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Anti-estrogenic and anti-aromatase activities of citrus peels major compounds in breast cancer
Estrogen signaling is crucial for breast cancer initiation and progression. Endocrine-based therapies comprising estrogen receptor (ER) modulators and aromatase inhibitors remain the mainstay of treatment. This study aimed at investigating the antitumor potential of the most potent compounds in citr...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Nature Publishing Group UK
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8007834/ https://www.ncbi.nlm.nih.gov/pubmed/33782546 http://dx.doi.org/10.1038/s41598-021-86599-z |
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author | El-Kersh, Dina M. Ezzat, Shahira M. Salama, Maha M. Mahrous, Engy A. Attia, Yasmeen M. Ahmed, Mahmoud Salama Elmazar, Mohey M. |
author_facet | El-Kersh, Dina M. Ezzat, Shahira M. Salama, Maha M. Mahrous, Engy A. Attia, Yasmeen M. Ahmed, Mahmoud Salama Elmazar, Mohey M. |
author_sort | El-Kersh, Dina M. |
collection | PubMed |
description | Estrogen signaling is crucial for breast cancer initiation and progression. Endocrine-based therapies comprising estrogen receptor (ER) modulators and aromatase inhibitors remain the mainstay of treatment. This study aimed at investigating the antitumor potential of the most potent compounds in citrus peels on breast cancer by exploring their anti-estrogenic and anti-aromatase activities. The ethanolic extract of different varieties of citrus peels along with eight isolated flavonoids were screened against estrogen-dependent breast cancer cell lines besides normal cells for evaluating their safety profile. Naringenin, naringin and quercetin demonstrated the lowest IC(50s) and were therefore selected for further assays. In silico molecular modeling against ER and aromatase was performed for the three compounds. In vivo estrogenic and anti-estrogenic assays confirmed an anti-estrogenic activity for the isolates. Moreover, naringenin, naringin and quercetin demonstrated in vitro inhibitory potential against aromatase enzyme along with anticancer potential in vivo, as evidenced by decreased tumor volumes. Reduction in aromatase levels in solid tumors was also observed in treated groups. Overall, this study suggests an antitumor potential for naringenin, naringin and quercetin isolated from citrus peels in breast cancer via possible modulation of estrogen signaling and aromatase inhibition suggesting their use in pre- and post-menopausal breast cancer patients, respectively. |
format | Online Article Text |
id | pubmed-8007834 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | Nature Publishing Group UK |
record_format | MEDLINE/PubMed |
spelling | pubmed-80078342021-04-01 Anti-estrogenic and anti-aromatase activities of citrus peels major compounds in breast cancer El-Kersh, Dina M. Ezzat, Shahira M. Salama, Maha M. Mahrous, Engy A. Attia, Yasmeen M. Ahmed, Mahmoud Salama Elmazar, Mohey M. Sci Rep Article Estrogen signaling is crucial for breast cancer initiation and progression. Endocrine-based therapies comprising estrogen receptor (ER) modulators and aromatase inhibitors remain the mainstay of treatment. This study aimed at investigating the antitumor potential of the most potent compounds in citrus peels on breast cancer by exploring their anti-estrogenic and anti-aromatase activities. The ethanolic extract of different varieties of citrus peels along with eight isolated flavonoids were screened against estrogen-dependent breast cancer cell lines besides normal cells for evaluating their safety profile. Naringenin, naringin and quercetin demonstrated the lowest IC(50s) and were therefore selected for further assays. In silico molecular modeling against ER and aromatase was performed for the three compounds. In vivo estrogenic and anti-estrogenic assays confirmed an anti-estrogenic activity for the isolates. Moreover, naringenin, naringin and quercetin demonstrated in vitro inhibitory potential against aromatase enzyme along with anticancer potential in vivo, as evidenced by decreased tumor volumes. Reduction in aromatase levels in solid tumors was also observed in treated groups. Overall, this study suggests an antitumor potential for naringenin, naringin and quercetin isolated from citrus peels in breast cancer via possible modulation of estrogen signaling and aromatase inhibition suggesting their use in pre- and post-menopausal breast cancer patients, respectively. Nature Publishing Group UK 2021-03-29 /pmc/articles/PMC8007834/ /pubmed/33782546 http://dx.doi.org/10.1038/s41598-021-86599-z Text en © The Author(s) 2021 Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/. |
spellingShingle | Article El-Kersh, Dina M. Ezzat, Shahira M. Salama, Maha M. Mahrous, Engy A. Attia, Yasmeen M. Ahmed, Mahmoud Salama Elmazar, Mohey M. Anti-estrogenic and anti-aromatase activities of citrus peels major compounds in breast cancer |
title | Anti-estrogenic and anti-aromatase activities of citrus peels major compounds in breast cancer |
title_full | Anti-estrogenic and anti-aromatase activities of citrus peels major compounds in breast cancer |
title_fullStr | Anti-estrogenic and anti-aromatase activities of citrus peels major compounds in breast cancer |
title_full_unstemmed | Anti-estrogenic and anti-aromatase activities of citrus peels major compounds in breast cancer |
title_short | Anti-estrogenic and anti-aromatase activities of citrus peels major compounds in breast cancer |
title_sort | anti-estrogenic and anti-aromatase activities of citrus peels major compounds in breast cancer |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8007834/ https://www.ncbi.nlm.nih.gov/pubmed/33782546 http://dx.doi.org/10.1038/s41598-021-86599-z |
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