Radiolabeling, autoradiogram and in vivo imaging of atherosclerosis- specific peptide

Hwa Young Lee, Wonjung Kwak, Hai Yan Hong, Byung Heon Lee, In San Kim, Byeong Cheol Ahn, Jaetae Lee, Jeongsoo Yoo, Kyehan Rhee

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Abstract

The aim of this study is the detection of atherosclerosis by using radiolabeled small peptides via non-invasive nuclear imaging. A small peptide, which shows high binding affinity for atherosclerotic lesions in vessels (AP), was synthesized by using a standard Fmoc method and diethylenetriaminepentaacetic acid (DTPA) or tyrosine was conjugated at the N-terminal of the AP to provide DTPA-AP-CC or Y-AP, respectively. The prepared peptide was labeled by " 99mTc, 111In or 123I. The labeled peptides were injected into atherosclerosis-induced mice (LDLr(-/-) knockout mice) and control mice via the tail vein. At 15 min post injection, the aortas of the LDLr(-/-) knockout and control mice were excised for an autoradiogram study. Gamma scintigraphic images were obtained at 30 min and 1 h. The optimized labeling yield of [ 99mTc]DTPA-AP-CC, [111In]DTPA-AP-CC and [ 123I]Y-AP was over 35%, 100% and over 20%, respectively. Autoradiographic studies showed that the aorta uptakes of [99mTc] DTPA-AP-CC and [111In]DTPA-AP-CC in the LDLr(-/-) knockout mice were much higher than the corresponding uptakes in the control mice. In contrast, the aorta uptake of [123I]Y-AP in LDLr(-/-) and normal mice were comparable. Scintigraphic images, however, did not show any noticeable uptake differences between the LDLr(-/-) knockout and the control mice, which is mostly due to the high background in the abdominal region and to the non-sufficient resolution of gamma camera imaging for the aorta of the mice.

Original languageEnglish
Pages (from-to)858-864
Number of pages7
JournalJournal of the Korean Physical Society
Volume52
Issue number3 PART 1
DOIs
Publication statusPublished - 2008 Mar

Keywords

  • Atherosclerosis
  • Autoradiogram
  • I
  • In
  • Peptide
  • Radiolabeling
  • Tc

ASJC Scopus subject areas

  • Physics and Astronomy(all)

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  • Cite this

    Lee, H. Y., Kwak, W., Hong, H. Y., Lee, B. H., Kim, I. S., Ahn, B. C., Lee, J., Yoo, J., & Rhee, K. (2008). Radiolabeling, autoradiogram and in vivo imaging of atherosclerosis- specific peptide. Journal of the Korean Physical Society, 52(3 PART 1), 858-864. https://doi.org/10.3938/jkps.52.858