• 한국식품영양과학회지
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• 제31권5호
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• pp.905-909
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• 2002

일상생활에서 애용되고 있는 감자는 조리 시 껍질이 거의 폐기되고 있는 점을 감안하여, 폐기 농산물의 재활용의 측면에서 감자껍질(Solanum tubverosum Peel)을 수거하여 추출, 분획한 후 항균 및 항발암 효과를 살펴보았다. 항균성 검사로는 5가지의 균주에 대한 감자껍질의 분획물의 농도별 항균활성을 측정한 결과, 전반적으로 SPMEE에서 가장 큰 항균력을 보였으며, 특히 Pseudomonas aeruginosa 균주에서는 앞서 4가지 균에서는 활성이 없던 수층인 SPMA에서 항균활성이 크게 나타났다 감자껍질의 암세포 증식억제 효과를 MTT assay로 실험 한 결과,3종류의 암세포 HepG2, HeLa 및 MCF- 7세포주에서 모두 ethylether분획층인 SPMEE층에서 암세포 증식억제 효과가 크게 나타났으며 특히 MCF-7의 경우는 저농도 첨가 시부터 SPW층에서 높은 억제효과를 보였다. 또 HepG2세포를 이용한 감자껍질의 분획물의 암예방 QR 유도 활성효과를 본 결과, butanol 분획층인 SPMB에서 괄목할 만큼 높은 QR 유도 활성이 증가되었다. 본 실험 결과, 감자껍질에는 전반적으로 SPMEE층에서 높은 항균성을 보여 항균제로서의 개발가능성이 충분히 엿보이며, 나아가 암세포 증식억제효과도 SPMEE층에서 아주 컸다. SPMB와 SPMEA층에서도 그 효과가 돋보인다. 암을 예방하는 inducer는 SPMB층에 많이 존재하는 것으로 사료되며 이와 같은 연구결과를 기초로 하여 폐기 감자껍질을 이용한 단계적인 생리활성 물질의 분리 동정이 계속 이루어져 폐기식품 활용 및 건강 대체 식품 개발의 연구 대상으로서 기대가 되는 바이다.

• Asian Pacific Journal of Cancer Prevention
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• 제14권5호
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• pp.3191-3196
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• 2013

Leaf extracts of Cassia alata L (akapulko), traditionally used for treatment of a variety of diseases, were evaluated for their potential antitumor properties in vitro. MTT assays were used to examine the cytotoxic effects of crude extracts on five human cancer cell lines, namely MCF-7, derived from a breast carcinoma, SK-BR-3, another breast carcinoma, T24 a bladder carcinoma, Col 2, a colorectal carcinoma, and A549, a nonsmall cell lung adenocarcinoma. Hexane extracts showed remarkable cytotoxicity against MCF-7, T24, and Col 2 in a dose-dependent manner. This observation was confirmed by morphological investigation using light microscopy. Further bioassay-directed fractionation of the cytotoxic extract led to the isolation of a TLC-pure isolate labeled as f6l. Isolate f6l was further evaluated using MTT assay and morphological and biochemical investigations, which likewise showed selectivity to MCF-7, T24, and Col 2 cells with $IC_{50}$ values of 16, 17, and 17 ${\mu}g/ml$, respectively. Isolate f6l, however, showed no cytotoxicity towards the non-cancer Chinese hamster ovarian cell line (CHO-AA8). Cytochemical investigation using DAPI staining and biochemical investigation using terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL)-a method used to detect DNA fragmentation-together with caspase assay, demonstrated apoptotic cell death. Spectral characterization of isolate f6l revealed that it contained polyunsaturated fatty acid esters. Considering the cytotoxicity profile and its mode of action, f6l might represent a new promising compound with potential for development as an anticancer drug with low or no toxicity to non-cancer cells used in this study.

• Archives of Pharmacal Research
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• 제28권7호
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• pp.823-828
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• 2005

Multidrug resistance (MDR) is one of the most significant obstacles in cancer chemotherapy. One of the mechanisms involved in the development of MDR is the over-expression of P-glycoprotein (P-gp). It is widely known that natural compounds found in vegetables, fruits, plant-derived beverages and herbal dietary supplements not only have anticancer properties, but may also modulate P-gp activity. Therefore, the purpose of this investigation was to examine the effects of naturally occurring products on P-gp function in human breast cancer cell lines, MCF-7 (sensitive) and MCF-7/ADR (resistant). The accumulation of daunomycin (DNM), a P-gp substrate, was greater in the sensitive cells compared to the resistant cells, while the efflux of DNM was higher in the resistant cells compared to the sensitive cells over a period of 2h. The $IC_{50}$ value of DNM in the resistant cells was about 22 times higher than that in the sensitive cells, indicating an over-expression of P-gp in the resistant cells, MCF-7/ADR. All of the compounds tested, with the exception of fisetin, significantly decreased the $IC_{50}$ value of DNM. Biochanin A showed the greatest increase in $[^3H]-DNM$ accumulation, increasing by $454.3{\pm}19.5%$ in the resistant cells, whereas verapamil, the positive control, increased the accumulation by $229.4{\pm}17.6%$. Also, the accumulation of $[^3H]-DNM$ was increased substantially by quercetin and silymarin while it was reduced by fisetin. Moreover, biochanin A, silymarin, and naringenin significantly decreased DNM efflux from MCF-7/ADR cells compared with the control. These results suggest that some flavonoids such as biochanin A and silymarin may reverse MDR by inhibiting the P-gp function.

