• Bulletin of the Korean Chemical Society
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• 제30권7호
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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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• 제30권3호
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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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• 제17권3호
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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.

• 한국식품영양학회지
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• 제28권4호
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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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• 제59권6호
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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'.

• 생명과학회지
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• 제24권5호
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• pp.515-521
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• 2014

한방에서 지혈 및 어혈 제거용으로 사용되고 있는 눈개승마는, 최근 약용 산채로 그 수요가 급증하고 있다. 본 연구에서는 눈개승마의 항혈전 활성을 평가하고자 눈개승마 지상부로부터 에탄올 추출물 및 이의 순차적 유기용매 분획물을 조제하여 이들의 혈액응고 저해활성 및 혈소판 응집저해 활성을 평가하였다. 그 결과, 눈개승마의 에탄올 추출물(0.5 mg/ml)에서 1.4~2.3배의 우수한 TT, PT, aPTT 연장효과를 확인하였으며, 특히 내인성 혈액응고 인자 저해효과가 우수함을 확인하였다. 분획물에서는 ethylacetate 분획에서 가장 우수한 aPTT 연장효과를, butanol 분획에서는 혈액응고 촉진효과를 확인하였다. 혈소판 응집저해 활성평가의 경우, 눈개승마 에탄올 추출물은 임상에서 사용하는 항혈소판제인 아스피린에 필적하는 효과를 나타내었으며, 특히 butanol 분획은 0.25 mg/ml 농도에서 아스피린 0.5 mg/ml 에 해당하는 강력한 혈소판 응집저해능을 나타내었다. 상기의 에탄올 추출물과 활성 분획물들은 0.5 mg/ml 농도까지 인간 적혈구에 대한 용혈활성을 나타내지 않아, 눈개승마가 천연물 유래의 항혈전제로 개발 가능함을 확인하였으며, 특히 상기 활성분획들이 높은 함량의 total polyphenol, total flavonoid, total sugar를 포함함을 고려할 때, 활성물질의 정제시에는 더욱 강력한 항혈전 활성을 나타내리라 판단된다. 본 연구결과는 눈개승마의 항혈전 활성의 최초 보고이다.

• 한국식품저장유통학회지
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• 제21권5호
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• pp.727-734
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• 2014

식용 및 약용으로 이용되고 있는 우엉 지하부의 혈전 관련 활성과 항산화 활성을 평가하고자, 우엉의 ethanol 추출물 및 이의 순차적 유기용매 분획물을 조제하여 혈액응고 저해 활성, 혈소판 응집저해 활성, 인간 적혈구 용혈활성 및 in-vitro 항산화 활성을 평가하였다. 먼저 우엉 추출 수율은 10.94%로 다른 식용 및 약용식물보다 높았으며, ethanol 추출물의 경우 total polyphenol 함량은 5.01 mg/g으로 낮았으나, 694.53 mg/g의 높은 총당 함량을 나타내었다. 순차적 유기용매 분획의 경우, n-hexane, ethylacetate(EA), n-butanol 분획 수율은 각각 1.62, 0.42 및 5.98%로 나타났으며, 물 잔류물은 85.38%였다. 우엉 시료들의 혈액응고 저해활성을 TT, PT, aPTT를 측정한 결과, ethanol 추출물에서는 유의적인 활성이 나타나지 않았으나, EA 분획에서 강력한 TT, PT, aPTT 연장효과를 확인하였으며, 농도 의존적 혈액응고 저해활성을 확인하였다. 한편 물 잔류물에서는 내인성 혈액응고인자 활성화에 의한 aPTT 감소효과를 확인하여 혈전생성 촉진효과가 있음을 확인하였다. 혈소판 응집저해 활성평가의 경우, 우엉 ethanol 추출물 및 분획물들은 임상에서 사용하는 항혈소판제인 아스피린보다 강력한 저해효과를 나타내었으며, 특히 EA 분획은 정제되지 않은 상태에서도 아스피린의 2배 이상의 강력한 혈소판 응집저해능을 나타내었다. 또한 항산화 활성 평가 결과, EA 분획물은 DPPH 음이온, ABTS 양이온, nitrite에 대해 우수한 소거능 및 환원력을 나타내었다. 또한 우엉 추출물과 분획물들은 0.5 mg/mL 농도까지 인간 적혈구에 대한 특이한 용혈활성을 나타내지 않았다. 상기 결과들은, 우엉 EA 분획물이 천연물 유래의 안전한 항혈전제로 개발 가능함을 제시하고 있다.

• 한국미생물·생명공학회지
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• 제42권3호
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• pp.258-266
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• 2014

고구마 소주는 전분과 섬유질이 많은 고구마를 발효시킨 후 상압증류하여 제조되어 특유의 부드러운 맛과 향미를 가진다. 본 연구에서는 별도의 용도가 없어 폐기되고 있는 고구마 소주 주박의 효율적인 이용을 위해, 주박의 ethanol 및 열수 추출물을 조제하고 이들을 순차적 유기용매 분획하여 각각의 hexane, ethylacetate (EA), butanol 분획물과 물 잔류물을 조제하여 각 시료의 항균 및 항혈전 활성을 평가하였다. 그 결과, 주박의 ethanol 추출 효율이 열수 추출 효율보다 1.36배 높았으며, 분획물 중에서는 EA 분획물이 가장 높은 total polyphenol 함량을 나타냄을 확인하였다. 고구마 소주 주박의 추출물 및 분획물(0.5 mg/ml)은 인간 적혈구에 대한 용혈활성을 나타내지 않았으며, 열수 및 ethanol 추출물의 EA 분획물에서만 광범위 항세균 활성과 강력한 혈액응고 저해 활성이 나타났다. 또한 혈소판 응집저해 활성의 경우 열수 추출물의 EA 분획에서만 아스피린과 유사한 응집저해를 나타내었다. 본 연구결과는 폐기되고 있는 고구마 소주 주박의 열수 추출물의 EA 분획이 신규의 항세균 및 항혈전제로 개발될 수 있음을 제시하고 있다.

• 대한본초학회지
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• 제33권3호
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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.

• 한국축산식품학회지
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• 제34권4호
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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.