Anticancer Effects of Baicalein on Hepatocellular Carcinoma Cells

Zheng, Yijing; Liang, Yin; Grahn, Tan Hooi Min; Ye, Ai-Fang; Zhao, Yanrong; Zhang, Qiyu

doi:10.1002/ptr.5135

Cited by 55 publications

(51 citation statements)

References 19 publications

(20 reference statements)

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“…Previous studies have reported that baicalein could arrest the cell cycle of HCC cells at all three phase, including G0/G1, S and G2/M. For instance, Zheng et al [4] found that baicalein could induced G0/G1 arrest in Bel-7404 cell line; Yu et al [30] reported that baicalein cause cell cycle arrest at S phase in HepG2 and SMMC-7721 cell lines; whereas the Kuo et al [31] study showed baicalein exerted cytotoxic effect on J5 cells resulting in G2/M arrest, these previous studies indicated that there are substantial differences in mechanism of the cell cycle arrest induced by baicalein for different HCC cell lines.…”

Section: Discussionmentioning

confidence: 99%

“…1), a purified flavonoid compound with defined chemical structure extracted from the dry roots of Scutellaria radix that is a broadly used herb in China, has been demonstrated that it has potential anti-tumor effects on many types of cancer cells, including HCC [4]. Previous studies have demonstrated that baicalein can inhibit the growth, invasion and metastasis of HCC through inducing cell cycle arrest and apoptosis, autophagy via several cancer-related signaling or molecules including MEK/ERK, JNK, Bcl-2, mTOR, CD24, 12-LOX, NF-κB [5-11].…”

Section: Introductionmentioning

confidence: 99%

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Baicalein, a Natural Anti-Cancer Compound, Alters MicroRNA Expression Profiles in Bel-7402 Human Hepatocellular Carcinoma Cells

Bie

Sun

et al. 2017

Cell Physiol Biochem

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Background/Aims: Baicalein has been shown to possess significant anti-hepatoma activity by inhibiting cell proliferation. Whether the anti-proliferative effect of baicalein is related to its modulation of miRNA expression in hepatocellular carcinoma (HCC) is still unknown. Methods: The anti-proliferative effects of baicalein on HCC cell line Bel-7402 was assessed by detecting the proliferation activity, cell cycle distribution, expression changes of p21/CDKN1A, P27/CDKN1B, total Akt and phosphoryted AKT. Microarray analysis was conducted to determine the miRNA expression profiles in baicalein-treated or untreated Bel-7402 cells and then validated by qRT-PCR in two HCC cell lines (Bel-7402 and Hep3B). The gain-of-function of miR-3127-5p was performed by detecting anti-proliferative effects after transfecting miRNA mimics in cells. Finally, the expression level of miR-3127-5p in different HCC cell lines was determined by qRT-PCR. Results: Baicalein was able to inhibit the proliferation of Bel-7402 cells by inducing cell cycle arrest at the S and G2/M phase via up-regulating the expression of p21/CDKN1A and P27/CDKN1B and suppressing the PI3K/Akt pathway. Baicalein could alter the miRNA expression profiles in Bel-7402 cells. Putative target genes for differentially expressed miRNAs could be enriched in terms of cell proliferation regulation, cell cycle arrest and were mainly involved in MAPK, PI3K-Akt, Wnt, Hippo and mTOR signaling pathways. MiR- 3127-5p, one of up-regulated miRNAs, exhibits low expression level in several HCC cell lines and its overexpression could inhibit cell growth of Bel-7402 and Hep3B cell lines by inducing S phase arrest by up-regulating the expression of p21and P27 and repressing the PI3K/Akt pathway. Conclusions: Modulation of miRNA expression may be an important mechanism underlying the anti-hepatoma effects of baicalein.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Baicalein, a Natural Anti-Cancer Compound, Alters MicroRNA Expression Profiles in Bel-7402 Human Hepatocellular Carcinoma Cells

Bie

Sun

et al. 2017

Cell Physiol Biochem

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“…Balcalein is a flavonoid, originally isolated from the roots of Scutellaria baicalensis and Scutellaria lateriflora with anticancer activity (78)(79)(80). Apigenin, present in many plants, is a natural product belonging to the flavone class, structurally similar to balcalein and 4' ,5,7-trihydroxyflavanone.…”

Section: Plasminogen Activation System As Potential Therapeutic Targementioning

confidence: 99%

Plasminogen activation system in oral cancer: Relevance in prognosis and therapy (Review)

