• Title/Summary/Keyword: Chelating

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Radiolabeling of NOTA and DOTA with Positron Emitting $^{68}$Ga and Investigation of In Vitro Properties (양전자 방출핵종 $^{68}$Ga을 이용한 NOTA와 DOTA의 표지 및 시험관내 특성 연구)

  • Jeong, Jae-Min;Kim, Young-Ju;Lee, Yun-Sang;Lee, Dong-Soo;Chung, June-Key;Lee, Myung-Chul
    • Nuclear Medicine and Molecular Imaging
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    • v.43 no.4
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    • pp.330-336
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    • 2009
  • Purpose: We established radiolabeling conditions of NOTA and DOTA with a generator-produced PET radionuclide $^{68}$Ga and studied in vitro characteristics such as stability, serum protein binding, octanol/water distribution, and interference with other metal ions. Materials and Methods: Various concentrations of NOTA 3HCl and DOTA 4HCl were labeled with 1 mL $^{68}$GaCl$_3$ (0.18$\sim$5.75 mCi in 0.1 M HCl in various pH. NOTA 3HCl (0.373 mM) was labeled with $^{68}$GaCl$_3$(0.183$\sim$0.232 mCi/0.1 M HCl 1.0 mL) in the presence of CuCl$_2$, FeCl$_2$, InCl$_3$, FeCl$_3$, GaCl$_3$, MgCl$_2$ or CaCl$_2$ (0$\sim$6.07 mM) at room temperature. The labeling efficiencies of $^{68}$Ga-NOTA and $^{68}$Ga-DOTA were checked by ITLC-SG using acetone or saline as mobile phase. Stabilities, protein bindings, and octanol distribution coefficients of the labeled compounds also were investigated. Results: $^{68}$Ga-NOTA and $^{68}$Ga-DOTA were labeled optimally at pH 6.5 and pH 3.5, respectively, and the chelates were stable for 4 hr either in the reaction mixture at room temperature or in the human serum at 37$^{\circ}C$. NOTA was labeled at room temperature while DOTA required heating for labeling. $^{68}$Ga-NOTA labeling efficiency was reduced by CuCl$_2$, FeCl$_2$, InCl$_2$, FeCl$_3$ or CaCl$_3$, however, was not influenced by MgCl$_2$ or CaCl$_2$. The protein binding was low (2.04$\sim$3.32%). Log P value of $^{68}$Ga-NOTA was -3.07 indicating high hydrophilicity. Conclusion: We found that NOTA is a better bifunctional chelating agent than DOTA for $^{68}$Ga labeling. Although, $^{68}$Ga-NOTA labeling is interfered by various metal ions, it shows high stability and low serum protein binding.

Antioxidant and anti-inflammatory activities of fruiting bodies of Dyctiophora indusiata (흰망태버섯 자실체의 메탄올 및 열수추출물의 항산화 및 항염증 활성)

  • Nguyen, Trung Kien;Shin, Do Bin;Lee, Kyung Rim;Shin, Pyung Gyun;Cheong, Jong Chun;Yoo, Young Bok;Lee, Min Woong;Jin, Ga-Heon;Kim, Hye Young;Im, Kyung Hoan;Lee, Tae Soo
    • Journal of Mushroom
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    • v.11 no.4
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    • pp.269-277
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    • 2013
  • Dictyophora indusiata is an edible mushroom belongs to Family Phallaceae of Phallales, Basidiomycota. The purpose of this study was to investigate the antioxidant and anti-inflammatory activities of methanol and hot water extracts prepared from fruiting bodies of Dictyophora indusiata. Besides measuring of 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity, a reducing power and a chelating activity on ferrous ions were also measured to evaluate the antioxidant activity for those extracts. To measure the anti-inflammatory activities for the extracts, nitric oxide(NO) production from lipopolysaccharide(LPS) treated RAW 264.7 macrophage cells and carrageenan-induced acute hind paw edema of rats were investigated. The results showed that the extracts have excellent DPPH scavenging and chelating activity on the ferrous ions compared with positive control. The nitric oxide(NO) production in LPS-stimulated RAW 264.7 macrophage cells were decreased as we increased the concentration of the mushroom extracts. Significant reduction of paw edema of rats were observed at 2~6 h after treatment of methanol and hot-water extracts with 50 mg/kg concentration to the rats which are induced acute hind paw edema by carrageenan administration. Therefore, the experimental results suggested that methanol and hot-water extracts of Dictyophora indusiata fruiting bodies might be used for natural sources of antioxidant and anti-inflammatory agents.

