Anti-Androgenic Activity of Icarisid II from Epimedium Herb in Prostate Cancer LNCaP Cells

Miura, Yoko; Oyama, Masayoshi; Iguchi, Kazuhiro; Ito, Tetsuro; Baba, Misako; Shikama, Yuji; Usui, Shigeyuki; Hirano, Kazuyuki; Iinuma, Munekazu; Mikamo, Hiroshige

doi:10.3177/jnsv.61.201

Cited by 9 publications

(5 citation statements)

References 21 publications

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“…In an in vivo study, reduction of tumor growth was seen in murine models implanted with androgen-sensitive and CRPC cells, due to inhibition of AR signaling by icaritin (Sun et al, 2015a ). In another study, the treatment of androgen receptor-positive prostate cancer cells with icariside II resulted in downregulation of expression of KLK3 gene, showing the role of icariside II in inhibition of AR signaling (Miura et al, 2015 ).…”

Section: Anticancer Propertiesmentioning

confidence: 99%

Anti-Cancer Properties of the Naturally Occurring Aphrodisiacs: Icariin and Its Derivatives

et al. 2016

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Epimedium (family Berberidaceae), commonly known as Horny Goat Weed or Yin Yang Huo, is commonly used as a tonic, aphrodisiac, anti-rheumatic and anti-cancer agent in traditional herbal formulations in Asian countries such as China, Japan, and Korea. The major bioactive compounds present within this plant include icariin, icaritin and icariside II. Although it is best known for its aphrodisiac properties, scientific and pharmacological studies suggest it possesses broad therapeutic capabilities, especially for enhancing reproductive function and osteoprotective, neuroprotective, cardioprotective, anti-inflammatory and immunoprotective effects. In recent years, there has been great interest in scientific investigation of the purported anti-cancer properties of icariin and its derivatives. Data from in vitro and in vivo studies suggests these compounds demonstrate anti-cancer activity against a wide range of cancer cells which occurs through various mechanisms such as apoptosis, cell cycle modulation, anti-angiogenesis, anti-metastasis and immunomodulation. Of note, they are efficient at targeting cancer stem cells and drug-resistant cancer cells. These are highly desirable properties to be emulated in the development of novel anti-cancer drugs in combatting the emergence of drug resistance and overcoming the limited efficacy of current standard treatment. This review aims to summarize the anti-cancer mechanisms of icariin and its derivatives with reference to the published literature. The currently utilized applications of icariin and its derivatives in cancer treatment are explored with reference to existing patents. Based on the data compiled, icariin and its derivatives are shown to be compounds with tremendous potential for the development of new anti-cancer drugs.

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Section: Anticancer Propertiesmentioning

confidence: 99%

Anti-Cancer Properties of the Naturally Occurring Aphrodisiacs: Icariin and Its Derivatives

et al. 2016

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“…Likewise, rutin, another flavonol glycoside isolated from Solanum macaonense releaved to have selective moderate cytotoxicity toward DU145 cancer cell lines (IC 50 = 31.8 μM) [241]. A flavonoid glycoside from Epimedium herb extract, icarisid II, indicated a very potent antiproliferative effect on LNCaP cells at 10 µM with less than 25% of cell viability and suppressed the expression of the androgen-responsive KLK3 gene [220].…”

Section: Plant Extracts and Plant-derived Bioactives In Prostate Cmentioning

confidence: 99%

Phytochemicals in Prostate Cancer: From Bioactive Molecules to Upcoming Therapeutic Agents

et al. 2019

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Prostate cancer is a heterogeneous disease, the second deadliest malignancy in men and the most commonly diagnosed cancer among men. Traditional plants have been applied to handle various diseases and to develop new drugs. Medicinal plants are potential sources of natural bioactive compounds that include alkaloids, phenolic compounds, terpenes, and steroids. Many of these naturally-occurring bioactive constituents possess promising chemopreventive properties. In this sense, the aim of the present review is to provide a detailed overview of the role of plant-derived phytochemicals in prostate cancers, including the contribution of plant extracts and its corresponding isolated compounds.

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“…Importantly, recent studies also suggested that non-androgens including various growth factors, cytokines, protein kinases or interacting with selective coactivators could also transactivate AR in an androgen-independent mechanism [ 11 ]. Targeting AR, instead of targeting the androgens with antiandrogens, to better suppress the AR-mediated CRPC progression is urgently needed [ 12 , 13 ].…”

Section: Introductionmentioning

confidence: 99%

Baicalein suppresses the androgen receptor (AR)-mediated prostate cancer progression via inhibiting the AR N-C dimerization and AR-coactivators interaction

Chen

Liu

et al. 2017

Oncotarget

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BackgroundAndrogen receptor (AR) plays a critical role in prostate cancer (PCa) development and progression. Androgen deprivation therapy with antiandrogens to reduce androgen biosynthesis or prevent androgens from binding to AR are widely used to suppress AR-mediated PCa growth. However, most of ADT may eventually fail with development of the castration resistance after 12-24 months. Here we found that a natural product baicalein can effectively suppress the PCa progression via targeting the androgen-induced AR transactivation with little effect to AR protein expression.MethodsPCa cells including LNCaP, CWR22Rv1, C4-2, PC-3, and DU145, were treated with baicalein and luciferase assay was used to evaluate their effect on the AR transactivation. Cell growth and IC50 were determined by MTT assay after 48 hrs treatment. RT-PCR was used to evaluate the mRNA levels of AR target genes including PSA, TMPRSS2, and TMEPA1. Western blot was used to determine AR and PSA protein expression.ResultsThe natural product of baicalein can selectively inhibit AR transactivation with little effect on the other nuclear receptors, including ERα, and GR. At a low concentration, 2.5 μM of baicalein effectively suppresses the growth of AR-positive PCa cells, and has little effect on AR-negative PCa cells. Mechanism dissection suggest that baicalein can suppress AR target genes (PSA, TMPRSS2, and TMEPA1) expression in both androgen responsive LNCaP cells and castration resistant CWR22Rv1 cells, that may involve the inhibiting the AR N/C dimerization and AR-coactivators interaction.ConclusionsBaicalein may be developed as an effective anti-AR therapy via its ability to inhibit AR transactivation and AR-mediated PCa cell growth.

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Anti-Androgenic Activity of Icarisid II from Epimedium Herb in Prostate Cancer LNCaP Cells

Cited by 9 publications

References 21 publications

Anti-Cancer Properties of the Naturally Occurring Aphrodisiacs: Icariin and Its Derivatives

Anti-Cancer Properties of the Naturally Occurring Aphrodisiacs: Icariin and Its Derivatives

Phytochemicals in Prostate Cancer: From Bioactive Molecules to Upcoming Therapeutic Agents

Baicalein suppresses the androgen receptor (AR)-mediated prostate cancer progression via inhibiting the AR N-C dimerization and AR-coactivators interaction

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