• Proceedings of the Korean Society of Applied Pharmacology
• /
• 2003.11a
• /
• pp.90-90
• /
• 2003

The acetylation of histone is one of the mechanisms involved in the regulation of gene expression and is tightly controlled by two core enzymes, histone acetyltransferase (HAT) and deacetylase (HDAC). There are several reports that imbalance of HAT and HDAC activity is associated with abnormal behavior of the cells in morphology, cell cycle, differentiation, and carcinogenesis. Recently, an increasing number of structurally diverse HDAC inhibitors have been identified that inhibit proliferation and induce differentiation and/or apoptosis of tumor cells in vivo and in vitro. In this study, we have investigated the effects of novel HDAC inhibitors, IN2001 on ER positive and ER negative human breast cancer cell lines. The growth inhibition, cell cycle arrest and apoptosis of cells by HDAC inhibitors were determined using SRB assay, DNA fragmentation, and flow cytometry. We found that IN 2001 as well as Trichostatin A inhibited cell growth dose-dependently in both ER positive and ER negative human breast cancer cell lines. The growth inhibition with HDAC inhibitors was associated with profound morphological change. The result of cell cycle analysis after 24 h exposure of IN2001 showed G2-M cell cycle arrest in MCF-7 cell and apoptosis in T47D and MDA-MB-231 cell. In summary, IN2001 has antiproliferative effect on human breast cancer cells regardless of the expression of estrogen receptor. These findings heights the possibility of developing HDAC inhibitors as potential anticancer therapeutic agents for the treatment of breast cancer.

• Proceedings of the Korea Society of Environmental Toocicology Conference
• /
• 2003.10a
• /
• pp.180-180
• /
• 2003

The acetylation of histone is one of the mechanisms involved in the regulation of gene expression and is tightly controlled by two core enzymes, histone acetyltransferase (HAT) and deacetylase (HDAC). There are several reports that imbalance of HAT and HDAC activity is associated with abnormal behavior of the cells in morphology, cell cycle, differentiation, and carcinogenesis. Recently, an increasing number of structurally diverse HDAC inhibitors have been identified that inhibit proliferation and induce differentiation and/or apoptosis of tumor cells in vivo and in vitro. In this study, we have investigated the effects of novel HDAC inhibitors, IN2001 on ER positive and ER negative human breast cancer cell lines. The growth inhibition, cell cycle arrest and apoptosis of cells by HDAC inhibitors were determined using SRB assay, DNA fragmentation, and flow cytometry. We found that IN 2001 as well as Trichostatin A inhibited cell growth dose-dependently in both ER Positive and ER negative human breast cancer cell lines. The growth inhibition with HDAC inhibitors was associated with profound morphological change. The result of cell cycle analysis after 24 h exposure of IN2001 showed G2-M cell cycle arrest in MCF-7 cell and apoptosis in T47B and MDA-MB-231 cell. In summary, IN2001 has antiproliferative effect on human breast cancer cells regardless of the expression of estrogen receptor. These findings heights the possibility of developing HDAC inhibitors as potential anticancer therapeutic agents for the treatment of breast cancer.

• Asian Pacific Journal of Cancer Prevention
• /
• v.17 no.sup3
• /
• pp.125-130
• /
• 2016

Nepeta cataria L. has been used in traditional medicine of some countries. Here the cytotoxic and apoptogenic activity of methanol extracts, n-hexane, dichloromethane, ethyl acetate, n-butanol, and acqueous extracts and the essential oil obtained from the aerial parts of the plant were evaluated with PC3, DU-145 and MCF-7 cell lines. Cell viability, histograms of PI stained fragmented DNA in apoptotic cells and Western blot analysis of proteins involved in the cascade of apoptosis were compared in all samples. Thirty components were identified as volatile, representing 99.7% of essential oil composition after GC-MS analysis of the oil obtained from aerial parts of the N. cataria by hydro-distillation. The major oil components of the essential oil were nepetalactone stereoisomers. Comparing IC50 values showed estrogen receptor positive PC3 cells were more sensitive to the cytotoxic effects of N. cataria in comparison with low hormone-receptor presenting DU-145 cells. Among multiple extracts and essential oils of the plant, only the ethyl acetate extract could significantly decrease cell viability in PC3 cells, in a concentration dependent manner. Ethyl acetate extract of N. cataria treated cells showed a sub-G1 peak in PC3 cells in a concentration dependent manner that indicates the involvement of an apoptotic process in ethyl acetate extract-induced cell death. Western blotting analysis showed that in PC3 cells treated with ethyl acetate (48 h) caspase 3 and PARP were cleaved to active forms. Overall, the results suggest that further analytical elucidation of N. cataria in respect to finding new cytotoxic chemicals with anti-tumor activity is warranted.

