• 대한화학회지
• /
• 제12권1호
• /
• pp.35-38
• /
• 1968

Radio iodination of various aromatic derivatives (aniline, toluene, iodobenzene, acetanilide, benzene, benzoic acid) were achieved at low temperature by a chloroamine-T procedures in presence of polar solvent(dioxane). Organic base (piperidine) was used as the catalyst. Iodine replacement reaction had occured on the aromatic or alicyclic ring by this reaction, and the kind and ratio of iodinated products were proved to be different from those of usual iodide reaction in organic solvent at low temperature. The reactivity of various aromatic or alicyclic compounds towards the present iodination system was evaluated and the scope and limitation of the present procedures in the preparation of radio pharmaceuticals were discussed.

• 생약학회지
• /
• 제11권3_4호통권43호
• /
• pp.133-140
• /
• 1980

In order to develop the radio-immunoassay procedure for the ginsenoside $Rg_1$ we prepared the $Rg_1-BSA$ conjugate and $Rg_1-tyramine$ conjugate by condensing the $Rg_1-azide$, which was prepared by a series of six step chemical modification of the $Rg_1-side$ chain, with bovine serum albumin(BSA) or with tyramine. Rabbits were immunized by repeated injection of $Rg_1-BSA$ conjugate with Freund's Complete Adjuvant for 5 month long to obtain very potent $anti-Rg_1$ serum. The radio-labelled haptene was prepared by direct radio-iodination $(125_J)$ of $Rg_1-tyramine$ according to the chloramine-T method. The radio-immunoassay procedure was successfully furnished by using DCC method (dextran coated charcoal) and the anti-body titer of the anti-serum was found as being $1600{\sim}3200$ by using 15000cpm tracer per test. Calibration test using non-labelled $Rg_1$ showed linear competetive binding response in the $(8-300){\times}34pg$. range of non-labelled $Rg_1$. The cross reaction test using 19 ginsenoside analogues enabled us a full structure-activity analysis on the antigen-antibody reaction that the anti-body in the serum would recognize the full structure of ginsenoside $Rg_1$ except the side chain moiety.

• Bulletin of the Korean Chemical Society
• /
• 제31권9호
• /
• pp.2649-2655
• /
• 2010

$PKC{\delta}$-catalytic V5 Heptapeptide (FEQFLDI, FP7) interacts with heat shock protein 27 (HSP27) and inhibits HSP27-mediated resistance to cell death against various stimuli including radiation therapy. Here, we prepared radio-iodinated heptapeptide and further investigated its uptake properties in HSP27 expression cells. Peptide sequence of FP7 and a negative control peptide (WSLLEKR, QP7) was modified by substituting their C-terminus residue to tyrosine (FP6Y and QP6Y) to label radio-iodine. Iodinated peptides were confirmed by LC mass analysis with cold iodine reaction mixture. Accumulation of [$^{125}I$]iodo-FP6Y and [$^{125}I$]iodo-QP6Y in NCI-H1299 cell line, with higher level of HSP27, and NCI-H460 cell line, with lower level of HSP27, was measured by NaI(Tl) scintillation counter. The modification of substituting C-terminus residue of FP7 to tyrosine (FP6Y) did not affect its interaction with HSP27. Accumulation of [$^{125}I$]iodo-FP6Y in NCI-H1299 cells was 3 fold higher than in NCI-H460 cells. The novel radio-iodinated FP6Y would be used as a tracer for targeting HSP27 protein.

• 대한화학회지
• /
• 제11권2호
• /
• pp.51-55
• /
• 1967

放射性 沃化反應 中 分解하기 쉬운 化合物의 沃化反應으로 有用한 低溫沃化反應에 關하여 硏究하였다. Chloroamine-T를 利用한 沃化反應은 低溫에서 높은 收率로 放射性 沃化反應을 進行시킬 수 있었으며, 活性化된 芳香核이 있는 또는 이에 類似한 아미노酸, 蛋白質化合物, 各 種 Phenol類의 沃化가 不可能하였으나 二重結合化合物 및 一般化合物엔 큰 效果가 없었다. 反應收率은 $100{\sim}60%$이었으며, 各 化合物의 試藥에 對한 反應度는 親電子反應에 對한 芳香核의 反應度와 比例하는 것이었다. 反應操作을 記述하였으며 反應過程을 考察하였다.

