Imaging paclitaxel (chemotherapy)-induced tumor apoptosis with 99mTc C2A, a domain of synaptotagmin I: a preliminary study

Nucl Med Biol. 2008 Apr;35(3):359-64. doi: 10.1016/j.nucmedbio.2007.12.007.

Abstract

Purpose: To evaluate the dynamics and feasibility of imaging non-small cell lung cancer (NSCLC) apoptosis induced by paclitaxel treatment using 99mTc-labeled C2A domain of synaptotagmin I in a mouse model.

Materials and methods: H460 tumor-bearing mice were treated with intravenous paclitaxel, and 12, 24, 48 and 72 h later, 99mTc-C2A-GST was injected intravenously, and planar images were acquired at 2, 4 and 6 h postinjection on a dual-head gamma camera fitted with a pinhole collimator. Tumor-to-normal tissue ratios (T/NT) were calculated by ROI analysis and reflected specific binding of 99mTc-C2A-GST. Mice were sacrificed after 6-h imaging; caspase-3 as apoptosis executer was determined by flow cytometry; DNA fragmentation was analyzed by terminal deoxynucleotidytransferase mediated dUTP nick-end labeling (TUNEL) assay. Whereas nonspecific accumulation was estimated using inactivated C2A-GST. The imaging data were correlated with TUNEL-positive nuclei and caspase-3 activity.

Results: T/NT significantly increased after paclitaxel inducement, whereas it was low in untreated tumors (T/NT=1.24+/-0.23). In terms of % ID/g, activity in Group 2 (12 h), Group 3 (24 h), Group 4 (48 h) and Group 5 (72 h) after the treatment was 2.05+/-0.20, 3.02+/-1.01, 3.17+/-1.16 and 3.96+/-1.72, respectively. Whereas in the nontreated group, Group 1 % ID/g was 1.21+/-0.51. The radiotracer uptake was positively correlated to the apoptotic index (r=0.70, P<.01), as well as caspase-3 activity (r=0.75, P<.01).

Conclusion: This study addresses the dynamics and feasibility of imaging non-small cell lung tumor apoptosis using 99mTc-labeled C2A.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / therapeutic use
  • Apoptosis / drug effects*
  • Carcinoma, Non-Small-Cell Lung / diagnostic imaging*
  • Carcinoma, Non-Small-Cell Lung / drug therapy
  • Caspase 3 / drug effects
  • Caspase 3 / metabolism
  • Cell Line, Tumor
  • DNA Fragmentation / drug effects
  • Disease Models, Animal
  • Female
  • Humans
  • Injections, Intravenous
  • Lung Neoplasms / diagnostic imaging*
  • Lung Neoplasms / drug therapy
  • Male
  • Mice
  • Paclitaxel / therapeutic use*
  • Protein Structure, Tertiary
  • Radioligand Assay / methods
  • Radionuclide Imaging
  • Radiopharmaceuticals / pharmacokinetics
  • Synaptotagmin I / chemistry*
  • Synaptotagmin I / drug effects
  • Technetium / pharmacokinetics*
  • Tissue Distribution

Substances

  • Antineoplastic Agents, Phytogenic
  • Radiopharmaceuticals
  • Synaptotagmin I
  • Technetium
  • Casp3 protein, mouse
  • Caspase 3
  • Paclitaxel