Abstract
We report here an investigation that focuses on the organ distribution of metal complexes that are chelated by the amphipolar corrole whose macrocycle is decorated by two sulphonic acid head groups, which are emerging potential therapeutics against cancer (the cytotoxic Ga chelate) and diseases that are characterized by excessive production of ROS and RNS (the cytoprotective Mn and Fe derivatives). We show that the intraperitoneally injected fluorescent gallium(III) derivative accumulates in tissues sections of the kidney, liver, lung, heart, and pancreas. It also reaches the brain blood vessels, but does not cross the blood brain barrier. These findings are of prime importance for future in vivo studies on disease models, as they point toward a large utility of this kind of corrole chelates for treating cancer, neurodegenerative diseases characterized by “leaking BBB”, cardiovascular diseases and diabetes.
Keywords: Imaging, oxidative stress, bioavailability, bio-distribution, corroles, cancer, diabetes, neurodegenerative diseases, metallocorroles, cell-internalizing motifs, of penicillin/streptomycin/nystatin, Minimum Essential Medium, paraformaldehyde solution, cholesterol biosynthesis, b cells (insulinoma)
Anti-Cancer Agents in Medicinal Chemistry
Title: Cellular Uptake and Organ Accumulation of Amphipolar Metallocorroles with Cytoprotective and Cytotoxic Properties
Volume: 11 Issue: 4
Author(s): Zoya Okun, Lana Kupershmidt, Moussa B. H. Youdim and Zeev Gross
Affiliation:
Keywords: Imaging, oxidative stress, bioavailability, bio-distribution, corroles, cancer, diabetes, neurodegenerative diseases, metallocorroles, cell-internalizing motifs, of penicillin/streptomycin/nystatin, Minimum Essential Medium, paraformaldehyde solution, cholesterol biosynthesis, b cells (insulinoma)
Abstract: We report here an investigation that focuses on the organ distribution of metal complexes that are chelated by the amphipolar corrole whose macrocycle is decorated by two sulphonic acid head groups, which are emerging potential therapeutics against cancer (the cytotoxic Ga chelate) and diseases that are characterized by excessive production of ROS and RNS (the cytoprotective Mn and Fe derivatives). We show that the intraperitoneally injected fluorescent gallium(III) derivative accumulates in tissues sections of the kidney, liver, lung, heart, and pancreas. It also reaches the brain blood vessels, but does not cross the blood brain barrier. These findings are of prime importance for future in vivo studies on disease models, as they point toward a large utility of this kind of corrole chelates for treating cancer, neurodegenerative diseases characterized by “leaking BBB”, cardiovascular diseases and diabetes.
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Cite this article as:
Okun Zoya, Kupershmidt Lana, B. H. Youdim Moussa and Gross Zeev, Cellular Uptake and Organ Accumulation of Amphipolar Metallocorroles with Cytoprotective and Cytotoxic Properties, Anti-Cancer Agents in Medicinal Chemistry 2011; 11 (4) . https://dx.doi.org/10.2174/187152011795677535
DOI https://dx.doi.org/10.2174/187152011795677535 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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