• Title/Summary/Keyword: radio labeling

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Synthesis and Evaluation of a Ligand Targeting the Somatostatin Receptor for Drug Delivery to Tumor Cell (암세포 내로의 약물 전달 증진 목적의 신규 소마토스타틴 수용체 타겟리간드 합성 및 평가)

  • Choi, SunJu;Hong, YoungDon;Lee, SoYoung;Jung, SungHee
    • Journal of Radiation Industry
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    • v.9 no.4
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    • pp.193-198
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    • 2015
  • Most of targeted therapies block the action of certain enzymes, proteins, or other molecules involved in the growth and spread of cancer cells to produce its cytotoxic effect. Either small molecule drugs or monoclonal antibodies are mostly used in targeted therapies. Unfortunately, targeted therapy has a certain degree of unwanted side effect like other cytotoxicity inducing chemotherapies. To overcome and to reduce unwanted side effects during a cancer therapy, recently radiopeptide therapies has got the worlds' attraction for the tumor targeting modalities due to its beneficial effect on less side effect compared to cytotoxic chemotherapies. Among radiopeptide therapies, $^{177}Lu$-DOTATATE is a major modality as an effective one invented so far in treating neuroendocrine tumor (NET) and it has been in clinical trials at least one decade. Although it does have rather effective therapeutic effect on NET, it has less effective in rather large solid tumor. There are many ways to improve or increase therapeutic effect of radiopeptide are a finding the potent small molecules to target the tumor site selectively, or a labeling with radioisotope of emitting high energy, or an improving its biological half-life by introducing different moieties to increase lipophilicity. Present study was focus to increase a biological half-life of radio somatostatin which will target the somatostatin receptor by altering the bifunctional chelator (BFCA) by introducing lipophilic moiety to the somatostatin, which would make the labeled peptide stay longer in the tumor site and thus it can intensify the therapeutic effect on tumor cell itself and around tissues.

Radiolabeling of antibody-mimetic scaffold protein with 99mTc tricarbonyl precursor via hexahistidine (His6)-tag

  • Shim, Ha Eun;Kim, Do Hee;Lee, Chang Heon;Choi, Dae seong;Lee, Dong-Eun
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.5 no.1
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    • pp.11-17
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    • 2019
  • Recently, antibody-like scaffold proteins have received a great deal of interest in diagnosis and therapy applications because of their intrinsic features that are often required for tumor imaging and therapy. Intrinsic issues that are associated with therapeutic application of antibody-like scaffold proteins, particularly in cancer treatment, include an efficient and straightforward radiolabeling for understanding in vivo biodistribution and excretion route, and monitoring therapeutic responses. Herein, we report an efficient and straightforward method for radiolabeling of antibody-like scaffold proteins with the $[^{99m}Tc(OH_2)_3(CO)_3]^+$ ($^{99m}Tc$-tricarbonyl) by using a site-specific direct labeling method via hexahistidine-tag, which is a widely used for general purification of recombinant proteins with His-affinity chromatography. Repebody is a new class of antibody-like scaffold protein that consists of highly diverse leucine-rich repeat (LRR) modules. Although all possible biomedical applications with repebody are ongoing, it's in vivo biodistribution and excretion pathway has not yet been explored. In this study, hexahistidine ($His_6$)-tag bearing repebody (rEgH9) was labeled with [$^{99m}Tc$]-tricarbonyl. Repebody protein was radiolabeled with high radiolabeling efficiency (>90%) and radiolabeled compound was more than 99% pure after purification. These results clearly demonstrate that the present radiolabeling method will be useful molecular imaging study.

Evaluation of Biocompatibility of Extracorporeal Circuit - Development of a Quantification Technique using in-vivo Injection of Tc99m Radioactive Platelets - (체외순환도관의 혈액적합성 평가 - 방사선 동위원소(Tc99m) 활성화 혈소판의 생체 내 주입을 이용한 정량분석법의 개발 -)

