• Title/Summary/Keyword: $SnCl_2$

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A new efficient route for synthesis of R,R- and S,S-hexamethylpropyleneamine oxime for labeling with technetium-99m

  • Vinay Kumar Banka;Young Ju Kim;Yun-Sang Lee;Jae Min Jeong
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.6 no.2
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    • pp.75-91
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    • 2020
  • [99mTc]Tc-Hexamethylpropylene amine oxime (HMPAO) is currently used as a regional cerebral blood flow imaging agent for single photon emission computed tomography (SPECT). The HMPAO ligand exists in two isomeric forms: d,l and meso showing different properties in vivo. Later studies indicated that brain uptake patterns of 99mTc-complexes formed from separated enantiomers differed. Separation of enantiomers is difficult by fractional crystallizations method. Usually, the substance is obtained in low chemical yield in a time-consuming procedure. Furthermore, the final product still contains some impurity. So we have developed new efficient route for synthesis of R,R- and S,S-HMPAO enantiomeric compounds in 6-steps. Nucleophilic substitution (SN2) reactions of 2,2-dimethylpropane-1,3-diamine either with S- (1a) or R-methyl2-chloropropanoate (1b) were performed to produce compounds R,R- (2a) or S,S-isomer (2b) derivatives protected with benzylchloroformate (Cbz), respectively. And then Weinreb amide and methylation reaction using Grignard reagent, oxime formation with ketone group and deprotectiion of Cbz group by hydrogenolysis gave S,S- (7a) or R,R-HMPAO (7b), respectively. Entaniomeric compounds were synthesied with high yield and purity without any undesired product. The 7a or 7b kits containing 10 ㎍ SnCl2-2H2O were labeled with 99mTc with high radiolabeling yield (90%).

The dyeability and antimicrobial activity of Sophora Radix ethanol extracts - Characteristics of dyed silk - (고삼 에탄올 추출액의 염색성과 항균성 - 염색 견포를 중심으로 -)

  • 박선영;남윤자;김동현
    • Textile Coloration and Finishing
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    • v.14 no.1
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    • pp.1-10
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    • 2002
  • The aim of study was to elucidate dyeability and antimicrobial and antifungal activity of silk fabrics dyed with Sophora Radix extracts according to different mordants. Dyes were extracted from Sophora Radix using ethanol. Then, silk fabrics were dyed with extracts two times by post-mordanting method in which the extract was 60%(owf), the mordant was 3%(owf), L.R was 1:20, the temperature was $60~60^\circ{C}$, the time of dyeing was 60min., and the time of mordanting was 60min. The dyeability was evaluated by surface color, K/S values and durability of dye. The skin microorganisms used in this study was S. sureus, B. subtilis, S. epidermidis, P. acnes, P. aeruginosa, E coli, A. niger, C. albicans and T. mentatrophytes. The results are as follows; 1. When mordants were added, K/S value of silk dyed was not improved much and surface color was 2.2Y to 8.8Y in H(hue) value which indicated greenish yellow to raddish yellow 2. The color fastness tests to light, perspiration, dry-cleaning, rubbing, and stain fabric washing show 4~5th degree which were valuated excellent. The color fastness to fade washing was improved to 3~4th degree by addition of $K_2CrO_7$ mordants. 3. Antibacterial activity of silk dyed using no-mordant as well as mordants was excellent on S. aureus, B. subtilis, S.epidermidis and P.acnes, but showed poor antibacterial activities on P.aeruginosa and E.coli such as gram negative baterials 4. Antifungal activity of silk dyed with ethanol extracts was good on A.niger, C.candida and T.mentagrophytes. Especially, on T. mentagrophytes there was no growth of fungus during 72 gous in silk dyed mordanting with $SnCl_2\cdot{2H}_2O$.

Studies on Preparation of $^{99m}Tc$ Labelled 3-Iodo-2,4,6-trimethyl-iminodiacetic acid $(^{99m}Tc-IOTIDA)$ for Diagnosis of Hepatobiliary Disease (간.담도계 질환 진단용 $^{99m}Tc$ 표지 3-요오도-2,4,6-트리메틸 이미노 2초산$(^{99m}Tc-IOTIDA)$의 제조에 관한 연구)

