Alantolactone sensitizes human pancreatic cancer cells to EGFR inhibitors through the inhibition of STAT3 signaling

被引:52
作者
Zheng, Hailun [1 ]
Yang, Lehe [1 ,2 ,3 ]
Kang, Yanting [1 ,4 ]
Chen, Min [1 ]
Lin, Shichong [2 ]
Xiang, Youqun [2 ]
Li, Caleb [5 ]
Dai, Xuanxuan [2 ]
Huang, Xiaoying [2 ]
Liang, Guang [1 ]
Zhao, Chengguang [1 ,3 ]
机构
[1] Wenzhou Med Univ, Sch Pharmaceut Sci, Chem Biol Res Ctr, Chashan St, Wenzhou 325035, Zhejiang, Peoples R China
[2] Wenzhou Med Univ, Affiliated Hosp 1, Key Lab Heart & Lung, Div Pulm Med, Wenzhou 325000, Zhejiang, Peoples R China
[3] Wenzhou Med Univ, Affiliated Yueqing Hosp, Dept Resp Med, Wenzhou, Zhejiang, Peoples R China
[4] Yichun Peoples Hosp, Dept Ultrasonog, Yichun, Jiangxi, Peoples R China
[5] Coffman High Sch, Dublin, OH USA
基金
国家重点研发计划;
关键词
alantolactone; EGFR; inhibitor; pancreatic cancer; STAT3; DE-NOVO RESISTANCE; LUNG-CANCER; FEEDBACK ACTIVATION; DRUG-RESISTANCE; GEMCITABINE; MUTATIONS; MECHANISM; ERLOTINIB; DOCKING; GROWTH;
D O I
10.1002/mc.22951
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Several studies have implicated the feedback activation of signal transducer and activator of transcription 3 (STAT3) as a new cancer drug-resistance mechanism and linked it to the failure of epidermal growth factor receptor (EGFR)-targeted therapies. In this study, we discovered that Alantolactone, a natural sesquiterpene lactone, potently inhibited human pancreatic cancer cells and suppressed constitutively activated STAT3. In contrast, Alantolactone had little effect on the EGFR pathway. Moreover, combination of Alantolactone and an EGFR inhibitor, Erlotinib or Afatinib, demonstrated a remarkable synergistic anti-cancer effect against pancreatic cancer cells both in vitro and in vivo. Our results suggested that Alantolactone could sensitize human pancreatic cancer cells to EGFR inhibitors possibly through down-regulating the STAT3 signaling. Alantolactone, when combined with other EGFR targeted agents, could be further developed as a potential therapy for pancreatic cancer.
引用
收藏
页码:565 / 576
页数:12
相关论文
共 41 条
[1]  
[Anonymous], J CHROMATOGR B
[2]   Analysis of natural product regulation of cannabinoid receptors in the treatment of human disease [J].
Badal, S. ;
Smith, K. N. ;
Rajnarayanan, R. .
PHARMACOLOGY & THERAPEUTICS, 2017, 180 :24-48
[3]   Erlotinib in cancer treatment [J].
Bareschino, M. A. ;
Schettino, C. ;
Troiani, T. ;
Martinelli, E. ;
Morgillo, F. ;
Ciardiello, F. .
ANNALS OF ONCOLOGY, 2007, 18 :35-41
[4]   Three-dimensional structure of the Stat3β homodimer bound to DNA [J].
Becker, S ;
Groner, B ;
Müller, CW .
NATURE, 1998, 394 (6689) :145-151
[5]   Met Activation in Non-Small Cell Lung Cancer Is Associated with de Novo Resistance to EGFR Inhibitors and the Development of Brain Metastasis [J].
Benedettini, Elisa ;
Sholl, Lynette M. ;
Peyton, Michael ;
Reilly, John ;
Ware, Christopher ;
Davis, Lenora ;
Vena, Natalie ;
Bailey, Dyane ;
Yeap, Beow Y. ;
Fiorentino, Michelangelo ;
Ligon, Azra H. ;
Pan, Bo-Sheng ;
Richon, Victoria ;
Minna, John D. ;
Gazdar, Adi F. ;
Draetta, Giulio ;
Bosari, Silvano ;
Chirieac, Lucian R. ;
Lutterbach, Bart ;
Loda, Massimo .
AMERICAN JOURNAL OF PATHOLOGY, 2010, 177 (01) :415-423
[6]   Silibinin and STAT3: A natural way of targeting transcription factors for cancer therapy [J].
Bosch-Barrera, Joaquim ;
Menendez, Javier A. .
CANCER TREATMENT REVIEWS, 2015, 41 (06) :540-546
[7]   Alantolactone selectively suppresses STAT3 activation and exhibits potent anticancer activity in MDA-MB-231 cells [J].
Chun, Jaemoo ;
Li, Rui-Juan ;
Cheng, Mao-Sheng ;
Kim, Yeong Shik .
CANCER LETTERS, 2015, 357 (01) :393-403
[8]   Impact of STAT3 Phosphorylation on the Clinical Effectiveness of Anti-EGFR Based Therapy in Patients With Metastatic Colorectal Cancer [J].
Dobi, Erion ;
Monnien, Franck ;
Kim, Stefano ;
Ivanaj, Arben ;
N'Guyen, Thiery ;
Demarchi, Martin ;
Adotevi, Olivier ;
Thierry-Vuillemin, Antoine ;
Jary, Marie ;
Kantelip, Bernadette ;
Pivot, Xavier ;
Godet, Yann ;
Degano, Severine Valmary ;
Borg, Christophe .
CLINICAL COLORECTAL CANCER, 2013, 12 (01) :28-36
[9]   Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2 [J].
Foster, Scott A. ;
Whalen, Daniel M. ;
Oezen, Aysxeguel ;
Wongchenko, Matthew J. ;
Yin, JianPing ;
Yen, Ivana ;
Schaefer, Gabriele ;
Mayfield, John D. ;
Chmielecki, Juliann ;
Stephens, Philip J. ;
Albacker, Lee A. ;
Yan, Yibing ;
Song, Kyung ;
Hatzivassiliou, Georgia ;
Eigenbrot, Charles ;
Yu, Christine ;
Shaw, Andrey S. ;
Manning, Gerard ;
Skelton, Nicholas J. ;
Hymowitz, Sarah G. ;
Malek, Shiva .
CANCER CELL, 2016, 29 (04) :477-493
[10]   Combined targeting of TGF-β, EGFR and HER2 suppresses lymphangiogenesis and metastasis in a pancreatic cancer model [J].
Gore, Jesse ;
Imasuen-Williams, Imade E. ;
Conteh, Abass M. ;
Craven, Kelly E. ;
Cheng, Monica ;
Korc, Murray .
CANCER LETTERS, 2016, 379 (01) :143-153