• Food Science and Preservation
• /
• v.15 no.2
• /
• pp.274-279
• /
• 2008

This study investigated the antimutagenic and anticancer effects of soybean sauce (kanjang) supplemented with deep sea water and Sea Tangle. The Ames test indicated that kanjang had no mutagenicity but it significantly inhibited mutations induced by N-methyl-N'-nitro-N-nitrosoguanidine(MNNG) and 4-nitroquinoline-1-oxide (4NQO). Kanjang (200 ug/plate) with supplementary deep sea water and Sea Tangle had approximately 90.9% and 62.0% inhibitory effect, respectively, against mutagenesis of TA100 induced by MNNG and 4NQO. There was 61.7% inhibition of mutagenesis induced by 4NQO against the TA98 strain. Kanjang inhibited growth of cell lines of human cervical adenocarcinoma (HeLa), human hepatocellular carcinoma (Hep3B), human gastric carcinoma (AGS), human lung carcinoma (A549), and human breast adenocarcinoma (MCF-7) in a concentration-dependent manner. Treatment with kanjang supplemented with 1.0 mg/mL deep sea water had cytotoxicities of 69.4% 70.5% 55.6% 82.1 % and 73.2% against HeLa, Hep3B, AGS, A549 and MCF-7 cells respectively. In contrast kanjang supplemented with 1 mg/mL deep sea water had only $10{\sim}40%$ cytotoxicity on normal human embryonal kidney cells (293). Kanjang supplemented with deep sea water significantly inhibited tumor growth in mice injected sarcoma-180 cells. In particular, kanjang supplemented with deep sea water (25 mg/kg) inhibited tumor cell activity by 40.9%.

• Food Science and Biotechnology
• /
• v.16 no.4
• /
• pp.600-604
• /
• 2007

In this study, we first prepared 3 kinds of powders with different molecular masses from the crude protein-bound polysaccharide extract of Agraricus blazei Murill through ultrafiltration, followed by spray-drying. Then, the antitumor activities of the powders were analyzed. Size exclusion chromatography coupled with a multi-angle laser-light-scattering system showed the 3 powders had the following molecular ranges: below 10 kDa (SD-1), 10 to 150 kDa (SD-2), and above 150 kDa (SD-3), representing peak molecular weights of $8.26{\times}10^3,\;9.65{\times}10^4$, and $5.94{\times}10^6\;g/mol$, respectively. All the powders stimulated macrophage RAW264.7 cells to produce nitric oxide, of which SD-2 and SD-3 were superior to the crude extract powder (CP-SD), while SD-1 showed the lowest activity. Similar results were found for their cytotoxicities against human cancer cell lines (A549, MCF-7, and AGS), where the highest activity was obtained with the SD-2 treatment for 72 hr at $1,000\;{\mu}g/mL$. The MCF-7 cell line was less sensitive to the powders than the other cells. From this research we found that ultrafiltration, in combination with spray-drying, is applicable for preparing protein-bound polysaccharide powders with higher antitumor activities.

• Toxicological Research
• /
• v.22 no.4
• /
• pp.391-395
• /
• 2006

Flavonoids are polyphenolic compounds that are ubiquitous in plants. They have been shown to possess a variety of biological activities, such as antioxidant and anticancer. Reactive oxygen species (ROS) lead to damages of cellular molecules and it is the one of various factors to induce cancer. The one of flavonoids, Luteolin, was found to scavenge 1,1-diphenyl-2-piculhydrazyl (DPPH) radical and intracellular reactive oxygen species (ROS). Moreover luteolin showed protection on hamster lung fibroblast cells (V79-4 cell) damage induced by $H_2O_2$. And then it was investigated whether it may show cytotoxicity effect against various cancer cells by MTT, Luteolin at $10{\mu}g/ml$ showed the cell viability of 63.2%, 34.7%, 18.4% and 71.4% against NCl-H460, HeLa, U937 and MCF-7, respectively. As a result, luteolin shows more sensitive to U937 cells among the tested cancer cell lines. In summary, luteolin has antioxidant and cytotoxicity effect or various cancer cell lines.

