• Archives of Pharmacal Research
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• v.24 no.1
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• pp.16-20
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• 2001

2-(Allylthio)pyrazine derivatives were designed as a novel cancer chemopreventive agent that functions through selective inhibtion of cytochrome P-450 and induction of phase 11 enzymes involved in the detoxification of carcinogens. A practical preparation method of 2-(allylthio) pyrazine derivatives was established by the reaction of 2-mercaptopyrazine and allylbromides in the presence of a catalytic antioxidant, DABCO (1,4-diazabicyclo[2,2,2] octane), in dimethyl-formamide at below $50^{\circ}C$.

• Toxicological Research
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• v.33 no.4
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• pp.273-282
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• 2017

Chemoprevention entails the use of synthetic agents or naturally occurring dietary phytochemicals to prevent cancer development and progression. One promising chemopreventive agent, procyanidin, is a naturally occurring polyphenol that exhibits beneficial health effects including anti-inflammatory, antiproliferative, and antitumor activities. Currently, many preclinical reports suggest procyanidin as a promising lead compound for cancer prevention and treatment. As a potential anticancer agent, procyanidin has been shown to inhibit the proliferation of various cancer cells in "in vitro and in vivo". Procyanidin has numerous targets, many of which are components of intracellular signaling pathways, including proinflammatory mediators, regulators of cell survival and apoptosis, and angiogenic and metastatic mediators, and modulates a set of upstream kinases, transcription factors, and their regulators. Although remarkable progress characterizing the molecular mechanisms and targets underlying the anticancer properties of procyanidin has been made in the past decade, the chemopreventive targets or biomarkers of procyanidin action have not been completely elucidated. This review focuses on the apoptosis and tumor inhibitory effects of procyanidin with respect to its bioavailability.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.4
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• pp.1569-1573
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• 2012

Luteolin (LUT), a bioflavonoid has been used as a chemopreventive agent world-wide against chemically induced cancer. Hence we designed an experiment to assess chemopreventive action of LUT on lipid peroxidation (LPO) and glycoconjugates in azoxymethane (AOM)-induced colon carcinogenesis. Colon cancer was induced by 15 mg/body kg. body weight of AOM and administration of LUT (at the dose of 1.2 mg/kg. body weight) was till end of the study. Analysis of lipid peroxidative end products such as protein carbonyl (PC), malonadehyde (MDA) and conjucated dienes (CD) demonstrated significant increase in in AOM-induced animals with reduction by LUT (p<0.05). Increased levels of glycoconjugates such as hexose, hexosamine, sialic acid, fucose and mucoprotein were analyzed in serum and colon tissues examined histopathologically by periodic acid Schiff's (PAS) staining were also reversed by LUT l(p<0.05). The secondary marker of colon cancer mucin depleted foci (MDF) was assessed in control and experimental group of animals. A characteristic increase of MDF was observed in AOM-induced colon cancer animals. Treatment with LUT decreased the incidence of MDF. These results suggest that LUT alters the expression of glycoconjugates and suppress colon cancer. Hence, we speculate that LUT can be used as a chemopreventive agent to treat colon cancer.

• Proceedings of the Korean Society of Toxicology Conference
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• 2001.10a
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• pp.35-36
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• 2001

Nutrition influences cancer incidence and offers a variety of preventive dietary factors including non-nutritive plant metabolites. To identify novel potential chemopreventive agents, we have set up cell- and enzyme-based in vitro marker systems relevant for prevention of carcinogenesis in vivo. This experimental approach led to the identification of Xanthohumol (Xn), a prenylated chalcone from hop (Humulus lupulus L.) as a most promising broad-spectrum chemopreventive agent.(omitted)

• Journal of Microbiology and Biotechnology
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• v.14 no.1
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• pp.158-161
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• 2004

Scenedesmus spp. were cultured for 51 days in newly developed medium, KEP I (Kim and Ecopeace: initials of corresponding author and environmental company) made with Bacterio-Mineral-Water (3%, v/v) that had been bio-reacted with swine urine medium to 10% (v/v) Bold's Basal medium, and investigated for cancer chemopreventive potential by measuring the induction of quinone reductase (QR), glutathione S-transferase (GST), and reduced glutathione (GSH), and inhibition of cytochrome P450 (CYP) 1A1 activity. The activitives of QR and GST of Scenedesmus spp. cultured in KEP I medium were increased by 3.0-fold and 1.5-fold, respectively. However, Scenedesmus spp. cultured in control medium (CT) increased the activitives of QR and GST by 1.8-fold and 1.3-fold, respectively. Scenedesmus spp. in KEP I medium strongly inhibited CYP 1Al activity. These results show that Scenedesmus spp. in KEP I medium has cancer chemopreventive potential and may be a candidate for further development as a chemopreventive agent.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.85.3-86
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• 2003

