Cytotoxic effects of natural and semisynthetic cucurbitacins on lung cancer cell line A549
Summary: Cucurbitacins and their derivatives are triterpenoids that are found in various plant families, and are known for their pharmacological and biological activities, including anti-cancer effects. Lung cancer represents a major public health problem, with non-small-cell lung cancer (NSCLC) bei...
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2016
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Acceso en línea: | https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_01676997_v34_n2_p139_Silva http://hdl.handle.net/20.500.12110/paper_01676997_v34_n2_p139_Silva |
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paper:paper_01676997_v34_n2_p139_Silva2023-06-08T15:16:47Z Cytotoxic effects of natural and semisynthetic cucurbitacins on lung cancer cell line A549 Apoptosis Cucurbitacins Invasion Metastasis 2 deoxy 2 bromocucurbitacin B 2,16 diacetyl cucurbitacin B 22 deoxy 22 hydroxy 25 deacetoxy cucurbitacin B caspase cucurbitacin cucurbitacin B cyclin B1 focal adhesion kinase gelatinase A gelatinase B mitogen activated protein kinase paclitaxel unclassified drug caspase cucurbitacin cyclin B1 focal adhesion kinase gelatinase A gelatinase B tumor necrosis factor A549 cell line apoptosis Article cancer inhibition cell cycle arrest cell cycle G2 phase cell cycle M phase cell cycle progression cell migration cell proliferation controlled study down regulation drug cytotoxicity drug structure enzyme activation human human cell IC50 in vitro study lung cancer lung metastasis priority journal protein expression signal transduction A-549 cell line cell cycle checkpoint cell motion chemistry drug effects enzymology Lung Neoplasms metabolism non small cell lung cancer pathology phosphorylation tumor invasion A549 Cells Apoptosis Carcinoma, Non-Small-Cell Lung Caspases Cell Cycle Checkpoints Cell Movement Cell Proliferation Cucurbitacins Cyclin B1 Down-Regulation Focal Adhesion Protein-Tyrosine Kinases Humans Lung Neoplasms Matrix Metalloproteinase 2 Matrix Metalloproteinase 9 Neoplasm Invasiveness Phosphorylation Signal Transduction Tumor Necrosis Factor-alpha Summary: Cucurbitacins and their derivatives are triterpenoids that are found in various plant families, and are known for their pharmacological and biological activities, including anti-cancer effects. Lung cancer represents a major public health problem, with non-small-cell lung cancer (NSCLC) being the most frequent and aggressive type of lung cancer. The objective of this work was to evaluate four cucurbitacins (CUCs) for their cytotoxic activity, effects on apoptosis induction, cell cycle progression, anti-migratory, and anti-invasive effects on the human NSCLC cell line (A549 cells). Our findings showed that these CUCs could suppress human NSCLC cell growth in vitro through their effects on the PI3Kinase and MAPK pathways, which lead to programmed cell death induction, as well as inhibition of cell migration and cell invasion. Additionally, these effects culminate in apoptosis induction and G2/M cell cycle arrest by modulating cyclin B1 expression, and in the mitigation of strategic steps of lung cancer metastasis, including migration and invasion of A549 cells. These results suggest that two natural (DDCB and CB) and two novel semisynthetic derivatives of cucurbitacin B (ACB and DBCB) could be considered as promising compounds with antitumor potential. © 2016 Springer Science+Business Media New York. 2016 https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_01676997_v34_n2_p139_Silva http://hdl.handle.net/20.500.12110/paper_01676997_v34_n2_p139_Silva |
institution |
Universidad de Buenos Aires |
institution_str |
I-28 |
repository_str |
R-134 |
collection |
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) |
topic |
Apoptosis Cucurbitacins Invasion Metastasis 2 deoxy 2 bromocucurbitacin B 2,16 diacetyl cucurbitacin B 22 deoxy 22 hydroxy 25 deacetoxy cucurbitacin B caspase cucurbitacin cucurbitacin B cyclin B1 focal adhesion kinase gelatinase A gelatinase B mitogen activated protein kinase paclitaxel unclassified drug caspase cucurbitacin cyclin B1 focal adhesion kinase gelatinase A gelatinase B tumor necrosis factor A549 cell line apoptosis Article cancer inhibition cell cycle arrest cell cycle G2 phase cell cycle M phase cell cycle progression cell migration cell proliferation controlled study down regulation drug cytotoxicity drug structure enzyme activation human human cell IC50 in vitro study lung cancer lung metastasis priority journal protein expression signal transduction A-549 cell line cell cycle checkpoint cell motion chemistry drug effects enzymology Lung Neoplasms metabolism non small cell lung cancer pathology phosphorylation tumor invasion A549 Cells Apoptosis Carcinoma, Non-Small-Cell Lung Caspases Cell Cycle Checkpoints Cell Movement Cell Proliferation Cucurbitacins Cyclin B1 Down-Regulation Focal Adhesion Protein-Tyrosine Kinases Humans Lung Neoplasms Matrix Metalloproteinase 2 Matrix Metalloproteinase 9 Neoplasm Invasiveness Phosphorylation Signal Transduction Tumor Necrosis Factor-alpha |
