• Journal of Microbiology and Biotechnology
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• v.14 no.3
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• pp.628-630
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• 2004

Antitumor activities of a peptide fraction isolated from traditional Korean soy sauce (SSP) were investigated in vitro and in vivo using cancer cell lines and F9 teratocarcinoma-bearing BALB/c mice. SSP exerted a dose-dependent antiproliferative effect on P388D1 mouse lymphoma, F9 mouse teratocarcinoma, and DLD-l human colon cancer cells with $IC_{50}$ values of 11, 50, and $50\mug/ml$, respectively. Tumor growth in F9 teratocarcinoma-bearing BALB/c mice, orally administered with 80 and 200 mg/kg/day of SSPs, was inhibited 10.3% and 52.4%, respectively, and survival days increased by 11.9% and 22.1%, respectively, compared to the control group. The results of antitumor activities exerted by SSP in vitro and in vivo suggest the feasibility of using SSP as an antitumor agent.

• Asian Pacific Journal of Cancer Prevention
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• v.17 no.7
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• pp.3559-3567
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• 2016

Background: In recent years, there has been considerable research on recycling of agro-industrial waste for production of bioactive compounds. The food processing industry produces large amounts of citrus peels that may be an inexpensive source of useful agents. Objective: The present work aimed to explore the phytochemical content, antioxidant, anticancer, antiproliferation, and antigenotxic activities of lemon, grapefruit, and mandarin peels. Materials and Methods: Peels were extracted using 98% ethanol and the three crude extracts were assessed for their total polyphenol content (TPC), total flavonoid content (TFC), and antioxidant activity using DPPH (1, 1-diphenyl-2-picrylhydrazyl). Their cytotoxic and mitogenic proliferation activities were also studied in human leukemia HL-60 cells and mouse splenocytes by CCK-8 assay. In addition, genotoxic/antigenotoxic activity was explored in mouse splenocytes using chromosomal aberrations (CAs) assay. Results: Lemon peels had the highest of TPC followed by grapefruit and mandarin. In contrast, mandarin peels contained the highest of TFC followed by lemon and grapefruit peels. Among the extracts, lemon peel possessed the strongest antioxidant activity as indicated by the highest DPPH radical scavenging, the lowest effective concentration 50% ($EC_{50}=42.97{\mu}g\;extract/mL$), and the highest Trolox equivalent antioxidant capacity (TEAC=0.157). Mandarin peel exhibited moderate cytotoxic activity ($IC_{50}=77.8{\mu}g/mL$) against HL-60 cells, whereas grapefruit and lemon peels were ineffective anti-leukemia. Further, citrus peels possessed immunostimulation activity via augmentation of proliferation of mouse splenocytes (T-lymphocytes). Citrus extracts exerted non-cytotoxic, and antigenotoxic activities through remarkable reduction of CAs induced by cisplatin in mouse splenocytes for 24 h. Conclusions: The phytochemical constituents of the citrus peels may exert biological activities including anticancer, immunostimulation and antigenotoxic potential.

• The Korean Journal of Physiology and Pharmacology
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• v.16 no.5
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• pp.321-326
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• 2012

Resveratrol, a natural compound, has been shown to possess anti-cancer, anti-aging, anti-inflammatory, anti-microbial, and neuroprotective activities. In this study, we examined the antiproliferative and cytotoxicity properties of resveratrol in Rat B103 neuroblastoma cells; although it's molecular mechanisms for the biological effects are not fully defined. Here, we examined the cellular cytotoxicity of resveratrol by cell viability assay, antiproliferation by BrdU assay, DNA fragmentation by DNA ladder assay, activation of caspases and Bcl-2 family proteins were detected by western blot analyses. The results of our investigation suggest that resveratrol increased cellular cytotoxicity of Rat B103 neuroblastoma cells in a dose-and time-dependent manner with $IC_{50}$ of 17.86 ${\mu}M$ at 48 h. On the other hand, incubation of neuroblastoma cells with resveratrol resulted in S-phase cell cycle arrests which dose-dependently and significantly reduced BrdU positive cells through the downregulation of cyclin D1 protein. In addition, resveratrol dose-dependently and significantly downregulated the expression of anti-apoptotic protein includes Bcl-2, Bcl-xL and Mcl-1 and also activates cleavage caspase-9 and-3 via the downregulation of procaspase-9 and -3 in a dose-dependent manner which indicates that involvement of intrinsic mitochondria-mediated apoptotic pathway. In conclusion, resveratrol increases cellular cytotoxicity and inhibits the proliferation of B103 neuroblastoma cells by inducing mitochondria-mediated intrinsic caspase dependent pathway which suggests this natural compound could be used as therapeutic purposes for neuroblastoma malignancies.

