• The Korean Journal of Community Living Science
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• v.26 no.2
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• pp.405-414
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• 2015

This study examines the effects of purple Kohlrabi fresh and peel ethanol extracts on the antioxidative activity and antiproliferation of human cancer cells (Hep G2 human liver, HCT-116 human colon, and A549 human lung cancer cells.) The total flavonoid and anthocyanin content of purple Kohlrabi ethanol extracts were much greater in the peel than in the flesh. The DPPH radical scavenging activity and antioxidative index of purple Kohlrabi peel extracts were similar to those of the BHA and the BHT. Antiproliferation effects of purple Kohlrabi peel extracts on human cancer cells (Hep G2, HCT-116, and A549) strengthened in a dose-dependent manner. In particular, the antiproliferation activity of purple Kohlrabi peel extracts exceeded 40% in colon cancer cells. These results indicate that the purple Kohlrabi peel may contain bioactive compounds such as flavonoids as well as anthocyanin and that these compounds may facilitate cancer prevention.

• The Korean Journal of Community Living Science
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• v.26 no.1
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• pp.103-113
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• 2015

This study examines the effects of Korean Crataegi fructrus(KCF) and Chinese Crataegi fructrus(CCF) on the antioxidative activity and antiproliferation of human cancer cells(HCT-116 human colon, Hep G2 human liver, and A549 human lung cancer cells). The total polyphenol and flavonoid contents, and antioxidative index of the Crataegi fructrus ethanol extracts were significantly higher in KCF than in CCF. The DPPH radical-scavenging activity of the KCF ethanol extract was 82.26%(1000 ppm), and that of the CCF ethanol extract was 77.64%. Antiproliferation effects of 80% ethanol extracts of KCF and CCF on human cancer cells(HCT-116, Hep G2 and A549) increased in a dose-dependent manner. Inhibitory effects of KFC on HCT-116 and A549 cells were greater than those of CCF. The results suggest that ethanol extracts of Crataegi fructrus have antioxidative and hyperplasia inhibition effects on human cancer cells.

• Journal of the Korean Society of Food Science and Nutrition
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• v.38 no.12
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• pp.1672-1678
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• 2009

This study was carried out to investigate the total polyphenol, total flavonoid content, antioxidant activity, angiotensin I-converting enzyme (ACE) inhibitory activity, $\alpha$-glucosidase inhibitory activity, and antiproliferation activity of the citron seed. The citron seed were separated to hull and embryo, and extracted with n-hexane and 70% ethanol. Antioxidant activity of ethanol extract was higher than that of n-hexane extract. IC50 value for DPPH radical scavenging activity of ethanol extract of hull (CSE1) and embryo (CSE2) were 3.18 and 8.43 mg/mL, and those of total antioxidant activity were 19.96 and 11.28 mg AA eq/g, respectively. ACE inhibitory activity and $\alpha$-glucosidase inhibitory activity on CSE1 showed the highest values of 31.61 and 45.17%, respectively. Antiproliferation effects on the MCF7, HepG2, H460, HCT-116, and PC3 cell line showed the highest values of 14.09, 19.12, 12.29, 9.78, and 9.12% in extract concentration of 5 mg/mL, respectively. These results suggested that citron seed can be used for development of functional food material which have biological activities.

• Horticultural Science & Technology
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• v.28 no.5
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• pp.857-863
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• 2010

This study was conducted to evaluate the antioxidant activity, Angiotensin I Converting Enzyme (ACE) inhibitory activity, ${\alpha}$-glucosidase inhibitory activity, nitrate synthesis inhibitory activity, and antiproliferation inhibitory effect on ethanol extract and its solvent fractions of $Coreopsis$ $tinctoria$ Nutt. Ethyl acetate fraction was the strongest at 1,1-diphenyl-2-picryl hydrazyl (DPPH) ($IC_{50}=0.100mg{\cdot}mL^{-1}$) and 2,2'-Azino-bis-(3-ethylbenozothiazoline-6-sulfonic acid) (ABTS) (15.785 mg AA $eq{\cdot}10mg^{-1}$) radical scavenging activity, ACE (40.96% at $1mg{\cdot}mL^{-1}$), and ${\alpha}$-glucosidase ($IC_{50}=0.125mg{\cdot}mL^{-1}$) inhibitory effect among the solvent fractions. Nitrate synthesis inhibitory activity of ethanol extract, chloroform fraction, and ethyl acetate fraction effectively inhibited NO formation in a dose-dependent manner without the cytotoxic effect. Ethanol extract and its solvent fractions inhibited growth of HCT-116 colon cancer cells in a dose-dependent manner. n-Hexane fraction showed the highest antiproliferation inhibitory effect of $0.041mg{\cdot}mL^{-1}$ among fractions.