  • Lee, Sung-Ho;Sun, Kyung;Choi, Jai-Geol;Son, Ho-Sung;Jung, Jae-Seung;Ahn, Sang-Soo;Oh, Hye-Jung;Lee, Whan-Sung;Lee, Hye-Won;Kim, Kwang-Taik;Jeong, Yoon-Seop;Kim, Young-Ha;Kim, Hyoung-Mook
    • Journal of Chest Surgery
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    • v.35 no.3
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    • pp.171-176
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    • 2002
  • Background: Blood-foreign interaction cause activation of coagulation and inflammatory process that may lead to multiorgan dysfunction and determine the surgical outcomes. Of the methods for assessing the biocompatibility, the platelet adhesion study is considered as the most valuable evaluation step in blood-foreign interaction. As the most studies have used in-vitro or ex-vivo conditions, we have developed a technique of quantification for platelet adhesion on the blood contact surface by using in-vivo injection of radioactive platelets. Material and Method: A coupled bypass circuit was designed to connect the proximal and descending thoracic aorta in 6 piglets(20∼25 Kg). One side of the circuit tube was consisted of a heparin coated PVC tube(10mm in ID, n=6, Experimental group), and the other, a non-heparin coated PVC tube(10mm in ID, n=6, Control group). After cannulation, the blood was circulated through the circuit for 2 hours. Platelet concentrate was prepared from homologous pig blood 24 hours before the experiment. The platelet concentrate was incubated with Tc-99m-HMPAO for 30 min and then centrifuged for 10 min. The supernatant was discarded and the radio-labeling efficacy was measured. The radio-labeled platelet concentrate was mixed with the autologous plasma to make the volume 5 ml, and the mixture was injected intravenously into the experimental animal. After 2 hour circulation, 5 pieces of the specimen(10mm in length each) were obtained from each PVC tube. The radioisotopes were counted with a gamma counter(Cobra ll, Packard, USA), and the ratio of radioisotope count was compared between the control and experimental group. Result: The radioisotope count number was 537.3221.1 Ci/min in the control group and 311.1 184.5 Ci/min in the experimental group(p=0.0104). The ratio between the groups was 1 to 0.58 (p=0.004). Conclusion: In vivo quantification using technetium-99m-HMPAO labeled platelets is simple and reproducible in evaluating platelet adhesion on a foreign surface. We suggest this technique to be a useful tool for blood compatibility test.

A Study on the Effective Educational and Promotional Strategies for the Special Act on the Safety Management of Children's Dietary Life (어린이 식생활 안전관리 특별법에 관한 효과적 교육 및 홍보 방안 연구)

  • Hong, Jin-Im;Jeong, Hee-Sun
    • Culinary science and hospitality research
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    • v.18 no.5
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    • pp.176-189
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    • 2012
  • This study was conducted to investigate the effective educational and promotional strategies for the Special Act on the Safety Management of Children's Dietary Life on the basis of the survey conducted on parents. First of all, its result showed that most parents are well aware of the main contents of the law. They answered that, when choosing safe favorite food for children, the most important part is the article "Regulations on the standards for children's favorite food should be reinforced." As for the index of safety management for children's dietary life, most respondents think safety the most important; housewives and nuclear family members choose safety (p<.01), while large family members do nutrition. For the question asking how they get the information on safety management for children's dietary life, most of them answered that they generally use mass media, family and friends as a reference. Those with high income usually get the information from special books, those between 30s and 50 from mass media, and those with college graduates from civil social groups (p<.05). In case of taking the safety education programs for children's dietary life, they told that the most necessary information is concerned with hygienic dietary life and nutrition labeling on processed food; housewives are interested in the latter, while working people in the former (p<.05). As a method of informing parents of the Special Act on the Safety Management of Children's Dietary Life, mass media such as TV and radio, and school education are suggested in this survey. Therefore, this study proposes that mass media be considered as the most effective way of promoting the Special Act on the Safety Management of Children's Dietary Life and getting information concerning the law.

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Synthesis of Cyclen-Based Copper Complexes as a Potential Estrogen Receptor Ligand (에스트로젠 수용체 리간드로서 사이클렌을 기본 구조로 한 구리 착물의 합성)

  • Park, Jeong-Chan;Pandya, Darpan N.;Jeon, Hak-Rim;Lee, Sang-Woo;Ahn, Byeong-Cheol;Lee, Jae-Tae;Yoo, Jeong-Soo
    • Nuclear Medicine and Molecular Imaging
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    • v.41 no.4
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    • pp.326-334
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    • 2007
  • Purpose: The estrogen receptor (ER), which is over-expressed in ER-positive breast tumors, has been imaged by positron emission tomography (PET) using $[^{18}F]$ labeled estrogen ligands, especially $[^{18}F]FES$. However, $[^{18}F]$ has relatively short-lived half-life ($t_{1/2}$ =1.8 h) and the labeling yield of radio-fluorination is usually low compared with $^{64}Cu\;(t_{1/2}=12.7\;h)$. 1,4,7,10-tetraazacyclododecane (cyclen) is used to form stable metal complexes with copper, indium, gallium, and gadolinium. With these in mind, we prepared cyclen-based Cu complexes which mimic estradiol in aspect of two hydroxyl groups. Materials and Methods: 1.7-Protected cyclen, 1.7-bis (benzyloxycarbonyl)-cyclen was synthesized according to the reported procedure. After introducing two 4-benzyloxybenzyl groups at 4,10-positions, the benzyloxycarbonyl and benzyl groups were removed at the same time by hydrogenation on Pd/C to give 1,7-bis(4-hydroxybenzyl)-1,4,7,10-tetraazacyclododecane (1). Results: The prepared ligand 1 was fully characterized by $^1H,\;^{13}C$ NMR, and mass spectrometer. The synthesized ligand was reacted with copper chloride and copper perchlorate to give copper complexes $[Cu(1)]^{2+}2(CIO_4^-)\;and\;[Cu(1)Cl]^+Cl^-$ which were confirmed by high-resolution mass (FAB). Conclusion: We successfully synthesized a cyclen derivative of which two phenol groups are located on trans position of N-atoms. And, two Cu(ll) complexes of +2 and +1 overall charge, were prepared as a potential PET tracers for ER imaging.