Wyganowska‐Świątkowska

Jankun

2015

International Journal of Oncology

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Abstract.Research on carcinogenesis and progress in cancer treatment have reduced mortality of cancer patients. Mortality rates decreased by 1.5% per year from 2001 through 2010 for most types of cancer in men and women. However, oral cancer is still a significant global health problem since incidence and mortality rates are increasing. Oral cavity cancer is ranked the 8th in men and the 14th in women based on data collected between 2006 and 2010 by the National Institute of Health. Furthermore, an increasing incidence of head and neck neoplasms, particularly the tongue cancer among young adults has been reported recently. It is most likely due to increasing human papillomavirus (HPV) infection or the early start of tobacco and alcohol consumption. Treatment of oral cancer patients is mainly surgical and often leads to esthetic and functional deformities, with severe impact on the quality of life. Thus, novel form of treatments and selection of patients with high and low risk of mortality is of high priority for clinical studies. The expression of proteolytic enzymes in tumor and stromal tissues has been shown to have prognostic significance in many human cancers and inhibiting proteolysis can reduce tumor growth in many in vivo and in vitro models. Plasmin, with its activators and inhibitors are of great importance in many human malignances and collectively are called plasminogen activation system (PAS). In this comprehensive review we examine expression, possible prognostic markers and importance for therapy of the PAS members in oral cancer. Literature review suggests that overexpression of urokinase and its receptor are markers of poor outcome, thus, their inhibition can be explored in oral cancer therapy. Role of plasminogen activator inhibitor (PAI-1) is complex and depends on its concentration. Overexpression of PAI-1 favors angiogenesis, metastasis and poor prognosis, although when applied in very high concentrations it inhibits angiogenesis and tumor growth, the phenomenon is described as the PAI-1 paradox.

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“…26,27 It possesses a direct cytotoxicity to a large panel of human malignant cell lines by inducing apoptotic cell death. [26][27][28][29][30][31] The anti-cancer properties of baicalein were recently shown to be mediated through the inhibition of cell growth and induction of apoptosis in HCT116 human colon cancer cells. 28 Cell viability was significantly decreased by treatment of baicalein in a concentration-dependent manner.…”

Section: Modulation Of Anti-tumor Activitymentioning

confidence: 99%

“…35 In hepatocellular carcinoma including H22, Bel-7404 and HepG2 cell lines, treatment with baicalein showed anticancer effects by regulating the transcription of cyclin D1 via a -catenin-dependent mechanism. 29 Baicalein also affects the invasion and expression of migration signaling molecules, such as matrix metalloproteinase (MMP)-2 and MMP-9 in human hepatoma cells. 36 According to recent studies, baicalein treatment showed inhibition of migration and invasion in gastric and cervical cancer cells via transforming growth factor- and extracellular signal-regulated kinase signal pathways, respectively.…”

Section: Modulation Of Anti-tumor Activitymentioning

confidence: 99%

Modulation of Colitis-associated Colon Tumorigenesis by Baicalein and Betaine

Kim¹,

Sung²,

Chung³

et al. 2014

Journal of Cancer Prevention

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In this review, we will summarize the current understanding of modulation of colitis-associated colon tumorigenesis by two natural products, baicalein and betaine, which have anti-inflammatory activities. Baicalein and betaine have been shown to provide various health benefits to organism in many ways. Baicalein is a phenolic flavonoid derived originally from the root of Scutellaria baicalensis Georgi. From ancient times, baicalein has widely been used in oriental medicines as an anti-inflammatory and anti-cancer therapy. Betaine, trimethylglycine, is an essential biochemical molecule of the methionine/homocysteine cycle and is synthesized by conversion of choline. Betaine is an important human nutrient obtained from various foods including sugar beet and lycium. Betaine has provided various health benefits including disease prevention. However, the action mechanisms of their activity remain poorly understood. Recent studies reported the effects of baicalein and betaine on cytotoxicity against colon cancer cells and chemically induced colitis-associated colon tumorigenesis in mice. Administrations of baicalein and betaine containing diets significantly inhibited the incidence of tumors and hyperplasia with down-regulation of inflammation. Therefore, baicalein and betaine might be applicable to the prevention of inflammation-associated colon carcinogenesis.

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Anticancer Effects of Baicalein on Hepatocellular Carcinoma Cells

Cited by 55 publications

References 19 publications

Baicalein, a Natural Anti-Cancer Compound, Alters MicroRNA Expression Profiles in Bel-7402 Human Hepatocellular Carcinoma Cells

Baicalein, a Natural Anti-Cancer Compound, Alters MicroRNA Expression Profiles in Bel-7402 Human Hepatocellular Carcinoma Cells

Plasminogen activation system in oral cancer: Relevance in prognosis and therapy (Review)

Modulation of Colitis-associated Colon Tumorigenesis by Baicalein and Betaine

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