Cytotoxicity of flavones and flavonols to a human esophageal squamous cell carcinoma cell line (KYSE-510) by induction of G2/M arrest and apoptosis

Zhang, Qiang; Zhao, Xin‐Huai; Zhu-jun, Wang

doi:10.1016/j.tiv.2009.04.007

Cited by 167 publications

(131 citation statements)

References 40 publications

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“…Chrysin, the most abundant Free-B-Ring flavonoid in honey, was found to potentiate the antiproliferative effect of various chemotherapeutic agents (14). Furthermore, chrysin was found to be capable of inhibiting cell proliferation and inducing apoptosis in human cervical carcinoma (15), leukemia (16), esophageal squamous cell carcinoma (17), malignant glioma, breast carcinoma (18) and prostate cancer cell lines (19). To extend our knowledge of the antineoplastic role of chrysin, the present study demonstrated the ability of chrysin to induce colon cancer cell death more efficiently compared to 5-FU.…”

Section: Discussionmentioning

confidence: 99%

Free-B-Ring flavonoids as potential lead compounds for colon cancer therapy

Ibrahim

Sobeh

Ismail

et al. 2014

Molecular and Clinical Oncology

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Abstract. Although flavonoids have been identified as a versatile source of anticancer agents, to the best of our knowledge, no study has yet investigated their anticolon cancer activity in depth. Therefore, the aim of this study was to investigate the association between the structural characteristics of flavonoids and their anticolon cancer activity in the Caco-2 human colon cancer cell line. Our findings demonstrated that the hydroxylation of C5 and C7 in ring A significantly enhanced the anticolon cancer activity of flavonoids over that of 5-fluorouracil, the classic reference cytotoxic agent. By contrast, the glycosylation or the presence of hydroxyl groups in ring B significantly decreased flavonoid anticancer activity. Collectively, these findings suggest a novel, rational design of flavonoid-related compounds that may improve the treatment of colorectal cancer.

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Section: Discussionmentioning

confidence: 99%

Free-B-Ring flavonoids as potential lead compounds for colon cancer therapy

Ibrahim

Sobeh

Ismail

et al. 2014

Molecular and Clinical Oncology

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“…These results suggest that hydroxytyrosol may prevent cancer by efficiently preventing the mutagenic activity caused by oxidative stress, or may interfere with other steps inducing cell cycle arrest, thereby reducing the growth and proliferation of cancerous cells and subsequently, inducing apoptosis and necrosis death. Other major components of the studied extracts such as oleuropein, hydroxytyrosol, hydroxytyrosol acetate, and the flavonoids luteolin, luteolin-7-O-glucoside, and luteolin-49-O-glucoside also induce cell cycle arrest [65][66][67][68][69]. Several cell cycle regulators such as p27 and p53 have been identified as potential prognostic markers for the outcome of HCC [70][71][72].…”

Section: Discussionmentioning

confidence: 99%

Olive Leaves and Mill Waste Exert Anti-Tumoral Properties in Hepatoma Cell Line

2014

J Carcinog & Mutagen

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Different phenolic compounds such as oleuropein and hydroxytyrosol have demonstrated antitumoral activity in cancer cell lines. Olive derivatives have demonstrated beneficial properties in cardiovascular diseases. The study was addressed to show the potential beneficial properties of olive leaves and olive oil mill waste extracts in hepatoma cell lines. Aflatoxin B1 (AFB1) was administered to hepatoma cell line (HepG2). Different parameters related to cell death, cell proliferation and DNA damage were determined. The expression of p53 and c-Src (activated and inhibitory phosphorylated state) was assessed by Western blot analysis in HepG2. The olive leaves and olive oil mill waste extracts contained oleuropein and hydroxytyrosol, respectively. AFB1 induced cell proliferation and death, associated to a rise on p53 and c-Src expression in HepG2 cells. Oleuropein and hydroxytyrosol reduced cell necrosis and DNA damage in HepG2 cells. However, the administration of olive leaves and olive oil mill waste extracts increased cell necrosis, DNA damage. These effects of natural extracts were associated with a reduction of activated c-Src expression and cell proliferation in AFB1-treated HepG2 cells. These results support that olive leaves extract and olive oil mill waste extracts, but not oleuropein and hydroxytyrosol, may exert antitumoral effect against a hepatoma cancer cell line.

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“…Other secondary metabolites of class of flavones, such as apigenin, luteolin and tangertin, with anticancer properties blocked the cell cycle either in the G 0 /G1 phase (33,34) or in the G 2 /M phase (35)(36)(37). Since most of the antineoplastic drugs in clinical use block the cell cycle in the S or G 2 /M phases whereas chrysin blocks the cell cycle in the G 1 phase, a combination of chrysin with currently used drugs might possibly improve melanoma therapies.…”

Section: Discussionmentioning

confidence: 99%

Acacia honey and chrysin reduce proliferation of melanoma cells through alterations in cell cycle progression

Canini¹

2010

Int J Oncol

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Abstract. Honey has long been used in medicine for different purposes. Only recently, however, its antioxidant property and preventive effects against different diseases, such as cancer, have been highlighted. Chrysin (5,7-dihydroxyflavone) is a natural flavone commonly found in acacia honey. It has previously been shown to be an anti-tumor agent. In this study, we investigated the antiproliferative role of honey or chrysin on human (A375) and murine (B16-F1) melanoma cell lines. The results of the 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay and the trypan blue exclusion test showed that both the tested compounds were able to induce an antiproliferative effect on melanoma cells in a dose-and time-dependent manner. Flow cytometry analysis indicated that cytotoxicity induced by honey or chrysin was mediated by G 0 /G 1 cell cycle arrest and induction of hyperploid progression. Our results suggest that the anti-proliferative effects of honey are due mainly to the presence of chrysin. Chrysin may therefore be considered a potential candidate for both cancer prevention and treatment. Further investigation is needed to validate the contribution of chrysin in tumor therapy in vivo.

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Cytotoxicity of flavones and flavonols to a human esophageal squamous cell carcinoma cell line (KYSE-510) by induction of G2/M arrest and apoptosis

Cited by 167 publications

References 40 publications

Free-B-Ring flavonoids as potential lead compounds for colon cancer therapy

Free-B-Ring flavonoids as potential lead compounds for colon cancer therapy

Olive Leaves and Mill Waste Exert Anti-Tumoral Properties in Hepatoma Cell Line

Acacia honey and chrysin reduce proliferation of melanoma cells through alterations in cell cycle progression

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