摘要
趋化因子受体CXCR4在多数恶性肿瘤中高表达,其小分子拮抗剂AMD3100可用于肿瘤治疗。以N,N-二(3-氨丙基)乙基乙胺为原料合成了AMD3100,并用放射性金属核素99 Tcm标记制备99 Tcm-AMD3100,研究其在正常NH小鼠体内生物分布及荷Hep-G2肝癌鼠SPECT显像。结果显示,以N,N-二(3-氨丙基)乙基乙胺为原料,合成AMD3100总的合成效率为5.8%。99 Tcm-AMD3100的标记率大于98%。生物分布结果表明,CXCR4高表达的肝组织放射性摄取较高。显像结果表明,荷Hep-G2肝癌组织可浓集放射性。以上结果表明,99 Tcm-AMD3100是一种潜在的肿瘤CXCR4表达显像剂。
Most of human tumors over-express CXCR4. AMD3100, a nonpeptide antagonist for CXCR4 receptor, can be used for therapy of those tumors. It was found that metal ion complex, such as Cuz＋ , with AMD3100 enhanced its binding affinity to the receptor 10-fold higher as compared to AMD3100 alone. AMD3100 was synthesis from 3-aminopropyl ethyl- ene diamine. 99Tcm-AMD3100 was labeled directly. Biodistribution studies were carried out in NH mice. SPECT imaging was performed in Hep-G2 tumor bearing mouse. The synthet- ic yield was 5.8% from 3-aminopropyl ethylene diamine to AMD3100. The labeling yield of 99Tcm-AMD3100 was over 98%. Biodistribution studies showed high accumulation of radio- tracer in liver which had high-expression of CXCR4. SPECT imaging results showed that uptake in Hep-G2 tive candidate for CR4. tumor was high. The further development results showed that 99Tcm-AMD3100 was an attrac- of SPECT radiotracer potentially suitable for CX
出处
《同位素》
CAS
2013年第3期158-162,共5页
Journal of Isotopes
基金
国家自然科学基金资助(81071170)
