Treatment with a Combination of Metformin and 2-Deoxyglucose Upregulates Thrombospondin-1 in Microvascular Endothelial Cells: Implications in Anti-Angiogenic Cancer Therapy

<p dir="ltr">Metformin, the most widely used anti-diabetic drug, also exhibits anti-cancer properties; however, the true potential of metformin as an anticancer drug remains largely unknown. In this study using mouse microvascular endothelial cells (MMECs), we investigated the effect...

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Main Author: Samson Mathews Samuel (18808246) (author)
Other Authors: Noothan Jyothi Satheesh (18808249) (author), Suparna Ghosh (9698402) (author), Dietrich Büsselberg (11008857) (author), Yasser Majeed (9417974) (author), Hong Ding (135247) (author), Chris R. Triggle (4278688) (author)
Published: 2019
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author Samson Mathews Samuel (18808246)
author2 Noothan Jyothi Satheesh (18808249)
Suparna Ghosh (9698402)
Dietrich Büsselberg (11008857)
Yasser Majeed (9417974)
Hong Ding (135247)
Chris R. Triggle (4278688)
author2_role author
author
author
author
author
author
author_facet Samson Mathews Samuel (18808246)
Noothan Jyothi Satheesh (18808249)
Suparna Ghosh (9698402)
Dietrich Büsselberg (11008857)
Yasser Majeed (9417974)
Hong Ding (135247)
Chris R. Triggle (4278688)
author_role author
dc.creator.none.fl_str_mv Samson Mathews Samuel (18808246)
Noothan Jyothi Satheesh (18808249)
Suparna Ghosh (9698402)
Dietrich Büsselberg (11008857)
Yasser Majeed (9417974)
Hong Ding (135247)
Chris R. Triggle (4278688)
dc.date.none.fl_str_mv 2019-11-06T03:00:00Z
dc.identifier.none.fl_str_mv 10.3390/cancers11111737
dc.relation.none.fl_str_mv https://figshare.com/articles/journal_contribution/Treatment_with_a_Combination_of_Metformin_and_2-Deoxyglucose_Upregulates_Thrombospondin-1_in_Microvascular_Endothelial_Cells_Implications_in_Anti-Angiogenic_Cancer_Therapy/26019433
dc.rights.none.fl_str_mv CC BY 4.0
info:eu-repo/semantics/openAccess
dc.subject.none.fl_str_mv Biomedical and clinical sciences
Oncology and carcinogenesis
Pharmacology and pharmaceutical sciences
angiogenesis
cancer
combination therapy
metformin
organic cation transporter (OCT)
tumor endothelial cells
dc.title.none.fl_str_mv Treatment with a Combination of Metformin and 2-Deoxyglucose Upregulates Thrombospondin-1 in Microvascular Endothelial Cells: Implications in Anti-Angiogenic Cancer Therapy
dc.type.none.fl_str_mv Text
Journal contribution
info:eu-repo/semantics/publishedVersion
text
contribution to journal
description <p dir="ltr">Metformin, the most widely used anti-diabetic drug, also exhibits anti-cancer properties; however, the true potential of metformin as an anticancer drug remains largely unknown. In this study using mouse microvascular endothelial cells (MMECs), we investigated the effects of metformin alone or in combination with the glycolytic inhibitor, 2-deoxyglucose (2DG), on angiogenesis-a process known to be an integral part of tumor growth, cancer cell survival and metastasis. MMECs were exposed to 2DG (1–10 mM) for 48 h in the absence or presence of metformin (2 mM). The status of angiogenic and anti-angiogenic marker proteins, proteins of the mTOR pathway and cell-cycle-related proteins were quantified by Western blot analysis. Assays for cell proliferation, migration and tubulogenesis were also performed. We observed robust up-regulation of anti-angiogenic thrombospondin-1 (TSP1) and increased TSP1-CD36 co-localization with a marked decrease in the levels of phosphorylated vascular endothelial growth factor receptor-2 (pVEGFR2; Y1175) in 2DG (5 mM) exposed cells treated with metformin (2 mM). Additionally, treatment with metformin and 2DG (5 mM) inhibited the Akt/mTOR pathway and down-regulated the cell-cycle-related proteins such as p-cyclin B1 (S147) and cyclins D1 and D2 when compared to cells that were treated with either 2DG or metformin alone. Treatment with a combination of 2DG (5 mM) and metformin (2 mM) also significantly decreased cell proliferation, migration and tubulogenic capacity when compared to cells that were treated with either 2DG or metformin alone. The up-regulation of TSP1, inhibition of cell proliferation, migration and tubulogenesis provides support to the argument that the combination of metformin and 2DG may prove to be an appropriate anti-proliferative and anti-angiogenic therapeutic strategy for the treatment of some cancers.</p><h2>Other Information</h2><p dir="ltr">Published in: Cancers<br>License: <a href="https://creativecommons.org/licenses/by/4.0/" target="_blank">https://creativecommons.org/licenses/by/4.0/</a><br>See article on publisher's website: <a href="https://dx.doi.org/10.3390/cancers11111737" target="_blank">https://dx.doi.org/10.3390/cancers11111737</a></p>
eu_rights_str_mv openAccess
id Manara2_073984cc8483bd112283b44da2c0dee4
identifier_str_mv 10.3390/cancers11111737
network_acronym_str Manara2
network_name_str Manara2
oai_identifier_str oai:figshare.com:article/26019433
publishDate 2019
repository.mail.fl_str_mv