• Horticultural Science & Technology
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• v.28 no.5
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• pp.857-863
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• 2010

This study was conducted to evaluate the antioxidant activity, Angiotensin I Converting Enzyme (ACE) inhibitory activity, ${\alpha}$-glucosidase inhibitory activity, nitrate synthesis inhibitory activity, and antiproliferation inhibitory effect on ethanol extract and its solvent fractions of $Coreopsis$ $tinctoria$ Nutt. Ethyl acetate fraction was the strongest at 1,1-diphenyl-2-picryl hydrazyl (DPPH) ($IC_{50}=0.100mg{\cdot}mL^{-1}$) and 2,2'-Azino-bis-(3-ethylbenozothiazoline-6-sulfonic acid) (ABTS) (15.785 mg AA $eq{\cdot}10mg^{-1}$) radical scavenging activity, ACE (40.96% at $1mg{\cdot}mL^{-1}$), and ${\alpha}$-glucosidase ($IC_{50}=0.125mg{\cdot}mL^{-1}$) inhibitory effect among the solvent fractions. Nitrate synthesis inhibitory activity of ethanol extract, chloroform fraction, and ethyl acetate fraction effectively inhibited NO formation in a dose-dependent manner without the cytotoxic effect. Ethanol extract and its solvent fractions inhibited growth of HCT-116 colon cancer cells in a dose-dependent manner. n-Hexane fraction showed the highest antiproliferation inhibitory effect of $0.041mg{\cdot}mL^{-1}$ among fractions.

• Korean Journal of Food Science and Technology
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• v.36 no.6
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• pp.1001-1007
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• 2004

Chloroform layer from methanol extract of Corni fructus (Cornaceae) showed strong antiproliferation effect on human cancer cell lines by SRB assay. Anticarcinogenic-active compound was isolated and purified by silica gel column and thin layer chromatograpies, and identified as ursolic acid ($3{\beta}$-hydroxyrus-12-ene-28-oic acid, MW:456) by mass and IR spectrophotometries, and $^1H-and\;^{13}C-NMRs$. The compound inhibited proliferation of A549 (human lung cancer cell line) and MCF-7 (human breast cancer cell line) cells in dose-dependant manner when treated for 48 hr. Inhibition rates of both cells were over 40% and 90% compared with control cells at the $30\;{\mu}g/mL\;and\;100\;{\mu}g/mL$, respectively. Morphology of cells treated with the compound for 15 hr at $10\;{\mu}g/mL$ was distorted with shrinked cell mass, and cell number was lower than that of control cells. Cell cycle analysis showed sub-G1 phase arrest in both cell lines following 15 hr exposure to the compound; % of cell phase increased to 11.7 and 11.2% compared to the control of 4.0% and 2.1% in A549 and MCP-7 cells, respectively.

