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제106회 대한화학회 학술발표회, 총회 및 기기전시회 안내 In vivo Molecular Imaging of Cancer using Gold Nanoparticle Probes functionalized with 125I and cyclic RGD-PEG

2010년 8월 31일 11시 06분 03초
Ⅳ-MAT.P-149 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
금 <발표Ⅳ>
저자 및
홍수현, 남좌민
서울대학교 화학부, Korea
We designed and synthesized 13 nm gold nanoparticles which are PEGlyated and functionalized with cyclic RGD for targeting cancer cells. These probes were labeled with 125I by electrostatic interaction. 125I-labeled cyclic RGD-gold nanoparticle-probes show high stability in high salt and temperature conditions and high specificity for integrin αvβ3 expressing cells (U87MG). αvβ3 expressing human glioblastoma cancer cell (U87MG) and non-expressing breast cancer cell (MCF7) were treated with 125I-echistatin as the integrin αvβ3-specific radioligand in competitive binding assay with cyclic RGD-gold nanoparticles and cyclic RGD peptides. The IC50 values obtained from this competitive binding assays were 2.17 nM for cyclic RGD-gold nanoparticles and 154 nM for cyclic RGD peptides. MCF7 cells showed the same uptake efficiency for both cases. To determine internalization of cyclic RGD conjugated gold nanoparticles, TEM images of U87MG and MCF7 were acquired and they showed intracellular localization of the probes only in U87MG cells but not in MCF7 cells. Cell viability assay results showed that these probes have no cytotoxic effects upto 500 μg/ml probe concentration and 72 h incubation for both U87MG and MCF7 cell lines. The uptake and clearance of 125I-labeled cyclic RGD-gold nanoparticles in vivo was evaluated by serial SPECT/CT studies in a U87MG tumor bearing mouse using a dedicated small animal SPECT/CT system. These in vivo imaging results (Figure 1) showed high uptake of the probes in the U87MG xenografted tumor and blood pool up to 1 h post-injection and also showed clearance of these probes from the body by renal and urinary excretion > 1 h after injection. In this study, we demonstrated that 125I-labeled cyclic RGD-gold nanoparticles can define αvβ3 expressing cancer cells both in vitro and in vivo. These probes may have a potential in tumor and angiogenesis targeted imaging technique which will be useful for various diagnostic and therapeutic applications.