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Antinociceptive and antitumor activity of novel synthetic mononuclear Ruthenium (II) compounds

BACKGROUND: From the thousands of years, metal compounds have been used in medicine for treatment of various diseases including various types of cancers. Ruthenium was seen as a promising metal due to its similar kinetics to platinum and its lower toxicity. Therefore, we aimed to evaluate the newer...

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Autores principales: Sunder A, Shyam, Dhulipala, Satyavati, Thota, Sreekanth, Yerra, Rajeshwar, Balzarini, Jan, De Clercq, Erik
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Medknow Publications & Media Pvt Ltd 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3732902/
https://www.ncbi.nlm.nih.gov/pubmed/23930118
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author Sunder A, Shyam
Dhulipala, Satyavati
Thota, Sreekanth
Yerra, Rajeshwar
Balzarini, Jan
De Clercq, Erik
author_facet Sunder A, Shyam
Dhulipala, Satyavati
Thota, Sreekanth
Yerra, Rajeshwar
Balzarini, Jan
De Clercq, Erik
author_sort Sunder A, Shyam
collection PubMed
description BACKGROUND: From the thousands of years, metal compounds have been used in medicine for treatment of various diseases including various types of cancers. Ruthenium was seen as a promising metal due to its similar kinetics to platinum and its lower toxicity. Therefore, we aimed to evaluate the newer mononuclear ruthenium (II) compounds for antinociceptive and antitumor activities. MATERIALS AND METHODS: Ruthenium (II) compounds were evaluated for antinociceptive and antitumor activity using the various in vitro and in vivo models. The compounds were injected to mice at concentrations of 1 and 2 mg kg(-1) intraperitoneally and were screened for antinociceptive activity, and the antiproliferative effect was evaluated against murine leukemia cells (L1210), human T-lymphocyte cells (CEM) and human cervix carcinoma cells (HeLa) using MTT assay. RESULTS: The results for antitumor activity clearly indicated that compound R(1) was potent cytotoxic agent than R(2) with IC(50) values ranging from 4-6 μM for R(1), whereas IC(50) values for compound R(2) ranging from 65-103 μM. The compounds have shown a significant anti-inflammatory effect in carrageenan and dextran models but do not having the central analgesic activity, this indicating that the antinociceptive activity is related to the peripheral nervous system. The results for 5-Lipoxygenase (5-LOX) activity showed that both R(1) and R(2) compounds were found to be significant 5-LOX inhibitory activity with IC(50) values of 14.35 μg ml(-1) and 29.24 μg ml(-1) respectively. CONCLUSION: These findings concluded that the new ruthenium compounds might be the promising antiproliferative agents as these compounds showing significant 5-LOX inhibitory activity and potential agents in the management of pain related disorders.
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spelling pubmed-37329022013-08-08 Antinociceptive and antitumor activity of novel synthetic mononuclear Ruthenium (II) compounds Sunder A, Shyam Dhulipala, Satyavati Thota, Sreekanth Yerra, Rajeshwar Balzarini, Jan De Clercq, Erik J Res Med Sci Original Article BACKGROUND: From the thousands of years, metal compounds have been used in medicine for treatment of various diseases including various types of cancers. Ruthenium was seen as a promising metal due to its similar kinetics to platinum and its lower toxicity. Therefore, we aimed to evaluate the newer mononuclear ruthenium (II) compounds for antinociceptive and antitumor activities. MATERIALS AND METHODS: Ruthenium (II) compounds were evaluated for antinociceptive and antitumor activity using the various in vitro and in vivo models. The compounds were injected to mice at concentrations of 1 and 2 mg kg(-1) intraperitoneally and were screened for antinociceptive activity, and the antiproliferative effect was evaluated against murine leukemia cells (L1210), human T-lymphocyte cells (CEM) and human cervix carcinoma cells (HeLa) using MTT assay. RESULTS: The results for antitumor activity clearly indicated that compound R(1) was potent cytotoxic agent than R(2) with IC(50) values ranging from 4-6 μM for R(1), whereas IC(50) values for compound R(2) ranging from 65-103 μM. The compounds have shown a significant anti-inflammatory effect in carrageenan and dextran models but do not having the central analgesic activity, this indicating that the antinociceptive activity is related to the peripheral nervous system. The results for 5-Lipoxygenase (5-LOX) activity showed that both R(1) and R(2) compounds were found to be significant 5-LOX inhibitory activity with IC(50) values of 14.35 μg ml(-1) and 29.24 μg ml(-1) respectively. CONCLUSION: These findings concluded that the new ruthenium compounds might be the promising antiproliferative agents as these compounds showing significant 5-LOX inhibitory activity and potential agents in the management of pain related disorders. Medknow Publications & Media Pvt Ltd 2013-03 /pmc/articles/PMC3732902/ /pubmed/23930118 Text en Copyright: © Journal of Research in Medical Sciences http://creativecommons.org/licenses/by-nc-sa/3.0 This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Article
Sunder A, Shyam
Dhulipala, Satyavati
Thota, Sreekanth
Yerra, Rajeshwar
Balzarini, Jan
De Clercq, Erik
Antinociceptive and antitumor activity of novel synthetic mononuclear Ruthenium (II) compounds
title Antinociceptive and antitumor activity of novel synthetic mononuclear Ruthenium (II) compounds
title_full Antinociceptive and antitumor activity of novel synthetic mononuclear Ruthenium (II) compounds
title_fullStr Antinociceptive and antitumor activity of novel synthetic mononuclear Ruthenium (II) compounds
title_full_unstemmed Antinociceptive and antitumor activity of novel synthetic mononuclear Ruthenium (II) compounds
title_short Antinociceptive and antitumor activity of novel synthetic mononuclear Ruthenium (II) compounds
title_sort antinociceptive and antitumor activity of novel synthetic mononuclear ruthenium (ii) compounds
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3732902/
https://www.ncbi.nlm.nih.gov/pubmed/23930118
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