• Title/Summary/Keyword: L(3, 2, 1)-labeling

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Automated Synthesis of [$^{18}F$]Fallypride for Routine Clinical Use (자동합성장치를 이용한 [$^{18}F$]Fallypride의 합성)

  • Park, Jun-Hyung;Moon, Byung-Seok;Lee, Hong-Jin;Lee, Hyo-Jun;Lee, In-Won;Lee, Byung-Chul;Kim, Sang-Eun
    • The Korean Journal of Nuclear Medicine Technology
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    • v.14 no.2
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    • pp.104-109
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    • 2010
  • Purpose: $[^{18}F]$Fallypride plays an effective radiotracer for the study of dopamine $D_2/D_3$ receptor occupancy, neuropsychiatric disorders and aging in humans. This tracer has the potential for clinical use, but automated labeling efficiency showed low radiochemical yields about 5~20% with relatively long labelling time of fluorine-18. In present study, we describe an improved automatic synthesis of [$^{18}F$]Fallypride using different base concentration for routine clinical use. Materials and Methods: Fully automated synthetic process of [$^{18}F$]Fallypride was perform using the TracerLab $FX_{FN}$ synthesizer under various labeling conditions and tosyl-fallypride was used as a precursor. [$^{18}F$]Fluoride was extracted with various concentration of $K_{2.2.2.}/K_2CO_3$ from $^{18}O$-enriched water trapped on the ion exchange cartridge. After azeotropic drying, the labeling reaction proceeded in $CH_3CN$ at $100^{\circ}C$ for 10 or 30 min. The reaction mixture was purified by reverse phase HPLC and collected organic solution was exchanged by tc-18 Sep-Pak for the clinically available solution. Results: The optimal labeling condition of [$^{18}F$]Fallypride in the automatic production was that 2 mg of tosyl-fallypride in acetonitrile (1 mL) was incubated at $100^{\circ}C$ for 10 min with $K_{2.2.2.}/K_2CO_3$ (11/0.8 mg). [$^{18}F$]Fallypride was obtained with high radiochemical yield about $66{\pm}1.4%$ (decay-corrected, n=28) within $51{\pm}1.2$ min including HPLC purification and solid-phase purification for the final formulation. Conclusion: [$^{18}F$]Fallypride was prepared with a significantly improved radiochemical yield with high specific activity and shorten synthetic time. In addition, this automated procedure provides the high reproducibility with no synthesis failures (n=28).

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Apoptosis of Germ Cells after Vasectomy in Rats (수컷 랫드에서 졍관절제술에 의한 생식세포의 Apoptosis)

  • Choi, Jong-yun;Cho, Sung-whan;Ryu, Si-yoon;Jee, Young-heun;Lee, Geun-jwa;Son, Hwa-young
    • Korean Journal of Veterinary Research
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    • v.43 no.3
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    • pp.485-492
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    • 2003
  • The pathological mechanism of impaired spermatogenesis after vasectomy has not been completely investigated. In this study, we examined pathological changes of the testis and the Fas-Fas ligand (FasL) mediated signaling pathway in apoptotic germ cell death after vasectomy in rats. Ten-weeks old Sprague-Dawley rats were underwent bilateral vasectomy and sacrificed after 1 day, 2 days, 3 days, 5 days, 1 week, 2 weeks, and 4 weeks of surgery and the testes were removed. Histopathological evaluation of spermatogenesis was performed by hematoxylin-eosin and periodic acid-Schiff-hematoxylin staining. To elucidate the pathophysiology of seminiferous tubule damage, terminal dUTP nick end labeling staining, electrophoresis assay of DNA fragmentation, and Western blotting analysis for Fas-FasL were performed. Relative weights of testes were decreased from 5 days after vasectomy. Germ cell degeneration were first found in the spermatogonia and spermatocytes at stages I-VI, and XII-XIV seminiferous tubules. Mean incidence of apoptotic germ cells after vasectomy progressively increased to peak in 5 days, and then gradually decreased to the control levels in 2 weeks after vasectomy. The expression of Fas-FasL reached maximum level at 5 days after vasectomy and then declined. In conclusion, impaired spermatogenesis after vasectomy associated with an increase in germ cell apoptasis, which is partly mediated by the activation of Fas-FasL.