• Archives of Pharmacal Research
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• v.29 no.5
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• pp.354-362
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• 2006

Dietary flavonoids have attracted a great deal of attention as agents for preventing estrogen-related diseases, such as postmenopausal symptoms, and for reducing the risk of estrogen-dependent cancer. Kaempferol is one of the most commonly found dietary phytoestrogen. The aim of this study was to investigate the estrogenic and/or antiestrogenic effect of kaempferol, which can confirm its potency as a preventive agent against estrogen-related diseases. Kaempferol has both estrogenic and antiestrogenic activity, which are biphasic response on estrogen receptor. The estrogenic activity of kaempferol induced via ER-mediated pathway depending on $E_2$ concentration $(\leq\;10^{-12}M)$. Kaempferol $(10^{-5}\;M)$ also caused antiproliferative effect on MCF-7 cell in the presence of $E_2\;(10^{-11}\;M)$ and restored to the addition of excess $E_2\;(10^{-7}\;M)$, which confirms that antiproliferation of kaempferol was induced via ER-dependent pathway. However, at $10^{-4}\;M$, concentration higher than the concentrations at which the estrogenic effects of kaempferol are detected $(10^{-5}\;M)$, kaempferol induced strong antiproliferative effect, but were unaffected by the addition of excess $E_2\;(10^{-7}\;M)$ indicating that kaempferol exerts antiproliferation via ER-independent pathway. In particular, kaempferol blocked the focus formation induced by $E_2$, which confirms that kaempferol might inhibit the malignant transformation caused by estrogens. Therefore, we suggested that kaempferol might regulate a suitable level of estrogenic activity in the body and is expected to have potential beneficial effects in preventing estrogen imbalance diseases (breast cancer, osteoporosis, cardiovascular disease and etc.).

• Journal of the Korean Society of Food Science and Nutrition
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• v.43 no.5
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• pp.682-689
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• 2014

This study was carried out to discriminate the effects of the ramie leaf according to the drying methods (hot air drying and freeze drying) on antioxidative activity in vitro and antiproliferation in human cancer cells. There were no significant differences in total polyphenol content of ramie leaf ethanol extracts depending on the drying methods, but total flavonoid content was significantly higher in hot air dried ramie leaf (HR) than in freeze dried ramie leaf (FR). The DPPH radical scavenging activity of HR and FR ethanol extracts were found to be 77.74%, and 77.29% in 1000 ppm, respectively. Antioxidative index of HR and FR ethanol extracts measured by Rancimat were lower than those in BHT, BHA, and ascorbic acid, but were higher than that in control. The antiproliferation effect of 80% ethanol extracts of HR and FR on liver cancer cell line (H460), stomach cancer cell line (AGS), and lung cancer cell line (A549) were increased with a dose-dependent manner. The cancer cell growth inhibition activities of HR and FR ethanol extracts at the concentration of $800{\mu}g/mL$ showed greater than 80% on Hep G2 and A549 cell line, and greater than 75% on AGS cell line. These results suggest that HR and FR ethanol extracts possess potential antioxidative effect and antiproliferation in human cancer cells, and those activities of ramie leaf ethanol extracts depending on the drying methods were similar.