• 약학회지
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• 제39권6호
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• pp.681-688
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• 1995

An n-hexane extract of the roots of Aralia cordata Thunb. (Araliaceae) was found to show significant in vitro cytotoxic activity against P388D$_{1}$ lymphocytic leukemia cell in culture. Bioactivity-directed fractionation of this extract led to the isolation of four polyacetylenes, falcarindiol (1), dehydrofalcarindiol (2), falcarindiol-8-acetate (3) and dehydrofalcarindiol-8-acetate (4). Cytotoxicity of compounds 1 and 3 was found to be better than that of compounds 2 and 4 when these compounds were tested against eight in vitro tumor cell lines, namely, A549, HCT15, DLD1, MCF7, SKOV3, HL60, K562 and P388D$_{1}$. The fact that the cytotoxicity of compounds 1 and 3 against series of tumor cell lines was much stronger than that of compounds 2 and 4 suggested that the saturated carbon chain at the termial and the hydroxyl group at the C-3 are important for the activities. The requirement for the activity was further confirmed by synthesizing and assaying the acetate derivatives of compounds 1 and 2.

• 한국식품영양학회지
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• 제32권5호
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• pp.511-521
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• 2019

The purpose of this study was to investigate the inhibitory effect of enzyme activity and anti-proliferation of human cancer cell lines (HCT 116, NCI-H460 and MCF-7) of peanut skin depending on cultivars (Arachis hypogaea L. cv. K-Ol, cv. Sinpalkwang, cv. Daan, cv. Heuksaeng) and extraction solvent. Peanut skin was extracted with 80% ethanol, 80% methanol, 80% acetone, and distilled water, followed by analysis of the enzyme inhibitory activity and anticancer activity. Methanol extract of Daan cultivar most effectively inhibited ${\alpha}$-gluosidase (65.08%, 0.025 mg/mL), tyrosinase (82.49%, 2 mg/mL) and ACE (73.61%, 10 mg/mL). The inhibitory effect of peanut skin extracts on colon cancer cell (HCT-116), lung cancer cell (NCI-H460) and breast cancer cell (MCF-7) growth were investigate using MTT assay. The highest anti-proliferation of cancer cell line of peanut skin extracts was observed in the methanol extract of Daan cultivar. The cell viability on HCT 116, NCI-H460 and MCF-7 cell lines of methanol extracts from peanut skin of Daan cultivar was 48.13%, 41.03%, and 36.02% at $200{\mu}g/mL$, respectively. These results suggest that peanut skin extracts may mediate physiological activity, and provide valuable information for the use of peanut byproduct as a functional food material.

• Archives of Pharmacal Research
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• 제20권6호
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• pp.579-585
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• 1997

To gain further insight into the mechanism of action of antiestrogens, we examined the interaction of antiestrogen with the estrogen receptor system and with estrogen- noncompetable antiestrogen binding sites. In addition to binding directly to the estrogen receptor, antiestrogens can be found associated with binding sites that are distinct from the estrogen receptor. In contrast to the restriction of estrogen receptors to estrogen target cells, such as those of uterus and mammary glands, antiestrogen binding sites are present in equal amounts in estrogen receptor-positive and -negative human breast cancer cell lines, such as MCF-7, T47D, and MDA-MB-231 that differ markedly in their sensitivity to antiestrogens. In order to gain greater insight into the role of these antiestrogen binding sites in the action of antiestrogens, we have examined the biopotency of different antiestrogens for the antiestrogen binding sites and that is CI628 > tamoxifen > trans-hydroxy tamoxifen > CI628M > H1285 > LY117018. This order of affinities does not parallel the affinity of these compounds for the estrogen receptor nor the potency of these compounds as antiestrogens. Indeed, compounds with high affinity for the estrogen receptor and greatest antiestrogenic potency have low affinities for these antiestrogen binding sites. Antiestrogenic potency correlates best with estrogen receptor affinity and not with affinity for antiestrogen binding sites. In summary, our findings suggested that interaction with the estrogen receptor is most likely the mechanism through which antiestrogens evoke their growth inhibitory effects.