Neuroprotective effects of L-carnitine against oxygen-glucose deprivation in rat primary cortical neurons

  • Kim, Yu-Jin;Kim, Soo-Yoon;Sung, Dong-Kyung;Chang, Yun-Sil;Park, Won-Soon
    • Clinical and Experimental Pediatrics
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    • v.55 no.7
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    • pp.238-248
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    • 2012
  • Purpose: Hypoxic-ischemic encephalopathy is an important cause of neonatal mortality, as this brain injury disrupts normal mitochondrial respiratory activity. Carnitine plays an essential role in mitochondrial fatty acid transport and modulates excess acyl coenzyme A levels. In this study, we investigated whether treatment of primary cultures of rat cortical neurons with L-carnitine was able to prevent neurotoxicity resulting from oxygen-glucose deprivation (OGD). Methods: Cortical neurons were prepared from Sprague-Dawley rat embryos. L-Carnitine was applied to cultures just prior to OGD and subsequent reoxygenation. The numbers of cells that stained with acridine orange (AO) and propidium iodide (PI) were counted, and lactate dehydrogenase (LDH) activity and reactive oxygen species (ROS) levels were measured. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay and the terminal uridine deoxynucleotidyl transferase-mediated deoxyuridine triphosphate nick-end labeling assay were performed to evaluate the effect of L-carnitine (1 ${\mu}M$, 10 ${\mu}M$, and 100 ${\mu}M$) on OGD-induced neurotoxicity. Results: Treatment of primary cultures of rat cortical neurons with L-carnitine significantly reduced cell necrosis and prevented apoptosis after OGD. L-Carnitine application significantly reduced the number of cells that died, as assessed by the PI/AO ratio, and also reduced ROS release in the OGD groups treated with 10 ${\mu}M$ and 100 ${\mu}M$ of L-carnitine compared with the untreated OGD group (P<0.05). The application of L-carnitine at 100 ${\mu}M$ significantly decreased cytotoxicity, LDH release, and inhibited apoptosis compared to the untreated OGD group (P<0.05). Conclusion: L-Carnitine has neuroprotective benefits against OGD in rat primary cortical neurons in vitro.

Syntheis and $^{99m}Tc$ labeling of Ethylcystein Dimer and Its Brain SPECT Image (두뇌 혈류영상용 방사성의약품인 Ethylcystein Dimer(ECD)의 합성과 $^{99m}Tc$ 표지 및 뇌단일광자단층영상 구성)

  • Jeong, Jae-Min;Lee, Myung-Chul;Chung, Soo-Wook;Lee, Kyung-Han;Cho, Jung-Hyuck;Kwark, Cheol-Eun;Lee, Dong-Soo;Chung, June-Key;Koh, Chang-Soon
    • The Korean Journal of Nuclear Medicine
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    • v.28 no.2
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    • pp.167-171
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    • 1994
  • Ethylcystein dimer (ECD) was synthesized by dimerizatlon of L-thiazolidine-4-carboxylic acid in liquid ammania with sodium metal and successive esterification in ethanolic solution of hydrogen chlorde. The purified product was labeled with $^{99m}Tc$ in the presence of sodium glucarate(pH= 5.6) and stannous chloride. Best result was obtained from the preparation con sisting of 0.1mg ECD, $40{\mu}l$ of 0.4M sodium glucarate (pH=5.6), and $20{\mu}g$ of stannous chloride. The labeling efficiency was 90% with previous condition. The labeled $^{99m}Tc$-ECD was stable at least for 3 hours in PBS(pH=7.4) at room temperature. About 10mCi of $^{99m}Tc$-ECD was injected to normal volunteer, and SPECT image of brain was obtained by triple head camera 10 minutes after inection. The image showed similar distribution of radioactivity in brain with that of HMPAO image.

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Preparation and Animal Imaging of $^{153}Sm$-EDTMP as a Bone Seeking Radiopharmaceutical (골친화성 방사성의약품 $^{153}Sm$-EDTMP의 합성과 동물영상)

  • Choi, Tae-Hyun;Kim, Se-Jung;Shin, Byung-Chul;Woo, Kwang-Sun;Chung, Wee-Sup;Choi, Chang-Woon;Lim, Sang-Moo
    • The Korean Journal of Nuclear Medicine
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    • v.39 no.1
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    • pp.44-48
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    • 2005
  • Purpose: Ethylenediamine-tetramethylenephosphonic acid (EDTMP) has widely used chelator for the labeling of bone seeking radiopharmaceuticals complexed with radiometals. $^{153}Sm$ can be produced by the HANARO reactor at the Korea Atomic Energy Research Institute, Taejon, Korea. $^{153}Sm$ has favourable radiation characteristics $T1/2=46.7\;h,\;{\beta}_{max}=0.81\;MeV\;(20%),\;0.71\;MeV\;(49%),\;0.64\;MeV\;(30%)\;and\;{\gamma}=103\;keV\;(30%)$ emission which is suitable for imaging purposes during therapy. We investigated the labeling condition of $^{153}Sm$-EDTMP and imaging of $^{153}Sm$-EDTMP in normal rats. Materials and methods: EDTMP 20 mg was solved in 0.1 mL 2 M NaOH. $^{153}SmCl^3$ was added to EDTMP solution and pH of the reaction mixtures was adjusted to 3 and 12, respectively. Radiochemical purity was determined with paper chromatography. After 30 min. reaction, reaction mixtures were neutralized to pH 7.4, and the stability was estimated upto 120 hrs. Imaging studies of each reaction were perfomed in normal rats (37 MBq/0.1 mL). Results: The labeling yield of $^{153}Sm$-EDTMP was 99%. The stability of pH 8 reaction at 60, 96 and 120 hr was 99%, 95%, 89% and that of pH 12 at 36, 60, 96 and 120 hr was 99%, 95%, 88%, 66%, respectively. The $^{153}Sm$-EDTMP showed constantly higher bone uptake from 2 to 48 hr after injection. Conclusion: $^{153}Sm$-EDTMP, labeled at pH 8 reaction condition, has been stably maintained. Image of $^{153}Sm$-EDTMP at 2, 24, 48 hr after injection, demonstrate that $^{153}Sm$-EDTMP is a good bone seeking radiopharmaceuticals.

