Icaritin inhibits the invasion and epithelial‐to‐mesenchymal transition of glioblastoma cells by targeting EMMPRIN via PTEN/AKt/HIF‐1<i>α</i> signalling

Xu, Bo; Jiang, Chunmiao; Han, Hongxing; Liu, Hong; Tang, Ming; Liu, Longxi; Ji, Wenyan; Lu, Xuechao; Yang, Xiuli; Zhang, Yunxu; Liu, Yongji

doi:10.1111/1440-1681.12488

Cited by 37 publications

(27 citation statements)

References 56 publications

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“…α‐Mangostin suppressed viability and EMT by downregulating the PI3K/Akt pathway in pancreatic cancer . Icaritin, a hydrolytic product of icariin that is isolated from members of the Epimedium genus , induced the trans‐differentiation of embryonic stem cells into cardiomyocytes, prevented steroid‐associated osteonecrosis and stimulated neuronal differentiation . Icaritin inhibited invasion and EMT via targeting the PTEN/Akt/HIF‐1α signaling pathway …”

Section: Small Molecules Against Emtmentioning

confidence: 99%

Small molecule inhibitors of epithelial‐mesenchymal transition for the treatment of cancer and fibrosis

Feng

Chen

Vaziri

et al. 2019

Medicinal Research Reviews

104

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Tissue fibrosis and cancer both lead to high morbidity and mortality worldwide; thus, effective therapeutic strategies are urgently needed. Because drug resistance has been widely reported in fibrotic tissue and cancer, developing a strategy to discover novel targets for targeted drug intervention is necessary for the effective treatment of fibrosis and cancer. Although many factors lead to fibrosis and cancer, pathophysiological analysis has demonstrated that tissue fibrosis and cancer share a common process of epithelial‐mesenchymal transition (EMT). EMT is associated with many mediators, including transcription factors (Snail, zinc‐finger E‐box‐binding protein and signal transducer and activator of transcription 3), signaling pathways (transforming growth factor‐β1, RAC‐α serine/threonine‐protein kinase, Wnt, nuclear factor‐kappa B, peroxisome proliferator‐activated receptor, Notch, and RAS), RNA‐binding proteins (ESRP1 and ESRP2) and microRNAs. Therefore, drugs targeting EMT may be a promising therapy against both fibrosis and tumors. A large number of compounds that are synthesized or derived from natural products and their derivatives suppress the EMT by targeting these mediators in fibrosis and cancer. By targeting EMT, these compounds exhibited anticancer effects in multiple cancer types, and some of them also showed antifibrotic effects. Therefore, drugs targeting EMT not only have both antifibrotic and anticancer effects but also exert effective therapeutic effects on multiorgan fibrosis and cancer, which provides effective therapy against fibrosis and cancer. Taken together, the results highlighted in this review provide new concepts for discovering new antifibrotic and antitumor drugs.

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Section: Small Molecules Against Emtmentioning

confidence: 99%

Small molecule inhibitors of epithelial‐mesenchymal transition for the treatment of cancer and fibrosis

Feng

Chen

Vaziri

et al. 2019

Medicinal Research Reviews

104

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“…[8][9][10][11] Icaritin was found to exert its anticancer activities by inhibiting cell viability, proliferation, invasion, migration, and inducing apoptosis of GBM cells. [11][12][13][14] However, whether icaritin affects the glycolysis in cancer cells remains unclear. In the current study, we investigated the effect of icaritin on glycolysis in GBM cells.…”

Section: Introductionmentioning

confidence: 99%

Icaritin inhibits glioblastoma cell viability and glycolysis by blocking the IL‐6/Stat3 pathway

Liang

Wang

2018

J of Cellular Biochemistry

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Glioblastoma (GBM) is a common and aggressive brain tumor that is associated with significant increase in glycolysis for energy production. Icaritin is a natural compound and exhibits anticancer activity in GBM. However, the effect of icaritin on glycolysis in GBM cells remains unclear. The aim of the current study was to investigate the effect of icaritin on glycolysis in GBM cells. The human GBM cell lines U87 and T98G were treated with icaritin or the inhibitor of Stat3 (S3I‐201) in the presence or absence of recombinant human interleukin (IL)‐6. Cell viability was measured using the 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5 diphenyltetrazolium bromide (MTT) assay. The glycolysis was analyzed by detecting the glucose consumption and lactate production. The Western blot analysis was conducted to detect the expressions of hexokinase 2 (HK2), signal transducer and activator of transcription 3 (Stat3), p‐Stat3, and B lymphoma Mo‐MLV insertion region 1 (Bmi‐1). Results showed that icaritin inhibited the viability of U87 and T98G cells in a dose‐dependent manner. The decreased glucose consumption and lactate production, accompanied by reduced expressions of HK2, were found in both U87 and T98G cells. Icaritin inhibited the IL‐6/Stat3 pathway, which is evidenced by the decreased expressions of p‐Stat3 and Bmi‐1. IL‐6 treatment induced the phosphorylation of Stat3 and Bmi‐1 expression, increased cell viability, as well as elevated glucose consumption, lactate production, and HK2 expression; however, the effects of IL‐6 were attenuated by icaritin or S3I‐201 treatment. In conclusion, icaritin exerted inhibitory effects on cell viability and glycolysis in GBM cells, which was mediated by the IL‐6/Stat3 pathway.

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“…In that context; it was shown earlier that EMMPRIN can be a target in anticancer therapies against gliomas. For example; the flavonoid icaritin from the herb Epimedium genus inhibited the invasion of the glioblastoma cell line U87MG by targeting EMMPRIN via the PTEN/Akt/HIF-1alpha pathway [78]. Furthermore; the invasion of the glioblastoma cell line U251 was inhibited by antisense RNA of EMMPRIN [79].…”

Section: Discussionmentioning

confidence: 99%

Cerium Oxide Nanoparticles as Novel Tool in Glioma Treatment: An In vitro Study

Sack-Zschauer¹,

Bader²,

Brenneisen³

2017

J Nanomed Nanotechnol

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Icaritin inhibits the invasion and epithelial‐to‐mesenchymal transition of glioblastoma cells by targeting EMMPRIN via PTEN/AKt/HIF‐1α signalling

Cited by 37 publications

References 56 publications

Small molecule inhibitors of epithelial‐mesenchymal transition for the treatment of cancer and fibrosis

Small molecule inhibitors of epithelial‐mesenchymal transition for the treatment of cancer and fibrosis

Icaritin inhibits glioblastoma cell viability and glycolysis by blocking the IL‐6/Stat3 pathway

Cerium Oxide Nanoparticles as Novel Tool in Glioma Treatment: An In vitro Study

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