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Cycloartane-3,24,25-triol inhibits MRCKα kinase and demonstrates promising anti prostate cancer activity in vitro
BACKGROUND: Given the high occurrence of prostate cancer worldwide and one of the major sources of the discovery of new lead molecules being medicinal plants, this research undertook to investigate the possible anti-cancer activity of two natural cycloartanes; cycloartane-3,24,25-diol (extracted in...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
BioMed Central
2012
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3520828/ https://www.ncbi.nlm.nih.gov/pubmed/23151005 http://dx.doi.org/10.1186/1475-2867-12-46 |
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author | Lowe, Henry I C Watson, Charah T Badal, Simone Toyang, Ngeh J Bryant, Joseph |
author_facet | Lowe, Henry I C Watson, Charah T Badal, Simone Toyang, Ngeh J Bryant, Joseph |
author_sort | Lowe, Henry I C |
collection | PubMed |
description | BACKGROUND: Given the high occurrence of prostate cancer worldwide and one of the major sources of the discovery of new lead molecules being medicinal plants, this research undertook to investigate the possible anti-cancer activity of two natural cycloartanes; cycloartane-3,24,25-diol (extracted in our lab from Tillandsia recurvata) and cycloartane-3,24,25-triol (purchased). The inhibition of MRCKα kinase has emerged as a potential solution to restoring the tight regulation of normal cellular growth, the loss of which leads to cancer cell formation. METHODS: Kinase inhibition was investigated using competition binding (to the ATP sites) assays which have been previously established and authenticated and cell proliferation was measured using the WST-1 assay. RESULTS: Cycloartane-3,24,25-triol demonstrated strong selectivity towards the MRCKα kinase with a Kd(50) of 0.26 μM from a total of 451 kinases investigated. Cycloartane-3,24,25-triol reduced the viability of PC-3 and DU145 cell lines with IC(50) values of 2.226 ± 0.28 μM and 1.67 ± 0.18 μM respectively. CONCLUSIONS: These results will prove useful in drug discovery as Cycloartane-3,24,25-triol has shown potential for development as an anti-cancer agent against prostate cancer. |
format | Online Article Text |
id | pubmed-3520828 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2012 |
publisher | BioMed Central |
record_format | MEDLINE/PubMed |
spelling | pubmed-35208282012-12-13 Cycloartane-3,24,25-triol inhibits MRCKα kinase and demonstrates promising anti prostate cancer activity in vitro Lowe, Henry I C Watson, Charah T Badal, Simone Toyang, Ngeh J Bryant, Joseph Cancer Cell Int Primary Research BACKGROUND: Given the high occurrence of prostate cancer worldwide and one of the major sources of the discovery of new lead molecules being medicinal plants, this research undertook to investigate the possible anti-cancer activity of two natural cycloartanes; cycloartane-3,24,25-diol (extracted in our lab from Tillandsia recurvata) and cycloartane-3,24,25-triol (purchased). The inhibition of MRCKα kinase has emerged as a potential solution to restoring the tight regulation of normal cellular growth, the loss of which leads to cancer cell formation. METHODS: Kinase inhibition was investigated using competition binding (to the ATP sites) assays which have been previously established and authenticated and cell proliferation was measured using the WST-1 assay. RESULTS: Cycloartane-3,24,25-triol demonstrated strong selectivity towards the MRCKα kinase with a Kd(50) of 0.26 μM from a total of 451 kinases investigated. Cycloartane-3,24,25-triol reduced the viability of PC-3 and DU145 cell lines with IC(50) values of 2.226 ± 0.28 μM and 1.67 ± 0.18 μM respectively. CONCLUSIONS: These results will prove useful in drug discovery as Cycloartane-3,24,25-triol has shown potential for development as an anti-cancer agent against prostate cancer. BioMed Central 2012-11-14 /pmc/articles/PMC3520828/ /pubmed/23151005 http://dx.doi.org/10.1186/1475-2867-12-46 Text en Copyright ©2012 Lowe et al.; licensee BioMed Central Ltd. http://creativecommons.org/licenses/by/2.0 This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Primary Research Lowe, Henry I C Watson, Charah T Badal, Simone Toyang, Ngeh J Bryant, Joseph Cycloartane-3,24,25-triol inhibits MRCKα kinase and demonstrates promising anti prostate cancer activity in vitro |
title | Cycloartane-3,24,25-triol inhibits MRCKα kinase and demonstrates promising anti prostate cancer activity in vitro |
title_full | Cycloartane-3,24,25-triol inhibits MRCKα kinase and demonstrates promising anti prostate cancer activity in vitro |
title_fullStr | Cycloartane-3,24,25-triol inhibits MRCKα kinase and demonstrates promising anti prostate cancer activity in vitro |
title_full_unstemmed | Cycloartane-3,24,25-triol inhibits MRCKα kinase and demonstrates promising anti prostate cancer activity in vitro |
title_short | Cycloartane-3,24,25-triol inhibits MRCKα kinase and demonstrates promising anti prostate cancer activity in vitro |
title_sort | cycloartane-3,24,25-triol inhibits mrckα kinase and demonstrates promising anti prostate cancer activity in vitro |
topic | Primary Research |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3520828/ https://www.ncbi.nlm.nih.gov/pubmed/23151005 http://dx.doi.org/10.1186/1475-2867-12-46 |
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