  • Park, Kyung-Bae;Awh, Ok-Doo;Kim, Jae-Rok
    • The Korean Journal of Nuclear Medicine
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    • v.24 no.1
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    • pp.49-55
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    • 1990
  • For the development of $^{99m}Tc-labelled$ 3-iodo-2,4,6-trimethyl-iminodiacetic acid $(^{99m}Tc-IOTIDA)$, various experiments such as synthesis of IOTIDA, establishment of labelling conditions, determination of radiochemical purity, examination of stability, and organ distribution of rat were carried out. 1) IOTIDA was synthesized with a total yield of 42% from the starting material of 2,4-6-trimethylaniline via chloroacetylation, iodination, and condensation with iminodiacetic acid (IDA). 2) Freeze-dried instant labelling kits were prepared from aqueous solution $(pH\;5.8\sim6.0)$ so as to contain 40 mg IDA compound and 0.4 mg $SnCl_2$, per vial. Labelling of the contents of kit vials with $Na^{99m}TcO_4$, exhibited formation of two kinds of complex which was identified by ITLC-SA. After labelling, complex ( I ) was gradually converted to complex (II) with time. Labelling yield and radiochemical purity were above 99.5% based on the two complexes over-all. 3) $^{99m}Tc-IOTIDA$ maintained high radiochemical purity of above 99% until 6 hours after preparation at room temperature. Instant labelling kits stored at $4^{\circ}C$ for 6 month period also exhibited high labelling yield of above 99%. 4) Results obtained from animal experiments showed that most of the $^{99m}Tc-IOTIDA$ was rapidly excreted through hepatobiliary track into the intestines but with negligible renal excretion.

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Study of 188Re(V)-DMSA for Treatment of Cancer: Radiolabeling and Biodistribution (암 치료를 위한 188Re(V)-DMSA에 관한 연구: 방사성동위원소 표지와 생체내 분포)

  • Kim, Young Ju;Jeong, Jae Min;Chang, Young Soo;Lee, Dong Soo;Chung, June-Key;Lee, Myung Chul;Koh, Chang-Soon
    • The Korean Journal of Nuclear Medicine
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    • v.32 no.1
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    • pp.81-88
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    • 1998
  • The purpose of this study was to examine the radiolabeling and biodistribution of $^{188}Re(V)$-DMSA as a therapeutic cancer radiopharmaceutical. We made a DMSA kit($NaHCO_3$ 1.5 mg, meso-2,3-dimercaptosuccinic acid 1.0 mg, L(+)-ascorbic acid 0.7 mg, $SnCl_2{\cdot}2H_2O$ 0.34 mg, pH 2.9) for labeling with $^{188}Re$. In this kit, $^{188}ReO_4{^-}$ 5 mCi/2 ml added and boiled at $100^{\circ}C$ for 3 hr in water bath. The final pH adjusted to 7.5 with 7% $NaHCO_3$ solution. We checked the labelling efficacy with TLC-SG(n-butanol : acetic acid : $H_2O$ = 3 : 2 : 3) and examined the stability both in room temperature and in serum at $37^{\circ}C$. Biodistribution(1, 3, 13, 24, 48 hr) of $^{188}Re(V)$-DMSA compound was evaluated in Sarcoma 180 tumor-bearing mice. Each labeling efficiency and stability at room temperature for 48 hours was over 98% and 95%, respectively. The stability in serum were 82%(6 hr) and 85%(48 hr). Tumor uptake of $^{188}Re(V)$-DMSA in Sarcoma 180-bearing mice were $0.66{\pm}0.15%$(1 hr), $0.51{\pm}0.10%$(3 hr), $0.19{\pm}0.05%$(24 hr) and $0.13{\pm}0.02%$(48 hr). These result are consistent with those of $^{99m}Tc(V)$-DMSA which were reported previously. In conclusion, $^{188}Re(V)$-DMSA may be a useful therapeutic radiopharmaceutical for treating some cancers and metastatic bone lesion.

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The Dyeability and Antimicrobial Activity of Cotton Fabric Dyed with Sophora Radix Extracts on Skin Microorganisms (고삼 추출액를 이용한 염색 면포의 염색성와 피부 미생물 억제효과)

