The Anticancer Properties of Herba Epimedii and Its Main Bioactive Componentsicariin and Icariside II

Abstract

Cancer is one of the leading causes of deaths worldwide. Compounds derived from traditional Chinese medicines have been an important source of anticancer drugs and adjuvant agents to potentiate the efficacy of chemotherapeutic drugs and improve the side effects of chemotherapy. Herba Epimedii is one of most popular herbs used in China traditionally for the treatment of multiple diseases, including osteoporosis, sexual dysfunction, hypertension and common inflammatory diseases. Studies show Herba Epimedii also possesses anticancer activity. Flavonol glycosides icariin and icariside II are the main bioactive components of Herba Epimedii. They have been found to possess anticancer activities against various human cancer cell lines in vitro and mouse tumor models in vivo via their effects on multiple biological pathways, including cell cycle regulation, apoptosis, angiogenesis, and metastasis, and a variety of signaling pathways including JAK2-STAT3, MAPK-ERK, and PI3k-Akt-mTOR. The review is aimed to provide an overview of the current research results supporting their therapeutic effects and to highlight the molecular targets and action mechanisms.

The impact of Icariside II on human prostate cancer cell proliferation, mobility, and autophagy via PI3K-AKT-mTOR signaling pathway

“…12 A number of studies have explored the ability of ICA II to modulate the invasivity and migratory capabilities of lung, gastric, and esophageal cancer cells. 10,16 Herein, we determined that ICA II was able to signi cantly inhibit DU145 PC cell invasion and migration.…”

“…13,14 Several different anti-tumor drugs seek to modulate these activities via either disrupting tumor cell proliferation and/or via inducing apoptotic tumor cell death. 10,15 Traditional herbal medicines represent a potentially ideal source of compounds for use in chemotherapeutic regimens, 16 with drugs such as camptothecin, paclitaxel, and emodin all having been developed from natural plant sources. 17,18 Previous work has demonstrated that ICA II is capable of mediating anti-tumor activity against hepatic carcinoma, breast cancer, and gastric cancer via a range of mechanisms.…”

“…17,18 Previous work has demonstrated that ICA II is capable of mediating anti-tumor activity against hepatic carcinoma, breast cancer, and gastric cancer via a range of mechanisms. 10,16 The P13K-Akt-mTOR signaling axis is a key regulator of protein synthesis within cells stimulated using an array of growth factors, in uencing both autophagic activity and survival in a context-dependent fashion. ICA II treatment of osteosarcoma cells has recently been shown to be associated with reduced PI3k-AKT pathway activation.…”

“…9 ICA II has been shown to inhibit the COX-2/PGE 2 pathway and to induce mitochondria-dependent apoptosis in PC-3 PC cells. 10 The present study was therefore designed with the goal of evaluating the impact of ICA II on the proliferative, migratory, and autophagy activity of human PC cells, and to explore the mechanisms underlying such activity.…”

A network pharmacology approach to explore the mechanisms of action of Epimrdii Herba-Coicis Semen for treatment of Alzheimer's disease

“…Epimrdii Herba (Epimedium) [8] is a TCM originating from Epimedium Brevicornu Maxim., Epimedium sagittatum Maxim., Epimedium pubescens Maxim., or Epimedium koreanum Nakai. It has been reported to treat diseases [9] such as cancer, osteoporosis, cardiovascular disease and brain disease, it also improves sexual function. Coicis Semen is a mature dry kernel of the gramineous plant Coix lacryma-jobi L. var.…”