• Asian Pacific Journal of Cancer Prevention
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• 제16권13호
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• pp.5471-5476
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• 2015

2-deoxy-D-Glucose (2DG) causes cytotoxicity in cancer cells by disrupting thiol metabolism. It is an effective component in therapeutic strategies. It targets the metabolism of cancer cells with glycolysis inhibitory activity. On the other hand, MLN4924, a newly discovered investigational small molecule inhibitor of NAE (NEDD8 activating enzyme), inactivates SCF E3 ligase and causes accumulation of its substrates which triggers apoptosis. Combination of these components might provide a more efficient approach to treatment. In this research, 2DG and MLN4924 were co-applied to breast cancer cells (MCF-7 and SKBR-3) and cytotoxic and apoptotic activity were evaluated the by Micro culture tetrazolium test (MTT), TUNEL and ELISA methods. Caspase3 and Bcl2 genes expression were evaluated by real time Q-PCR methods. The results showed that MLN4924 and MLN4924/2DG dose-dependently suppressed the proliferation of MCF7 and SKBR-3 cells. Cell survival of breast cancer cells exposed to the combination of 2DG/MLN4924 was decreased significantly compared to controls (p<0.05), while 2DG and MLN4924 alone had less pronounced effects on the cells. The obtained results suggest that 2DG/MLN4924 is much more efficient in breast cancer cell lines with enhanced cytotoxicity via inducing a apoptosis cell signaling gene, caspase-3.

• Asian Pacific Journal of Cancer Prevention
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• 제15권20호
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• pp.8829-8836
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• 2014

Background: Cyclooxygenase-2 (COX-2), considered to have tumor-promoting potential, is highly expressed in a variety of tumors, including breast cancer. Since the functions and action mechanisms of COX-2 in breast cancer have not been fully elucidated, in the present study, the effects of target inhibiting COX-2 with recombinant adenovirus Ad-COX-2-shRNA on malignant biological behavior were investigated in representative cell lines. Materials and Methods: Breast cancer MDA-MB-231 and MCF-7 cells were transfected with Ad-COX-2-shRNA and COX-2 expression was tested by RT-PCR and Western blotting. Changes in proliferation, apoptosis and invasion of breast cancer cells were detected with various assays including MTT, colony forming, flowcytometry and Transwell invasion tests. The expression of related proteins involved in the cell cycle, apoptosis, invasion and signaling pathways was assessed by Western blotting. Results: COX-2 expression was significantly reduced in both breast cancer cell lines infected with Ad-COX-2-shRNA, with obvious inhibition of proliferation, colony forming rate, G2/M phase passage and invasion, as well as induction of apoptosis, in MDA-MB-231 and MCF-7 cells, respectively. At the same time, proteins related to the cell cycle, anti-apoptosis and invasion were significantly downregulated. In addition, c-myc expression and phosphorylation activation of Wnt/${\beta}$-catenin and p38MAPK pathways were reduced by the Ad-COX-2-shRNA. Conclusions: COX-2 expression is associated with proliferation, apoptosis and invasion of breast cancer cells, and its mechanisms of action involve regulating expression of c-myc through the p38MAPK and Wnt/${\beta}$-catenin pathways.

• 한국식품영양과학회지
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• 제30권1호
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• pp.80-85
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• 2001

Various lines of evidence suggest that dietary components protect the initiation step of carcinogenesis. In this study, the ethylacetate (PGMEA), ethylether (PGMEE), butanol (PGMB) and aqueous (PGMA) soluble fractions of Punica granatum L. (PG) were screened for their growth inhibition using the MTT assay on HepG2, HeLa, C6, MCF-7 and HT-29 cells and for their activity to induce quinone reductase (QR) in HepG2 cells. Among various fractions of Punica granatum L., the PGMEE showed the strongest growth inhibition at 500 $\mu\textrm{g}$/mL which resulted 92.5% on Hela cell lines and 97.8% on C6 cell lines. The PGMEA and PGMB also showed significant growth inhibition. The assay of QR induction on HepG2 cells, grown in the presence of PGMEE at the concentration of 50$\mu\textrm{g}$/mL, was 1.4 times more effective compared with the control value of1.0. These results suggested that useful cancer chemoprevention materials could be isolated from PGMEE fraction of Punica granatum L.

• Bulletin of the Korean Chemical Society
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• 제29권3호
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• pp.595-598
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• 2008

Emodin (3-methyl-1,6,8-trihydroxyanthraquinone) is a natural chemotherapeutic compound with diverse biological properties including an antitumor activity. Emodin, a specific inhibitor of the protein tyrosine kinase, has a number of cellular targets in related to it. Its inhibition activity affects the mammalian cell cycle regulation in specific oncogene. Practically, it has been proven to inhibit HER-2/neu tyrosine kinase expressing breast cancer cells as an anticancer agent. 2-[123I]iodoemodin has been synthesized and evaluated human breast cancer cells (MDA-MB-231, MCF-7, fibroblast as a control) which express basal levels of HER-2/neu tyrosine kinase to investigate its suitability as a breast cancer imaging agent and 2-iodoemodin has been synthesized as a standard compound. The radiochemical yield of the 2-[123I]iodoemodin was about 72% and its radiochemical purity was over 97% after purification. The radioactivity of the 2-[123I]iodoemodin was increased in a time dependent manner in both cell lines and the ratio of MDA-MB-231 and MCF7 to fibroblast was 2.9 and 1.7, respectively.