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

He, Jun; Wang, Yan; Duan, Fei; Jiang, Hao; Chen, Minfeng; Tang, Siyuan

doi:10.1055/s-0030-1250042

Cited by 51 publications

(42 citation statements)

References 40 publications

(52 reference statements)

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“…The present study demonstrated that icaritin inhibits Bcl-2 protein expression in COLO-205 cells. A previous study also reported that icaritin induces the apoptosis of HepG2 cells through modulating the Bax/Bcl-2 ratio (18) and that of breast cancer cells through the downregulation of Bcl-2 expression (16). In present study, icaritin significantly inhibited Bcl-2 expression in COLO-205 cells.…”

Section: Discussionsupporting

confidence: 74%

“…Previous reports have also demonstrated that icaritin's active ingredients can induce G1 phase retardation in prostate cancer cells, and cell growth was significantly inhibited as a consequence (17). Extensive research demonstrated that the active ingredients of icaritin can alter the extracellular signal-regulated kinase Anticancer effect of icaritin inhibits cell growth of colon cancer through reactive oxygen species, Bcl-2 and cyclin D1/E signaling signaling pathway of liver cancer cells (16,18). All the above results confirmed that icaritin has certain antitumor effects.…”

Section: Introductionmentioning

confidence: 98%

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Anticancer effect of icaritin inhibits cell growth of colon cancer through reactive oxygen species, Bcl-2 and cyclin D1/E signaling

Peng

Song

et al. 2016

Oncology Letters

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Abstract. Icaritin has an advantage in enhancing immunity. Besides, with its anticancer effect, it may be of great help in cancer treatment and recovery of cancer patients. As a result, icaritin is likely to become a novel anticancer drug. However, the anticancer effect of icaritin against colon cancer has not been elucidated thus far. The present study investigated the latent anticancer effect of icaritin on the inhibition of colon cancer cell growth by regulating reactive oxygen species (ROS), B-cell lymphoma (Bcl)-2 and cyclin D1/E signaling. The COLO-205 colon cancer cell line was used as a colon cancer cell model in the present study. First, cell growth and apoptosis were measured to analyze the anticancer effect of icaritin against colon cancer. Next, the possible mechanism of icaritin against colon cancer, including ROS, Bcl-2, cyclin D1, cyclin E and caspase-3/9, was explored. The results revealed that icaritin could inhibit cell growth and induce the apoptosis of COLO-205 cells. In addition, icaritin significantly induced ROS generation, suppressed Bcl-2, cyclin D1 and cyclin E protein expression, and activated caspase-3/9 activity in COLO-205 cells. The present findings demonstrated that icaritin exerted antiproliferative and anticancer effects against colon cancer through the activation of ROS generation and the suppression of Bcl-2, cyclin D1 and cyclin E signaling.

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Section: Discussionsupporting

confidence: 74%

Section: Introductionmentioning

confidence: 98%

Anticancer effect of icaritin inhibits cell growth of colon cancer through reactive oxygen species, Bcl-2 and cyclin D1/E signaling

Peng

Song

et al. 2016

Oncology Letters

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“…Acta Pharmacologica Sinica npg tosis in many tumor cells, such as human endometrial cancer cells [6] , HepG 2 cells [20] , and human prostatic smooth muscle cells [19] . Icaritin caused sustained ERK1/2 activation and induced apoptosis in human endometrial cancer cells, and icaritin could also induce apoptosis in HepG2 cells via the JNK1 signaling pathway.…”

Section: Wwwchinapharcom Wang Xf Et Almentioning

confidence: 99%

“…Based on the inhibitory effects of icaritin on the expression of MMP-2 and MMP-9, icaritin may have potential as a treatment for patients with advanced osteosarcoma. According to previous studies, the mechanisms underlying the antitumor activity of icaritin include the induction of apoptosis by multiple signaling pathways [5,6,20,23] . The caspase (cysteinyl aspartate specific protease) family is involved in apoptotic signal transduction and plays an important role in regulating apoptosis [37,38] .…”

