1, 3, 6-Trihydroxy-7-Methyl-9, 10-Anthracenedione Isolated from genus Lindera with Anti-Cancer Activity,Anti-Cancer Agents in Medicinal Chemistry

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1, 3, 6-Trihydroxy-7-Methyl-9, 10-Anthracenedione Isolated from genus Lindera with Anti-Cancer Activity
Anti-Cancer Agents in Medicinal Chemistry ( IF 2.6 ) Pub Date : 2017-10-16 , DOI: 10.2174/1871520617666171016124248
Guoqing Wei ₁ , Hui Chen ₁ , Fangyuan Nie ₂ , Xiaofeng Ma ₃ , Hezhong Jiang ₄

Affiliation

Background Natural products inhibiting fatty acid synthase are potential therapeutic agents to treat cancer. Objective To investigate the chemical constituents of the root tubers of Lindera aggregate and the stems of Linderanacusua, and to find natural inhibitors on the expression level on fatty acid synthase in human breast cancer MDA-MB-231 cells. Methods The isolation and purification of the extracts were conducted by the methods of percolation and partition extraction, silica and gel column chromatography, recrystallization and by NMR and spectroscopic analysis method. The cell viability was assessed by Cell Counting Kit assay. Results Seven compounds were elucidated, mainly including five sesquiterpenes, one anthraquinoe and one γ-butanolide, in which compounds 6 was firstly reported from genus Lindera, and compound 7 was isolated from Linderanacusuafor the first time. Among them, 1,3,6-Trihydroxy-7-methyl-9,10-anthracenedione (TMA, compound 6) showed strong inhibitory effect on the expression level on fatty acid synthase in human breast cancer MDA-MB-231 cells. In addition, TMA was found to reduce breast cancer cells viability dose-dependently. Conclusion The fatty acid synthase was a potent therapeutic target for cancers, these findings suggest that TMA has the application potential for treating human cancers.

更新日期：2017-10-16

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