• Bulletin of the Korean Chemical Society
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• v.30 no.7
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• pp.1463-1469
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• 2009

Eleven novel oxiranyl and thiiranyl phenolic compounds were synthesized as potential antitumor agents using epichlorohydrin and epithiohydrin in the presence of $K_2CO_3$. Cytotoxicities were found in range of I$C_{50}$ values of 2.5-14.8 $\mu$M, which was partially attributed to topoisomerase II inhibition. Bis-thiiranyl anthraquinone analog, 19 showed more cytotoxicity against MDA-MB-231 (breast cancer cell) and PC3 (prostate cancer cell) after 24 and/or 48 h and more potent topoisomerase II inhibitory activity than etoposide.

• Toxicological Research
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• v.30 no.3
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• pp.211-220
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• 2014

Resveratrol has received considerable attention as a polyphenol with various biological effects such as anti-inflammatory, anti-oxidant, anti-mutagenic, anti-carcinogenic, and cardioprotective properties. As part of the overall safety assessment of HS-1793, a novel resveratrol analogue free from the restriction of metabolic instability and the high dose requirement of resveratrol, we assessed genotoxicity in three in vitro assays: a bacterial mutation assay, a comet assay, and a chromosomal aberration assay. In the bacterial reverse mutation assay, HS-1793 did not increase revertant colony numbers in S. typhimurium strains (TA98, TA100, TA1535 and TA1537) or an E. coli strain (WP2 uvrA) regardless of metabolic activation. HS-1793 showed no evidence of genotoxic activity such as DNA damage on L5178Y $Tk^{+/-}$ mouse lymphoma cells with or without the S9 mix in the in vitro comet assay. No statistically significant differences in the incidence of chromosomal aberrations following HS-1793 treatment was observed on Chinese hamster lung cells exposed with or without the S9 mix. These results provide additional evidence that HS-1793 is non-genotoxic at the dose tested in three standard tests and further supports the generally recognized as safe determination of HS-1793 during early drug development.

• Fisheries and Aquatic Sciences
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• v.17 no.3
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• pp.305-311
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• 2014

Dieckol is a polyphenol compound isolated from brown algae that has anti-oxidant, anti-inflammatory, and anti-tumor activity. We examined the anti-angiogenic effects of dieckol in endothelial cells under hypoxic conditions. Treatment with $CoCl_2$, a hypoxic mimetic agent, increased proliferation, adhesion, migration, and tube formation in HUVECs, as well as vessel sprouting in rat aortic rings, which correlated well with increased expression of hypoxia-inducible factor 1-alpha ($HIF1{\alpha}$) and ${\beta}1$-integrin. Dieckol suppressed $CoCl_2$-induced adhesion, migration, and tube formation in HUVECs and vessel sprouting in rat aortic rings. Dieckol treatment decreased $CoCl_2$-induced overexpression of $HIF1{\alpha}$ and its downstream signaling molecules, including ${\beta}1$-integrin/Fak, Akt/eNOS, and p38 MAPK. These results suggest that dieckol is a novel angiogenesis inhibitor and a potential treatment for angiogenesis-dependent diseases in humans, such as malignant tumors.

• The Korean Journal of Food And Nutrition
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• v.28 no.4
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• pp.620-627
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• 2015

The present study was carried out to investigate the biological activity of ethanol extracts from fermented Opuntia humifusa with 3 different mushroom mycelia: Phellinus linteus, Lentinula edodes, and Pleurotus ostreatus. Fermented Opuntia humifusa by Phellinus linteus (FOP) and Lentinula edodes (FOL) showed more DPPH and ABTS radical scavenging activities than non-fermented Opuntia humifusa (NFO) and fermented Opuntia humifusa by Pleurotus ostreatus (FOPO). At a concentration of 250 ppm, the ABTS radical scavenging activities of the FOP and FOL were similar to that of BHA, a synthetic antioxidant. The total polyphenol content had a similar tendency to that of the radical scavenging activity. However, the flavonoid content was increased in the order of NFO, FOL, FOPO, and FOP. At all concentrations, the tyrosinase inhibitory activity of FOP and FOPO were significantly higher than that of kojic acid. During adipocyte differentiation, NFO and FOL showed no significant difference in lipid accumulation in 3T3-L1 cells. FOP and FOPO showed a higher fat accumulation inhibitory effect than NFO and FOL. These results provide baseline data for Opuntia humifusa as a novel functional food.

