• Bulletin of the Korean Chemical Society
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• 제33권5호
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• pp.1586-1592
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• 2012

A series of Novel Mannich bases has been synthesized and evaluated $in$ $vitro$ cytotoxic activity against the human hepatocellular carcinoma (HepG2), human lung carcinoma (SK-LU-1), and human breast cancer (MCF-7). Compound $\mathbf{9f}$ was found to be most potent against three cell lines with $IC_{50}$ values of 1.57, 1.16 and 1.21 ${\mu}g$/mL, respectively. In addition, compounds $\mathbf{9g}$, $\mathbf{10f}$ exhibited very significant activity against MCF-7 cell line with $IC_{50}$ values of 2.0 ${\mu}g$/mL.

• 응용통계연구
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• 제24권4호
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• pp.609-622
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• 2011

The pattern of methylation draws significant attention from cancer researchers because it is believed that DNA methylation and gene expression have a causal relationship. As the interest in the role of methylation patterns in cancer studies (especially drug resistant cancers) increases, many studies have been done investigating the association between gene expression and methylation. However, a model-based approach is still in urgent need. We developed a finite mixture model in the Bayesian framework to find a possible relationship between gene expression and methylation. For inference, we employ Expectation-Maximization(EM) algorithm to deal with latent (unobserved) variable, producing estimates of parameters in the model. Then we validated our model through simulation study and then applied the method to real data: wild type and hydroxytamoxifen(OHT) resistant MCF7 breast cancer cell lines.

• Journal of Microbiology and Biotechnology
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• 제20권4호
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• pp.821-827
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• 2010

Gene delivery that provides targeted delivery of therapeutic genes to the cells of a lesion enhances therapeutic efficacy and reduces toxic side effects. This process is especially important in cancer therapy when it is advantageous to avoid unwanted damage to healthy normal cells. Incorporating cancer-specific ligands that recognize receptors overexpressed on cancer cells can increase selective binding and uptake and, as a result, increase targeted transgene expression. In this study, we investigated whether a peptide capable of homing to hepatocellular carcinoma (HCC) could facilitate targeted gene delivery by cationic liposomes. This homing peptide (HBP) exhibited selective binding to a human hepatocarcinoma cell line, HepG2, at a concentration ranging from 5 to 5,000 nM. When conjugated to a cationic liposome, HBP substantially increased cellular internalization of plasmid DNA to increase the transgene expression in HepG2 cells. In addition, there was no significant enhancement in gene transfer detected for other human cell lines tested, including THLE-3, AD293, and MCF-7 cells. Therefore, we demonstrate that HBP provides targeted gene delivery to HCC by cationic liposomes.

• Molecular & Cellular Toxicology
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• 제5권1호
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• pp.67-74
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• 2009

Exposures to environmental chemicals that mimic endogenous hormones are proposed for a number of adverse health effects, including infertility, abnormal prenatal and childhood development and above all cancers. In addition, recently miRNA (micro RNA) has been recognized to play an important role in various diseases and in cellular and molecular responses to toxicants. In this study, endocrine disrupting environmental toxicant, nonylphenol (NP) was treated to MCF-7 (Human breast cancer cell) and HepG2 (Human hepatocellular liver carcinoma) cell line at 3 hrs and 48 hrs time point and miRNA analysis using $mirVana^{TM}$ miRNA bioarray was performed and compared with total mRNA microarray data for the same cell line and treatment. Robust data quality was achieved through the use of dye-swap. Analysis of microarray data identifies a total of 20 and 11 miRNA expressions at 3 hrs and 48 hrs exposure to NP in MCF-7 cell line and a total of 14 and 47 miRNA expression at 3 hrs and 48 hrs exposure respectively to NP in HepG2 cell line. Expression profiling of the selected miRNA (let-7c, miR-16, miR-195, miR-200b, miR200c, miR-205, and miR-589) reveals changes in the expression of target genes related to metabolism, immune response, apoptosis, and cell differentiation. The present study can be informative and helpful to understand the role of miRNA in molecular mechanism of chemical toxicity and their influence on hormone dependent disease. Also this study may prove to be a valuable tool for screening potential estrogen mimicking pollutants in the environment.

