• Journal of Life Science
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• v.16 no.3 s.76
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• pp.546-554
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• 2006

To understand antitumor activity of Zanthoxylum schinfolium, which has been used as an aromatic and medicinal plant in Korea, the cytotoxic effect of various organic solvent extracts of its leaves on human tumor cells were investigated. Among these extracts such as methanol extract (SL-13), methylene chloride extract (SL-14), ethyl acetate extract (SL-15), n-butanol extract (SL-16), and residual fraction (SL-17), SL-14 appeared to contain the most cytotoxic activity against leukemia and breast cancer cells tested. The methylene chloride extra.1 (SL-14) possessed an apoptogenic activity causing apoptotic DNA fragmentation of human acute leukemia Jurkat T cells via mitochondrial cytochrome c release into cytoplasm, subsequent activation of caspase-9 and caspase-3, and cleavage of PARP, which could be negatively regulated by antiapoptotic protein Bcl-xL. The GC-MS analysis of SL-14 revealed that the twenty-two ingredients of SL-14 were 9,19-cyclolanost-24-en-3-ol (15.1%), 2-a-methyl-17, b-hop-21-ene (15.1%), 15-methyl-2,3-dihydro-1H benzazepin (11.95%), phytol (10.38%), lupeol (9.92%), 12-methylbenzofuran (8.23%), hexadecanoic acid (5.96%), cis,cis,cis-9,12,15-octadecatrienoic acid-methyl-ester (5.49%), 9,12,15-octadecatrienoic acid-methylester (3.59%), 15-methyl-4-(1-methylethylidene)-2-(4-nitrophenyl) (3.36%), hexadecanoic acid methyl ester (1.93%), vitamine E (1.88%), beta-amyrin (0.96%), and auraptene (0.89%). These results demonstrate that the cytotoxicity of the methylene chloride extract of the leaves of Z. schinifolium toward Jurkat T cells is mainly attributable to apoptosis mediated by mitochondria-dependent caspase cascade regulated by Bcl-xL, and provide an insight into the mechanism underlying antitumor activity of the edible plant Z. schinifolium.

• Journal of the Korean Society of Food Science and Nutrition
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• v.31 no.5
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• pp.924-930
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• 2002

Ixeris dentata extracts exllibited antimicrobial activity against some bacteria and fungi. Also EtOH extracts showed strong antioxidant activity and RC$_{50}$ value was 28 $\mu\textrm{g}$/mL. The inhibitory effect of Ixeris dentata on the mutagenicity in Salmonella and cytotoxicity on cancer cell were studied. Ixeris dentata extracts showed anti-mutagenic effects of 78.83 and 75.96% on B(a)P in S. typhimurium TA98 and Th100, respectively. These extracts showed 78.72% antimutagenicity on TA100 against MNNG. The Ixeris dentata extract with strong antimutagenic activities was further fractionated by hexane, ethyl acetate, butanol and water. Butanol fraction was found to be highest in antimutagenic activity against MNNG than the other fractions. Butanol fraction of Ixreis dentate revealed the highest cytotoxicity against AS49 human lung carcinoma cells in which cell growth was inhibited by 93.75% at 375 $\mu\textrm{g}$/mL. Hexane fraction of ixeris dentate exhibited 68.56% inhibition against MCF-7 human breast adenocarcinoma cells at 500 $\mu\textrm{g}$/mL. Hexane fraction of Ixeris dentata exhibited 84.91% inhibition against Hep 3B human hepatocellular carcinoma cells at 500 $\mu\textrm{g}$/mL. From these results, it is considered that Ixeris dentata has strong antimutagenic and anticancer effects in vitro. However, these extracts and fractions did not show any cytotoxic effect against 293 cells.

