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
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