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Planta Med 2010; 76(16): 1834-1839
DOI: 10.1055/s-0030-1250042
Pharmacology
Original Papers
© Georg Thieme Verlag KG Stuttgart · New York

Icaritin Induces Apoptosis of HepG2 Cells via the JNK1 Signaling Pathway Independent of the Estrogen Receptor

Jun He1 , Yan Wang2 , Fei Duan2 , Hao Jiang2 , Min-Feng Chen4 , Si-Yuan Tang3
  • 1Department of General Surgery, The First Affiliated Hospital of South China University, Hengyang, Hunan, China
  • 2Department of Oncology, The First Affiliated Hospital of South China University, Hengyang, Hunan, China
  • 3The School of Nursing, Central South University, Changsha, Hunan, China
  • 4Department of Urology, Xiangya Hospital, Central South University, Changsha, Hunan, China
Further Information

Publication History

received October 7, 2009 revised May 9, 2010

accepted May 11, 2010

Publication Date:
17 June 2010 (online)

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Abstract

Chinese herbs have become a focus in cancer treatment. Icaritin, a prenylflavonoid derivative from Chinese herbs of the Epimedium genus, has selective estrogen receptor (ER) modulating activity. This study evaluates the effects of icaritin on the apoptosis of HepG2 hepatocellular carcinoma cells. Icaritin (at 5–50 µM) induced apoptosis of HepG2 cells. Few changes in icaritin-induced apoptosis were observed after pretreatment with ICI182780. Consistent with apoptosis induction, icaritin increased the Bax/Bcl-2 ratio and caspase-3 activation in HepG2 cells. Furthermore, icaritin was capable of stimulating the c-Jun N-terminal kinase 1 (JNK1), but not the JNK2, ERK1/2, and p38 subgroups of the mitogen-activated protein kinase (MAPK) family. Coincidently, icaritin-induced cell apoptosis was abolished by SP600125, a specific inhibitor for JNK. Collectively, our results suggest a novel pro-apoptotic activity of icaritin mediated via the JNK1 signaling pathway that is not associated with ER in HepG2 cells.

Key words

icaritin - Epimedium - Berberidaceae - apoptosis - c‐Jun N‐terminal kinase - HepG2 cells

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Prof. Si-Yuan Tang

The School of Nursing of Central South University

172# Tongzipo Road, Changsha

Hunan 410013

China

Phone: + 86 73 18 26 5 02 64

Fax: + 86 7 31 82 65 02 62

Email: tangsyuan@yahoo.com.cn

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