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In Vitro and In Vivo Anti-Angiogenic Activities of Panduratin A
BACKGROUND: Targeting angiogenesis has emerged as an attractive and promising strategy in anti-cancer therapeutic development. The present study investigates the anti-angiogenic potential of Panduratin A (PA), a natural chalcone isolated from Boesenbergia rotunda by using both in vitro and in vivo a...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Public Library of Science
2012
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3364190/ https://www.ncbi.nlm.nih.gov/pubmed/22666456 http://dx.doi.org/10.1371/journal.pone.0038103 |
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author | Lai, Siew-Li Cheah, Shiau-Chuen Wong, Pooi-Fong Noor, Suzita Mohd Mustafa, Mohd Rais |
author_facet | Lai, Siew-Li Cheah, Shiau-Chuen Wong, Pooi-Fong Noor, Suzita Mohd Mustafa, Mohd Rais |
author_sort | Lai, Siew-Li |
collection | PubMed |
description | BACKGROUND: Targeting angiogenesis has emerged as an attractive and promising strategy in anti-cancer therapeutic development. The present study investigates the anti-angiogenic potential of Panduratin A (PA), a natural chalcone isolated from Boesenbergia rotunda by using both in vitro and in vivo assays. METHODOLOGY/PRINCIPAL FINDINGS: PA exerted selective cytotoxicity on human umbilical vein endothelial cells (HUVECs) with IC(50) value of 6.91±0.85 µM when compared to human normal fibroblast and normal liver epithelial cells. Assessment of the growth kinetics by cell impedance-based Real-Time Cell Analyzer showed that PA induced both cytotoxic and cytostatic effects on HUVECs, depending on the concentration used. Results also showed that PA suppressed VEGF-induced survival and proliferation of HUVECs. Furthermore, endothelial cell migration, invasion, and morphogenesis or tube formation demonstrated significant time- and dose-dependent inhibition by PA. PA also suppressed matrix metalloproteinase-2 (MMP-2) secretion and attenuated its activation to intermediate and active MMP-2. In addition, PA suppressed F-actin stress fiber formation to prevent migration of the endothelial cells. More importantly, anti-angiogenic potential of PA was also evidenced in two in vivo models. PA inhibited neo-vessels formation in murine Matrigel plugs, and angiogenesis in zebrafish embryos. CONCLUSIONS/SIGNIFICANCE: Taken together, our study demonstrated the distinctive anti-angiogenic properties of PA, both in vitro and in vivo. This report thus reveals another biological activity of PA in addition to its reported anti-inflammatory and anti-cancer activities, suggestive of PA’s potential for development as an anti-angiogenic agent for cancer therapy. |
format | Online Article Text |
id | pubmed-3364190 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2012 |
publisher | Public Library of Science |
record_format | MEDLINE/PubMed |
spelling | pubmed-33641902012-06-04 In Vitro and In Vivo Anti-Angiogenic Activities of Panduratin A Lai, Siew-Li Cheah, Shiau-Chuen Wong, Pooi-Fong Noor, Suzita Mohd Mustafa, Mohd Rais PLoS One Research Article BACKGROUND: Targeting angiogenesis has emerged as an attractive and promising strategy in anti-cancer therapeutic development. The present study investigates the anti-angiogenic potential of Panduratin A (PA), a natural chalcone isolated from Boesenbergia rotunda by using both in vitro and in vivo assays. METHODOLOGY/PRINCIPAL FINDINGS: PA exerted selective cytotoxicity on human umbilical vein endothelial cells (HUVECs) with IC(50) value of 6.91±0.85 µM when compared to human normal fibroblast and normal liver epithelial cells. Assessment of the growth kinetics by cell impedance-based Real-Time Cell Analyzer showed that PA induced both cytotoxic and cytostatic effects on HUVECs, depending on the concentration used. Results also showed that PA suppressed VEGF-induced survival and proliferation of HUVECs. Furthermore, endothelial cell migration, invasion, and morphogenesis or tube formation demonstrated significant time- and dose-dependent inhibition by PA. PA also suppressed matrix metalloproteinase-2 (MMP-2) secretion and attenuated its activation to intermediate and active MMP-2. In addition, PA suppressed F-actin stress fiber formation to prevent migration of the endothelial cells. More importantly, anti-angiogenic potential of PA was also evidenced in two in vivo models. PA inhibited neo-vessels formation in murine Matrigel plugs, and angiogenesis in zebrafish embryos. CONCLUSIONS/SIGNIFICANCE: Taken together, our study demonstrated the distinctive anti-angiogenic properties of PA, both in vitro and in vivo. This report thus reveals another biological activity of PA in addition to its reported anti-inflammatory and anti-cancer activities, suggestive of PA’s potential for development as an anti-angiogenic agent for cancer therapy. Public Library of Science 2012-05-30 /pmc/articles/PMC3364190/ /pubmed/22666456 http://dx.doi.org/10.1371/journal.pone.0038103 Text en Lai et al. http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are properly credited. |
spellingShingle | Research Article Lai, Siew-Li Cheah, Shiau-Chuen Wong, Pooi-Fong Noor, Suzita Mohd Mustafa, Mohd Rais In Vitro and In Vivo Anti-Angiogenic Activities of Panduratin A |
title |
In Vitro and In Vivo Anti-Angiogenic Activities of Panduratin A |
title_full |
In Vitro and In Vivo Anti-Angiogenic Activities of Panduratin A |
title_fullStr |
In Vitro and In Vivo Anti-Angiogenic Activities of Panduratin A |
title_full_unstemmed |
In Vitro and In Vivo Anti-Angiogenic Activities of Panduratin A |
title_short |
In Vitro and In Vivo Anti-Angiogenic Activities of Panduratin A |
title_sort | in vitro and in vivo anti-angiogenic activities of panduratin a |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3364190/ https://www.ncbi.nlm.nih.gov/pubmed/22666456 http://dx.doi.org/10.1371/journal.pone.0038103 |
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