Abstract
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.
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.
Keywords: Anthraquinone, breast cancer, fatty acid synthase, inhibit, Lindera aggregate, Lindera nacusua, 1, 3, 6-Trihydroxy-7-methyl-9, 10- anthracenedione (TMA).
Anti-Cancer Agents in Medicinal Chemistry
Title:1, 3, 6-Trihydroxy-7-Methyl-9, 10-Anthracenedione Isolated from genus Lindera with Anti-Cancer Activity
Volume: 17 Issue: 11
Author(s): Guoqing Wei, Hui Chen, Fangyuan Nie, Xiaofeng Ma*Hezhong Jiang*
Affiliation:
- College of Life Sciences, University of Chinese Academy of Sciences, Beijing 100049,China
- School of Life Science and Engineering, Southwest Jiaotong University, Chengdu, 610031,China
Keywords: Anthraquinone, breast cancer, fatty acid synthase, inhibit, Lindera aggregate, Lindera nacusua, 1, 3, 6-Trihydroxy-7-methyl-9, 10- anthracenedione (TMA).
Abstract: 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.
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.
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Cite this article as:
Wei Guoqing, Chen Hui, Nie Fangyuan, Ma Xiaofeng*, Jiang Hezhong*, 1, 3, 6-Trihydroxy-7-Methyl-9, 10-Anthracenedione Isolated from genus Lindera with Anti-Cancer Activity, Anti-Cancer Agents in Medicinal Chemistry 2017; 17 (11) . https://dx.doi.org/10.2174/1871520615666150914114649
DOI https://dx.doi.org/10.2174/1871520615666150914114649 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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