Antioxidant, anti-inflammatory and anti-acetylcholinesterase activities of fruiting bodies of Phellinus xeranticus (기와층버섯 자실체의 메탄올 및 열수추출물의 항산화, 항염증 및 아세틸콜린에스테라제 저해 활성)

  • Nguyen, Trung Kien;Shin, Do Bin;Lee, Kyung Rim;Shin, Pyung Gyun;Cheong, Jong Chun;Yoo, Young Bok;Lee, Min Woong;Jin, Ga-Heon;Kim, Hye Young;Im, Kyung Hoan;Lee, Tae Soo
    • Journal of Mushroom
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    • v.11 no.4
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    • pp.278-286
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    • 2013
  • Phellinus xeranticus is an medicinal mushroom belongs to Family Hymenochaetaceae of Polyporales, Basidiomycota. The purpose of this study was to investigate the antioxidant, anti-inflammatory and anti-acetylcholinesterase activities of methanol and hot water extracts prepared from fruiting bodies of Phellinus xeranticus. Besides measuring of 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity, a reducing power and a chelating activity on ferrous ions were also measured to evaluate the antioxidant activity of the extracts. To measure the anti-inflammatory activities of the extracts, nitric oxide(NO) production from lipopolysaccharide (LPS) stimulated RAW 264.7 macrophage cells and carrageenan-induced acute hind paw edema of rats were investigated. The results showed that the extracts have excellent DPPH scavenging and chelating activity on the ferrous ions compared with positive controls. The nitric oxide (NO) production in LPS-induced RAW 264.7 macrophage cells were decreased as the concentration of the mushroom extracts increased. Significant reduction of paw edema of rats were observed at 2~6 h after treatment of methanol and hot-water extracts with 50 mg/kg concentration to the rats which are induced acute hind paw edema by carrageenan administration. The anti-acetylcholinesterase activity of the methanol extract of the mushroom showed 83.34% inhibition on AcHE which is lower than that of positive control galanthamine. The experimental results suggested that methanol and hot-water extracts of Phellinus xeranticus fruiting bodies might be used for good sources of antioxidant, anti-inflammatory and anti-acetylcholinesterase agents.

Growth-promoting Effect of New Iron-chelating Fertilizer on Lettuce (산세수와 게껍질을 이용한 신기능성 철분 비료의 상추 생육 촉진 효과)

  • Hwang, Ji Young;Jun, Sang Eun;Park, Nam-Jo;Oh, Ju Sung;Lee, Yong Jik;Sohn, Eun Ju;Kim, Gyung-Tae
    • Journal of Life Science
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    • v.27 no.4
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    • pp.390-397
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    • 2017
  • Iron (Fe) is an important micronutrient for the health and growth of plants. Iron is usually provided by fertilizers, and iron-chelate fertilizers are well absorbed by plants. This study presents the plant growth-promoting effects of a new functional iron fertilizer, Fe-chelating crab shell powder (FCSP), which is generated from the chelation of Fe ions with crab shell powder. Iron chelate was derived from spent pickling liquor, which is rich in reductive iron, iron(II) oxide. To analyze the effects of FCSP on plant growth, we treated lettuce with several concentrations of FCSP in both lab- and field-scale experiments. In the lab-scale test, the treatment of 50 ppm of FCSP highly promoted growth and resulted in increases in the size, weight, number and chlorophylls content of leaves of plants compared to the treatment of crab shell powder. Fifty ppm of FCSP also increased the size and weight of leaves up to 2 times compared to the application of chemical fertilizer and/or compost in field conditions. In addition, the FCSP treatment resulted in the highest ion uptake of Fe in lettuce leaves. Moreover, FCSP led to increases in the amounts of Fe, Ca, available phosphorus and organic matter in treated soil, indicating that soil quality was improved. Taken together, our results demonstrate that FCSP promotes lettuce growth via enhancement of Fe availability and improves soil quality. Therefore, FCSP can be utilized as a new functional iron fertilizer.

