Acta Academiae Medicinae Sinica

Acta Academiae Medicinae Sinica

Acta Academiae Medicinae Sinica ›› 2006, Vol. 28 ›› Issue (6): 786-789.

• Original Articles • Previous Articles     Next Articles

Synthesis and Animal Imaging of 99mTc-Hydrazinonicotinamide-Folate as a New Folate Receptor-Targeted Tumor Imaging Agent

LIU Li-qin, WANG Shi-zhen, LI Fang, TENG Bao, WANG Ke-zhan, QIU Fei-chan   

  1. Department of Nuclear Medicine, PUMC Hospital, CAMS and PUMC, Beijing 100730, China
  • Received:2006-01-30 Revised:1900-01-01 Online:2006-12-30 Published:2006-12-30
  • Contact: LIU Li-qin

Abstract: ABSTRACT:Objective The synthesis, biodistribution, and animal imaging of 99mTc- hydrazinonicotinamide-folate (99mTc-HYNIC-Folate) were studied as a folate receptor-targeted tumor imaging agent. Methods HYNIC-Folate was synthesized by a muti-step reaction and radiolabeled with 99mTc using tricine and trisodium phenylphosphine-3, 3’, 3’’-trisulfonate (TPPTS) as coligands. The radiochemical purity and stability of 99mTc-HYNIC-Folate was measured. The biodistributions of 99mTc-HYNIC-Folate in normal mice and tumor-bearing mice were detected. Whole-body gamma imaging was performed using an athymic mouse tumor xenograft model. Results The ligand HYNIC-Folate was successfully synthesized and characterized by hydrogen nuclear magnetic resonance (1HNMR) and mass spectrometry (MS). The radiochemical purity of 99mTc-HYNIC-Folate was 96% under optimal conditions. Data from γ scintigraphy and the biodistribution in tumor-bearing mice showed that 99mTc-HYNIC-Folate predominantly accumulated in tumor,its uptake rate per gram tissue αm was 5.620±0.753. The uptakes of 99mTc-HYNIC-Folate in the other non-target tissues were very low,except it was high in the kidneys(αm was 41.959±6.759). Conclusion 99mTc-HYNIC-Folate has the potential to be used as a noninvasive radiodiagnostic imaging agent for the detection of folate receptor-positive human cancers.

Key words: folate receptor, folate derivatives, isotope labelinc, biodistribution, imacinc