction of glucose metabolism and ATP depletion and eventually inhibited the proliferation of the breast cancer cells.