• Development and Reproduction
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• v.20 no.1
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• pp.1-10
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• 2016

Molecular targeting for the altered signaling pathways has been proven to be effective for the treatment of many types of human cancer, including colorectal cancer (CRC). The dual phosphatidylinositol-3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor BEZ235 has shown to exhibit potent antitumor activity against solid tumors. Autophagy is a cellular lysosomal catabolic process to maintain metabolic homeostasis, which has been known to be induced in response to many therapeutic agents in cancer cells. This process is negatively regulated by mTOR and often acts as prosurvival or prodeath mechanism following cancer therapeutics. The current study was designed to investigate the antiproliferation activity of BEZ235 and to evaluate the role of autophagy induced by BEZ235 using HCT15 CRC cells bearing ras oncogene mutation. We found that BEZ235 decreases cell viability, which was mostly dependent on $G_1$ arrest of cell cycle via suppression of cyclin A expression. BEZ235 affects PI3K/Akt/mTOR signaling pathway by increasing the phosphorylation of AKT at $Ser^{473}$ and RAS/RAF/MEK/ERK pathway by decreasing the phosphorylation of ERK at $Tyr^{204}$. BEZ235 also stimulated autophagy induction as evidenced by the increased expression of LC3-II and abundant acidic vesicular organelles (AVOs) in the cytoplasm. In addition, the combination of BEZ235 with autophagy inhibitor chloroquine, a known antagonist of autophagy, counteracted the antiproliferation effect of BEZ235. Thus, our study indicates that autophagy induced in response to BEZ235 treatment appears to act as cell death mechanism in HCT15 CRC cells.

• Food Science and Biotechnology
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• v.16 no.5
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• pp.802-806
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• 2007

There has been growing interest in the antioxidative and anticarcinogenic effects of vegetables. This study was aimed at evaluating the antioxidative and antiproliferative activities of 13 leafy vegetables consumed in Korea. New-beet and ornamental kale contained >1,000 mg of polyphenolics/100g fresh weight (FW), which was the greatest amount among the test vegetable extracts. Ornamental kale also contained the greatest amount (232.84 mg/100g FW) of flavonoids. With the exception of chicory, values of 1.1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical scavenging activities showed similar trends. New-beet was found to be the greatest antioxidant among the test vegetable extracts. New-beet exhibited the highest antiproliferative activity (>60%) against all tumor cells. No relationship was found between antiproliferative activity and antioxidant contents or antioxidant activities among samples.

• Journal of Ginseng Research
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• v.39 no.3
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• pp.274-278
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• 2015

Background: Steaming of ginseng is known to change its chemical composition and biological activity. This study was carried out to investigate the effect of different steaming time-scales on chemical constituents and antiproliferative activity of Vietnamese ginseng (VG). Methods: VG was steamed at $105^{\circ}C$ for 2-20 h. Its saponin constituents and antiproliferative activity were studied. The similarity of chemical compositions between steamed samples at $105^{\circ}C$ and $120^{\circ}C$ were compared. Results: Most protopanaxadiol and protopanaxatriol ginsenosides lost the sugar moiety at the C-20 position with 10-14 h steaming at $105^{\circ}C$ and changed to their less polar analogues. However, ocotillol (OCT) ginsenosides were reasonably stable to steaming process. Antiproliferative activity against A549 lung cancer cells was increased on steaming and reached its plateau after 12 h steaming. Conclusion: Steaming VG at $105^{\circ}C$ showed a similar tendency of chemical degradation to the steaming VG at $120^{\circ}C$ except the slower rate of reaction. Its rate was about one-third of the steaming at $120^{\circ}C$.

• BMB Reports
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• v.46 no.1
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• pp.59-64
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• 2013

Signal transducer and activator of transcription 3 (STAT3) and telomerase are considered attractive targets for anticancer therapy. The in vitro anticancer activity of the gold(I) compound auranofin was investigated using MDA-MB 231 human breast cancer cells, in which STAT3 is constitutively active. In cell culture, auranofin inhibited growth in a dose-dependent manner, and N-acetyl-L-cysteine (NAC), a scavenger of reactive oxygen species (ROS), markedly blocked the effect of auranofin. Incorporation of 5-bromo-2'-deoxyuridine into DNA and anchorage-independent cell growth on soft agar were decreased by auranofin treatment. STAT3 phosphorylation and telomerase activity were also attenuated in cells exposed to auranofin, but NAC pretreatment restored STAT3 phosphorylation and telomerase activity in these cells. These findings indicate that auranofin exerts in vitro antitumor effects in MDA-MB 231 cells and its activity involves inhibition of STAT3 and telomerase. Thus, auranofin shows potential as a novel anticancer drug that targets STAT3 and telomerase.