• Journal of Ginseng Research
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• v.39 no.3
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• pp.274-278
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• 2015

Background: Steaming of ginseng is known to change its chemical composition and biological activity. This study was carried out to investigate the effect of different steaming time-scales on chemical constituents and antiproliferative activity of Vietnamese ginseng (VG). Methods: VG was steamed at $105^{\circ}C$ for 2-20 h. Its saponin constituents and antiproliferative activity were studied. The similarity of chemical compositions between steamed samples at $105^{\circ}C$ and $120^{\circ}C$ were compared. Results: Most protopanaxadiol and protopanaxatriol ginsenosides lost the sugar moiety at the C-20 position with 10-14 h steaming at $105^{\circ}C$ and changed to their less polar analogues. However, ocotillol (OCT) ginsenosides were reasonably stable to steaming process. Antiproliferative activity against A549 lung cancer cells was increased on steaming and reached its plateau after 12 h steaming. Conclusion: Steaming VG at $105^{\circ}C$ showed a similar tendency of chemical degradation to the steaming VG at $120^{\circ}C$ except the slower rate of reaction. Its rate was about one-third of the steaming at $120^{\circ}C$.

• Journal of the Korean Society of Food Science and Nutrition
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• v.38 no.11
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• pp.1478-1484
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• 2009

The antioxidant, antiproliferation, and nitrate synthesis inhibitory effects of Magnolia denudata extracts (ME) were evaluated. The ME was extracted with 70% (v/v) ethanol and fractionated with solvents of hexane, chloroform, ethyl acetate, n-buthanol and aqueous. The ethyl acetate fraction contained the highest phenolic and flavonoid contents of 427.10 mg garlic acid eq/g and 356.05 mg catechin eq/g, respectively. The ethyl acetate fraction showed strong 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity with a 50% inhibition concentration ($IC_{50}$) of 0.20 mg/mL and total antioxidant activity was 0.90 mg AA eq/100 mg. From the results of cytotoxic effects of HCT116, NCL-H460, and HepG2 human cancer cells by MTT assay on the ME and its solvent fraction, chloroform fraction showed the highest cytotoxic effect ($IC_{50}$ value: 0.14, 0.37, and 0.41 mg/mL, respectively). Nitrate synthesis inhibitory effect of ME and its solvent fractions on nitric oxide synthase activity in LPS stimulated RAW 264.7 cells were decreased in dose-dependent manners, and $IC_{50}$ value of hexane and chloroform fractions were 0.39 and 0.49 mg/mL, respectively.

• Biomedical Science Letters
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• v.11 no.2
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• pp.175-183
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• 2005

The two major isoflavones in soy, genistein and daidzein, are well known to prevent hormone-dependent cancers by their anti estrogenic activity. The exact molecular mechanisms for the protective action are, however, not provided yet. It has been reported that genistein and daidzein have a potential anticancer activity through their antiproliferative effect in many hormone-dependent cancer cell lines. Transforming growth $factor-\beta1(TGF-\beta1)$ has also been found to have cell growth inhibitory effect, especially in mammary epithelial cells. This knowledge led to a hypothetical mechanism that the soy isoflavones-induced growth inhibitory effect can be derived from the regulation of $TGF-\beta1$ and $TGF-\beta$ receptors. In order to test this hypothesis, the effects of the soy isoflavones at various concentrations and periods on the expression of $TGF-\beta1$and $TGF-\beta$ receptors were investigated by using Northern blot analysis in human breast carcinoma epithelial cell lines, an estrogen receptor positive cell line (MCF-7) and an estrogen receptor negative cell line (MDA-MB-231). As a result, only genistein has shown a profound dose-dependent effect on $TGF-\beta1$ expression in the $ER^+$ cell line within the range of doses tested, and the expression levels are correspondent to their inhibitory activities of cell growth. Moreover, daidzein showed down-regulated $TGF-\beta1$ expression at a low dose, the cell growth proliferation was promoted at the same condition. Therefore, antiproliferative activity of the soy isoflavones can be mediated by $TGF-\beta1$ expression, and the effects are mainly, if not all, occurred by ER dependent pathway. The expression of $TGF-\beta$ receptors was induced at a lower dose than the one for $TGF-{\beta}1$ induction regardless of the presence of ER, and the expression patterns are similar to those of the cell growth inhibition. These results indicated that the regulation of $TGF-\beta$ receptor expression as well, prior to $TGF-\beta1$ expression, may be involved in the antiproliferative activity of soy isoflavones. Little or no expression of $TGF-\beta$ receptors was found in the MCF-7 and MDA-MB-231 cells, suggesting refractory properties of the cells to growth inhibitory effect of the $TGF-\beta$. The soy isoflavones can seemingly restore the sensitivity of growth inhibitory responses to $TGF-\beta1$ by re-inducing $TGF-\beta$ receptors expression. In conclusions, our findings presented in this study show that the antitumorigenic activity of the soy isoflavones could be mediated by not only $TGF-\beta1$induction but $TGF-\beta$ receptor restoration. Thus, soy isoflavones could be good model molecules to develop new nonsteroidal antiestrogenic chemopreventive agents, associated with, regulation of $TGF-\beta$ and its receptors.

