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Cancers 2016, 8(10), 93;

Hypericin in the Dark: Foe or Ally in Photodynamic Therapy?

Center for Interdisciplinary Biosciences, PJ Safarik University in Kosice, Kosice 040 01, Slovakia
Department of Biophysics, Faculty of Natural Sciences, PJ Safarik University in Kosice, Kosice 040 01, Slovakia
Author to whom correspondence should be addressed.
Academic Editor: Michael R. Hamblin
Received: 30 July 2016 / Revised: 29 September 2016 / Accepted: 4 October 2016 / Published: 14 October 2016
(This article belongs to the Special Issue Photodynamic Cancer Therapy)
Full-Text   |   PDF [950 KB, uploaded 14 October 2016]   |  


Photosensitizers (PSs) in photodynamic therapy (PDT) are, in most cases, administered systemically with preferential accumulation in malignant tissues; however, exposure of non-malignant tissues to PS may also be clinically relevant, when PS molecules affect the pro-apoptotic cascade without illumination. Hypericin (Hyp) as PS and its derivatives have long been studied, regarding their photodynamic and photocytotoxic characteristics. Hyp and its derivatives have displayed light-activated antiproliferative and cytotoxic effects in many tumor cell lines without cytotoxicity in the dark. However, light-independent effects of Hyp have emerged. Contrary to the acclaimed Hyp minimal dark cytotoxicity and preferential accumulation in tumor cells, it was recently been shown that non-malignant and malignant cells uptake Hyp at a similar level. In addition, Hyp has displayed light-independent toxicity and anti-proliferative effects in a wide range of concentrations. There are multiple mechanisms underlying Hyp light-independent effects, and we are still missing many details about them. In this paper, we focus on Hyp light-independent effects at several sub-cellular levels—protein distribution and synthesis, organelle ultrastructure and function, and Hyp light-independent effects regarding reactive oxygen species (ROS). We summarize work from our laboratories and that of others to reveal an intricate network of the Hyp light-independent effects. We propose a schematic model of pro- and anti-apoptotic protein dynamics between cell organelles due to Hyp presence without illumination. Based on our model, Hyp can be explored as an adjuvant therapeutic drug in combination with chemo- or radiation cancer therapy. View Full-Text
Keywords: hypericin; PKC; Bcl2; BAX; oxidative stress; glioma cells; endothelial cells; cancer hypericin; PKC; Bcl2; BAX; oxidative stress; glioma cells; endothelial cells; cancer

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Huntosova, V.; Stroffekova, K. Hypericin in the Dark: Foe or Ally in Photodynamic Therapy? Cancers 2016, 8, 93.

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