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Evaluation of a (99m)Tc-tricine Vascular Disrupting Agent as an In-vivo Imaging in 4T1 Mouse Breast Tumor Model

Colchicine as a vascular disrupting agent creates microtubule destabilization which induces vessel blockage and consequently cell death. Accordingly, colchicines and its analogues radiolabeled with (99m)Tc may have potential for visualization of tumor. In this work, deacetylcolchicine a colchicine a...

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Autores principales: Erfani, Mostafa, Shirmardi, Seyed Pezhman, Shafiei, Mohammad
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Shaheed Beheshti University of Medical Sciences 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5610754/
https://www.ncbi.nlm.nih.gov/pubmed/29201088
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author Erfani, Mostafa
Shirmardi, Seyed Pezhman
Shafiei, Mohammad
author_facet Erfani, Mostafa
Shirmardi, Seyed Pezhman
Shafiei, Mohammad
author_sort Erfani, Mostafa
collection PubMed
description Colchicine as a vascular disrupting agent creates microtubule destabilization which induces vessel blockage and consequently cell death. Accordingly, colchicines and its analogues radiolabeled with (99m)Tc may have potential for visualization of tumor. In this work, deacetylcolchicine a colchicine analogue was labeled with (99m)Tc via tricine as a coligand and characterized for its tumor targeting properties. The in-vitro radiochemical stability and the biodistribution were studied in 4T1 breast tumor model bearing mice. Labeling yield of more than 90% was obtained corresponding to a specific activity of 46 MBq/µmol. In-vivo biodistribution studies demonstrated that radiocomplex had high tumor to muscle and tumor to blood ratios at early time points. Planer gamma imaging of tumor bearing mice showed that this radioconjugate was able to clearly visualize tumors. According to high tumor uptake, presented radiocomplex may have a potential for targeted imaging studies.
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spelling pubmed-56107542017-12-01 Evaluation of a (99m)Tc-tricine Vascular Disrupting Agent as an In-vivo Imaging in 4T1 Mouse Breast Tumor Model Erfani, Mostafa Shirmardi, Seyed Pezhman Shafiei, Mohammad Iran J Pharm Res Original Article Colchicine as a vascular disrupting agent creates microtubule destabilization which induces vessel blockage and consequently cell death. Accordingly, colchicines and its analogues radiolabeled with (99m)Tc may have potential for visualization of tumor. In this work, deacetylcolchicine a colchicine analogue was labeled with (99m)Tc via tricine as a coligand and characterized for its tumor targeting properties. The in-vitro radiochemical stability and the biodistribution were studied in 4T1 breast tumor model bearing mice. Labeling yield of more than 90% was obtained corresponding to a specific activity of 46 MBq/µmol. In-vivo biodistribution studies demonstrated that radiocomplex had high tumor to muscle and tumor to blood ratios at early time points. Planer gamma imaging of tumor bearing mice showed that this radioconjugate was able to clearly visualize tumors. According to high tumor uptake, presented radiocomplex may have a potential for targeted imaging studies. Shaheed Beheshti University of Medical Sciences 2017 /pmc/articles/PMC5610754/ /pubmed/29201088 Text en © 2017 by School of Pharmacy, Shaheed Beheshti University of Medical Sciences and Health Services This is an Open Access article distributed under the terms of the Creative Commons Attribution License, (http://creativecommons.org/licenses/by/3.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Article
Erfani, Mostafa
Shirmardi, Seyed Pezhman
Shafiei, Mohammad
Evaluation of a (99m)Tc-tricine Vascular Disrupting Agent as an In-vivo Imaging in 4T1 Mouse Breast Tumor Model
title Evaluation of a (99m)Tc-tricine Vascular Disrupting Agent as an In-vivo Imaging in 4T1 Mouse Breast Tumor Model
title_full Evaluation of a (99m)Tc-tricine Vascular Disrupting Agent as an In-vivo Imaging in 4T1 Mouse Breast Tumor Model
title_fullStr Evaluation of a (99m)Tc-tricine Vascular Disrupting Agent as an In-vivo Imaging in 4T1 Mouse Breast Tumor Model
title_full_unstemmed Evaluation of a (99m)Tc-tricine Vascular Disrupting Agent as an In-vivo Imaging in 4T1 Mouse Breast Tumor Model
title_short Evaluation of a (99m)Tc-tricine Vascular Disrupting Agent as an In-vivo Imaging in 4T1 Mouse Breast Tumor Model
title_sort evaluation of a (99m)tc-tricine vascular disrupting agent as an in-vivo imaging in 4t1 mouse breast tumor model
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5610754/
https://www.ncbi.nlm.nih.gov/pubmed/29201088
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