Anti-tumor effect of germacrone on human hepatoma cell lines through inducing G2/M cell cycle arrest and promoting apoptosis

Liu, Yunyi; Wang, Wei; Fang, Bin; Ma, Fengyun; Zheng, Qian; Deng, Pengyi; Zhao, Shasha; Chen, Mingjie; Yang, Guangxiao; He, Guoqing

doi:10.1016/j.ejphar.2012.10.013

Cited by 99 publications

(62 citation statements)

References 27 publications

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“…Germacrone is a sesquiterpene derivative and has been shown to be one of the most promising agents against several types of cancer, including liver and breast cancer (9,10). However, to the best of our knowledge, its effect on glioma and the underlying molecular mechanism has not been previously explored.…”

Section: Discussionmentioning

confidence: 97%

“…Another study showed that the treatment of HepG2 and Bel7402 hepatoma cell lines with germacrone promoted apoptosis associated with the upregulation of bax and the downregulation of bcl-2. The upregulation of p53 and an increase in reactive oxygen species were observed, which suggested that germacrone is a novel potent drug candidate for liver cancer (9). Furthermore, germacrone was found to inhibit the proliferation of breast cancer cell lines MCF-7 and MDA-MB-231 by inducing cell cycle arrest in the G0/G1 and G2/M phase as well as apoptosis through a mitochondria-mediated caspase pathway (10).…”

Section: Introductionmentioning

confidence: 96%

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Germacrone inhibits the proliferation of glioma cells by promoting apoptosis and inducing cell cycle arrest

Liu

Gao

Wang

et al. 2014

Molecular Medicine Reports

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Germacrone is one of the major bioactive components of the traditional Chinese Medicinal plant Curcuma aromatica Salisb. and has been shown to possess anti‑tumor properties. In the present study, the anti‑proliferative effect of germacrone on human glioma cells and the molecular mechanism underlying its cytotoxicity were investigated. Treatment of the U87 and U251 human glioma cell lines with germacrone inhibited the cell proliferation in a dose‑ and time‑dependent manner as assessed by MTT assay, while significantly lower effects were observed on normal human astrocytes. Flow cytometric analysis and DNA fragmentation revealed that germacrone promoted apoptosis of glioma cells, associated with an increased expression of p53 and bax and decreased expression of bcl‑2. Furthermore, flow cytometric cell cycle analysis revealed that germacrone induced G1 phase arrest, associated with an obvious decrease in the expression of cyclin D1 and CDK2 and an increased expression of p21. In conclusion, the present study suggested that germacrone may be a novel potent chemopreventive drug candidate for gliomas via regulating the expression of proteins associated with apoptosis and G1 cell cycle arrest.

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Section: Discussionmentioning

confidence: 97%

Section: Introductionmentioning

confidence: 96%

Germacrone inhibits the proliferation of glioma cells by promoting apoptosis and inducing cell cycle arrest

Liu

Gao

Wang

et al. 2014

Molecular Medicine Reports

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“…The cyclin B1 and cdc2 complex (CDK1) is the specific regulator in G2/M phase that promotes one cell dividing into two [25]. The complex is activated by the binding of cyclin B1 to cdc2 and cdc2 phosphorylation at Thr161, and inactivated via phosphorylation at Thr14 and Tyr15 of cdc2 [26].…”

Section: Sklb316 Induced G2/m Phase Arrest Of Tumor Cellsmentioning

confidence: 99%

SKLB316, a novel small-molecule inhibitor of cell-cycle progression, induces G2/M phase arrest and apoptosis in vitro and inhibits tumor growth in vivo

et al. 2014

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“…Proliferation of cells was evaluated by MTT assay [10]. Cells were inoculated at 1.0 × 10 4 cells/mL with 200 μL in each well of 96-well plate and allowed to adhere to the plates overnight.…”

Section: Methodsmentioning

confidence: 99%

“…Germacrone is a main bioactive constituent found in Zedoary oil product which is extracted from Curcuma zedoaria Roscoe [7]. The Germacrone (Figure 1) presents extensive bioactivities including antiulce, antiinflammatory, depressant, vasodilator, antibacterial, choleretic, antitussive, antitumor, antifeedant, antifungal and hepatoprotector effects [8–10]. …”

Section: Introductionmentioning

confidence: 99%

Germacrone derivatives: synthesis, biological activity, molecular docking studies and molecular dynamics simulations

Feng

Han

et al. 2017

Oncotarget

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Germacrone is one of the major bioactive components in the Curcuma zedoaria oil product, which is extracted from Curcuma zedoaria Roscoe, known as zedoary. The present study designed some novel germacrone derivatives based on combination principles, synthesized these compounds, and investigated their inhibitions on Bel-7402, HepG2, A549 and HeLa cells. Meanwhile, the study evaluated inhibitions of these derivatives on c-Met kinase, which has been detected in a number of cancers. The results suggested that the majority of the compounds showed stronger inhibitory effect on cancers and c-Met kinase than germacrone. Furthermore, our docking experiments analyzed the results and explained the molecular mechanism. Molecular dynamics simulations were then applied to perform further evaluation of the binding stabilities between compounds and their receptors.

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Anti-tumor effect of germacrone on human hepatoma cell lines through inducing G2/M cell cycle arrest and promoting apoptosis

Cited by 99 publications

References 27 publications

Germacrone inhibits the proliferation of glioma cells by promoting apoptosis and inducing cell cycle arrest

Germacrone inhibits the proliferation of glioma cells by promoting apoptosis and inducing cell cycle arrest

SKLB316, a novel small-molecule inhibitor of cell-cycle progression, induces G2/M phase arrest and apoptosis in vitro and inhibits tumor growth in vivo

Germacrone derivatives: synthesis, biological activity, molecular docking studies and molecular dynamics simulations

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