Section: Wwwchinapharcom Wang Xf Et Almentioning

confidence: 99%

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Icaritin suppresses the proliferation of human osteosarcoma cells in vitro by increasing apoptosis and decreasing MMP expression

Wang

2014

Acta Pharmacol Sin

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Aim: To explore whether icaritin, a prenylflavonoid derivative of the Chinese tonic herb Epimedium, could suppress the proliferation of human osteosarcoma cells in vitro, and to elucidate the mechanisms of the action. Methods: Human osteosarcoma SaOS 2 cell line was used in the present study. The proliferation of the cells was examined using MTT assay and immunofluorescence DAPI staining. Cell motility was studied with the scratch assay. Cell apoptosis was determined by Annexin V-FITC and PI double staining using flow cytometry. Western blotting and RT-PCR were used to measure the expression of mRNAs and proteins in the cells. Results: Icaritin (5-15 μmol/L) suppressed the proliferation of SaOS 2 cells in vitro in a dose-dependent manner. Furthermore, the cell motility was significantly decreased after exposure to icaritin. Moreover, icaritin (5 μmol/L) time-dependently induced the apoptosis of SaOS 2 cells, markedly suppressed MMP-2 and MMP-9 expression, upregulated caspase-3 and caspase-9 expression, and increased the level of cleaved caspase-3 in the cells. Co-exposure to the caspase-3 inhibitor zVAD-fmk (10 μmol/L) compromised the icaritininduced caspase-3 expression and apoptosis in SaOS 2 cells. Conclusion: Icaritin suppresses the proliferation of SaOS 2 human osteosarcoma cells by increasing apoptosis and downregulating MMP expression.

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New insights into the anticancer therapeutic potential of icaritin and its synthetic derivatives

Reyes‐Hernández,

Figueroa‐González,

Quintas‐Granados

et al. 2024

Drug Development Research

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Icaritin is a natural prenylated flavonoid derived from the Chinese herb Epimedium. The compound has shown antitumor effects in various cancers, especially hepatocellular carcinoma (HCC). Icaritin exerts its anticancer activity by modulating multiple signaling pathways, such as IL‐6/JAK/STAT3, ER‐α36, and NF‐κB, affecting the tumor microenvironment and immune system. Several clinical trials have evaluated the safety and efficacy of icaritin in advanced HCC patients with poor prognoses, who are unsuitable for conventional therapies. The results have demonstrated that icaritin can improve survival, delay progression, and produce clinical benefits in these patients, with a favorable safety profile and minimal adverse events. Moreover, icaritin can enhance the antitumor immune response by regulating the function and phenotype of various immune cells, such as CD8+ T cells, MDSCs, neutrophils, and macrophages. These findings suggest that icaritin is a promising candidate for immunotherapy in HCC and other cancers. However, further studies are needed to elucidate the molecular mechanisms and optimal dosing regimens of icaritin and its potential synergistic effects with other agents. Therefore, this comprehensive review of the scientific literature aims to summarize advances in the knowledge of icaritin in preclinical and clinical studies as well as the pharmacokinetic, metabolism, toxicity, and mechanisms action to recognize the main challenge, gaps, and opportunities to develop a medication that cancer patients can use. Thus, our main objective was to clarify the current state of icaritin for use as an anticancer drug.

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

Cited by 51 publications

References 40 publications

Anticancer effect of icaritin inhibits cell growth of colon cancer through reactive oxygen species, Bcl-2 and cyclin D1/E signaling

Anticancer effect of icaritin inhibits cell growth of colon cancer through reactive oxygen species, Bcl-2 and cyclin D1/E signaling

Icaritin suppresses the proliferation of human osteosarcoma cells in vitro by increasing apoptosis and decreasing MMP expression

New insights into the anticancer therapeutic potential of icaritin and its synthetic derivatives

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