• 한국식품영양학회지
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• 제25권3호
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• pp.447-453
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• 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.

• 한국식품영양과학회지
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• 제37권3호
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• pp.288-293
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• 2008

막걸리의 암 예방효과를 알아보기 위하여 막걸리 농축물을 핵산, 메탄올, 부탄올 및 물로 순차적으로 분획하여 각 분획별로 암세포에 대한 성장 억제효과와 암 예방 지표인 QR활성 증가 효과를 측정하였다. 그 결과 메탄올 분획물의 경우 낮은 농도의 시료첨가에도 불구하고 괄목할 만한 높은 암세포 성장 억제효과를 나타내었으며 4종의 모든 암세포주 HepG2, B16-F10, HT29 및 MCF-7에서 농도 의존적인 암세포 성장 억제효과를 나타내었다. 또한 HepG2에서 측정한 QR활성 증가 효과에 있어서도 메탄올 분획물이 가장 높은 QR활성 증가 효과를 보여 암에 대한 예방효과가 기대된다. 따라서 앞으로 막걸리를 이용하여 항암관련 기능성식품을 개발할 수 있는 가능성이 보이며, 이를 위하여 특히 메탄올 분획물에 대한 집중적인 연구가 요구된다.

• Natural Product Sciences
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• 제16권1호
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• pp.43-49
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• 2010

Thirty-two methanol extracts of thirty-one Vietnamese medicinal plants were evaluated for the cytotoxic activity against five human cancer cell lines, including A549, MCF-7, HT 1080, Huh-7, and HepG2. Of these, the nine extracts of Acanthopanax trifoliatus (4), Acanthopanax gracilistylus (5), Siegesbeckia orientalis (10), Betula alnoides (11), Passiflora edulis (18), Zanthoxylum simulans (leaf, 23), Adenosma caeruleum (26), Solanum verbascifolium (29), and Alpinia malaccensis (31), exhibited high potent cytotoxic activity showing a certain degree of selectivity against the different cell types, with $IC_{50}$ values ranging from 2.1 to $3.8\;{\mu}g/mL$.

• 한국식품과학회지
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• 제46권6호
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• pp.665-670
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• 2014

오미자 추출물의 n-hexane 분획으로부터 open column chromatography, 분취용 HPLC 등 여러 가지 크로마토그라피를 이용하여 총 15종의 화합물을 분리하였다. 분리된 화합물들은 각각의 기기분석 데이터를 문헌치와 비교하여, 각각 wuweizisu C (1), gomisin N (2), deoxyschisandrin (3), gomisin A (4), schisandrin (5), chamigrenal (6), schisanlactone D (7), methylgomisin O (8), angeloylgomisin O (9), (-)-gomisin $L_2$ (10), schisandronic acid (11), (-)-gomisin $L_1$ (12), (+)-gomisin $K_3$ (13), gomisin J (14), tigloylgomisin H (15)으로 동정하였다. 이들 중 methylgomisin O (8)는 이 식물에서 처음으로 분리되었다. 분리된 화합물들은 HL-60 (human leukemia), HeLa (human cervical carcinoma) 및 MCF-7 (breast cancer cells) 세포주에 대하여 세포독성 실험을 실시하였다. 그 결과 화합물 7, 8 및 9는 HL-60 세포주에 대하여 각각 7.37, 6.60 및 $8.00{\mu}M$의 $IC_{50}$로 비교적 강한 세포독성 효과를 나타냈다. 화합물 6은 MCF-7에 대하여 $IC_{50}$ $30.50{\mu}M$로 적정한 세포독성을 나타냈다. 그리고 화합물 8은 HeLa cells에 대하여 $IC_{50}$ $1.46{\mu}M$로 비교적 강한 세포 독성으로 나타냈다.