NMR Studies on the Structure of Human Annexin I

  • Lee, Yeon-Hee;Han, Hee-yong;Oh, Jee-Young;Na, Doe-Sun;Lee, Bong-Jin
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1997.04a
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    • pp.86-86
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    • 1997
  • Human annexin I is a member of annexin family of calcium dependent phospholipid binding proteins, which have been implicated in various physiological roles including phospholipase A$_2$ (PLA$_2$) inhibition, membrane fusion and calcium channel activity. In this work, the structure of N-terminally truncated human annexin I (Δ-annexin I) and its interactions with Ca$\^$2+/, ATP and cAMP were studied at atomic level by using $^1$H, $\^$15/N, $\^$l3/C NMR (nuclear magnetic resonance) spectroscopy. The effect of Ca$\^$2+/ binding on the structure of Δ-annexin I was investigated, and compared with that of Mg$\^$2+/ binding. The addition of Ca$\^$2+/ to Δ-annexin I caused some changes in the high field and low field regions of $^1$H NMR spectra. Whereas, upon addition of Mg$\^$2+/ to Δ-annexin I, almost no change could be observed. Also we found that the binding ratio of ATP to Δ-annexin I is 1. Because Δ-annexin I is a large protein with 35 kDa molecular weight, site-specific (carbonyl-$\^$l3/C, amide-$\^$15/N) labeling technique was used to determine the interaction sites of Δ-annexin I with Ca$\^$2+/ and ATP. Assignments of all the histidinyl carbonyl carbon resonances have been completed by using Δ-annexin I along with its specific 1,2-subdomain. The carbonyl carbon resonances originating from His52 and His246 of Δ-annexin I were significantly affected by Ca$\^$2+/ binding, and some Tyr and Phe resonances were also affected. The carbonyl carbon resonances originating from His52 is significantly affected by ATP binding, therefore His52 seems to be involved in the ATP binding site of Δ-annexin I.

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$\beta$-Glucan enhanced apoptosis in human colon cancer cells SNU-C4

  • Kim, Mi-Ja;Hong, Se-Young;Kim, Sun-Kyu;Cheong, Chul;Park, Hong-Ju;Chun, Hye-Kyung;Jang, Ki-Hyo;Yoon, Byung-Dae;Kim, Chul-Ho;Kang, Soon-Ah
    • Nutrition Research and Practice
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    • v.3 no.3
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    • pp.180-184
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    • 2009
  • The apoptotic effect of bacteria-derived $\beta$-glucan was investigated in human colon cancer cells SNU-C4 using terminal deoxynucleotidyl transferase (TdT)-mediated dUTP nick end labeling (TUNEL) assay, reverse transcription-polymerase chain reaction (RT-PCR) expressions of Bcl-2, Bax, and Caspase-3 genes, and assay of caspase-3 enzyme activity. $\beta$-Glucan of 10, 50, and $100{\mu}g$/mL decreased cell viability in a dose-dependent manner with typical apoptotic characteristics, such as morphological changes of chromatin condensation and apoptotic body formation from TUNEL assay. In addition, $\beta$-glucan ($100{\mu}g$/mL) decreased the expression of Bc1-2 by 0.6 times, whereas the expression of Bax and Caspase-3 were increased by 3.1 and 2.3 times, respectively, compared to untreated control group. Furthermore, the caspase-3 activity in the $\beta$-glucan-treated group was significantly increased compared to those in control group (P < 0.05). Bacterial derived $\beta$-glucan could be used as an effective compound inducing apoptosis in human colon cancer.