  • 박선영;남윤자;김동현
    • Journal of the Korean Society of Clothing and Textiles
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    • v.26 no.3_4
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    • pp.464-472
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    • 2002
  • The aim of this study was to elucidate dyeability and antimicrobial activity of cotton fabrics dyed with Sophora Radix extracts according to various mordants. Dyes were extracted from Sophora Radix using ethanol. Then, cotton fabrics were dyed with extracts two times by post-mordanting method in which the extract was 60% (owf, the mordant was 3% (owf), L.R was 1:20, the temperature was 60~7$0^{\circ}C$, the time of dyeing was 60min., and the time of mordanting was 60min.. The dyeability was evaluated by surface color and color fastness. The skin microorganism was evaluated on S. sureus, B. subtilis, S. epidermidis, P. acnes, P. aeruginosa, E. coli, A. niger, C. albicans and T. mentagrophytes. The results are as follows; 1. When mordants were treated, surface color was 3.3Y to 0.1 GY in H (hue) value which indicated greenish yellow to yellow 2. The color fastness to perspiration, dry-cleaning, rubbing, and washing stain fabric showed 4~5 degree. The color fastness to light was improved to 4 degree by treatment of mordants. The color fastness to washing was 2 degree which was somewhat poor. 3. Cotton dyed with ethanol extracts was excellent on S. aureus, B. subtilis, S. epidermidis and p. antis. But that showed poor antibacterial activities on P. aeruginosa and E. coli such as gram negative baterials 4. Antibacterial activity of cotton fabrics dyed didn't be improved by treatment of mordant 5. Antifungal activity of cotton dyed with ethanol extracts was excellent on T. mentagrophytes. Especially, on T. mentagrophytes there was no growth of fungus during 72 hours in cotton dyed mordanting with SnCl$_2$.$_2$$H_2O$.

Studies on the Selective Separation and Preconcentration of Cr(VI) Ion by XAD-16-Chromotropic Acid Chelating Resin (XAD-16-Chromotropic Acid 킬레이트 수지에 의한 몇 가지 금속이온의 선택적 분리 및 농축에 관한 연구)

  • Lee, Won;Lee, Chang-Youl;Kim, Mi-Kyoung;Kim, In-Whan
    • Analytical Science and Technology
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    • v.17 no.3
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    • pp.199-210
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    • 2004
  • A new polystyrene-divinylbenzene chelating resin containing 4,5-dihydroxy-naphthalene-2,7-disulfonic acid (chromotropic acid : CTA) as functional group has been synthesized and characterized. The sorption and desorption properties of this chelating resin for Cr(III) ion and Cr(VI) ion including nine metal bloodstain. As a results, FOB test kit could be effectively applied to identification of human blood at chelating resin was stable in acidic and alkaline solution. The Cr(VI) ion is selectively separated from Cr (III) ion at pH 2 and the maximum sorption capacity of Cr(VI) ion is 1.2 mmol/g. In the presence of anions such as $F^-$, $SO{_4}^{2-}$, $CN^-$, $CH_3COO^-$, $NO{_3}^-$, the sorption of Cr(VI) ion was reduced but anions such as $PO{_4}^{3-}$ and $Cl^-$ revealed no interference effect. The elution order of metal ions obtained from breakthrough capacity and overall capacity at pH 2 was Cr(VI)>Sn(II)>Fe(III)>Cu(II)>Cd(II)${\simeq}Pb(II){\simeq}Cr(III){\simeq}Mn(II){\simeq}Ni(II){\simeq}Al(III)$. Desorption characteristics for Cr(VI) ion was investigated with desorption agents such as $HNO_3$, HCl, and $H_2SO_4$. It was found that the ion showed high desorption efficiency with 3 M HCl. As the result, the chelating resin, XAD-16-CTA was successfully applied to separation and preconcentration of Cr (VI) ion from several metal ions in metal finishing works.

Effect of Carrier on Labeling and Biodistribution of Re-188-Hydroxyethylidene diphosphonate (담체가 Re-188-Hydroxyethylidene Diphosphonate의 표지와 생체내분포에 미치는 영향)

  • Chang, Young-Soo;Jeong, Jae-Min;Kim, Bo-Kwang;Cho, Jung-Hyuk;Lee, Dong-Soo;Chung, June-Key;Lee, Seung-Jin;Jin, Ren-Jie;Lee, Sang-Eun;Lee, Myung-Chul
    • The Korean Journal of Nuclear Medicine
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    • v.34 no.4
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    • pp.344-352
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    • 2000
  • Purpose: Re-188-Hydroxyethylidene diphosphonate (HEDP) is a new cost-effective agent for systemic radioisotope therapy of metastatic bone pain. We investigated the influence of carrier for labeling and biodistribution of Re-188-HEDP using HEDP kit with or without carrier ($KReO_4$). Materials and Methods: The kits (HEDP 15 mg, gentisic acid 4 mg and $SnCl_2.2H_2O_2$ 4.5 mg) with or without carrier ($KReO_4$ 0.1 mg) were labeled with Re-188 solution, made available from an in-house generator by boiling for 15 min. We compared the labeling efficiency and stability of carrier-added and carrier-free preparations of Re-188-HEDP Biodistribution and imaging studies of each preparation were performed in ICR mice ($1.85{\sim}3.7MBq/0.1ml$) and SD rats ($74.1{\sim}85.2MBq/0.5ml$). Results: The carrier-added preparation showed high labeling efficiency (95% at pH 5) and high stability in serum (88%, 3 hr). However, the carrier-free preparation showed low labeling efficiency (59% at pH 5) and low stability (43%, 3 hr). The carrier-added preparation showed high uptake in bone and low uptake in stomach and kidneys. However, the carrier-free preparation showed lower uptake in bone and higher uptake in both stomach and kidneys, which is supposed to be due to released perrhenate. The carrier-added preparation also showed better images with higher skeletal accumulation, lower uptake in other organs and lower soft tissue uptake than the carrier-free preparation. Conclusion: The results of these studies clearly demonstrate that addition of carrier perrhenate is required for high labeling efficiency, stability, bone uptake and good image quality of Re-188-HEDP.

