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Cassaine Diterpenoid Amide from Stem Bark of Erythrophleum fordii Suppresses Cytotoxic and Induces Apoptosis of Human Leukemia Cells
Cassaine diterpenoids amides from the stem bark of Vietnamese Erythrophleum fordii Oliver were screened for their cytotoxic activity against human cancer cells. The cell proliferation assay results showed that, among the active compounds, 3β-acetyl-nor-erythrophlamide (3AEP) exhibited the most poten...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7397343/ https://www.ncbi.nlm.nih.gov/pubmed/32708204 http://dx.doi.org/10.3390/molecules25143304 |
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author | Nguyen, Tu Thanh Thi To, Dao Cuong Vo, Phuong Hien Thi Tran, Thanh Hoa Nguyen, Phi Hung Nguyen, Hien Minh Tran, Manh Hung |
author_facet | Nguyen, Tu Thanh Thi To, Dao Cuong Vo, Phuong Hien Thi Tran, Thanh Hoa Nguyen, Phi Hung Nguyen, Hien Minh Tran, Manh Hung |
author_sort | Nguyen, Tu Thanh Thi |
collection | PubMed |
description | Cassaine diterpenoids amides from the stem bark of Vietnamese Erythrophleum fordii Oliver were screened for their cytotoxic activity against human cancer cells. The cell proliferation assay results showed that, among the active compounds, 3β-acetyl-nor-erythrophlamide (3AEP) exhibited the most potential cytotoxicity against human leukemia HL-60 and KG cells with IC(50) values of 12.0 ± 1.2 and 18.1 ± 2.7 µM, respectively. Treatment of 3AEP resulted in the apoptosis of HL-60 cells via the activation of caspase 3, and poly (ADP-ribose) polymerase (PARP). Molecular docking in silico results showed that the 3AEP can bind to both the procaspase-3 allosteric site and the PARP-1 active site, with binding energies of −7.51 and −9.63 kcal/mol respectively. These results indicated that the stem bark of Vietnamese E. fordii and its cassaine diterpenoid amides may be useful in the apoptosis induction of human leukemia cancer cells. |
format | Online Article Text |
id | pubmed-7397343 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-73973432020-08-16 Cassaine Diterpenoid Amide from Stem Bark of Erythrophleum fordii Suppresses Cytotoxic and Induces Apoptosis of Human Leukemia Cells Nguyen, Tu Thanh Thi To, Dao Cuong Vo, Phuong Hien Thi Tran, Thanh Hoa Nguyen, Phi Hung Nguyen, Hien Minh Tran, Manh Hung Molecules Article Cassaine diterpenoids amides from the stem bark of Vietnamese Erythrophleum fordii Oliver were screened for their cytotoxic activity against human cancer cells. The cell proliferation assay results showed that, among the active compounds, 3β-acetyl-nor-erythrophlamide (3AEP) exhibited the most potential cytotoxicity against human leukemia HL-60 and KG cells with IC(50) values of 12.0 ± 1.2 and 18.1 ± 2.7 µM, respectively. Treatment of 3AEP resulted in the apoptosis of HL-60 cells via the activation of caspase 3, and poly (ADP-ribose) polymerase (PARP). Molecular docking in silico results showed that the 3AEP can bind to both the procaspase-3 allosteric site and the PARP-1 active site, with binding energies of −7.51 and −9.63 kcal/mol respectively. These results indicated that the stem bark of Vietnamese E. fordii and its cassaine diterpenoid amides may be useful in the apoptosis induction of human leukemia cancer cells. MDPI 2020-07-21 /pmc/articles/PMC7397343/ /pubmed/32708204 http://dx.doi.org/10.3390/molecules25143304 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Nguyen, Tu Thanh Thi To, Dao Cuong Vo, Phuong Hien Thi Tran, Thanh Hoa Nguyen, Phi Hung Nguyen, Hien Minh Tran, Manh Hung Cassaine Diterpenoid Amide from Stem Bark of Erythrophleum fordii Suppresses Cytotoxic and Induces Apoptosis of Human Leukemia Cells |
title | Cassaine Diterpenoid Amide from Stem Bark of Erythrophleum fordii Suppresses Cytotoxic and Induces Apoptosis of Human Leukemia Cells |
title_full | Cassaine Diterpenoid Amide from Stem Bark of Erythrophleum fordii Suppresses Cytotoxic and Induces Apoptosis of Human Leukemia Cells |
title_fullStr | Cassaine Diterpenoid Amide from Stem Bark of Erythrophleum fordii Suppresses Cytotoxic and Induces Apoptosis of Human Leukemia Cells |
title_full_unstemmed | Cassaine Diterpenoid Amide from Stem Bark of Erythrophleum fordii Suppresses Cytotoxic and Induces Apoptosis of Human Leukemia Cells |
title_short | Cassaine Diterpenoid Amide from Stem Bark of Erythrophleum fordii Suppresses Cytotoxic and Induces Apoptosis of Human Leukemia Cells |
title_sort | cassaine diterpenoid amide from stem bark of erythrophleum fordii suppresses cytotoxic and induces apoptosis of human leukemia cells |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7397343/ https://www.ncbi.nlm.nih.gov/pubmed/32708204 http://dx.doi.org/10.3390/molecules25143304 |
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