• Journal of Applied Biological Chemistry
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• v.60 no.2
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• pp.161-171
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• 2017

This study was aimed to evaluate and compare the proximate composition, antioxidant and antiproliferative activities of Sageretia thea (Osbeck) M.C.Johnst (S. thea) fruit and blueberry. The calorific value, crude protein, crude fat, crude ash, and carbohydrate were higher in S. thea fruit than in blueberry. S. thea fruit and blueberry have different profile of free sugars, in which amounts of fructose, glucose, and maltose were much higher in S. thea fruit than in blueberry. The methanol extracts of S. thea fruit contain higher amounts of total polyphenol and anthocyanin compared to those of blueberry extracts. In additions, 2,2-diphenyl-1-picrylhydrazyl (DPPH), alkyl, and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical scavenging activities are greater in S. thea fruit extracts. Ethyl acetate fractions and n-butanol fractions of S. thea fruit and blueberry show the most potent scavenging activity in DPPH-, alkyl-, and ABTS-radical scavenging assay. The ethyl acetate fractions of S. thea fruit and blueberry are the richest fraction in polyphenol contents while the n-butanol fractions of those are the highest fraction in anthocyanin contents. Furthermore, both S. thea fruit and blueberry extracts protect human dermal fibroblast cells against a $H_2O_2$-induced oxidative stress. The antiproliferative activities of n-hexane and chloroform fraction from S. thea fruit and blueberry were observed in AGS human gastric cancer and MDA-MB-231 human breast cancer cells. Therefore, our results suggest for the first time that the antioxidant and antiproliferative activities of S. thea fruit is comparable to that of blueberry and the nutritional value of the former is even superior to that of the latter.

• Journal of the Korean Society of Food Science and Nutrition
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• v.38 no.1
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• pp.25-31
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• 2009

This study was carried out to investigate the mutagenic, antimutagenic, cytotoxicity and antitumor effects of Adenophora triphylla (AT). AT was extracted with 70% ethanol and then further fractionated to hexane, chloroform, ethyl acetate, butanol and water. Antimutagenic, cytotoxicity and antitumor effects of AT extracts were measured by using Ames test, SRB method, and the tumor growth inhibition test. AT extracts did not show any mutagenicity in the Ames test; however, 70% ethanol extracts and its fractions had strong antimutagenic effects against mutation induced by N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) and 4-nitroquinoline-1-oxide (4NQO). The ethyl acetate fraction of AT (200 ${\mu}g$/plate) showed approximately 66.5% inhibitory effect on the mutagenesis induced by 4NQO against TA98 strain, whereas 83.3% and 75.1% inhibitions were observed on the mutagenesis induced by MNNG and 4NQO against TA100 strain. In anticancer effects, the cytotoxicity of AT extract and its fractions against cancer cell lines including human cervical adenocarcinoma (HeLa), human hepatocellular carcinoma (Hep3B), human breast adenocarcinoma (MCF-7), human gastric carcinoma (AGS), human lung carcinoma (A549) and transformed primary human embryo kidney (293) were investigated. The treatment of 1 mg/mL AT ethyl acetate faction had the highest cytotoxicity of 79.9%, 74.9%, 66.0%, 71.0% and 74.3% against HeLa, Hep3B, MCF-7, AGS and A549 cells, respectively. In contrast, the extract and its fractions showed only $3{\sim}36%$ cytotoxicity for a normal human kidney cell line (293). In vivo anti-cancer effect of Adenophora triphylla extract was tested using Balb/c mice transplanted sarcoma-180 cells. Adenophora triphylla ethyl acetate fraction showed the highest inhibition rate of 37.2% at the 50 mg/kg concentration.

• Journal of the Korean Society of Food Science and Nutrition
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• v.44 no.4
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• pp.516-523
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• 2015