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rights_invalid_str_mv CC BY 4.0
spelling Treatment with a Combination of Metformin and 2-Deoxyglucose Upregulates Thrombospondin-1 in Microvascular Endothelial Cells: Implications in Anti-Angiogenic Cancer TherapySamson Mathews Samuel (18808246)Noothan Jyothi Satheesh (18808249)Suparna Ghosh (9698402)Dietrich Büsselberg (11008857)Yasser Majeed (9417974)Hong Ding (135247)Chris R. Triggle (4278688)Biomedical and clinical sciencesOncology and carcinogenesisPharmacology and pharmaceutical sciencesangiogenesiscancercombination therapymetforminorganic cation transporter (OCT)tumor endothelial cells<p dir="ltr">Metformin, the most widely used anti-diabetic drug, also exhibits anti-cancer properties; however, the true potential of metformin as an anticancer drug remains largely unknown. In this study using mouse microvascular endothelial cells (MMECs), we investigated the effects of metformin alone or in combination with the glycolytic inhibitor, 2-deoxyglucose (2DG), on angiogenesis-a process known to be an integral part of tumor growth, cancer cell survival and metastasis. MMECs were exposed to 2DG (1–10 mM) for 48 h in the absence or presence of metformin (2 mM). The status of angiogenic and anti-angiogenic marker proteins, proteins of the mTOR pathway and cell-cycle-related proteins were quantified by Western blot analysis. Assays for cell proliferation, migration and tubulogenesis were also performed. We observed robust up-regulation of anti-angiogenic thrombospondin-1 (TSP1) and increased TSP1-CD36 co-localization with a marked decrease in the levels of phosphorylated vascular endothelial growth factor receptor-2 (pVEGFR2; Y1175) in 2DG (5 mM) exposed cells treated with metformin (2 mM). Additionally, treatment with metformin and 2DG (5 mM) inhibited the Akt/mTOR pathway and down-regulated the cell-cycle-related proteins such as p-cyclin B1 (S147) and cyclins D1 and D2 when compared to cells that were treated with either 2DG or metformin alone. Treatment with a combination of 2DG (5 mM) and metformin (2 mM) also significantly decreased cell proliferation, migration and tubulogenic capacity when compared to cells that were treated with either 2DG or metformin alone. The up-regulation of TSP1, inhibition of cell proliferation, migration and tubulogenesis provides support to the argument that the combination of metformin and 2DG may prove to be an appropriate anti-proliferative and anti-angiogenic therapeutic strategy for the treatment of some cancers.</p><h2>Other Information</h2><p dir="ltr">Published in: Cancers<br>License: <a href="https://creativecommons.org/licenses/by/4.0/" target="_blank">https://creativecommons.org/licenses/by/4.0/</a><br>See article on publisher's website: <a href="https://dx.doi.org/10.3390/cancers11111737" target="_blank">https://dx.doi.org/10.3390/cancers11111737</a></p>2019-11-06T03:00:00ZTextJournal contributioninfo:eu-repo/semantics/publishedVersiontextcontribution to journal10.3390/cancers11111737https://figshare.com/articles/journal_contribution/Treatment_with_a_Combination_of_Metformin_and_2-Deoxyglucose_Upregulates_Thrombospondin-1_in_Microvascular_Endothelial_Cells_Implications_in_Anti-Angiogenic_Cancer_Therapy/26019433CC BY 4.0info:eu-repo/semantics/openAccessoai:figshare.com:article/260194332019-11-06T03:00:00Z
spellingShingle Treatment with a Combination of Metformin and 2-Deoxyglucose Upregulates Thrombospondin-1 in Microvascular Endothelial Cells: Implications in Anti-Angiogenic Cancer Therapy
Samson Mathews Samuel (18808246)
Biomedical and clinical sciences
Oncology and carcinogenesis
Pharmacology and pharmaceutical sciences
angiogenesis
cancer
combination therapy
metformin
organic cation transporter (OCT)
tumor endothelial cells
status_str publishedVersion
title Treatment with a Combination of Metformin and 2-Deoxyglucose Upregulates Thrombospondin-1 in Microvascular Endothelial Cells: Implications in Anti-Angiogenic Cancer Therapy
title_full Treatment with a Combination of Metformin and 2-Deoxyglucose Upregulates Thrombospondin-1 in Microvascular Endothelial Cells: Implications in Anti-Angiogenic Cancer Therapy
title_fullStr Treatment with a Combination of Metformin and 2-Deoxyglucose Upregulates Thrombospondin-1 in Microvascular Endothelial Cells: Implications in Anti-Angiogenic Cancer Therapy
title_full_unstemmed Treatment with a Combination of Metformin and 2-Deoxyglucose Upregulates Thrombospondin-1 in Microvascular Endothelial Cells: Implications in Anti-Angiogenic Cancer Therapy
title_short Treatment with a Combination of Metformin and 2-Deoxyglucose Upregulates Thrombospondin-1 in Microvascular Endothelial Cells: Implications in Anti-Angiogenic Cancer Therapy
title_sort Treatment with a Combination of Metformin and 2-Deoxyglucose Upregulates Thrombospondin-1 in Microvascular Endothelial Cells: Implications in Anti-Angiogenic Cancer Therapy
topic Biomedical and clinical sciences
Oncology and carcinogenesis
Pharmacology and pharmaceutical sciences
angiogenesis
cancer
combination therapy
metformin
organic cation transporter (OCT)
tumor endothelial cells