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First preclinical evaluation of mono-[123I]iodohypericin as a necrosis-avid tracer agent

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European Journal of Nuclear Medicine and Molecular Imaging Aims and scope Submit manuscript

Abstract

Purpose

We have labelled hypericin, a polyphenolic polycyclic quinone found in St. John’s wort (Hypericum perforatum), with 123I and evaluated mono-[123I]iodohypericin (MIH) as a potential necrosis-avid diagnostic tracer agent.

Methods

MIH was prepared by an electrophilic radioiodination method. The new tracer agent was evaluated in animal models of liver infarction in the rat and heart infarction in the rabbit using single-photon emission computed tomography (SPECT), triphenyltetrazolium chloride (TTC) histochemical staining, serial sectional autoradiography and microscopy, and radioactivity counting techniques.

Results

Using in vivo SPECT imaging, hepatic and cardiac infarctions were persistently visualised as well-defined hot spots over 48 h. Preferential uptake of the tracer agent in necrotic tissue was confirmed by perfect match of images from post-mortem TTC staining, autoradiography (ARX) and histology. Radioactivity concentration in infarcted tissues was over 10 times (liver; 3.51% ID/g in necrotic tissue vs 0.38% ID/g in normal tissue at 60 h p.i.) and over 6 times (myocardium; 0.36% ID/g in necrotic tissue vs 0.054% ID/g in normal tissue; ratios up to 18 for selected parts on ARX images) higher than in normal tissues.

Conclusion

The results suggest that hypericin derivatives may serve as powerful necrosis-avid diagnostic agents for assessment of tissue viability.

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Acknowledgements

The authors wish to thank Peter Vermaelen for his much-appreciated help with the animal imaging studies. The Fund for Scientific Research – Flanders is acknowledged for financial support (research grant G.0257.05).

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Authors and Affiliations

  1. Department of Radiology, University Hospital Gasthuisberg, Leuven, Belgium

    Yicheng Ni, Feng Chen & Guy Marchal

  2. Laboratory of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, University of Leuven, Herestraat 49, 3000, Leuven, Belgium

    Dieter Huyghe, Kristin Verbeke, Alfons M. Verbruggen & Guy M. Bormans

  3. Laboratory of Pharmaceutical Biology and Phytopharmacology, Faculty of Pharmaceutical Sciences, University of Leuven, Leuven, Belgium

    Peter A. de Witte

  4. Department of Nuclear Medicine, University Hospital Gasthuisberg, Leuven, Belgium

    Johan Nuyts & Luc Mortelmans

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  1. Yicheng Ni
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Correspondence to Alfons M. Verbruggen.

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Ni, Y., Huyghe, D., Verbeke, K. et al. First preclinical evaluation of mono-[123I]iodohypericin as a necrosis-avid tracer agent. Eur J Nucl Med Mol Imaging 33, 595–601 (2006). https://doi.org/10.1007/s00259-005-0013-2

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  • DOI: https://doi.org/10.1007/s00259-005-0013-2

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