Adhesion of Kimchi Lactobacillus Strains to Caco-2 Cell Membrane and Sequestration of Aflatoxin B1 (김치 유산균의 Caco-2 세포막 부착성 및 Aflatoxin B1 제거 효과)

  • Lee, Jeongmin
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.34 no.5
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    • pp.581-585
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    • 2005
  • Five lactic acid bacteria (LAB) including 2 Lactobacillus strains isolated from Kimchi were evaluated to determine the binding ability to Caco-2 cells and $AFB_1$. LAB were divided into three different groups ; viable, heat-treated, and acid-treated cells. In the radioactive-labeling assay for bound cell counting, viable Lactobacillus Plantarum KCTC 3099 showed the higher adhesion to Caco-2 cells with the binding capacity of $39.2\%$, which was $149\%$ higher than Lactobacillus rhamnosus GG as a positive control. Leuconostoc mesenteroids KCTC 3100 showed the similar binding ability to L. rhamnosus GG. After 1 hour incubation at $37^{\circ}C$ with $AFB_1$, viable L. Planterum KTCC 3099 removed the toxin by $49.8\%$, which was similar level to L. rhamnosus GG. Both heat- and acid-treated groups showed high binding effect but acid-treated group was more effective for both Caco-2 cell binding and $AFB_1$ removal than the other. These results indicate that components of bacterial cell wall might be involved in tile binding to intestinal cells and toxins.

The Analysis for Calcium and Fructooligosaccharides Contents in Nutrients Fortified Dairy Products (유가공품 중 칼슘 및 프락토올리고당 영양강화 함량 분석)

  • Park, Ji-Sung;Park, Jae-Woo;Cho, Byung-Hoon;Song, Sung-Ok;Wee, Sung-Hwan;Oh, Soon-Min;Kim, Jin-Man
    • Food Science of Animal Resources
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    • v.33 no.6
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    • pp.781-786
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    • 2013
  • Nutrients fortified dairy products declare their contents on the label for nutrition claim and marketing. However, there are few monitoring studies about relations between actual quantities of fortified nutrients and the described ones on the label. This study was carried out for comparing actual fortified nutrient contents with labeled ones. Forty calcium fortified dairy products and twenty four fructooligosaccharides (FOS) fortified dairy products were sampled at supermarkets located in Anyang, Korea from March to November in 2010. Calcium contents were analyzed by using inductively coupled plasma optical emission spectrometry followed by microwave sample digestion, and FOS contents were analyzed by HPLC-ELSD followed by solvent extraction. In fresh milk, calcium contents ranged from 1.0 to 2.4 mg/mL, and those values were 87~127% of their labeled contents. In fermented milk products and cheeses, calcium contents ranged from 0.3 to 1.6 mg/g (89~131% of their labeled contents), 4.2 to 23.0 mg/g (83~127% of their labeled contents), respectively. FOS contents ranged from 9.09 to 18.89 mg/g in FOS contents labeled products and showed 83~154% compared to their labeled quantity, and ranged from 1.3~30.8 mg/g in products without quantity labeling. In conclusion, the amounts of calcium and FOS in dairy products were above 80% compared to their labeled ones and conformed to the Korean official livestock products labeling standard.

An implementation of 2D/3D Complex Optical System and its Algorithm for High Speed, Precision Solder Paste Vision Inspection (솔더 페이스트의 고속, 고정밀 검사를 위한 이차원/삼차원 복합 광학계 및 알고리즘 구현)

  • 조상현;최흥문
    • Journal of the Institute of Electronics Engineers of Korea SP
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    • v.41 no.3
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    • pp.139-146
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    • 2004
  • A 2D/3D complex optical system and its vision inspection algerian is proposed and implemented as a single probe system for high speed, precise vision inspection of the solder pastes. One pass un length labeling algorithm is proposed instead of the conventional two pass labeling algorithm for fast extraction of the 2D shape of the solder paste image from the recent line-scan camera as well as the conventional area-scan camera, and the optical probe path generation is also proposed for the efficient 2D/3D inspection. The Moire interferometry-based phase shift algerian and its optical system implementation is introduced, instead of the conventional laser slit-beam method, for the high precision 3D vision inspection. All of the time-critical algorithms are MMX SIMD parallel-coded for further speedup. The proposed system is implemented for simultaneous 2D/3D inspection of 10mm${\times}$10mm FOV with resolutions of 10 ${\mu}{\textrm}{m}$ for both x, y axis and 1 ${\mu}{\textrm}{m}$ for z axis. Experiments conducted on several nBs show that the 2D/3D inspection of an FOV, excluding an image capturing, results in high speed of about 0.011sec/0.01sec, respectively, after image capturing, with $\pm$1${\mu}{\textrm}{m}$ height accuracy.