Influence of Septic in Vibrio Vulnificus from Phytic Acid (피틴산(Phytic acid)이 비브리오(Vibrio vulnificus) 패혈증에 미치는 영향)

  • Chung, Young-Ho;Cho, Chun-Hwi;Lee, Sun-Woo;Lim, Chi-Hwan
    • Korean Journal of Agricultural Science
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    • v.32 no.1
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    • pp.71-80
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    • 2005
  • Phytic acid chelates excellently the metallic ions and the positive ions, especially has high affinity with $Fe^{2+}$ and $Ca^{2+}$. Merits of phytic acid can be taked in easily, edibile and harmless to body, so it was investigated that phytic acid can be substituted for EDTA in this study. 1. The Intensificative effect of chelating agent and disinfective osmotic shock of Vibrio vulnificus The number of initial existent fungi measured $1.7{\times}10^6$. The percentages of the survival fungi against the osmotic shock by distillated water were calculated at 1 minute, 3 minute and 5 minute after inoculation. The percentages of the survival fungi in $Mg^{2+}$ were 92.5%, 91.8% and 79.8% at each time, the average percentage was 88%. Also the sudden extinction was observed around 1 minute after inoculation and the survival fungi were not observed from 3 through 5 minute in spite of repeated experimentation. 2. Influence of Vibrio vulnificus on the survival of the mice. The first mouse started to die in 180 minute after inoculation in case that the inoculating number was $2.3{\times}10^7cfu/ml$. All died within 4.5 hour. The average of survival time was 226 minute. The first mouse started to die in 228 minute after inoculation in case that the inoculating number was $0.8{\times}10^6cfu/ml$. All died within 5 hour. The average of survival time was 300 minute and the survival time was 1.3 times high. The tendencies of death in two cases were similar, but the fatal rate were largely dependent on inoculating number.

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Antioxidant and Angiotensin Converting Enzyme I Inhibitory Activities of Extracts from Mulberry (Cudrania tricuspidata) Fruit subjected to Different Drying Methods (건조방법에 따른 꾸지뽕열매 추출물의 항산화활성과 Angiotensin Converting Enzyme I 저해활성)

  • Youn, Kwang-Sup;Kim, Jae-Won
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.41 no.10
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    • pp.1388-1394
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    • 2012
  • The physiological functionalities of 70% ethanol extracts (EE) from Cudrania tricuspidata fruit (ECFD, EE of C. tricuspidata subjected to freeze-drying; ECHD, EE of C. tricuspidata subjected to heat air drying; ECID, EE of C. tricuspidata subjected to infrared drying) were investigated. Yields of freeze-dried powders of ECFD, ECHD, and ECID were 51.50%, 53.91%, and 56.14%, respectively. Color $L^*$, $a^*$, $b^*$, and $H^{\circ}$ values of ECHD and ECID decreased. Dried ECHD and ECID had relatively higher contents of total polyphenolics and flavonoids than ECFD. Electron donating abilities at a concentration of 10 mg/mL (w/v) were in order of ECID (62.37%) >ECHD (80.17%)>ECFD (77.80%). Reducing powers ($OD_{700}$) of ECFD, ECHD, and ECID were 0.75, 1.70, and 1.89, respectively. Additionally, ABTS radical scavenging ability of ECID was the highest with a value of 62.37% at a concentration of 10 mg/mL (w/v). Nitrite scavenging activities of ECFD, ECHD, and ECID at a concentration of 10 mg/mL (w/v) were 28.76%, 30.69%, and 41.64%, respectively. SOD (superoxide dismutase)-like activities at 5 mg/mL (w/v) were in the order ECFD (891.93 mUnits)>ECHD (723.02 mUnits)>EFID (611.97 mUnits). Whereas ferrous ion chelating activity of ECFD (52.36%) and ECID (47.16%) was significantly higher than that of ECHD (30.04%). ACE inhibitory and xanthine oxidase (XO) inhibitory activities of ECHD and ECID at a concentration of 1 mg/mL (w/v) were higher than those of ECFD. In conclusion, we provided experimental evidence that extracts of pre-dried C. tricuspidata exhibit increased physiological functionalities. Further, infrared drying technique is the best method for enhancement of antioxidant activity of C. tricuspidata fruit.