Recognition of Food Additives of High School Students in Gwangju (광주지역 고등학생의 식품첨가물에 대한 인식)

  • Jung, Hwa-Young;Jung, Lan-Hee
    • Journal of Korean Home Economics Education Association
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    • v.21 no.4
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    • pp.1-17
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    • 2009
  • The purpose of this study was to investigate recognition of food additives, to provide the basic data for food education of high school students. The survey was conducted from 560 students who are boys and girls of high schools in Gwangju. Data were analyzed by a SAS program. According to the survey, an usual recognition for additive food according to related variable showed that it was the highest ratio of 4.18 that policy on complete labeling of foods should be requested for additive food but it showed the lowest 2.17 that additive food is promoting quality of food. In a difference of a degree of a correct answer of knowledge for additive food and knowledge according to related variable, a degree of a correct answer of knowledge for additive food showed a lot of interest in safety in that knowledge for safety showed 79.45 but were showed much lower 7.5% for a degree of a correct answer of actual knowledge of additive food among food ingredients labels. A a degree of a demand of information, safety concerns and understanding a uses of additive food according to sex and a grade showed that in a degree of a demand of information, the students have ever heard information of additive food was the girls were more than the boys and also freshmen were the most answered and have ever heard term of additive food was the boys were more than the girls and the sophomore students were the most answered questionnaire for media of TV. Radio. Newspaper and so forth. A degree of necessity the students know additive food was the most answered of positive from the boys and freshmen. Where the students would like to learn additive food was answered of media from the boys school teacher from the girls school teacher from the freshmen, media from the sophomore and the junior.

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Nutrition knowledge, eating attitudes, nutrition behavior, self-efficacy of childcare center foodservice employees by stages of behavioral change in reducing sodium intake (어린이집 조리종사자 대상의 나트륨 저감화 행동변화단계에 따른 영양지식, 식태도, 식행동, 자아효능감 비교)

  • Ahn, Yun;Kim, Kyung Won;Kim, Kyungmin;Pyun, Jinwon;Yeo, Ikhyun;Nam, Kisun
    • Journal of Nutrition and Health
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    • v.48 no.5
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    • pp.429-440
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    • 2015
  • Purpose: The purpose of this study was to examine sodium-related nutrition knowledge, eating attitudes, eating behaviors, and self-efficacy by stages of behavioral change in reducing sodium intake among childcare center foodservice employees. Methods: Subjects (n = 333) were categorized according to two groups based on the stages of change; Pre-action stage (PA group: precontemplation/contemplation/preparation stage), Action stage (A group: action/maintenance stage). Results: A major source of sodium-related nutrition information was TV/radio (56.6%) and only 166 people (49.8%) have experienced nutrition education specific to sodium. Although the A group showed slightly higher scores for nutrition knowledge than the PA group, the difference was not significant. The percentages of correct answers for 'daily goal of sodium intake for adults (27.0%)', 'calculation of sodium content in nutrition labeling (30.3%)' were low for both groups. The A group (total score: 40.3) had more desirable eating attitudes regarding reducing sodium intake than the PA group (36.6, p < 0.001). The total score for eating behaviors was slightly higher in the A group (49.6) than in the PA group (48.5), but without statistical significance. The A group (total score: 58.2) also received higher scores for self-efficacy regarding reducing sodium intake than the PA group (52.5, p < 0.001). Conclusion: This study suggests that nutrition education for childcare center foodservice employees should be expanded and customized education should be implemented according to the stages in reducing sodium intake. It is also suggested that food companies make efforts to develop low-sodium products.