Title: Radiolabeled iodohypericin as tumor necrosis tracer: diagnostic and therapeutic potential
Authors: Van de Putte, Marie
Fonge, Humphrey
Marysael, Thierry
Roskams, Tania
Miranda Cona, Marlein
Li, Junjie
Bormans, Guy
Verbruggen, Alfons
Ni, Yicheng
de Witte, Peter # ×
Issue Date: Jul-2012
Publisher: Wiley-Liss
Series Title: International Journal of Cancer vol:131 issue:2 pages:E129-E137
Abstract: It is estimated that 30-80% of solid tumor mass represents necrotic tissue that consists out of a significant number of dead and dying cells. The fact that these necrotic zones are restricted to dysplastic and malignant tissue and are rarely present in normal tissue makes necrosis an interesting target both for cancer diagnosis and therapy. In this study, the avidity of hypericin, [(123) I]iodohypericin and [(131) I]iodohypericin to tumor necrosis was explored for both diagnosis and therapy of experimental malignancies. The intratumoral distribution in RIF-1 tumors was investigated by means of fluorescence microscopy (hypericin) and autoradiography ([(123) I]iodohypericin). Results show high uptake of the tracers in necrosis at 24 hr, lasting for up to 72 hr p.i. Ratios of activity of [(123) I]iodohypericin in necrotic tissue over viable tumor reached up to 19.63 ± 4.66, correlating with 9.20% ID/g in necrosis. Nude mice bearing RIF-1 tumors that received three injections of 300 μCi over a 3-week treatment period showed stabilization in tumor growth for 5 days, as measured by caliper and micro-positron emission tomography using [(18) F]fluorodeoxyglucose. Based on these results, we suggest the potentials of radiolabeled hypericin (1) in diagnostic aspects including prognosis or staging assessment of bulky necrotic cancers, monitoring of treatments and therapeutic follow-up; and (2) in cancer treatment based on tumor necrosis. In conclusion, we showed that hypericin radiolabeled with iodine is a necrosis avid tracer that can be used both as a tumor diagnostic and therapeutic.
ISSN: 0020-7136
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Radiology
Theragnostic Laboratory (+)
Translational Cell & Tissue Research
× corresponding author
# (joint) last author

Files in This Item:

There are no files associated with this item.

Request a copy


All items in Lirias are protected by copyright, with all rights reserved.

© Web of science