• Horticulture, Environment, and Biotechnology : HEB
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• v.59 no.6
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• pp.835-845
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• 2018

We studied the role of ethylene control in regulating energy metabolism, antioxidant enzyme activity, and vase life of cut rose Rosa hybrida 'Carola'. Rose flowers at stage II were sprayed with one of the following solutions: water (control), $10{\mu}L\;L^{-1}$ 1-methylcyclopropene (1-MCP), or $0.5g\;L^{-1}$ 2-chloroethanephosphonic acid (ethephon). After harvest, ethylene production rate, respiration intensity, energy charge (EC), activities of energy metabolism-related and antioxidant enzymes, and malondialdehyde (MDA) content were measured. Results showed that 1-MCP enhanced the activities of superoxide dismutase, $H^+$-adenosine triphosphatase, $Ca^{2+}$-adenosine triphosphatase, succinic dehydrogenase, and cytochrome c oxidase, increased adenosine triphosphate (ATP) content, maintained high EC levels, inhibited respiration intensity, reduced peroxidase (POD) and polyphenol oxidase (PPO) activity and MDA accumulation, and prolonged vase life. Ethephon promoted ethylene production and respiration intensity, increased POD and PPO activity, reduced ATP content and EC levels, and accelerated senescence. Our results support a novel role for ethylene control in regulating senescence of 'Carola'.

• Journal of Life Science
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• v.24 no.5
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• pp.515-521
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• 2014

The oriental traditional medicine, Aruncus dioicus var kamtschaticus (ADK) is used for hemostasis (blood stopping) and the promotion of blood circulation. Recently, the demands of the aerial part of ADK as edible mountain herbs are rapidly increased due to its unique fragrance and bioactivity. In this study, to evaluate the anti-thrombosis activity of ADK, ethanol extract and organic solvent fractions were prepared from aerial parts of ADK, and their anticoagulation and anti-platelet aggregation activities were determined. In an anticoagulation activity assay, the ethanol extract of ADK increased the thrombin time, prothrombin time, and activated partial thromboplastin time (aPTT) 1.4-2.3 times at a concentration of 5 mg/ml. Among the fractions, the ethylacetate fraction showed strong inhibitory effects against blood clotting factors, as shown in an extension of the aPTT. In contrast, the butanol fraction strongly promoted blood clotting. In an anti-platelet aggregation assay, the activity of the ethanol extract was comparable to that of aspirin, a commercial anti-platelet aggregation agent, and the butanol fraction showed 2-fold higher aggregation inhibitory activity than aspirin. The aforementioned ethanol extract and active fractions have ignorable hemolytic activity against human red blood cells up to a concentration of 0.5 mg/ml. Considering the high content of total polyphenol, total flavonoid, and total sugar of the ethylacetate and butanol fractions, the purified active substances have potential as safe and novel anti-thrombosis agents. This report provides the first evidence of anti-thrombosis activity of ADK.

• Food Science and Preservation
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• v.21 no.5
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• pp.727-734
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• 2014

To investigate anti-thrombosis and anti-oxidation activities of the root of Arctium lappa L (RALL), which has been used as foodstuff and oriental medicine in Korea, the ethanol extract and its subsequent organic solvent fractions of the RALL were prepared. The yield of ethanol extraction was 10.94%, and the content of total polyphenol and total sugar of ethanol extract were 5.01 and 694.53 mg/g, respectively. The fraction yields of n-hexane, ethylacetate (EA), butanol and water residue were 1.62, 0.42, 5.98 and 85.38%, respectively. In anticoagulation activity assay, the ethanol extract of RALL did not show significant changes in thrombin time (TT), prothrombin time (PT) and activated partial thromboplastin time (aPTT), whereas the EA fractions showed 13 folds extended TT, PT, and aPTT respectively. Interestingly, the water residue showed strong activation effect against blood clotting factors with shortened aPTT, which might provide the evidence of coagulation agent of RALL in folk remedy. In anti-platelet aggregation assay, the activity of the ethanol extract and its fractions were comparable to that of aspirin. Especially the EA fraction showed 2-folds higher inhibitory activity than aspirin. In anti-oxidation activity assay, the EA fraction also showed strong in DPPH, ABTS and nitrite scavenging activity, and reducing power activity. The extract and fractions of RALL have ignorable hemolytic activity against human RBC up to 0.5 mg/mL concentration. Our results suggest that the EA fraction of RALL have potentials as safe and novel anti-thrombosis agent.

