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13,14‑bis(cis‑3,5‑dimethyl‑1‑piperazinyl)‑β‑elemene, a novel β‑elemene derivative, shows potent antitumor activities via inhibition of mTOR in human breast cancer cells

  • Authors:
    • Xiao‑Fei Ding
    • Mao Shen
    • Li‑Ying Xu
    • Jin‑Hua Dong
    • Guang Chen

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  • Published online on: February 27, 2013     https://doi.org/10.3892/ol.2013.1213
  • Pages: 1554-1558
Metrics: Total Views: 0 (Spandidos Publications: | PMC Statistics: )
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Abstract

Elemene has been approved for the treatment of advanced cancer in China, however, it inhibits cell growth only at high concentrations and is an essential oil with poor water solubility and stability. The discovery of new β‑elemene derivatives is of increasing interest. We recently reported that the compound 13,14‑bis(cis‑3,5‑dimethyl-1-piperazinyl)‑β‑elemene (IIi), a novel β‑elemene derivative with a cis‑2,6‑dimethylpiperazine substitution, is a potent agent for inhibiting the proliferation of SGC‑7901 and HeLa cells. In the present study, we further verified that IIi is cytotoxic to a wide spectrum of human cancer cells in culture, including those of breast, ovarian, lung, gastric, hepatocellular and colon cancer, as well as leukemia cell lines, with an average IC50 of 3.44 µmol/l. Notably, IIi showed significant cytotoxicity in two multidrug‑resistant (MDR) cell lines, with an average resistance factor (RF) of 1.66. Moreover, in mice with S‑180 sarcoma xenografts, the intraperitoneal administration of IIi inhibited tumor growth. The immunoblotting study showed that treatment with IIi decreases phosphorylated p70S6K1 and 4EBP1 levels in the human breast cancer MCF‑7 and MDA‑MB‑468 cells. In the MCF‑7 cells, IIi also significantly increased the expression of cleaved LC3. This indicated that IIi inhibits mTOR activity and induces autophagy. The mTOR inhibitory function and the potent antitumor activity, taken together with the appreciable anti‑multidrug resistance action, shows IIi to be a novel potential antitumor agent, which merits further research and development.
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May 2013
Volume 5 Issue 5

Print ISSN: 1792-1074
Online ISSN:1792-1082

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  • Impact Factor: 2.9
  • Ranked Oncology
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  • CiteScore: 6.3
  • CiteScore Rank: Q2: #119/366 Oncology
  • Source Normalized Impact per Paper (SNIP): 0.725
  • SCImago Journal Rank (SJR): 0.639
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Spandidos Publications style
Ding XF, Shen M, Xu LY, Dong JH and Chen G: 13,14‑bis(cis‑3,5‑dimethyl‑1‑piperazinyl)‑β‑elemene, a novel β‑elemene derivative, shows potent antitumor activities via inhibition of mTOR in human breast cancer cells. Oncol Lett 5: 1554-1558, 2013
APA
Ding, X., Shen, M., Xu, L., Dong, J., & Chen, G. (2013). 13,14‑bis(cis‑3,5‑dimethyl‑1‑piperazinyl)‑β‑elemene, a novel β‑elemene derivative, shows potent antitumor activities via inhibition of mTOR in human breast cancer cells. Oncology Letters, 5, 1554-1558. https://doi.org/10.3892/ol.2013.1213
MLA
Ding, X., Shen, M., Xu, L., Dong, J., Chen, G."13,14‑bis(cis‑3,5‑dimethyl‑1‑piperazinyl)‑β‑elemene, a novel β‑elemene derivative, shows potent antitumor activities via inhibition of mTOR in human breast cancer cells". Oncology Letters 5.5 (2013): 1554-1558.
Chicago
Ding, X., Shen, M., Xu, L., Dong, J., Chen, G."13,14‑bis(cis‑3,5‑dimethyl‑1‑piperazinyl)‑β‑elemene, a novel β‑elemene derivative, shows potent antitumor activities via inhibition of mTOR in human breast cancer cells". Oncology Letters 5, no. 5 (2013): 1554-1558. https://doi.org/10.3892/ol.2013.1213