Radiolabeled Silicon-Rhodamines as Bimodal PET/SPECT-NIR Imaging Agents

Radiolabeled fluorescent dyes are decisive for bimodal imaging as well as highly in demand for nuclear- and optical imaging. Silicon-rhodamines (SiRs) show unique near-infrared (NIR) optical properties, large quantum yields and extinction coefficients as well as high photostability. Here, we describ...

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Autores principales:	Thines Kanagasundaram, Markus Laube, Johanna Wodtke, Carsten Sven Kramer, Sven Stadlbauer, Jens Pietzsch, Klaus Kopka
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	multimodal imaging PET imaging SPECT imaging optical imaging organic chemistry near-infrared fluorophores Medicine R Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/465bfa818146467fa886498a4b4866cc
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spelling	oai:doaj.org-article:465bfa818146467fa886498a4b4866cc2021-11-25T18:39:47ZRadiolabeled Silicon-Rhodamines as Bimodal PET/SPECT-NIR Imaging Agents10.3390/ph141111551424-8247https://doaj.org/article/465bfa818146467fa886498a4b4866cc2021-11-01T00:00:00Zhttps://www.mdpi.com/1424-8247/14/11/1155https://doaj.org/toc/1424-8247Radiolabeled fluorescent dyes are decisive for bimodal imaging as well as highly in demand for nuclear- and optical imaging. Silicon-rhodamines (SiRs) show unique near-infrared (NIR) optical properties, large quantum yields and extinction coefficients as well as high photostability. Here, we describe the synthesis, characterization and radiolabeling of novel NIR absorbing and emitting fluorophores from the silicon-rhodamine family for use in optical imaging (OI) combined with positron emission tomography (PET) or single photon emission computed tomography (SPECT), respectively. The presented photostable SiRs were characterized using NMR-, UV-Vis-NIR-spectroscopy and mass spectrometry. Moreover, the radiolabeling conditions using fluorine-18 or iodine-123 were extensively explored. After optimization, the radiofluorinated NIR imaging agents were obtained with radiochemical conversions (RCC) up to 70% and isolated radiochemical yields (RCY) up to 54% at molar activities of g.t. 70 GBq/µmol. Radioiodination delivered RCCs over 92% and allowed to isolate the <sup>123</sup>I-labeled product in RCY of 54% at a molar activity of g.t. 7.6 TBq/µmol. The radiofluorinated SiRs exhibit in vitro stabilities g.t. 70% after two hours in human serum. The first described radiolabeled SiRs are a promising step toward their further development as multimodal PET/SPECT-NIR imaging agents for planning and subsequent imaging-guided oncological surgery.Thines KanagasundaramMarkus LaubeJohanna WodtkeCarsten Sven KramerSven StadlbauerJens PietzschKlaus KopkaMDPI AGarticlemultimodal imagingPET imagingSPECT imagingoptical imagingorganic chemistrynear-infrared fluorophoresMedicineRPharmacy and materia medicaRS1-441ENPharmaceuticals, Vol 14, Iss 1155, p 1155 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	multimodal imaging PET imaging SPECT imaging optical imaging organic chemistry near-infrared fluorophores Medicine R Pharmacy and materia medica RS1-441
spellingShingle	multimodal imaging PET imaging SPECT imaging optical imaging organic chemistry near-infrared fluorophores Medicine R Pharmacy and materia medica RS1-441 Thines Kanagasundaram Markus Laube Johanna Wodtke Carsten Sven Kramer Sven Stadlbauer Jens Pietzsch Klaus Kopka Radiolabeled Silicon-Rhodamines as Bimodal PET/SPECT-NIR Imaging Agents
description	Radiolabeled fluorescent dyes are decisive for bimodal imaging as well as highly in demand for nuclear- and optical imaging. Silicon-rhodamines (SiRs) show unique near-infrared (NIR) optical properties, large quantum yields and extinction coefficients as well as high photostability. Here, we describe the synthesis, characterization and radiolabeling of novel NIR absorbing and emitting fluorophores from the silicon-rhodamine family for use in optical imaging (OI) combined with positron emission tomography (PET) or single photon emission computed tomography (SPECT), respectively. The presented photostable SiRs were characterized using NMR-, UV-Vis-NIR-spectroscopy and mass spectrometry. Moreover, the radiolabeling conditions using fluorine-18 or iodine-123 were extensively explored. After optimization, the radiofluorinated NIR imaging agents were obtained with radiochemical conversions (RCC) up to 70% and isolated radiochemical yields (RCY) up to 54% at molar activities of g.t. 70 GBq/µmol. Radioiodination delivered RCCs over 92% and allowed to isolate the <sup>123</sup>I-labeled product in RCY of 54% at a molar activity of g.t. 7.6 TBq/µmol. The radiofluorinated SiRs exhibit in vitro stabilities g.t. 70% after two hours in human serum. The first described radiolabeled SiRs are a promising step toward their further development as multimodal PET/SPECT-NIR imaging agents for planning and subsequent imaging-guided oncological surgery.
format	article
author	Thines Kanagasundaram Markus Laube Johanna Wodtke Carsten Sven Kramer Sven Stadlbauer Jens Pietzsch Klaus Kopka
author_facet	Thines Kanagasundaram Markus Laube Johanna Wodtke Carsten Sven Kramer Sven Stadlbauer Jens Pietzsch Klaus Kopka
author_sort	Thines Kanagasundaram
title	Radiolabeled Silicon-Rhodamines as Bimodal PET/SPECT-NIR Imaging Agents
title_short	Radiolabeled Silicon-Rhodamines as Bimodal PET/SPECT-NIR Imaging Agents
title_full	Radiolabeled Silicon-Rhodamines as Bimodal PET/SPECT-NIR Imaging Agents
title_fullStr	Radiolabeled Silicon-Rhodamines as Bimodal PET/SPECT-NIR Imaging Agents
title_full_unstemmed	Radiolabeled Silicon-Rhodamines as Bimodal PET/SPECT-NIR Imaging Agents
title_sort	radiolabeled silicon-rhodamines as bimodal pet/spect-nir imaging agents
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/465bfa818146467fa886498a4b4866cc
work_keys_str_mv	AT thineskanagasundaram radiolabeledsiliconrhodaminesasbimodalpetspectnirimagingagents AT markuslaube radiolabeledsiliconrhodaminesasbimodalpetspectnirimagingagents AT johannawodtke radiolabeledsiliconrhodaminesasbimodalpetspectnirimagingagents AT carstensvenkramer radiolabeledsiliconrhodaminesasbimodalpetspectnirimagingagents AT svenstadlbauer radiolabeledsiliconrhodaminesasbimodalpetspectnirimagingagents AT jenspietzsch radiolabeledsiliconrhodaminesasbimodalpetspectnirimagingagents AT klauskopka radiolabeledsiliconrhodaminesasbimodalpetspectnirimagingagents
_version_	1718410829767901184

Radiolabeled Silicon-Rhodamines as Bimodal PET/SPECT-NIR Imaging Agents

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