• Microbiology and Biotechnology Letters
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• v.42 no.3
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• pp.258-266
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• 2014

Sweet potato soju (SPS), a form of traditional distilled alcoholic liquor in Korea, is manufactured by the distillation of fermented broth under normal pressure, thus providing it for a uniquely smooth taste infused with the flavor of sweet potato. After distillation, the lees of SPS is produced as by-product and discarded. In this study, the ethanol and hot water extracts of lees of SPS, and their subsequent organic solvent fractions using hexane, ethylacetate (EA), butanol, and water residue were prepared in an effort at the efficient re-use of the lees of SPS. The ethanol extraction yield was 1.36-fold higher than that of the hot water extraction, and the EA fraction revealed the highest total polyphenol content among the solvent fractions. The various extracts and solvent fractions did not demonstrate hemolytic activity at up to 0.5 mg/ml concentrations against human red blood cells. In the bioactivity assay, only the EA fraction displayed a broad spectrum of anti-microbial activity against different pathogenic and food spoilage bacteria, and demonstrated significant anti-coagulation activity by inhibitions of thrombin, prothrombin and blood coagulation factors. Furthermore, only the EA fraction from the hot water extract of the lees of SPS showed anti-platelet aggregation activity, which is comparable to aspirin (a commercially available drug). Our results suggest that the EA fraction of the hot water extract prepared from the lees of SPS has a high potential as a novel resource for anti-microbial and anti-thrombosis agents.

• The Korea Journal of Herbology
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• v.33 no.3
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• pp.37-43
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• 2018

Objectives : Butylated hydroxytoluene (BHT) and butylated hydroxyanisole (BHA) were well known as anti-oxidant, but they were limited to use because of toxicity. So, many studies are being done to develope natural anti-oxidant. Total phenolic and flavonoid contents along with total antioxidant capacity of the ethanolic extract of Plantaginis Herba (PH) were evaluated to explore the reliable and potential sources of novel natural antioxidants. Methods : Total polyphenol contents and total flavonoid contents in PH ethanol extract were determined by colorimetric method. And DPPH(1.1-diphenyl-2-picrylhydrazyl), ABTS(2'-azino-bis (3-ethylbenzothiazoline-6-Surfonicacid)) free radical scavenging capacity and reducing power inhibition activities of PH ethanol extract were measured at 100, 500, 1000, $5000{\mu}g/m{\ell}$ concentrations by spectrometric assay. Results : The total polyphenol contents and total flavonoid contents of the extract were 161.99 mg/g, 144.05 mg/g, respectively. Also, DPPH, ABTS free radical scavenging capacity and reducing power of PH ethanol extract in treated concentrations (100, 500, 1000, $5000{\mu}g/m{\ell}$) increased dose dependently. In particular, DPPH free radical scavenging capacity of PH ethanol extract from $500{\mu}g/m{\ell}$ was significantly increased compared to positive control (BHA). ABTS free radical scavenging capacity of PH ethanol extract from $1000{\mu}g/m{\ell}$ was significantly higher than BHA. Also, reducing power showed that PH ethanol extract from $500{\mu}g/m{\ell}$ was significantly increased compared to BHA. Conclusions : These results suggest that PH ethanol extract has effects to scavenge free radicals, thus PH has potential and applicable benefits for development of materials and products to have anti-oxidation functions.

• Food Science of Animal Resources
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• v.34 no.4
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• pp.408-414
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• 2014

Pungency of hot pepper has limited its usage even though it shows various health beneficial effects. This study was conducted to develop the novel yoghurt containing hot pepper with diminishing pungency and aimed to examine the quality characteristics of yoghurt prepared with fermented red pepper. Hot pepper was first fermented with Bacillus licheniformis SK1230 to reduce the pungency of capsaicin. We then examined the quality, sensory characteristics, and antioxidant activity of yoghurt containing the fermented red pepper. The titratable acidity of this yoghurt increased whereas the viscosity decreased with increasing amounts of added red pepper. The total polyphenol content increased in proportion to the amount of added red pepper. The antioxidant activity significantly increased with the addition of red pepper (p<0.05). Color evaluation showed that the L value decreased whereas the a and b values increased significantly with the amount of red pepper added (p<0.05). In the sensory evaluation, yoghurt prepared with higher amounts of fermented red pepper received lower scores. However, yoghurt containing fermented red pepper at a concentration of 0.05% received higher scores for taste, flavor, and overall acceptability than yoghurt prepared with non-fermented pepper. Therefore, it can be concluded that the application of red pepper fermented by Bacillus licheniformis SK1230 gives beneficial feature to the preparation of yoghurt.