• Title/Summary/Keyword: unknown compounds

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Antimicrobial Effect of Ursolic Acid and Oleanolic Acid against Methicillin-Resistant Staphylococcus aureus (Ursolic Acid와 Oleanolic Acid의 메티실린 저항성 Staphylococcus aureus에 대한 항균작용)

  • Kim, Saeng-Gon;Kim, Min-Jung;Jin, Dong-Chun;Park, Soon-Nang;Cho, Eu-Gene;Freire, Marcelo Oliveira;Jang, Sook-Jin;Park, Young-Jin;Kook, Joong-Ki
    • Korean Journal of Microbiology
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    • v.48 no.3
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    • pp.212-215
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    • 2012
  • The antimicrobial activity of ursolic acid (UA) and oleanolic acid (OA), both triterpenoid compounds, against methicillin-resistant Staphylococcus aureus (MRSA) is controversial. We examined the antimicrobial effects of UA and OA against 19 strains of MRSA isolated from Koreans by determining minimum inhibitory concentrations (MIC) and minimum bactericidal concentrations (MBC). The data showed that the methicillin-sensitive strain S. aureus KCTC $1621^T$ was more resistant to UA and OA than that of the MRSA strains. The MBC values of UA and OA against MRSA had broad ranges; 4 to 32 ${\mu}g/ml$ and 16 to >256 ${\mu}g/ml$, respectively. It was difficult to understand the different antimicrobial activities of UA and OA among the MRSA strains, because UA and OA antimicrobial mechanisms are unknown. These results indicate that the antimicrobial effects of UA and OA against MRSA are dependent on resistance to UA and OA in each strain.

Adverse Reproductive Effects on Plasma Vitellogenin and Sex Steroid Levels, and Gonadosomatic Index in Juvenile Common Carps (Cyprinus carpio) Exposed to 17$\beta$-Estradiol and D-2-Ethylhexyl Phthalate

  • Seo, Jinwon;Park, Kyung-Seo;Moon, Woon-Gi;Lee, Sung-Kyu
    • Proceedings of the Korea Society of Environmental Biology Conference
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    • 2002.11a
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    • pp.141-144
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    • 2002
  • Environmental estrogens are natural or synthetic substances present in the aquatic environment, especially in effluent from sewage treatment. However, the adverse effects of these estrogenic substances on fish reproduction are unknown. Di-2-ethylhexyl phthalate (DEHP) is the most common phthalate, which Ps used as a plasticizer in polyvinylchloride (PVC), and it is widespread in the environment and has been found in aquatic organisms and sediments. Therefore, juvenile common carps (Cyprinus carpio) were exposed to nominal concentrations of 17$\beta$-estradiol (E2) (0.5, 5, 50 $\mu\textrm{g}$/L) and DEHP (10, 100, 500 $\mu\textrm{g}$/L) for 21 days, to determine the adverse reproductive effects of these compounds on plasma vitellogenin (VTG) induction, sex steroid level, and gonad weight. Electrophoresis (SDS-PAGE) revealed that much of VTG was induced in fish exposed to 5 and 50 E$_2$ $\mu\textrm{g}$/L, but none of DEHP exposure showed induction. Enzyme-linked immunosorbent assay (ELISA) revealed that VTG was significantly induced in fish exposed to 5 and 50 E$_2$ $\mu\textrm{g}$/L, and combination of 50 E$_2$ $\mu\textrm{g}$/L with 10 and 500 DEHP $\mu\textrm{g}$/L, but none of DEHP exposure showed induction. Analysis of sex steroid levels in some fish revealed that testosterone (T) was detected in both male and female fish of the control and DEHP exposures, but none of fish exposed to 22 concentrations had detectable testosterone level. On the other hand, E$_2$ exposure induced 17$\beta$-estradiol in plasma of male fish, but there was no induction of 17$\beta$-estradiol in plasma of male fish exposed to DEHP. Comparison of gonadosomatic index (GSI) revealed that maximal E$_2$ exposure inhibited ovarian growth, but maximal DEHP exposure stimulated testicular growth. The results indicated that those comparisons can be a useful bio-indicator for determining adverse reproductive effect of endocrine disrupting chemicals (EDCs).