spellingShingle |
Apoptosis Cucurbitacins Invasion Metastasis 2 deoxy 2 bromocucurbitacin B 2,16 diacetyl cucurbitacin B 22 deoxy 22 hydroxy 25 deacetoxy cucurbitacin B caspase cucurbitacin cucurbitacin B cyclin B1 focal adhesion kinase gelatinase A gelatinase B mitogen activated protein kinase paclitaxel unclassified drug caspase cucurbitacin cyclin B1 focal adhesion kinase gelatinase A gelatinase B tumor necrosis factor A549 cell line apoptosis Article cancer inhibition cell cycle arrest cell cycle G2 phase cell cycle M phase cell cycle progression cell migration cell proliferation controlled study down regulation drug cytotoxicity drug structure enzyme activation human human cell IC50 in vitro study lung cancer lung metastasis priority journal protein expression signal transduction A-549 cell line cell cycle checkpoint cell motion chemistry drug effects enzymology Lung Neoplasms metabolism non small cell lung cancer pathology phosphorylation tumor invasion A549 Cells Apoptosis Carcinoma, Non-Small-Cell Lung Caspases Cell Cycle Checkpoints Cell Movement Cell Proliferation Cucurbitacins Cyclin B1 Down-Regulation Focal Adhesion Protein-Tyrosine Kinases Humans Lung Neoplasms Matrix Metalloproteinase 2 Matrix Metalloproteinase 9 Neoplasm Invasiveness Phosphorylation Signal Transduction Tumor Necrosis Factor-alpha Cytotoxic effects of natural and semisynthetic cucurbitacins on lung cancer cell line A549 |
topic_facet |
Apoptosis Cucurbitacins Invasion Metastasis 2 deoxy 2 bromocucurbitacin B 2,16 diacetyl cucurbitacin B 22 deoxy 22 hydroxy 25 deacetoxy cucurbitacin B caspase cucurbitacin cucurbitacin B cyclin B1 focal adhesion kinase gelatinase A gelatinase B mitogen activated protein kinase paclitaxel unclassified drug caspase cucurbitacin cyclin B1 focal adhesion kinase gelatinase A gelatinase B tumor necrosis factor A549 cell line apoptosis Article cancer inhibition cell cycle arrest cell cycle G2 phase cell cycle M phase cell cycle progression cell migration cell proliferation controlled study down regulation drug cytotoxicity drug structure enzyme activation human human cell IC50 in vitro study lung cancer lung metastasis priority journal protein expression signal transduction A-549 cell line cell cycle checkpoint cell motion chemistry drug effects enzymology Lung Neoplasms metabolism non small cell lung cancer pathology phosphorylation tumor invasion A549 Cells Apoptosis Carcinoma, Non-Small-Cell Lung Caspases Cell Cycle Checkpoints Cell Movement Cell Proliferation Cucurbitacins Cyclin B1 Down-Regulation Focal Adhesion Protein-Tyrosine Kinases Humans Lung Neoplasms Matrix Metalloproteinase 2 Matrix Metalloproteinase 9 Neoplasm Invasiveness Phosphorylation Signal Transduction Tumor Necrosis Factor-alpha |
description |
Summary: Cucurbitacins and their derivatives are triterpenoids that are found in various plant families, and are known for their pharmacological and biological activities, including anti-cancer effects. Lung cancer represents a major public health problem, with non-small-cell lung cancer (NSCLC) being the most frequent and aggressive type of lung cancer. The objective of this work was to evaluate four cucurbitacins (CUCs) for their cytotoxic activity, effects on apoptosis induction, cell cycle progression, anti-migratory, and anti-invasive effects on the human NSCLC cell line (A549 cells). Our findings showed that these CUCs could suppress human NSCLC cell growth in vitro through their effects on the PI3Kinase and MAPK pathways, which lead to programmed cell death induction, as well as inhibition of cell migration and cell invasion. Additionally, these effects culminate in apoptosis induction and G2/M cell cycle arrest by modulating cyclin B1 expression, and in the mitigation of strategic steps of lung cancer metastasis, including migration and invasion of A549 cells. These results suggest that two natural (DDCB and CB) and two novel semisynthetic derivatives of cucurbitacin B (ACB and DBCB) could be considered as promising compounds with antitumor potential. © 2016 Springer Science+Business Media New York. |
title |
Cytotoxic effects of natural and semisynthetic cucurbitacins on lung cancer cell line A549 |
title_short |
Cytotoxic effects of natural and semisynthetic cucurbitacins on lung cancer cell line A549 |
title_full |
Cytotoxic effects of natural and semisynthetic cucurbitacins on lung cancer cell line A549 |
title_fullStr |
Cytotoxic effects of natural and semisynthetic cucurbitacins on lung cancer cell line A549 |
title_full_unstemmed |
Cytotoxic effects of natural and semisynthetic cucurbitacins on lung cancer cell line A549 |
title_sort |
cytotoxic effects of natural and semisynthetic cucurbitacins on lung cancer cell line a549 |
publishDate |
2016 |
url |
https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_01676997_v34_n2_p139_Silva http://hdl.handle.net/20.500.12110/paper_01676997_v34_n2_p139_Silva |
_version_ |
1768544175433711616 |