Piperlongumine as a direct TrxR1 inhibitor with suppressive activity against gastric cancer
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- 作者：Peng Zoua ; b ; 1 ; Yiqun Xiac ; 1 ; Jiansong Jid ; Weiqian Chena ; d ; Jinsan Zhanga ; Xi Chena ; Vinothkumar Rajamanickama ; Gaozhi Chena ; Zhe Wanga ; Lingfeng Chena ; Yifeng Wanga ; Shulin Yangb ; bioshuliny@yahoo.com.cn" class="auth_mail" title="E-mail the corresponding author ; Guang Lianga ; wzmcliangguang@163.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：Thioredoxin reductase 1 ; Reactive oxygen species ; Piperlongumine ; ER stress ; Mitochondrial dysfunction
- 刊名：Cancer Letters
- 出版年：2016
- 出版时间：28 May 2016
- 年：2016
- 卷：375
- 期：1
- 页码：114-126
- 全文大小：4819 K
文摘
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Piperlongumine directly binds TrxR1 in vitro and inactivates TrxR1 in human gastric cancer cells.
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Stably overexpressing TrxR1 in SGC-7901 cells markedly rescued piperlongumine-induced growth inhibition
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Piperlongumine displays synergistic lethality with GSH inhibitors (BSO and Erastin) against gastric cancer cells.
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Piperlongumine treatment markedly reduces the TrxR1 activity and tumor cell burden in vivo.
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TrxR1 was significantly overexpressed in gastric cancer cell lines and human gastric cancer tissues.