A Study on the Cosmeceutical activities of Prunus Sargentii R. (산벚나무(Prunus sargentii R.) 수피의 화장품활성에 관한 연구)

  • Park, Jung-Mi;Lee, Jin-Young;Park, Tae-Soon;Hyun, Sok-Jun;Kim, Han-Hyuk;Cho, Young-Je;Kwon, O-Jun;Son, Ae-Ryang;Kim, Dong-Seok;An, Bong-Jeun
    • Applied Biological Chemistry
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    • v.51 no.1
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    • pp.70-78
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    • 2008
  • Prunus sargentii R. of Rosaceae familiy, has been reported to have radical scavenging activity and anti-inflammatory effect. On these facts, biological activity and safety test were conducted to evaluate biological activities of the extracts of P. sargentii R. as a potential pharmaceutical ingredient. The electron donating ability of its ethanol extracts at a 500 ppm level showed 92%, which was higher than that of hot water extract (59%), the superoxide dismutase (SOD)-like activity of the water extract of P. sargentii R. was about 50%, the ethanol extract of P. sargentii R. was about 40% at 1,000 ppm concentration. Xanthine oxidase inhibition by the water extract of P. sargentii R. was about 40% and that by the ethanol extract was 60% respectively at 500 ppm concentration. From the measurement on lipid oxidation, the $Cu^{2+}$ chelating effect of the ethanol extract was higher than that of hot water extract. The $Fe^{2+}$ chelating effect was also shown to be about 80% at a 500 ppm concentration in both hot water extract and ethanol extract. The tyrosinase inhibition effect related to skin-whitening was 26% by hot water extract and 20% by ethanol extract respectively at a 1,000 ppm. Hyaluronidase inhibition activity related to the anti-inflammation effect was 96% in ethanolic extract at a 500 ppm. Clear zones formed by P. sargentii R. against the human skin-resident micro-flora such as Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli and Propionibacterium acnes indicated that antimicrobial activity of the ethanol extract was higher than that of the hot water extract.

Antioxidant Effect according to Extraction Method in Extracts of Dendranthema zawadskii var. yezoense and Cosmos bipinnatus (추출 방법에 따른 남구절초와 코스모스 추출물의 항산화 효과)

  • Woo, Jeong-Hyang;Shin, So-Lim;Chang, Young-Deug;Lee, Cheol-Hee
    • Horticultural Science & Technology
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    • v.28 no.3
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    • pp.462-468
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    • 2010
  • Top parts of $Dendranthema$ $zawaskii$ var. $yezoense$ (DZY) and $Cosmos$ $bipinnatus$ (CB) are believed to contain substances with antioxidant effects and activity. Present experiments were undertaken to investigate an adequate and efficient extraction method which ensures the highest yield of antioxidant components. Extraction yield was 1.11-1.92 times higher by ultrasonic method than other methods in both species. By 45 minute ultrasonic extraction, total polyphenol contents reached the highest level, $80.70mg{\cdot}g^{-1}$ tannic acid equiv./DW in $Cosmos$ $bipinnatus$ and total flavonoid contents $50.41mg{\cdot}g^{-1}$ naringin equiv./DW in DZY. DPPH radical scavenging activity was almost the same among extraction methods or slightly higher in reflux extraction. The highest DPPH radical scavenging was observed by reflux extract in CB ($RC_{50}=0.135mg{\cdot}mL^{-1}$). ABTS radical scavenging activity was the highest by 15 minute ultrasonic wave in DZY and CB, $RC_{50}=0.159mg{\cdot}mL^{-1}$ and $RC_{50}=0.139mg{\cdot}mL^{-1}$, respectively. High ferrous ion chelating effects were obtained by 30-minute ultrasonic wave in DZY ($RC_{50}=0.803mg{\cdot}mL^{-1}$). Extracts of top parts of DZY obtained by reflux method showed the highest inhibition effect against peroxidation of linoleic acid, and extract of CB obtained by ultrasonic for 45 minutes showed the highest inhibition effect. In conclusion, optimum extraction method should be adjusted according to plant species and antioxidant substances.

