1, 3, 6-Trihydroxy-7-Methyl-9, 10-Anthracenedione Isolated from genus Lindera with Anti-Cancer Activity.
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 dosedependently.


CONCLUSIONS
The fatty acid synthase was a potent therapeutic target for cancers, these findings suggest that TMA has the application potential for treating human cancers.
School of Life Science and Engineering, Southwest Jiaotong University, Chengdu, 610031. China.
Guoqing
G
Wei
School of Life Science and Engineering, Southwest Jiaotong University, Chengdu, 610031. China.
Hui
H
Chen
College of Life Sciences, University of Chinese Academy of Sciences, Beijing 100049. China.
Fangyuan
F
Nie
College of Life Sciences, University of Chinese Academy of Sciences, Beijing 100049. China.
Xiaofeng
X
Ma
School of Life Science and Engineering, Southwest Jiaotong University, Chengdu, 610031. China.
Hezhong
H
Jiang
D000880:Anthraquinones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D027443:Lindera / Q000737:chemistry*; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured; D019014:fas Receptor / Q000037:antagonists & inhibitors / Q000096:biosynthesis
C000625647:1,3,6-trihydroxy-7-methyl-9,10-anthracenedione; D000880:Anthraquinones; D000972:Antineoplastic Agents, Phytogenic; C491901:FAS protein, human; D019014:fas Receptor
1; 10-
anthracenedione (TMA).; 3; 6-Trihydroxy-7-methyl-9; Anthraquinone; Lindera aggregate; Lindera nacusua; breast cancer; fatty acid synthase; inhibit