• The Korean Journal of Physiology and Pharmacology
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• v.16 no.2
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• pp.145-151
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• 2012

In the present work, we studied the structure-activity relationship (SAR) of tautomycetin (TMC) and its derivatives. Further, we demonstrated the correlation between the immunosuppressive fuction, anticancer activity and protein phosphatase type 1 (PP1) inhibition of TMC and its derivatives. We have prepared some TMC derivatives via combinatorial biosynthesis, isolation from fermentation broth or chemical degradation of TMC. We found that the immunosuppressive activity was correlated with anticancer activity for TMC and its analog compounds, indicating that TMC may home at the same targets for its immunosuppressive and anticancer activities. Interestingly, TMC-F1, TMC-D1 and TMC-D2 all retained significant, albeit reduced PP1 inhibitory activity compared to TMC. However, only TMC-D2 showed immunosuppressive and anticancer activities in studies carried out in cell lines. Moreover, TMC-Chain did not show any significant inhibitory activity towards PP1 but showed strong growth inhibitory effect. This observation implicates that the maleic anhydride moiety of TMC is critical for its phosphatase inhibitory activity whereas the C1-C18 moiety of TMC is essential for the inhibition of tumor cell proliferation. Furthermore, we measured $in$ $vivo$ phosphatase activities of PP1 in MCF-7 cell extracts treated with TMC and its related compounds, and the results indicate that the cytotoxicity of TMC doesn't correlate with its $in$ $vivo$ PP1 inhibition activity. Taken together, our study suggests that the immunosuppressive and anticancer activities of TMC are not due to the inhibition of PP1. Our results provide a novel insight for the elucidation of the underlying molecular mechanisms of TMC's important biological functions.

• The Korean Journal of Physiology and Pharmacology
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• v.13 no.2
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• pp.115-121
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• 2009

Functional defects in mitochondria are involved in the induction of cell death in cancer cells. We assessed the toxic effect of camptothecin against the human cervical and uterine tumor cell line SiHa with respect to the mitochondria-mediated cell death process, and examined the combined effect of camptothecin and anticancer drugs. Camptothecin caused apoptosis in SiHa cells by inducing mitochondrial membrane permeability changes that lead to the loss of mitochondrial membrane potential, decreased Bcl-2 levels, cytochrome c release, caspase-3 activation, formation of reactive oxygen species and depletion of GSH. Combination of camptothecin with other anticancer drugs (carboplatin, paclitaxel, doxorubicin and mitomycin c) or signaling inhibitors (farnesyltransferase inhibitor and ERK inhibitor) did not enhance the camptothecin-induced cell death and caspase-3 activation. These results suggest that camptothecin may cause cell death in SiHa cells by inducing changes in mitochondrial membrane permeability, which leads to cytochrome c release and activation of caspase-3. This effect is also associated with increased formation of reactive oxygen species and depletion of GSH. Combination with other anticancer drugs (or signaling inhibitors) does not appear to increase the anti-tumor effect of camptothecin against SiHa cells, but rather may reduce it. Combination of camptothecin with other anticancer drugs does not seem to provide a benefit in the treatment of cervical and uterine cancer compared with camptothecin monotherapy.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.15 no.2
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• pp.302-314
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• 2002

Shibyukmiyouki-Eum was a drug that treated carbuncle and cellulitis. So, the purpose of this study was to investigate effect of Shibyukmiyouki-Eum on the anticancer and inhibitive effects of the secondary effects by anticarcinogen We used Shibyukmiyouki-Eum extract(SYE) with freeze-dried, 8wks-old male mice(balb／c, ICR) and cancer cell lines(L1210. S-180) for this Study, The proliferation of cells was tested using a colorimetric tetrazoliun assay(MTT assay). and measurement of WBC, RBC, hemoglobin and platelet was tested by a automated hematology analyzer. The results of this study were obtained as follow; SYE was showed significantly cytotoxicity on the L1210 and S-180 cell lines. increased proliferation of thymocytes decreased by anticarcinogen. In combined effects of SYE and vincristine(0.005㎎／kg), SYE was significantly inhibited proliferation of L1210 cells and significantly increased proliferation of thymocytes. Also SYE was significantly increased count of WBC. platelet and increased count of RBC, hemoglobin. These results suggest that SYE has not only anticancar action but inhibitive effects of on the secondary effects by anticarcinogen.

• Journal of the Korean Society of Food Science and Nutrition
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• v.41 no.9
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• pp.1248-1252
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• 2012

Potassium added with bamboo salt showed better antioxidative effects than bamboo salt, solar salt, or purified salt. It also showed inhibitory effects on the mutagenicity of MNNG (N-methyl-N-nitro-N-nitrosoguanidine) in a Salmonella Typhimurium TA100 tester strain. At concentrations of 1.25 and 2.5 mg/plate, potassium bamboo salt and bamboo salt showed weaker co-mutagenicity effects than either purified salt or solar salt, respectively. Anticancer effects of salts were evaluated using MTT assay in HCT-116 human colon carcinoma cells. At a 1% salt concentration, the growth inhibitory rate of potassium bamboo salt was 54%, higher than that of 1 time baked bamboo salt (36%). However, purified salt and solar salt showed relatively lower inhibitory effects of 19% and 23%, respectively. To determine the inhibitory mechanisms of potassium bamboo salt, the expression levels of Bax and Bcl-2 genes in HCT-116 cells were determined by RT-PCR. Potassium bamboo salt significantly increased Bax and decreased Bcl-2 expression levels unlike bamboo salt, purified salt, and solar salt (p<0.05). Therefore, addition of potassium to salt decreased co-mutagenicity and increased in vitro antioxidative and anticancer effects.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.19
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• pp.8007-8018
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• 2014