• 한국식품저장유통학회지
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• 제10권3호
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• pp.394-400
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• 2003

가시오갈피 (Eleutherococcus senticosus Maxim) 열매의 에탄올 추출물 및 분획물의 항돌연변이원성 및 항암활성을 규명하였다. 항돌연변이원성 실험결과에서는 직접변이원인 MNNG, 4NQO 그리고 간접변이원인 B($\alpha$)p, Trp-P-1에 대해서 농도 의존적인 돌연변이 억제활성을 나타내었다. MNNG (0.4 $\mu\textrm{g}$/plate)의 격우 S. typhimurium TA100 균주에서는 시료농도 200$\mu\textrm{g}$/plate에서 클로로포름 분획물을 제외한 모든 분획물들에서 90%이상의 높은 억제효과를 나타내었다. 4NQO (0.15 $\mu\textrm{g}$/plate)에 대한 S. typhimurium TA98 균주의 경우 물 분획물의 경우 83.3%, TA100 균주에서는 에틸 아세테이트 분획물이 84.4%의 억제효과를 보였다. 간접변이원의 경우 B($\alpha$)P (10$\mu\textrm{g}$/plate)에서는 에탄을 추출물과 핵산 분획물은 시료농도 200$\mu\textrm{g}$/plate에 각각 96.1%와 97.5%로 가장 높은 억제효과를 나타내었다. 그리고 Trp-P-1 (0.15 $\mu\textrm{g}$/plate)에서는 TA100 균주의 경우 200 $\mu\textrm{g}$/plate 농도에서 에탄을 추출물과 물 분획물이 각각 95.5%차 90%로 높은 억제율을 보여주었고, TA98 균주에 대해서는 에틸아세테이트 분획물이 88.3%로 비교적 높은 억제효과를 나타내었다. 인간의 암세포인 폐암세포 (AS49), 위암세포 (AGS), 간암세포(Hep3B), 유방암세포(MCF-7)에 대한 세포독성 억제 효과를 검토한 결과 모든 암세포에서 각 분획물들은 1mg/mL 농도에서 60% 이상의 비교적 높은 암세포 성장 효과를 나타내었다. 특히 MCF-7에서 높은 암세포 성장억제 효과를 나타내었는데 핵산 분획물 (1 mg/mL)에서 92.7%의 높은 암세포 성장 억제 효과를 나타내었고 Hep3B에서는 부탄을 분획물 (1 mg/mL)에서 82%의 비교적 높은 성장억제효과를 나타내었다.

• Biomolecules & Therapeutics
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• 제28권5호
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• pp.473-481
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• 2020

Axl receptor tyrosine kinase has been implicated in cancer progression, invasion, and metastasis in various cancer types. Axl overexpression has been observed in many cancers, and selective inhibitors of Axl, including R428, may be promising therapeutic agents for several human cancers, such as breast, lung, and pancreatic cancers. Here, we examined the cell growth inhibition mediated by R428 and auranofin individually as well as in combination in the human breast cancer cell lines MCF-7 and MDA-MB-231 to identify new advanced combination treatments for human breast cancer. Our data showed that combination therapy with R428 and auranofin markedly inhibited cancer cell proliferation. Isobologram analyses of these cells indicated a clear synergism between R428 and auranofin with a combination index value of 0.73. The combination treatment promoted apoptosis as indicated by caspase 3 activation and poly (ADP-ribose) polymerase cleavage. Cancer cell migration was also significantly inhibited by this combination treatment. Moreover, we found that combination therapy significantly increased the expression level of Bax, a mitochondrial proapoptotic factor, but decreased that of the X-linked inhibitor of apoptosis protein. Furthermore, the suppression of cell viability and induction of Bax expression by the combination treatment were recovered by treatment with N-acetylcysteine. In conclusion, our data demonstrated that combined treatment with R428 and auranofin synergistically induced apoptosis in human breast cancer cells and may thus serve as a novel and valuable approach for cancer therapy.