Galangin induces human colon cancer cell death via the mitochondrial dysfunction and caspase-dependent pathway

Ha, Tae Kwon; Kim, Mi Eun; Yoon, Ju Hwa; Bae, Sung Jin; JiHye, Yeom; Lee, Jun Sik

doi:10.1177/1535370213497882

Cited by 64 publications

(39 citation statements)

References 16 publications

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“…It has been reported that galangin plays a proliferation suppressive role in various tumors [5-7, 9-12, 27-32]. For instance, Wen et al [12] reported that galangin inhibits proliferation of hepatocellular carcinoma cells by inducing mitochondrial dysfunction via upregulation of Bax and downregulation of Bcl-2, as well as upregulation of p21, p27, and p53.…”

Section: Discussionmentioning

confidence: 99%

“…1a), a naturally occurring bioflavonoid, is present at high concentration in the rhizome of Alpinia officinarum (Hance), which has been used in China for centuries as a traditional medicine for a variety of ailments such as stomach ache, colds, circulatory system, and vomit [4]. Galangin has anti-proliferative effects on several types of tumors including colon cancer [5], ovarian cancer cells [6], melanoma [7, 8], hepatocellular carcinoma cells [9-12], and promyelocytic leukemia [13]. …”

Section: Introductionmentioning

confidence: 99%

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Galangin Induces Apoptosis in MCF-7 Human Breast Cancer Cells Through Mitochondrial Pathway and Phosphatidylinositol 3-Kinase/Akt Inhibition

et al. 2018

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Aims: The study aimed to investigate the molecular mechanism of inhibition of proliferation and apoptosis induction by galangin against MCF-7 human breast cancer cells. Methods: Cell Counting Kit-8 assay was used to assess cell viability and flow cytometry was used to detect cell apoptosis. The expression level of apoptosis-related proteins (cleaved-caspase-9, cleaved-caspase-8, cleaved-caspase-3, Bad, cleaved-Bid, Bcl-2, Bax, p-phosphatidylinositol 3-kinase [PI3K], and p-Akt) and cell cycle-related proteins (cyclin D3, cyclin B1, cyclin-dependent kinases CDK1, CDK2, CDK4, p21, p27, p53) were evaluated by Western blotting. Results: Galangin increased the expression of Bax and decreased the expression of Bcl-2 in a concentration-dependent manner, inhibited cell viability, and induced apoptosis. Meanwhile, the expression of cleavage of caspase-9, caspase-8, caspase-3, Bid, and Bad increased significantly while the expression of p-PI3K and p-Akt proteins decreased. In addition, the protein levels of cyclin D3, cyclin B1, CDK1, CDK2, and CDK4 were downregulated while the expression levels of p21, p27, and p53 were upregulated significantly. Conclusion: Galangin could suppress the viability of MCF-7 cells and induce cell apoptosis via the mitochondrial pathway and PI3K/Akt inhibition as well as cell cycle arrest.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Galangin Induces Apoptosis in MCF-7 Human Breast Cancer Cells Through Mitochondrial Pathway and Phosphatidylinositol 3-Kinase/Akt Inhibition

et al. 2018

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“…Epicatechin Gallate, a polyphenol from tea catechins induces cell death via p53 activation and stimulation of p38 and JNK in human colon cancer SW480 cells (Cordero-Herrera et al, 2013). Galangin is a member of flavonols and found in Alpinia officinarum induces apoptosis mediated by caspase 3 and 9 in colon cancer (HCT-15 and HT-29) cell lines (Ha et al, 2013).…”

Section: Apoptosis and Crcmentioning

confidence: 99%

Dietary Non-nutritive Factors in Targeting of Regulatory Molecules in Colorectal Cancer: An Update

Pandurangan

Esa²

2013

Asian Pacific Journal of Cancer Prevention

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Colorectal cancer (CRC), a complex multi-step process involving progressive disruption of homeostatic mechanisms controlling intestinal epithelial proliferation/inflammation, differentiation, and programmed cell death, is the third most common malignant neoplasm worldwide. A number of promising targets such as inducible nitric acid (iNOS), cyclooxygenase (COX)-2, NF-E2-related factor 2 (Nrf2), Wnt/β-catenin, Notch and apoptotic signaling have been identified by researchers as useful targets to prevent or therapeutically inhibit colon cancer development. In this review article, we aimed to explore the current targets available to eliminate colon cancer with an update of dietary and non-nutritional compounds that could be of potential use for interaction with regulatory molecules to prevent CRC.

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“…This was consistent with previous reports of the anticancer activity of galangin in several cancer cell lines. 19,20) Because of the cytotoxic effects, the experiments to verify the antimelanogenic effects of cells required careful selection of the conditions. However, the IC 50 value of galangin was very low when tested in a cell-free system that showed no cytotoxic effects.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of Antimelanogenic Activity and Mechanism of Galangin <i>in Silico</i> and <i>in Vivo</i>

Chung

Jeong

Lee

et al. 2018

Biological & Pharmaceutical Bulletin

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Abnormal pigmentation owing to excessive melanin synthesis can result in serious problems such as freckles, age-spots, and melanoma. Tyrosinase inhibitors have been an interesting target for the treatment of hyperpigmentation because tyrosinase is the rate-limiting enzyme in melanin synthesis. The screening for strong tyrosinase inhibitors led to the finding of the flavonoid galangin, which showed notable inhibitory effects on mushroom tyrosinase. The IC 50 value of galangin (3.55 0.39 µM) was lower than that of kojic acid (48.55 1.79 µM), which was used as a positive control. In silico docking simulation and mechanistic studies demonstrated that galangin interacted with the catalytic sites of tyrosinase and competed with tyrosine. In B16F10 melanoma cells stimulated with α-melanocyte stimulating hormone, galangin inhibited tyrosinase activity as well as melanin production. Although high doses of galangin were cytotoxic, no cytotoxic effects were observed at low doses. In addition, the in vivo efficacy of galangin was evaluated in HRM2 melaninpossessing hairless mice. As measured by the skin-whitening index and melanin staining, repeated UVB exposure increased skin melanin synthesis. Galangin application significantly reduced melanogenesis induced by UVB exposure. Collectively, our data indicates that galangin shows strong tyrosinase inhibition activity, which suggests that it may be an effective skin-whitening agent.Key words galangin; melanogenesis; pigmentation; tyrosinase Galangin, a flavonoid compound, is found in high concentrations in Alpinia officinarum and Helichrysum aureonitens.

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Galangin induces human colon cancer cell death via the mitochondrial dysfunction and caspase-dependent pathway

Cited by 64 publications

References 16 publications

Galangin Induces Apoptosis in MCF-7 Human Breast Cancer Cells Through Mitochondrial Pathway and Phosphatidylinositol 3-Kinase/Akt Inhibition

Galangin Induces Apoptosis in MCF-7 Human Breast Cancer Cells Through Mitochondrial Pathway and Phosphatidylinositol 3-Kinase/Akt Inhibition

Dietary Non-nutritive Factors in Targeting of Regulatory Molecules in Colorectal Cancer: An Update

Evaluation of Antimelanogenic Activity and Mechanism of Galangin <i>in Silico</i> and <i>in Vivo</i>

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