• Food Science and Preservation
• /
• v.11 no.2
• /
• pp.214-220
• /
• 2004

This study was carried out to determine the antioxidative, antimutagenic, and anticancer effects of functional food manufactured from fermented soybean(FFMFS) using DPPH free radical donating method, Ames test and cytotoxicity, respectively. FFMFS extracted with ethanol and then further fractionated to n-hexane, chloroform, ethyl acetate(EtOAc), butanol and water, stepwise. Among five fractions, the EtOAc fractions showed highest electron donating activities (31.6 $\mu\textrm{g}$/mL). The inhibition rate of ethanol extract(200 $\mu\textrm{g}$/plate) of FFMFS in the S. typhimurium TA100 strain showed 84.8% against the mutagenesis induced by MNNG. In addition, the suppression of EtOAc fractions with same concentration of FFMFS the S. typhimurium TA98 and TA100 strains showed 88.7% and 92.8% inhibition against Trp-P-l, respectively. The cytotoxic effects of FFMFS against the cell lines with human lung carcinoma(A549), human gastric carcinoma(AGS) and human breast adenocarcinoma(MCF-7) were inhibited with the increase of the extract concentration. The treatment of 1.0 mg/mL FFMFS of EtOAc fraction showed strong cytotoxicities of 84.5%, 88.7% and 85.6% against A549, AGS and MCF-7, respectively.

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.37 no.3
• /
• pp.288-293
• /
• 2008

In this study, we investigated the anticancer activity of Makgeoly (MG). MG was fractionated into four fractions by using solvent partition method, affording hexane (MGH), methanol (MGM), butanol (MGB) and aquous (MGA) soluble fractions. We determined the cytotoxicity of these four fractions in four kinds of cancer cell lines, such as HepG2, MCF-7, B16-F10 and HT29 by MTT assay. Among the various fractions, the MGM showed the strongest cytotoxic effects on all cancer cell lines. The morphological changes such as membrane shrinking and blebbing of cells were also observed by MGM treatment in HepG2 cell. In addition, we observed quinone reductase (QR) activity stimulating effects in all fraction layers of MG on HepG2 cells. QR activity increased approximately 2.6 and 2.1 times in MGM and MGH treated HepG2 cell at $100{\mu}g/mL$, respectively, compared to that in control value. Although further studies are needed, the present work could suggest that the fin of MG has a potential to be used as a chemopreventive agent against cancer.

• The Korean Journal of Food And Nutrition
• /
• v.25 no.3
• /
• pp.447-453
• /
• 2012

Various types of tea are consumed as a popular beverage worldwide particularly in Asian countries such as Korea, China, and Japan. The purpose of this study was to investigate the mineral contents, antioxidant properties and anticancer activity of Yak-Sun tea that is prepared by six oriental medicinal herbs. The results of the mineral contents were as follows; Ca, Mg, and Na contents were higher than those of green tea, whereas Fe, P, and K contents were lower than those of green tea. The total phenolics and flavonoid content of the Yak-Sun tea were higher than those of green and black teas. The $IC_{50}$ values of DPPH radical, hydroxyl radical, hydrogen peroxide radical scavenging of Yak-Sun tea were 0.78, 1.58, and 2.04 $mg/m{\ell}$, respectively, whereas the radical scavenging values of ${\alpha}$-tocopherol was 0.06, 0.05, and 0.09 $mg/m{\ell}$, respectively. When cancer cells were treated with Yak-Sun tea, the anticancer activity increased in a dose dependent manner. HCT116 colon cancer cell lines were dramatically increased, as compared to other cancer cell lines, such as MCF-7, H460, and MKN45 cell lines. The results of this study demonstrated that Yak-Sun tea could function as a tea to enhance health conditions for antioxidant and anticancer activity.

• The Korean Journal of Food And Nutrition
• /
• v.26 no.4
• /
• pp.609-614
• /
• 2013

This study was carried out in order to investigate the functional properties of methanol extracts from two parts (root and fruit) of Xanthium strumarium by means of measuring the contents of total polyphenols and flavonoid as well as determining $ABTS{\cdot}^+$, DPPH radical scavenging activity, hydroxyl radical scavenging activity (OH${\cdot}$) and anticancer activity. The examination of physiologically active substances in the two parts revealed that the Xanthium strumarium fruit had high total polyphenol, flavonoid contents, $ABTS{\cdot}^+$ DPPH and hydroxyl radical scavenging activity. The Xanthium strumarium fruit has higher activities of anticancer activities on prostate cell lines compared to other cancer cell lines.