Cervical cancer is the most common gynecologic malignancy worldwide and development of new therapeutic strategies and anticancer agents is an urgent priority. Plants have remained an important source in the search for novel cytotoxic compounds and several polyphenolic flavonoids possess antitumor properties. In this review article, data about potential anticarcinogenic activity of common natural flavonoids on various human cervical cancer cell lines are compiled and analyzed showing perspectives for the use of these secondary metabolites in the treatment of cervical carcinoma as well as in the development of novel chemotherapeutic drugs. Such anticancer effects of flavonoids seem to differentially depend on the cellular type and origin of cervical carcinoma creating possibilities for specific targeting in the future. Besides the cytotoxic activity per se, several flavonoids can also contribute to the increase in efficacy of conventional therapies rendering tumor cells more sensitive to standard chemotherapeutics and irradiation. Although the current knowledge is still rather scarce and further studies are certainly needed, it is clear that natural flavonoids may have a great potential to benefit cervical cancer patients.

• Korean journal of food and cookery science
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• v.23 no.2 s.98
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• pp.227-234
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• 2007

Potato kimchi, fermentation was carried out at $10^{\circ}$C for 15 days using various ratios of potato to kimchi (2.5%, 5%, 10%). The samples were determined according to the fermentation time, pH, acidity and growth of lactic acid bacteria in potato kimchi. The addition ratio of potato to kimchi had little effect on the pH, acidity or growth of lactic acid bacteria in potato kimchi. In comparison to baechu kimchi and mul-kimchi, the pH, acidity and growth of lactic acid bacteria was better in potato kimchi than in the other kimchi samples. The in vitro anticancer effect of potato kimchi was investigated using human cancer cells, AGS human gastric adenocarcinoma cells and HT-29 human colon adenocarcinoma cells. MTT assay revealed that the methanol extract of potato kimchi showed the highest anticarcinogenic effects.

• Biomolecules & Therapeutics
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• v.5 no.4
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• pp.384-389
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• 1997

Neutropenia is a major dose-limiting side effect of cancer chemotherapy. The therapeutic effects of CJ-50001 were examined on neutropenia caused by anticancer agents. Neutropenia was induced by cyclophosphomide (130 mg/kg), doxorubicin (4.5 mg/kg), and vincristine (1 mg/kg) in normal ICR mice and by cyclophosphamide (200 mg/kg) in CT26 adenocarcinoma bearing BALB/C mice. After the subcutaneous injection of anticancer agents, we administered subcutaneously recombinant human granulocyte-colonystimulating factor (100$\mu$g/kg/day) to mice in order to stimulate neutrophil production. In normal and tumor-bearing mice, neutrophil production efficacy of CJ-50001 (rG-CSF) was similar to that of Grasin. These results suggest that CJ-50001 could be effective in its clinical use for neutropenia treatment.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.227.1-227.1
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• 2002

Cyclooxygenase (Cox-2) is involved in tumorigenesis. hence. considered to be a molecular target for chemoprevention and chemomodulation. Selective Cox-2 inhibitors including Celecoxib and Nimesulide have been studied for their anticancer activity when given alone and in combination with radiation or cytotoxic agents. In this study, we synthesized more than 140 analogues of Celecoxib and Nimesulide. and evaluated their inhibitory effects on Cox-l and Cox-2 activity as well as cytotoxicity in order to find promising anticancer agents having selective Cox-2 inhibitory effect. (omitted)

• Journal of Animal Reproduction and Biotechnology
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• v.37 no.1
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• pp.62-66
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• 2022

To date, the development of anticancer drugs has been conducted using two-dimensional (2D) cell culture systems. However, since cancer cells in the body are generated and developed in three-dimensional (3D) microenvironments, the use of 2D anticancer drug screening can make it difficult to accurately evaluate the anticancer effects of drug candidates. Therefore, as a step towards developing a cancer cell-friendly 3D microenvironment based on a combination of vinylsulfone-functionalized polyethylene glycol (PEG-VS) with dicysteine-containing crosslinker peptides with an intervening matrix metalloproteinase (MMP)-specific cleavage site, the types of MMPs secreted from human hepatocarcinoma HepG2 cells, a representative cancer cell, were analyzed transcriptionally and translationally. MMP3 was confirmed to be the most highly expressed protease secreted by HepG2 cells. This knowledge will be important in the design of a crosslinker necessary for the construction of PEG-based hydrogels customized for the 3D culture of HepG2 cells.

• Journal of the Korean Society of Food Science and Nutrition
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• v.27 no.4
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• pp.625-632
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• 1998

To enhance the antimutagenic and anticancer activities of chinese cabbage kimchi, 13 kinds of kimchi, which were different kinds and levels of sub-ingredient added kimchi, were prepared and fermented at 15℃ for 1 day and then at 5℃ up to pH 4.3. The antimutagenic effects of the methanol extracts of the kimchi were studied by using Ames mutagenicity test in Salmonella typhimurium TA100 and SOS chromotest in E. coli PQ37. Among the kimchi samples, high ratio of red pepper powder(7%) and garlic(2.8% or 5.2%) added kimchi, 1% chinese pepper powder added kimchi and organic cultivated chinese cabbage kimchi significantly reduced(p<0.05) the mutagenicity induced by aflatoxin B1(AFB1) in Ames test and SOS response against N-methyl-N'-nitro-N-nitrosoguanidine(MNNG) in SOS chromotest, and also the kimchi inhibited more effectively(p<0.05) the survival and growth of AGS human gastric adenocarcinoma cells than the standarized kimchi on the SRB assay, MTT assay and growth inhibition test. These results suggest that the antimutagenic and anticancer activites of kimchi can be increased by the sub-ingredients such as organic cultivated chinese cabbage, red pepper powder, garlic and chinese pepper powder.