Exploring diagnostic potentials of radioiodinated sennidin A in rat model of reperfused myocardial infarction

Int J Pharm. 2015 Nov 10;495(1):31-40. doi: 10.1016/j.ijpharm.2015.08.046. Epub 2015 Aug 21.

Abstract

Non-invasive "hot spot imaging" and localization of necrotic tissue may be helpful for definitive diagnosis of myocardial viability, which is essential for clinical management of ischemic heart disease. We labeled Sennidin A (SA), a naturally occurring median dianthrone compound, with (131)I and evaluated (131)I SA as a potential necrosis-avid diagnostic tracer agent in rat model of reperfused myocardial infarction. Magnetic resonance imaging (MRI) was performed to determine the location and dimension of infarction. (131)I-SA was evaluated in rat model of 24-hour old reperfused myocardial infarction using single-photon emission computed tomography/computed tomography (SPECT/CT), biodistribution, triphenyltetrazolium chloride (TTC) histochemical staining, serial sectional autoradiography and microscopy. Gamma counting revealed high uptake and prolonged retention of (131)I SA in necrotic myocardium and fast clearance from non-targeted tissues. On SPECT/CT images, myocardial infarction was persistently visualized as well-defined hotspots over 24h, which was confirmed by perfect matches of images from post-mortem TTC staining and autoradiography. Radioactivity concentration in infarcted myocardium was over 9 times higher than that of the normal myocardium at 24h. With favorable hydrophilicity and stability, radioiodinated SA may serve as a necrosis-avid diagnostic agent for assessment of myocardial viability.

Keywords: Biodistribution; Hypericin (PubChem CID: 5281051); Necrosis avidity; Radioiodinated Sennidin A; Reperfused myocardial infarction; SPECT; Sennidin A (PubChem CID: 122839).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anthracenes / metabolism*
  • Anthracenes / pharmacokinetics*
  • Autoradiography
  • Disease Models, Animal
  • Drug Stability
  • Hydrophobic and Hydrophilic Interactions
  • Iodine Radioisotopes / metabolism*
  • Magnetic Resonance Imaging
  • Male
  • Myocardial Reperfusion Injury / diagnostic imaging*
  • Myocardial Reperfusion Injury / pathology
  • Necrosis / diagnostic imaging
  • Radiography
  • Rats
  • Tissue Distribution
  • Tomography, Emission-Computed, Single-Photon

Substances

  • Anthracenes
  • Iodine Radioisotopes
  • dihydroxydianthrone