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Int. J. Mol. Sci. 2017, 18(7), 1388; doi:10.3390/ijms18071388

Analysis of Hypericin-Mediated Effects and Implications for Targeted Photodynamic Therapy

Department of Otorhinolaryngology, Head and Neck Surgery, Section of Experimental Oncology and Nanomedicine (SEON), Else Kröner-Fresenius-Stiftung-Professorship, Universitätsklinikum Erlangen, 91054 Erlangen, Germany
Friedrich-Alexander-Universität Erlangen-Nürnberg (FAU), 91054 Erlangen, Germany
Author to whom correspondence should be addressed.
Received: 24 May 2017 / Revised: 19 June 2017 / Accepted: 23 June 2017 / Published: 29 June 2017
(This article belongs to the Special Issue Tumor Targeting Therapy and Selective Killing)
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The phototoxic effect of hypericin can be utilized for Photodynamic Therapy (PDT) of cancer. After intravenous application and systemic distribution of the drug in the patient’s body, the tumor site is exposed to light. Subsequently, toxic reactive oxygen species (ROS) are generated, inducing tumor cell death. To prevent unwanted activation of the drug in other regions of the body, patients have to avoid light during and after the treatment cycles, consequently impairing quality of life. Here, we characterize toxicity and hypericin-mediated effects on cancer cells in vitro and confirm that its effect clearly depends on concentration and illumination time. To reduce side effects and to increase therapy success, selective accumulation of hypericin in the tumor region is a promising solution. Loading hypericin on superparamagnetic iron oxide nanoparticles (SPIONs) and guiding them to the desired place using an external magnetic field might accomplish this task (referred to as Magnetic Drug Targeting (MDT)). Thus, using a double targeting strategy, namely magnetic accumulation and laser induced photoactivation, might improve treatment effectivity as well as specificity and reduce toxic side effects in future clinical applications. View Full-Text
Keywords: nanomedicine; hypericin; magnetic drug targeting (MDT); photodynamic therapy (PDT); superparamagnetic iron oxide nanoparticles (SPION) nanomedicine; hypericin; magnetic drug targeting (MDT); photodynamic therapy (PDT); superparamagnetic iron oxide nanoparticles (SPION)

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Mühleisen, L.; Alev, M.; Unterweger, H.; Subatzus, D.; Pöttler, M.; Friedrich, R.P.; Alexiou, C.; Janko, C. Analysis of Hypericin-Mediated Effects and Implications for Targeted Photodynamic Therapy. Int. J. Mol. Sci. 2017, 18, 1388.

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