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Oestrogenic activity of mimosine on MCF-7 breast cancer cell line through the ERα-mediated pathway.

Hormone replacement therapy has been a conventional treatment for postmenopausal symptoms in women. However, it has potential risks of breast and endometrial cancers. The aim of this study was to evaluate the oestrogenicity of a plant-based compound, mimosine in MCF-7 cells and by in silico model. C...

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Main Authors: Huq, A. K. M. Moyeenul, Wai, Lam K., Rullah, Kamal, Mohd F. F., Mohd Aluwi, Stanslas, Johnson, Jamal, Jamia A.
Format: Article
Language:English
Published: John Wiley & Sons 2018
Online Access:http://umpir.ump.edu.my/id/eprint/22317/1/cbdd.13404
http://umpir.ump.edu.my/id/eprint/22317/
https://doi.org/10.1111/cbdd.13404
https://doi.org/10.1111/cbdd.13404
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spelling my.ump.umpir.223172019-01-29T04:54:10Z http://umpir.ump.edu.my/id/eprint/22317/ Oestrogenic activity of mimosine on MCF-7 breast cancer cell line through the ERα-mediated pathway. Huq, A. K. M. Moyeenul Wai, Lam K. Rullah, Kamal Mohd F. F., Mohd Aluwi Stanslas, Johnson Jamal, Jamia A. Hormone replacement therapy has been a conventional treatment for postmenopausal symptoms in women. However, it has potential risks of breast and endometrial cancers. The aim of this study was to evaluate the oestrogenicity of a plant-based compound, mimosine in MCF-7 cells and by in silico model. Cell viability and proliferation, ERα-SRC1 coactivator activity and expression of specific ERα-dependent marker TFF1 and PGR genes were evaluated. Binding modes of 17β-oestradiol and mimosine at the ERα ligand binding domain were compared using docking and molecular dynamics simulation experiments followed by binding interaction free energy calculation with molecular mechanics/Poisson Boltzmann surface area. Mimosine showed increased cellular viability (64450 cells/mL) at 0.1 μM with significant cell proliferation (120.5%) compared to 17β-oestradiol (135.2%). ER antagonist tamoxifen significantly reduced proliferative activity mediated by mimosine (49.9%). Mimosine at 1 μM showed the highest ERα binding activity through increased SRC1 recruitment at 186.9%. It expressed TFF1 (11.1 fold at 0.1 μM) and PGR (13.9 fold at 0.01 μM) genes. ERα-mimosine binding energy was -49.9 kJ/mol and it interacted with Thr347, Gly521 and His524 of ERα-LBD. The results suggested that mimosine has oestrogenic activity. This article is protected by copyright. All rights reserved. John Wiley & Sons 2018-09-24 Article PeerReviewed text en http://umpir.ump.edu.my/id/eprint/22317/1/cbdd.13404 Huq, A. K. M. Moyeenul and Wai, Lam K. and Rullah, Kamal and Mohd F. F., Mohd Aluwi and Stanslas, Johnson and Jamal, Jamia A. (2018) Oestrogenic activity of mimosine on MCF-7 breast cancer cell line through the ERα-mediated pathway. Chemical Biology & Drug Design. ISSN 1747-0285 (In Press) https://doi.org/10.1111/cbdd.13404 https://doi.org/10.1111/cbdd.13404
institution Universiti Malaysia Pahang
building UMP Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Malaysia Pahang
content_source UMP Institutional Repository
url_provider http://umpir.ump.edu.my/
language English
description Hormone replacement therapy has been a conventional treatment for postmenopausal symptoms in women. However, it has potential risks of breast and endometrial cancers. The aim of this study was to evaluate the oestrogenicity of a plant-based compound, mimosine in MCF-7 cells and by in silico model. Cell viability and proliferation, ERα-SRC1 coactivator activity and expression of specific ERα-dependent marker TFF1 and PGR genes were evaluated. Binding modes of 17β-oestradiol and mimosine at the ERα ligand binding domain were compared using docking and molecular dynamics simulation experiments followed by binding interaction free energy calculation with molecular mechanics/Poisson Boltzmann surface area. Mimosine showed increased cellular viability (64450 cells/mL) at 0.1 μM with significant cell proliferation (120.5%) compared to 17β-oestradiol (135.2%). ER antagonist tamoxifen significantly reduced proliferative activity mediated by mimosine (49.9%). Mimosine at 1 μM showed the highest ERα binding activity through increased SRC1 recruitment at 186.9%. It expressed TFF1 (11.1 fold at 0.1 μM) and PGR (13.9 fold at 0.01 μM) genes. ERα-mimosine binding energy was -49.9 kJ/mol and it interacted with Thr347, Gly521 and His524 of ERα-LBD. The results suggested that mimosine has oestrogenic activity. This article is protected by copyright. All rights reserved.
format Article
author Huq, A. K. M. Moyeenul
Wai, Lam K.
Rullah, Kamal
Mohd F. F., Mohd Aluwi
Stanslas, Johnson
Jamal, Jamia A.
spellingShingle Huq, A. K. M. Moyeenul
Wai, Lam K.
Rullah, Kamal
Mohd F. F., Mohd Aluwi
Stanslas, Johnson
Jamal, Jamia A.
Oestrogenic activity of mimosine on MCF-7 breast cancer cell line through the ERα-mediated pathway.
author_facet Huq, A. K. M. Moyeenul
Wai, Lam K.
Rullah, Kamal
Mohd F. F., Mohd Aluwi
Stanslas, Johnson
Jamal, Jamia A.
author_sort Huq, A. K. M. Moyeenul
title Oestrogenic activity of mimosine on MCF-7 breast cancer cell line through the ERα-mediated pathway.
title_short Oestrogenic activity of mimosine on MCF-7 breast cancer cell line through the ERα-mediated pathway.
title_full Oestrogenic activity of mimosine on MCF-7 breast cancer cell line through the ERα-mediated pathway.
title_fullStr Oestrogenic activity of mimosine on MCF-7 breast cancer cell line through the ERα-mediated pathway.
title_full_unstemmed Oestrogenic activity of mimosine on MCF-7 breast cancer cell line through the ERα-mediated pathway.
title_sort oestrogenic activity of mimosine on mcf-7 breast cancer cell line through the erα-mediated pathway.
publisher John Wiley & Sons
publishDate 2018
url http://umpir.ump.edu.my/id/eprint/22317/1/cbdd.13404
http://umpir.ump.edu.my/id/eprint/22317/
https://doi.org/10.1111/cbdd.13404
https://doi.org/10.1111/cbdd.13404
_version_ 1643669350296584192
score 13.211869

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