Remediation of Heavy Metal Contamination in OBOD Site with Soil Washing : Selection of Extractants (토양세척법에 의한 중금속오염 폐탄처리장 토양의 정화 : 세척액의 선정)

  • Lee, Sang-Hwan;Kim, Eul-Young;Seo, Sang-Kee;Kim, Gweon-Bo;Kim, Jae-Hwan;Lee, Jong-Keun
    • Journal of Soil and Groundwater Environment
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    • v.13 no.2
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    • pp.44-53
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    • 2008
  • The efficiences of mineral acid (HCl), neutral salts ($CaCl_2$), and chelating agent (citric acid and $Na_2$-EDTA) were tested for extracting heavy metals from open burning and open detonation (OBOD) site soil. The extraction efficiencies of Cd, Cu, Pb and Zn from soil for various extractants were in the order of HCl > citric acid > $Na_2$-EDTA > $CaCl_2$, HCl (1.0 M) extracted effectively 82%, 86%, 80%, and 46% of initial total concentrations of Cd, Cu, Pb, and Zn, respectively. Significant negative correlations were observed between pH of extractant and amount of extracted heavy metals. Initially, examined heavy metals were predominantly bound to carbonate and Fe, Mn-oxide fraction. Though the significant amount of carbonate and Fe, Mn-oxide bounded metals were removed but a significant amount remained metals shifted to exchangeable (more mobile) fraction by HCl and citric acid extraction. The increased mobility of remaining metals could be problematic for water resources, thus careful management is needed to control the movement of heavy metals.

Biological Compounds Extracted from Codium fragile by Enzymatic Hydrolysis and Their Biological Activities (효소적 가수분해를 이용한 청각으로부터 생리활성 물질의 추출 및 가수분해물의 생리활성)

  • Lee, Ka-Hwa;Senevirathne, Mahinda;Ahn, Chang-Bum;Je, Jae-Young
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.39 no.7
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    • pp.953-959
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    • 2010
  • We extracted bioactive materials from Codium fragile by enzymatic hydrolysis using four different proteases (Alcalase, Flavourzyme, Neutrase, and Protamex) and seven different carbohydrases (amyloglucosidase (AMG), Celluclast, Dextrozyme, Maltogenase, Promozyme, Termamyl, and Viscozyme), and evaluated their biological activities such as antioxidant, anti-acetylcholinesterase (AChE), and anti-inflammatory effects. All enzymatic hydrolysates showed good DPPH radical scavenging capacities, in particular, Flavourzyme and Promozyme hydrolysates possessed the highest activity. The two hydrolysates also exhibited strong hydrogen peroxide scavenging activity, $Fe^{2+}$ chelating activity, and reducing power in a dose-dependent manner. Furthermore, the two hydrolysates effectively protected DNA damage induced by hydroxyl radical by measuring the conversion of supercoiled DNA to the open circular DNA. All enzymatic hydrolysates also showed high anti-AChE inhibitory activities in a dose-dependent manner, and did not showed any significant cytotoxicity on RAW264.7 cells (p<0.05). In addition, the enzymatic hydrolysates significantly (p<0.05) inhibited lipopolysaccharide induced-nitric oxide production on RAW264.7 cells. These results suggest that the enzymatic extracts from Codium fragile would be good source as an ingredient of functional foods.