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Determination and Isolation of Antioxidative Serotonin Derivatives, N-(p-Coumaroyl)serotonin and N-feruoylserotonin from Safflower Seeds (홍화종자에서 항산화성 Serotonin계 화합물, N-(p-Coumaroyl)serotonin과 N-feruoylserotonin의 분리 및 정량분석)

  • Lee, Kang-Soo;Kim, Yun-Hee;Chung, Nam-Jin
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.53 no.2
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    • pp.171-178
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    • 2008
  • In the methanol extract from safflower seeds, two kinds of antioxidant were detected by preparative HPLC [$\mu$-Bondapak $C_{18}$ column ($7.8{\times}300\;mm$)]. Two unknown compounds were defined as CA and CB which had peaks at 22.1 min and 24.5 min, respectively. Antioxidant activity was measured by their scavenging ability on the stable tree radical of 1,1-diphenly-2-picrylhydrazyl (DPPH). For bulk extraction of antioxidants, the methanol extract was fractionated with hexan, chloroform, ethyl acetate and butanol. The ethyl acetate traction showing the highest DPPH radical scavenging activity was further purified by silica gel column chromatography to CA and CB. By NMR analysis, CA and CB were identified as N-(p-Coumaroyl)serotonin and N-feruoylserotonin, respectively. The content of N-(p-Coumaroyl)serotonin and N-feruoylserotonin were analyzed by reverse phase HPLC using a $\mu$-Bondapak $C_{18}$ column ($3.9{\times}300\;mm$) with linear gradient elution from 10% acetonitrile to 50% acetonitrile for 30min on UV detector at 300 nm. The contents of N-(p-Coumaroyl)serotonin and N-feruoylserotonin were 4.11 mg/g DW and 7.29 mg/g DW, respectively, and these two DPPH radical scavengers were detected only in the hull of seeds.

Anti-proliferation Effect of Coscinoderma sp. Extract on Human Colon Cancer Cells (Coscinoderma sp.의 대장암세포 증식 억제 효과)

  • Choi, Ki Heon;Jung, Joohee
    • Journal of Food Hygiene and Safety
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    • v.31 no.4
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    • pp.294-298
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    • 2016
  • Natural products are attractive as the source of new drug development. Especially, numerous unknown marine bioresources are an object of attention because the ocean occupies three fourth of the earth. Survival of marine bioresources in extreme environment may induce the production of biological active compounds. As previous study, we examined over 40 specimens of marine sponges collected from Micronesia and screened their anti-proliferative activities in various cancer cell lines. Among them, we investigated Coscinoderma sp.'s activity and mechanism in human colon carcinoma HCT116 and RKO cells. Furthermore, we also used the p53-knockout of HCT116 cells and the p53 loss of RKO cells for elucidating the role of p53. Coscinoderma sp. inhibited cellular viability independently of the p53 status. Therefore, we compared the expression level of cell death-related proteins by Coscinoderma sp. in HCT16 and in HCT116 p53KO cells. Coscinoderma sp. increased p53 level and NOXA levels and induced apoptosis under the condition of p53 existence. On the other hand, Coscinoderma sp. increased p21 and mTOR levels in HCT116 p53KO cells. These results suggest that Coscinoderma sp. induced anti-proliferation effect through different pathway depending on p53 status.

The Inhibitory Effect of Grapefruit Seed Extracts on the Physiological Function of Enterobacter pyrinus (Grapefruit 종자추출물이 Enterobacter pyrinus의 생리기능에 미치는 영향)

  • Lee, Tae-Ho;Jeong, Sook-Jung;Lee, Sang-Yeol;Kim, Jae-Won;Cho, Sung-Hwan
    • Korean Journal of Food Science and Technology
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    • v.27 no.6
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    • pp.985-990
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    • 1995
  • Grapefruit seed extracts(GFSE) have some unknown compounds which exhibit the antibiotic activities aganist microorganisms including bacteria and fungi. We have examined the effects of GFSE on the growth of Enterobacter pyrinus which was isolated from necrotic lesions of pear trees. During the cultivation, the growth of the bacteria was strongly inhibited at the low concentration(0.01%, w/w) of GFSE. Hydrophobic fraction extracted from GFSE by mixed solvents (chloroform : methanol : water, 1 : 2 : 0.8, v/v/v) had components which inhibited the growth of bacteria. There was, however, no inhibitory effect of GFSE on the activities of several enzymes including hexokinase, glucose 6-phosphate dehydrogenase, malate dehydrogenase and succinate dehydrogenase. $O-nitrophenyl-{\beta}-D-galactopyranoside(ONPG)$, the artificial substrate of ${\beta}-galactosidase$ was hydrolyzed in the presence of GFSE, indicating that the membrane was pertubated by the GFSE. From the results it was suggested that the antibiotic activity of GFSE is due to the change of membrane permeability of cell. GFSE was fractionated by high performance liquid chromatography equipped with $C_{18}$ reverse phase column. Among active fractions, three peaks were identified as 1-chloro-2-methyl-benzene (o-toluene), N,N-dimethyl-benzenemethaneamine, 1-[2-(2-ethylethoxy)ethoxy]-4- (1,1,3,3-tetramethyl)-bezene, respectively, while the other three remained unidentified.