This study investigated the antimutagenic and anticancer effects of Platycodon grandiflorum extract (PGE) and its fractions against carcinogenic N-nitrosodimethylamine (NDMA) and genotoxicity. The Ames Salmonella mutagenicity test employing histidine mutants of Salmonella Typhimurium TA98 and TA100 was used to examine the mutagenicity of PGE and its fractions. Bacterial reversion assay with S. Typhimurium TA98 and TA100 did not show a significantly increased number of revertant colonies. The same test was used to examine the ability of PGE and its fractions to prevent acquisition of N-methyl-N'-nitro-N-nitrosoguanidine- and 4-introquino-line-1-oxide-induced mutations. PGE and its fractions inhibited mutagenesis in a dose-dependent manner. Among the fractions, ethyl acetate fraction from PGE (PGEA) exhibited a higher antimutagenic effect than other fractions. PGE and its fractions suppressed the growth of cancer cell lines, including human cervical adenocarcinoma, human hepatocellular carcinoma, human breast adenocarcinoma, human lung carcinoma, and transformed primary human embryonic kidney cells. In addition, we evaluated the antitumor activity of PGEA and its fractions in sacorma-180 solid tumor-bearing mice. In vivo anticancer activity results showed that PGE and its fractions could more effectively suppress tumor growth than the control. PGEA showed higher in vitro and in vivo anticancer effects than PGE and other fractions, and PGEA inhibited NDMA formation. Thus, we showed that PGEA has antimutagenic and anticancer activities, making it a candidate anticancer material under these experimental conditions.

• Journal of Life Science
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• v.26 no.4
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• pp.439-445
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• 2016

Soybean leaves, a Korean edible plant material, have been reported to prevent the development of osteoporosis and breast cancer. Based on this rational, soybean fallen leaves ethanolic extract (SBFL) was used for the experiment of cell invasion related to metastasis and antioxidant activity. The effect of SBFL on matrix metalloproteinases (MMPs) in human fibrosarcoma cells, HT1080 as well as its anti-oxidant activity was investigated in this study. The effect of SBFL on scavenging activity of reactive oxygen species was evaluated in vitro using lipid peroxidation assay,DPPH radical and reducing power assay. SBFL showed the positive effects on antioxidant activity, compared with vitamin C and vitamin E used as positive controls. Furthermore, SBFL showed cytotoxicity above 16 µg/ml in MTT assay. In particular, it was found that SBFL decreased the activation of MMP-9 stimulated by phorbol 12-myristate 13-acetae (PMA) and phenazine methosulfate (PMS). SBFL treatment increased the expression levels of p-FoxO-1 and SOD-1. Moreover, SBFL inhibited cell invasion stimulated by vascular endothelial growth Factor (VEGF). These results indicate that SBFL could inhibit cell invasion related to the activation of MMP-9 and oxidative stress, suggesting that it could be available as a main ingredient for prevention of metastasis.

• Korean Journal of Food Science and Technology
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• v.32 no.4
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• pp.964-969
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• 2000

Di-(2-ethylhexyl) adipate(DEHA) has been used extensively as a plasticizer in the manufacture of plastic products such as PVC films. Though, phthalate esters plasticizers have been known to induce endocrine system-mediated responses, few studies have been conducted for the screening of estrogenic activity of DEHA, an adipate plasticizer. This study was initiated to evaluate the estrogenic activity of DEHA by in vitro E-screen assay and in vivo uterotrophic assay. MCF-7 human breast cancer cells were treated with $DEHA(5{\times}10^{-9}{\sim}5{\times}10^{-4}\;M)$, for 144 hr, and cell proliferation was determined by sulforhodamine B(SRB) assay. DEHA dissolved in corn oil was administered subcutaneously to ovariectomized(OVX) female Sprague-Dawley rats at dosage levels of 0, 2, 20 and 200 mg/kg/day for three consecutive days. Rats were sacrificed 24 hr after final treatment and vagina and uterus(wet and blotted) weights were obtained. E-screen assayed DEHA did not generate cell proliferation at treated concentrations$(5{\times}10^{-9}{\sim}5{\times}10^{-4}\;M)$, whereas 17 ${\beta}-estradiol$(E2), the positive control, induced cell proliferation at low concentrations$(5{\times}10^{-14}{\sim}5{\times}10^{-9}\;M)$. In the uterotrophic assay, DEHA did not change vagina and uterus(wet and blotted) weights at dosage levels up to 200 mg/kg/day treatment. These results demonstrated that DEHA did not exhibit the estrogenic activity as determined by in vitro E-screen assay and in vivo uterotrophic assay.