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Gene Cloning, Nucleotide Sequence and Efficent Expression of Peptidyl proryl cis-trans Isomerase from Bacillus stearothermophilus (Bacillus stearothermophilus의 Peptidyl Prolyl cis-trans Isomerase 유전자 분리 염기배열 및 발현)

  • 김동주
    • The Korean Journal of Food And Nutrition
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    • v.9 no.4
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    • pp.452-458
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    • 1996
  • A PPIase gene of Bacillus stearothermophilus was screened from a genomic library by plaque hybridization using the A-1 primer as a probe. A PPIase positive plaque contained a 3.0kb insert of the chromosomal DNA. A 3.0kb fragment was subcloned into pUC18, resulting pPI1-40. A DNA fragment encoding the N-terminal portion of the PPIase in pPi-40 was amplified by polymerase chain reaction(PCR) method using the A-1 and B-2 primers. The amplified fragment was cloned into the Sma I site of pUC18 and recombinant plasmid was designated as pSN-18. The nucleotide sequence of 167bp fragment was determined. The deduced amino acid sequence of PPIase was completely matched with the determined N-terminal amino acid sequence of PPIase B. stearothermophilus. The translated protein sequence of PPIase B. stearothermophilus was compared with sequence from periplasmic PPIase from Escherichina coil ; homogies of 16 and 58%, respectively, were found. The clond PPIase gene was over-expressed in E. coil cell using pUC19 as an expression vector. The enzyme was partially purified by heat treatment and colum chromatochraphy on DEAE-Sepharose CL-6B. The molecular weight of the enzyme was dermined to be about 18.0 kDal by SDS-PAGE.

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Synthesis and In vitro Evaluation of 99mTc-diglucosediethylenetriamine (DGTA) as a Potential Tumor Imaging Agent

  • Lee, Sang-Ju;Oh, Seung-Jun;Kim, Jung-Young;Ryu, Jin-Sook;Kim, Seog-Young;Moon, Dae-Hyuk
    • Bulletin of the Korean Chemical Society
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    • v.32 no.7
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    • pp.2410-2412
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    • 2011
  • Using a single step chemical synthesis, we synthesized the potential tumor imaging agent $^{99m}Tc$-diglucose-diethylenetriamine (DGTA) from diethylenetriamine and natural D-glucose. 10 min Incubation of 10 mg of precursor with 50 ${\mu}g$ of $SnCl_2{\cdot}2H_2O$ at room temperature yielded over 95% of $^{99m}Tc$ labeling. The stability for 6 hours in saline or human plasma was over 90%. In vitro tumor cell uptake assays using the SNU-C5 and 9 L cell lines showed that, in 0-400 mg/dL glucose medium, cell uptake of $^{99m}Tc$-DGTA was 1.5-8 times higher than that of [$^{18}F$]FDG. Moreover, [$^{18}F$]FDG uptake was dependent on glucose concentration in the medium, whereas cellular uptake of $^{99m}Tc$-DGTA was not dependent on glucose concentration, suggesting that the two compounds have different uptake mechanisms by tumor cells.

The Mineralogical and Geochemical Study on Korean Scheelites and its Application to the Ore Prospecting (한국산 灰重石鑛의 광물학적, 지화학적 연구 및 그의 探査에의 이용)

  • So, Chil-Sup;Park, Maeng-Eon
    • Economic and Environmental Geology
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    • v.12 no.2
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    • pp.79-93
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    • 1979
  • Twenty five samples of the scheelite-powellite series from twelve Korean tungsten deposits of various geologic settings were studied mineralogically and geochemically. Variations in the trace-element contents of the scheelite minerals are considered in relation to geologic settings and mineralogic properties. Scheelites from ore deposits developed in similar geologic settings and under similar physicochemical conditions are characterized by specific combinations of trace elements.

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