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Development of Rapid and Simple Drug Identification and Semi Quantitative Analytical Program by Gas Chromatography-Mass Spectrometry (가스크로마토그래피/질량분석기를 이용한 약물의 확인 및 간이 정량분석 프로그램 개발)

  • Kim, Eun-Mi;Han, Eun-Young;Hong, Hyo-Jeong;Jeong, Su-Jin;Choe, Sang-Gil;Rhee, Jong-Sook;Jung, Jin-Mi;Yeom, Hye-Sun;Lee, Han-Sun;Lee, Sang-Ki
    • YAKHAK HOEJI
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    • v.55 no.2
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    • pp.106-115
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    • 2011
  • Systematic toxicological analysis (STA) means the process for general unknown screening of drugs and toxic compounds in biological fluids. In order to establish STA, in previous study we investigated pattern of drugs & poisons in autopsy cases during 2007~2009 in Korea, and finally selected 62 drugs as target drugs for STA. In this study, rapid and simple drug identification and quantitative analytical program by gas chromatography-mass spectrometry(GC-MS) was developed. The in-house program, "DrugMan", consisted of modified chemstation data analysis menu and newly developed macro modules. Total 55 drugs among 62 target drugs were applied to this program, they were 14 antidepressants, 8 anti-histamines, 5 sedatives/hypnotics, 5 narcotic analgesics, 3 antipsychotic drugs, and etc. For calibration curves, fifty five drugs were divided into four groups of range considering their therapeutic or toxic concentrations in blood specimen, i.e. 0.05~1 mg/l, 0.1~1 mg/l, 0.1~5 mg/l or 0.5~10 mg/l. Standards spiked bloods were extracted by solid-phase extraction (SPE) with trimipramine-D3 as internal standard. Parameters such as retention times, 3 mass fragment ions, and calibration curves for each drug were registered to DrugMan. A series of identification, semi quantitation of target drugs and reporting the results were performed automatically. Calibration curves for most drugs were linear with correlation coefficients exceeding 0.98. Sensitivity rate of DrugMan was 0.90 (90%) for 55 drugs at the level of 0.5 mg/l. For standard spiked bloods at the level of 0.5 mg/l for 29 drugs, semi quantitative concentrations were ranged 0.36~0.64 mg/l by DrugMan. If more drugs are registered to database in DrugMan in further study, it will be useful tools for STA in forensic toxicology.

Application and High Throughput Screening of DPPH Free Radical Scavenging Activity by Using 96-Well Plate (96-well plate를 이용한 DPPH free radical 소거활성 측정과 그 응용)

  • Choi, Jung-Sup;Oh, Jung-Im;Hwang, In-Taek;Kim, Sung-Eun;Chun, Jae-Chul;Lee, Byung-Hoi;Kim, Jin-Seok;Kim, Tae-Joon;Cho, Kwang-Yun
    • The Korean Journal of Pesticide Science
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    • v.7 no.2
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    • pp.92-99
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    • 2003
  • A 96-well plate was applied to determine the DPPH free radical scavenging activity using 107 plant-specific enzyme inhibitors and 100 unknown plant-originated extracts. The final optimum volume was $250{\mu}L$ containing $100{\mu}M$ DPPH ethanolic solution at pH 7.8. In this condition, the radical scavenging activities were significantly increased by two known antioxidants consisting of ascorbate and a-tocopherol in a concentration-dependent manner. Among the 107 inhibitors, ampicillin and gallic acid showed 90.2% and 92.6% antioxidant activity at $100{\mu}M$, respectively, and these results were consisted with previous findings. In the tested 100 natural materials at $50{\mu}g/mL$, antioxidant activity of AT-407 resulted in the highest of 90.1%, and 10 extracts including AT-388 and AT-443 showed over 70%. Our results suggest that the use of 96-well plate for determining DPPH free radical scavenging activity would be a suitable method to select antioxidant-like substances of both synthetic compounds and natural products.