• Biomolecules & Therapeutics
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• v.22 no.4
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• pp.347-354
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• 2014

Larrea nitida is a plant that belongs to the Zygophyllaceae family and is widely used in South America to treat inflammatory diseases, tumors and menstrual pain. However, its pharmacological activity remains unclear. In this study we evaluated the property of selective estrogen receptor modulator (SERM) of Larrea nitida extracts (LNE) as a phytoestrogen that can mimic, modulate or disrupt the actions of endogenous estrogens, depending on the tissue and relative amount of other SERMs. To investigate the property of SERM of LNE, we performed MCF-7 cell proliferation assays, estrogen response element (ERE)-luciferase reporter gene assay, human estrogen receptor (hER) binding assays and in vivo uterotrophic assay. To gain insight into the active principles, we performed a bioassay-guided analysis of LNE employing solvents of various polarities and using classical column chromatography, which yielded 16 fractions (LNs). LNE showed high binding affinities for $hER{\alpha}$ and $hER{\beta}$ with $IC_{50}$ values of $1.20{\times}10^{-7}$ g/ml and $1.00{\times}10^{-7}$ g/ml, respectively. LNE induced $17{\beta}$-estradiol (E2)-induced MCF-7 cell proliferation, however, it reduced the proliferation in the presence of E2. Furthermore, LNE had an atrophic effect in the uterus of immature rats through reducing the expression level of progesterone receptor (PR) proteins. LN08 and LN10 had more potent affinities for binding on $hER{\alpha}$ and ${\beta}$ than other fractions. Our results indicate that LNE had higher binding affinities for $hER{\beta}$ than $hER{\alpha}$, and showed SERM properties in MCF-7 breast cancer cells and the rat uterus. LNE may be useful for the treatment of estrogen-related conditions, such as female cancers and menopause.

• Journal of the Korean Society of Radiology
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• v.14 no.6
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• pp.755-762
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• 2020

This study is desinged to examine the effects of Taheebo(Tabebuia avellanedae) extract on the prostate of male rats as a natural radiation protection agent. Taheebo extract is well known to inhibit cell growth for the cell lines of breast and prostate cancer. In this study, the X-ray 7 Gy was irradiated in the prostate of male rat to identify radiation protection effects by Taheebo Extracts, 1, 7, and 21 Days later, hematological changes, external toxicity assessments(LDH), antioxidant enzyme(SOD) activity changes and tissue change were observed. IR+TH group showed greater lymphocyte levels than the irradiation group, which is believed to affect the hematopoietic immune system's resilience. As a results of the external toxicity assessment, Taheebo extract's toxicity is maximum 18.128±5.16%, minimum 13.6945±4.43%. Taheebo is considered to be of little toxicity. The composition of prostate cell nuclei and cytoplasm in Control and TH group was honogeneous, whereas the cell nucleus cohesion in the prostate in irradiation group and inflammatory reactions in cytoplasm were shown. IR+TH group showed less inflammatory reactions of cytoplasm in the prostate than in the radiation irradiation group, but showed a cohesive phenomenon of cell nuclei. It is judged that Taheebo extract has radiation protection against prostate cells.

• KSBB Journal
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• v.17 no.2
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• pp.153-157
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• 2002

A fusion protein, consisting of a human epidermal growth factor as the recognition domain and human angiogenin as the toxin domain, can be used as a targeted therapeutic against breast cancer cells among others. The fusion protein was expressed as an inclusion body in recombinant E. coli, yet when the conventional solution-phase refolding process was used the refolding yield was very low due to severe aggregation, probably because of the opposite surface charge resulting from the vastly different pl values of each domain. Accordingly the solid-phase refolding process, which exploits the ionic interactions between a solid matrix and the protein, was tried, however the ionic binding yield was also very low regardless of the resins and pH conditions used. Therefore, to provide a higher affinity toward the solid matrix, six Iysine residues were tagged to the N-terminus of the hEGF domain. When cation exchange resins, such as heparin- or CM-Sepharose, were used as the matrix, the adsorption capacity increased 2.5~3-fold and the subsequent refolding yield increased nearly 15-fold compared to the conventional process. A similat result was also obtained when an Ni-NTA metal affinity resin was used.