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  • [J Control Release.] High-performance dendritic contrast agents for X-ray computed tomography imaging using potent tetraiodobenzene derivatives.

    2016년 04월호
    [J Control Release.] High-performance dendritic contrast agents for X-ray computed tomography imaging using potent tetraiodobenzene derivatives.

    한국생명공학연구원/유수연, 김윤경*

  • 출처
    J Control Release.
  • 등재일
    2016 Mar 28
  • 저널이슈번호
    226:258-67. d
  • 내용

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    Abstract

    The use of computed tomography (CT) for vascular imaging is critical in medical emergencies requiring urgent diagnostic decisions, such as cerebral ischemia and many cardiovascular diseases. Small-molecule iodinated contrast media are often injected intravenously as radiopaque agents during CT imaging to achieve high contrast enhancement of vascular systems. The rapid excretion rate of these agents is overcome by injecting a significantly high dose of iodine, which can have serious side effects. Here we report a simple method to prepare blood-pool contrast agents for CT based on dendrimers for the first time using tetraiodobenzene derivatives as potent radiopaque moieties. Excellent in vivo safety has been demonstrated for these small (13-22nm) unimolecular water-soluble dendritic contrast agents, which exhibit high contrast enhancement in the blood-pool and effectively extend their blood half-lives. Our method is applicable to virtually any scaffold with suitable surface groups and may fulfill the current need for safer, next-generation iodinated CT contrast agents.

     

     

    Author information

    You S1, Jung HY1, Lee C1, Choe YH1, Heo JY2, Gang GT3, Byun SK4, Kim WK4, Lee CH5, Kim DE6, Kim YI7, Kim Y8.

    1Biomedical Translational Research Center, Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-806, Republic of Korea.

    2Biomedical Translational Research Center, Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-806, Republic of Korea; Department of Chemistry, Korea Advanced Institute of Science and Technology, Daejeon 305-701, Republic of Korea.

    3Laboratory Animal Resource Center, Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-806, Republic of Korea.

    4Functional Genomics Research Center, Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-806, Republic of Korea; Korea University of Science and Technology (UST), Daejeon 305-350, Republic of Korea.

    5Laboratory Animal Resource Center, Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-806, Republic of Korea; Korea University of Science and Technology (UST), Daejeon 305-350, Republic of Korea.

    6Department of Neurology, Dongguk University Ilsan Hospital, Goyang 410-773, Republic of Korea.

    7Department of Radiology, Seoul National University Hospital, Seoul 110-744, Republic of Korea.

    8Biomedical Translational Research Center, Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-806, Republic of Korea; Korea University of Science and Technology (UST), Daejeon 305-350, Republic of Korea. Electronic address: ykim@kribb.re.kr 

     

  • 연구소개
    현재 병원에서 사용 중인 혈관내 주입용 저분자 요오드계 CT 조영제의 과량투여로 인한 일부 부작용의 문제를 해결하고자, 혈관내 지속시간을 늘리고, 체내 안전성이 매우 우수하며, 원활한 배출이 이루어지는, 나노크기 수준의 새로운 수용성 요오드계 조영제 4가지(직경 13, 16, 19, 22 nm)를 매우 간단한 방법에 의해 만들었음. 특히 본 논문의 CT 조영제는 덴드리머라는 유기합성에 의해 만들어지는 분자량이 일정하고 작은 구형의 고분자 화합물을 중심 골격으로 사용했으며, 기존 저분자 조영제의 요오드 원자 3개가 치환된 벤젠고리 화합물이 아닌, 요오드 원자 4개가 치환된 벤젠고리 다수를 덴드리머 골격에 붙여 요오드 함량의 효율적 증대를 도모하였음. 연계 연구의 분자설계 최적화를 통해 장차 주입용량을 보다 낮추고, 대부분의 나노화합물 조영제와 달리 저분자 의약품 수준으로 재현성이 완벽하고 안전한 조영제를 만들고자 함
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