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. 2016 Jun 29;7:191. doi: 10.3389/fphar.2016.00191

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Copyright © 2016 Tan, Chan, Pusparajah, Saokaew, Duangjai, Lee and Goh.

This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

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Anti-cancer mechanisms of icariin and its derivatives. Icariin and its derivatives mainly inhibit the growth of tumor through induction of apoptosis by targeting multiple signaling pathways. Cell cycle arrests also occur through downregulation of the expression of cell cycle regulatory proteins. Besides, there are anti-angiogenesis, anti-metastasis and immunomodulation. The compounds are also effective in targeting hormone-dependent cancers, cancer stem cells, and drug-resistant cancer cells. There are synergistic effects when icariin and its derivatives are used together with standard cancer therapy such as chemotherapy or radiotherapy.