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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...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Shaheed Beheshti University of Medical Sciences
2017
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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. |
format | Online Article Text |
id | pubmed-5610754 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | Shaheed Beheshti University of Medical Sciences |
record_format | MEDLINE/PubMed |
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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