Comparative molecular field analyses(CoMFA) on the growth inhibition activity of N-phenyl-3,4,5,6-tetrahydrophthalimide and N-phenyl-3,4-dimethylmaleimide Derivatives (N-치환 phenyl-3,4,5,6-tetrahydrophthalimide와 N-치환 phenyl-3,4-dimethylmaleimide 유도체의 생장 저해활성에 관한 l 분자장 분석 (CoMFA))

  • Sung, Nack-Do;Ock, Hwan-Suk;Song, Jong-Hwan;Lee, Yong-Gu
    • The Korean Journal of Pesticide Science
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    • v.7 no.2
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    • pp.75-82
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    • 2003
  • We discuss that the growth inhibition activities against root and shoot of rice plant (Oryza sativa L.) and barnyard grass (Echinochloa crus-galli) by N-phenyl-3,4,5,6-tetrahydrophthalimide (A) and N-phenyl-3,4-dimethylmaleimide (B) derivatives with changing substituents can be explained and predicted using comparative molecular field analyses (CoMPA) method. And the results show that the cross-validation value, $q^2$ at three components and Pearson correlation coefficient, $r^2$ were rice plant: shoot; $r^2=0.987$, $q^2=0.387$ & root; $r^2=0.923$, $q^2=0.307$ and barnyard grass: shoot; $r^2=0.902$, $q^2=0.535$ & root; $r^2=0.900$, $q^2=0.450$, respectively. In addition, The activities of unknown compounds were predicted by CoMFA method. From the contour map of (A) derivatives, the selective factors to remove barnyard grass takes positive charge on the benzylic carbon atom (C27), negative charged carbon atom (C29) of meta position and steric bulky groups on the cyclic imino ring (C7-C8).

Acute Toxicity of Oncheon Stream Water to the Sea Urchin, Hemicentrotus pulcherrimus (말똥성게에 대한 온천천수의 급성독성)

  • LEE Suk-MO;PARK Chung-Kil
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.17 no.5
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    • pp.414-422
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    • 1984
  • This research was conducted to evaluate the effect of polluted Oncheon Stream on the marine organisms in the Suyeong Bay. Water quality and 96 hr acute toxicity to the sea urchin, Hemicentrotns pulcherrimus by recirculation bioassay were examined from Feb. 20 to Apr. 15, 1984. The 96 hr $50\%$ effective concentration($EC_{50}$) on the attachment of the podia of the sea urchin was observed to occur at test concentrations between 40.0 and $51.0\%$ (v/v), and safe concentrations may be assumed to be within 4.0 and $5.1\%$. These values indicate as follows : 1. Oncheon Stream was extremely polluted by oxygen-demanding wastes and synthetic organic compounds from sewage and industrial waste water. 2. Linear alkylbenzene sulfonate(LAS) which has not been yet included in water quality standard was discharged above the TLm. 3. Unknown toxicity may be synergy among complex substances. In consideration of the relationship between COD values of Oncheon Stream and dilution water, the effect of toxicity of Oncheon Stream water reached to the area of the Suyeong Bay where the COD value was found to be 12.2 ppm.

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Betaine Induces Epidermal Differentiation by Enhancement of Autophagy through an mTOR-independent Pathway (Betaine의 mTOR 비의존적 자가포식 작용 촉진에 의한 표피 분화 유도 효과)

  • Choi, Seon-Guk;Kim, Mi-Sun;Kim, Jin-Hyun;Park, Sun Gyoo;Lee, Cheon Koo;Kang, Nae-Gyu
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.44 no.1
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    • pp.95-101
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    • 2018
  • The epidermis which is stratified by epithelial tissue renewal based on keratinocyte differentiation protects the organism from various environmental insults by forming a physical barrier. Autophagy is a mechanism which mediates lysosomal delivery and degradation of protein aggregates, damaged organelles and intracellular microorganisms. Recent reports have shown that autophagy has critical roles for proper terminal differentiation to stratum corneum via removing metabolic organelles and nuclei. However, whether increasing autophagy can activate epidermal differentiation is unknown. Here, we screened a library of natural single compounds and discovered that betaine specifically increased the LC3 positive cytosolic punctate vesicles and LC3-I to LC3-II conversion in HaCaT human keratinocyte cell line, indicating increased autophagy flux. mTOR pathway, which negatively regulates autophagy, was not affected by betaine treatment, suggesting betaine-induced autophagy through an mTOR-independent pathway. Betaine-induced autophagy was also observed in primary human keratinocyte and skin equivalent. Furthermore, epidermal thickness was increased in skin equivalent under betaine treatment. Overall, our finding suggests that betaine as a novel regulator of autophagy may induce epidermal turnover and improve the skin barrier abnormality of the aged epidermis.