• Journal of Life Science
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• v.31 no.2
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• pp.149-157
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• 2021

Prunus mume Sieb. et Zucc is widely distributed in East Asia (Korea, Japan, and China), and its fruit is often used as a medication and food material. However, because most previous studies have only investigated the state of Prunus mume fruit extract, studies on the various ways of processing this extract are still needed to increase its utilization. In this study, we evaluated the physicochemical properties and physiological activities of spray-dried Prunus mume vinegar powder (SPP). The sugar content, pH, total acidity, and moisture content of the SPP were 8.90 °Brix, 3.19, 1.05%, and 3.07%, respectively. The SPP exhibited significantly high antioxidant activity in terms of DPPH radical scavenging activity (65.55%), reducing power (1.48), and hydrogen peroxide scavenging activity (48.07%). In addition, the SPP remarkably decreased the cell viability of human breast MDA-MB-231 and human skin cancer SK-MEL-28 in a dose-dependent manner. The morphological results of the treatment of MDA-MB-231 cells with SPP were distorted, shrunken cell masses. Furthermore, apoptotic bodies and nuclear condensation formed in the SPP-treated MDA-MB-231 cells. The total polyphenol and flavonoid contents of the SPP were 59.58 ㎍/g (gallic acid equivalent) and 57.56 ㎍/g (quercetin equivalent). The results of this study indicate that SPP, which has antioxidant activity and anticancer effects, can be useful in the development of natural medicines and functional food ingredients.

• Journal of Life Science
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• v.27 no.12
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• pp.1470-1478
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• 2017

The aim of this study was to investigate biological activity and biochemical properties of extracts from Bacillus subtilis-fermented silkworm (Bombyx mori L., SP) powder of different origin (Buan, Namwon, and Boeun). An additional aim was to determine the inhibition of cancer cell (B16-F10, HT-29, LNcaP, and MCF-7) proliferation and nitric oxide (NO) production from lipopolysaccharide (LPS)-induced RAW264.7 cells. Biological activities (${\alpha},{\alpha}^{\prime}$-diphenyl-${\beta}$-picrylhydrazyl [DPPH], free radical scavenging activity, fibrinolytic activity, antiproliferation activity, and anti-inflammatory activity) and biochemical properties (compositional amino acid contents, and mineral contents) were examined in water extracts from silkworm powder and B. subtilis-fermented silkworm powder. The highest amino acid contents were detected in Buan silkworm powder (BU). After fermented, the highest contents were found in B. subtilis-fermented Buan silkworm powder (BBO). The major minerals detected were K, Ca, and Mg. Rates of these minerals, especially those of Na increased after fermented. DPPH radical scavenging activity and fibrinolytic activity were stronger in the fermented group than non-fermented group. DPPH radical scavenging activity and fibrinolytic activity were highest in the extract from BBO. The inhibition activities of LNcaP and MCF-7 cells viability were significantly decreased in the BBO, and there was no inhibition activity in other cancer cells (B16-F10 and HT-29). An SRB assay of the cell viability of RAW 264.7 cells exposed to extracts of silkworm powder and B. subtilis-fermented silkworm powder revealed no toxicity in any of the groups. Compared with the LPS-treated group, the biggest reduction in NO production was detected in the BBO group. Based on these results, extracts from Boeun silkworm powder fermented with B. subtilis could be a candidate material as a dietary supplement for use in healthy functional foods.