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Open AccessArticle

Piperlongumine Induces Cell Cycle Arrest via Reactive Oxygen Species Accumulation and IKKβ Suppression in Human Breast Cancer Cells

Department of Food Science and Biotechnology of Animal Resources, Konkuk University, Seoul 05029, Korea
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Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Antioxidants 2019, 8(11), 553; https://doi.org/10.3390/antiox8110553
Received: 21 October 2019 / Revised: 8 November 2019 / Accepted: 11 November 2019 / Published: 14 November 2019
(This article belongs to the Section Natural and Synthetic Antioxidants)
Piperlongumine (PL), a natural product derived from long pepper (Piper longum L.), is known to exhibit anticancer effects. However, the effect of PL on cell cycle-regulatory proteins in estrogen receptor (ER)-positive breast cancer cells is unclear. Therefore, we investigated whether PL can modulate the growth of ER-positive breast cancer cell line, MCF-7. We found that PL decreased MCF-7 cell proliferation and migration. Flow cytometric analysis demonstrated that PL induced G2/M phase cell cycle arrest. Moreover, PL significantly modulated the mRNA levels of cyclins B1 and D1, cyclin-dependent kinases 1, 4, and 6, and proliferating cell nuclear antigen. PL induced intracellular reactive oxygen species (hydrogen peroxide) accumulation and glutathione depletion. PL-mediated inhibition of IKKβ expression decreased nuclear translocation of NF-κB p65. Furthermore, PL significantly increased p21 mRNA levels. In conclusion, our data suggest that PL exerts anticancer effects in ER-positive breast cancer cells by inhibiting cell proliferation and migration via ROS accumulation and IKKβ suppression. View Full-Text
Keywords: piperlongumine; cell cycle arrest; oxidative stress; glutathione depletion; IKK suppression; reactive oxygen species (ROS) accumulation piperlongumine; cell cycle arrest; oxidative stress; glutathione depletion; IKK suppression; reactive oxygen species (ROS) accumulation
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MDPI and ACS Style

Jeong, C.H.; Ryu, H.; Kim, D.H.; Cheng, W.N.; Yoon, J.E.; Kang, S.; Han, S.G. Piperlongumine Induces Cell Cycle Arrest via Reactive Oxygen Species Accumulation and IKKβ Suppression in Human Breast Cancer Cells. Antioxidants 2019, 8, 553.

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