Oltipraz, a cancer chemopreventive agent, induces CYP1A1 to a certain extent by transactivation of the gene via the Ah receptor (AhR)-xenobiotic response element (XRE) pathway. Previously, we showed that oltipraz promoted CCAAT/enhancer binding protein (C/EBP ) activation, which leads to the induction of glutathione S-transferase. Given that oltipraz activates C/EBP for gene transactivation and that the putative C/CBP binding site is located in CY)1A1 promoter region, this study investigated the effect of oltipraz on CYP1A1 induction by 3-methylcholanthrene (3-MC). (omitted)

• Korean Journal of Plant Resources
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• v.22 no.3
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• pp.203-208
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• 2009

Lunasin is a unique 43-amino acid peptide which has shown a chemopreventive in mammalian cells and in a skin cancer mouse model. In search for new sources of lunasin and the role of cereals in cancer prevention, we report here the properties of lunasin purified from millet. Stability of millet lunasin was measured by in vitro digestibility assay using pepsin and pancreatin. Inhibition of HAT (histone acetyltransferase) and nuclear localization in mammalian cells were used to measure lunasin bioactivity as the cancer chemopreventive agent. Lunasin present in millet crude protein was stable to pepsin and pancreatin in in vitro digestion and inhibited the activities of HATs. When added exogenously, lunasin purified from millet internalized in the nuclei of mouse fibroblast cells. On the base of this result, we conclude that lunasin in millet is bioactive and consumption of millet may play an important role on cancer prevention in millet-consuming populations.

• Korean Journal of Pharmacognosy
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• v.38 no.1
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• pp.95-99
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• 2007

In order to find novel cancer chemopreventive agents, quinone reductase (QR) inductive activity of methanol extract of herbal medicines was examined using murine hepatoma, hepa1c1c7 cells. QR has been used as an anticarcinogenic marker enzyme in cancer chemoprevention study. The methanol extract of Alpinia officinarum (Zingiberace) showed showed significantly strong quinone reductase inductive activity compared to the control group. The methanol extract of Alpinia officinarum was successively fractionated with various solvents according to polarity. Hexane, ethyl acetate, buthanol and water fractions were obtained and theirs activities were assessed. The QR inductive effect was moved to the ethyl acetate fraction and was highly increased. The CD (concentration required to double the specific activity of QR) value of ethyl acetate fraction was 8.6 ${\mu}g/mL$. Alpinia officinarum also showed strong antioxidant activity. These results suggest that Alpinia officinarum can be developed as cancer chemopreventive agent.

• Journal of Food Hygiene and Safety
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• v.11 no.2
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• pp.115-121
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• 1996

In order to compare the suppressive effect of quercetin and several its glycosides, such as quercitrin (quercetin-3-rhamnoside), isoquercitrin (quercetin-3-glucoside), hyperin (quercetin-3-galactoside) and tutin (quercetin-3-rhamnosyl glucoside), on the genotoxicity by N-methyl-N-nitrosourea(MNU), in vitro sister chromatid exchange(SCE) test using mouse spleen lymphocytes and in vivo micronucleus test using mouse peripheral blood were performed. MNU-induced SCEs in vitro were not decreased by the simultaneous treatment of test compounds. Among them, quercetin and hyperin showed significant suppressive effects at high dose(10-5M). On the other hand, MNU-induced micronucleated reticulocytes(MNRETS) in vivo were significantly decreased with good dose-dependent manner in all compound tested. However, there were not significant differences between quercetin aglycone and its glycosides in the suppressive aglycone and its glycosides may act as an antigenotoxic agent in vivo and may be useful as a chemopreventive agent of alkylating agent.

• Asian Pacific Journal of Cancer Prevention
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• v.14 no.10
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• pp.5855-5860
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• 2013

Phytochemicals are among the natural chemopreventive agents with most potential for delaying, blocking or reversing the initiation and promotional events of carcinogenesis. They therefore offer cancer treatment strategies to reduce cancer related death. One such promising chemopreventive agent which has attracted considerable attention is sulforaphane (SFN), which exhibits anti-cancer, anti-diabetic, and anti-microbial properties. The present study was undertaken to assess effect of SFN alone and in combination with a chemotherapeutic agent, gemcitabine, on the proliferative potential of MCF-7 cells by cell viability assay and authenticated the results by nuclear morphological examination. Further we analyzed the modulation of expression of Bcl-2 and COX-2 on treatment of these cells with SFN by RT-PCR. SFN showed cytotoxic effects on MCF-7 cells in a dose- and time-dependent manner via an apoptotic mode of cell death. In addition, a combinational treatment of SFN and gemcitabine on MCF-7 cells resulted in growth inhibition in a synergistic manner with a combination index (CI)<1. Notably, SFN was found to significantly downregulate the expression of Bcl-2, an anti-apoptotic gene, and COX-2, a gene involved in inflammation, in a time-dependent manner. These results indicate that SFN induces apoptosis and anti-inflammatory effects on MCF-7 cells via downregulation of Bcl-2 and COX-2 respectively. The combination of SFN and gemcitabine may potentiate the efficacy of gemcitabine and minimize the toxicity to normal cells. Taken together, SFN may be a potent anti-cancer agent for breast cancer treatment.