Theranostics 2013; 3(9):667-676. doi:10.7150/thno.6650

Review

Necrosis Avidity: A Newly Discovered Feature of Hypericin and its Preclinical Applications in Necrosis Imaging

Binghu Jiang1, Jichen Wang1, Yicheng Ni2, Feng Chen1, 2✉

1. Department of Radiology, BenQ Medical Center, Nanjing Medical University, Nanjing 210019, China.
2. Theragnostic laboratory, Department of Imaging and Pathology, University Hospital, University of Leuven, 3000 Leuven, Belgium.

Abstract

Hypericin has been widely studied as a potent photosensitizer for photodynamic therapy in both preclinical and clinical settings. Recently, hypericin has also been discovered to have a specific avidity for necrotic tissue. This affinity is also observed in a series of radiolabeled derivatives of hypericin, including [123I]iodohypericin, [124I]iodohypericin, and [131I]iodohypericin. Hypericin, along with other necrosis-avid contrast agents, has been investigated for use in noninvasively targeting necrotic tissues in numerous disorders. Potential clinical applications of hypericin include the identification of acute myocardial infarction, evaluation of tissue viability, assessment of therapeutic responses to treatments, and interventional procedures for solid tumors. The mechanisms of necrosis avidity in hypericin remain to be fully elucidated, although several hypotheses have been suggested. In particular, it has been proposed that the necrosis avidity of hypericin is compound specific; for instance, cholesterol, phosphatidylserine, or phosphatidylethanolamine components in the phospholipid bilayer of cellular membranes may be the major targets for its observed selectivity. Further investigations are needed to identify the specific binding moiety that is responsible for the necrosis avidity of hypericin.

Keywords: hypericin, necrosis, avidity

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How to cite this article:
Jiang B, Wang J, Ni Y, Chen F. Necrosis Avidity: A Newly Discovered Feature of Hypericin and its Preclinical Applications in Necrosis Imaging. Theranostics 2013; 3(9):667-676. doi:10.7150/thno.6650. Available from http://www.thno.org/v03p0667.htm