• 대한방사성의약품학회지
• /
• 제4권1호
• /
• pp.3-10
• /
• 2018

The folate receptor (FR) is a promising cell membrane-associated target for nuclear imaging of various cancers (via imaging $FR-{\alpha}$) and potentially also inflammatory diseases (via imaging $FR-{\beta}$), through the use of folic acid-based radioconjugates. However, there have been several drawbacks of previously reported radioconjugates, such as a short half-life of the radiolabel ($^{68}Ga\;t_{1/2}$ 68 min), a complex and time-consuming multistep radiosynthesis, and a high renal uptake of radiolabeled folate derivatives. The goal of this study was to develop an imaging probe by directly labeling folate with radioactive iodine without using an extra prosthetic group. The radiolabeling of folate was optimized using various labeling conditions and the labeled tracers were isolated by high-performance liquid chromatography. The in vitro stability of labeled folate was checked in phosphate-buffered saline and serum. The tumor-targeting efficacy of the probe was also evaluated by biodistribution studies using a murine 4T1 tumor model.

• 대한핵의학회지
• /
• 제29권1호
• /
• pp.105-109
• /
• 1995

Tyrosine의 유도체인 [$^{123}I$]IMT를 각종 악성종양의 SPECT에 이용하기 위하여 표지시 반응조건과 뇌종양이식 백서에서의 체내 동태를 연구하여 다음과 같은 결과를 얻었다. AMT의 [$^{123}I$] 표지에 chloramine-T 보다 Iodobead를 이용하는 것이 훨씬 간편하고 수율이 높았으며, Iodobead 1개, AMT $200{\mu}g/100{\mu}L$ phosphate buffer, PH 5.5, 상온에서 7분간 반응시키는 것이 최적 반응조건이었다. 9L glioma 이식 백서 체내동태는 [$^{123}I$]IMT가 신장으로 배설됨과 체내에서 탈요오드 반응이 일어남이 추측되었고, 정상조직의 3배 방사능 섭취가 관찰되어, 각종 뇌종양의 진단 및 치료 후 경과 관찰에 이용 가능성이 보여 임상연구의 진행이 기대된다.

• Journal of Yeungnam Medical Science
• /
• 제10권2호
• /
• pp.432-444
• /
• 1993

Adriamycin과 vincristine 각각에 내성인 생쥐의 림프아세포성 백혈병세포 L1210세포의 특성과 내성관계 단백질을 찾아내고 항암제의 세포내 분포를 관찰하였다. 항암제의 내성생성은 adriamycin이 $10^{-5}M$과 $10^{-6}M$에서 자란 세포를 L1210-$AdR_5$와 $-AdR_6$로 하고 vincristine은 $10^{-6}M$과 $10^{-7}M$에서 자란 세포를 L1210-$VcR_6$와 $-VcR_7$로 하였다. 감수성세포는 L1210으로 하였다. 내성세포의 성장속도는 감수성세포에 비해 느렸으며 doubling time은 L1210가 29.7시간, L1210-$AdR_5$가 68.7시간 $-VdR_6$가 58.2시간이었다. 복합내성은 내성인자로 표기되었고 L1210-$AdR_5$는 vincristine에 대해 76.4배, $-VcR_6$는 adriamycin에 대해 98.6배로 나타냈다. 감수성세포와 내성세포의 세포막 단백질을 비교한 결과 L1210-$AdR_5$에서는 220, 158, 88 Kd의 내성관계단백질이 나타났고 $-VcR_6$에서는 158, 140 및 88Kd의 내성관계단백질이 관찰되었다. 세포막 표면단백질을 $^{125}I$로 결합시켜 자가방사선상으로 분석하였다. 세포막 표면단백질에 결합되는 $^{125}I$의 정도는 L1210에 0.95% L1210-$AdR_5$에 5.4%, $-VcR_6$에 1.7%였다. 세포막표면단백질은 L1210-$AdR_5$에서는 158, 72.8 및 42.4 Kd의 단백질, $-VcR_6$에서는 300, 158, 72.8 및 42.4 Kd의 단백질이 관찰되었다.