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Preparation, analysis and biodistribution in mice of iodine‐123 labelled derivatives of hypericin
Author(s) -
Bormans Guy,
Huyghe Dieter,
Christiaen Annemie,
Verbeke Kristin,
de Groot Tjibbe,
Vanbilloen Hubert,
de Witte Peter,
Verbruggen Alfons
Publication year - 2004
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.812
Subject(s) - chemistry , biodistribution , hypericin , labelling , iodine , radiochemistry , iodide , iodine monochloride , electrophile , halogenation , iodine 123 , specific activity , stereochemistry , pharmacology , biochemistry , organic chemistry , nuclear medicine , catalysis , enzyme , medicine , in vitro
The synthesis of iodine‐123 labelled mono‐ and di‐iodo derivatives of hypericin, an hydroxylated phenanthroperylenequinone which is used for photodynamic therapy and has been shown to accumulate in several tumour types, is reported. Labelling was performed by electrophilic substitution on hypericin or iodohypericin with [ 123 I]iodide in the presence of peracetic acid and provided both mono‐[ 123 I]iodohypericin and di‐[ 123 I]iodohypericin in good radiochemical yields (>80%). Mono‐[ 123 I]iodohypericin was obtained with a high specific activity (925 GBq/μmol) whereas di‐[ 123 I]iodohypericin was obtained in low specific activity (4 GBq/μmol) due to deiodination and subsequent iodination of iodohypericin which occurred during the labelling reaction. Biodistribution studies in mice showed a slow blood clearance and extensive hepatobiliary clearance as well as faecal excretion for both compounds. They will be further evaluated with regard to their tumor seeking properties. Copyright © 2004 John Wiley & Sons, Ltd.