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Berberine Derivatives Suppress Cellular Proliferation and Tumorigenesis In Vitro in Human Non-Small-Cell Lung Cancer Cells

Lung cancer is the leading cause of death in the world, and the most common type of lung cancer is non-small-cell lung cancer (NSCLC), accounting for 85% of lung cancer. Patients with NSCLC, when detected, are mostly in a metastatic stage, and over half of patients diagnosed with NSCLC die within on...

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Autores principales: Chang, Jia-Ming, Kam, Kam-Hong, Chao, Wen-Ying, Zhao, Pei-Wen, Chen, Shu-Hsin, Chung, Hui-Chen, Li, Yi-Zhen, Wu, Jin-Yi, Lee, Ying-Ray
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7352437/
https://www.ncbi.nlm.nih.gov/pubmed/32545770
http://dx.doi.org/10.3390/ijms21124218
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author Chang, Jia-Ming
Kam, Kam-Hong
Chao, Wen-Ying
Zhao, Pei-Wen
Chen, Shu-Hsin
Chung, Hui-Chen
Li, Yi-Zhen
Wu, Jin-Yi
Lee, Ying-Ray
author_facet Chang, Jia-Ming
Kam, Kam-Hong
Chao, Wen-Ying
Zhao, Pei-Wen
Chen, Shu-Hsin
Chung, Hui-Chen
Li, Yi-Zhen
Wu, Jin-Yi
Lee, Ying-Ray
author_sort Chang, Jia-Ming
collection PubMed
description Lung cancer is the leading cause of death in the world, and the most common type of lung cancer is non-small-cell lung cancer (NSCLC), accounting for 85% of lung cancer. Patients with NSCLC, when detected, are mostly in a metastatic stage, and over half of patients diagnosed with NSCLC die within one year after diagnosis; the 5-year survival rate is 24%. However, in patients with metastatic NSCLC, the 5-year survival rate is 6%. Therefore, development of a new therapeutic agent or strategy is urgent for NSCLCs. Berberine has been illustrated to be a therapeutic agent of NSCLC. In the present study, we synthesized six derivatives of berberine, and the anti-NSCLC activity of these agents was examined. Some of them exert increasing proliferation inhibition comparing with berberine. Further studies demonstrated that two of the most effective agents, 9-O-decylberberrubine bromide (B6) and 9-O-dodecylberberrubine bromide (B7), performed cell cycle regulation, in-vitro tumorigenesis inhibition and autophagic flux blocking, but not induction of cellular apoptosis in NSCLC cells. Moreover, B6 and B7 were determined to be green fluorescent and could be penetrated and localized in cellular mitochondria. Herein, B6 and B7, the berberine derivatives we synthesized, revealed better anti-NSCLC activity with berberine and may be used as therapeutic candidates for the treatment of NSCLCs.
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spelling pubmed-73524372020-07-15 Berberine Derivatives Suppress Cellular Proliferation and Tumorigenesis In Vitro in Human Non-Small-Cell Lung Cancer Cells Chang, Jia-Ming Kam, Kam-Hong Chao, Wen-Ying Zhao, Pei-Wen Chen, Shu-Hsin Chung, Hui-Chen Li, Yi-Zhen Wu, Jin-Yi Lee, Ying-Ray Int J Mol Sci Article Lung cancer is the leading cause of death in the world, and the most common type of lung cancer is non-small-cell lung cancer (NSCLC), accounting for 85% of lung cancer. Patients with NSCLC, when detected, are mostly in a metastatic stage, and over half of patients diagnosed with NSCLC die within one year after diagnosis; the 5-year survival rate is 24%. However, in patients with metastatic NSCLC, the 5-year survival rate is 6%. Therefore, development of a new therapeutic agent or strategy is urgent for NSCLCs. Berberine has been illustrated to be a therapeutic agent of NSCLC. In the present study, we synthesized six derivatives of berberine, and the anti-NSCLC activity of these agents was examined. Some of them exert increasing proliferation inhibition comparing with berberine. Further studies demonstrated that two of the most effective agents, 9-O-decylberberrubine bromide (B6) and 9-O-dodecylberberrubine bromide (B7), performed cell cycle regulation, in-vitro tumorigenesis inhibition and autophagic flux blocking, but not induction of cellular apoptosis in NSCLC cells. Moreover, B6 and B7 were determined to be green fluorescent and could be penetrated and localized in cellular mitochondria. Herein, B6 and B7, the berberine derivatives we synthesized, revealed better anti-NSCLC activity with berberine and may be used as therapeutic candidates for the treatment of NSCLCs. MDPI 2020-06-13 /pmc/articles/PMC7352437/ /pubmed/32545770 http://dx.doi.org/10.3390/ijms21124218 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
Chang, Jia-Ming
Kam, Kam-Hong
Chao, Wen-Ying
Zhao, Pei-Wen
Chen, Shu-Hsin
Chung, Hui-Chen
Li, Yi-Zhen
Wu, Jin-Yi
Lee, Ying-Ray
Berberine Derivatives Suppress Cellular Proliferation and Tumorigenesis In Vitro in Human Non-Small-Cell Lung Cancer Cells
title Berberine Derivatives Suppress Cellular Proliferation and Tumorigenesis In Vitro in Human Non-Small-Cell Lung Cancer Cells
title_full Berberine Derivatives Suppress Cellular Proliferation and Tumorigenesis In Vitro in Human Non-Small-Cell Lung Cancer Cells
title_fullStr Berberine Derivatives Suppress Cellular Proliferation and Tumorigenesis In Vitro in Human Non-Small-Cell Lung Cancer Cells
title_full_unstemmed Berberine Derivatives Suppress Cellular Proliferation and Tumorigenesis In Vitro in Human Non-Small-Cell Lung Cancer Cells
title_short Berberine Derivatives Suppress Cellular Proliferation and Tumorigenesis In Vitro in Human Non-Small-Cell Lung Cancer Cells
title_sort berberine derivatives suppress cellular proliferation and tumorigenesis in vitro in human non-small-cell lung cancer cells
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7352437/
https://www.ncbi.nlm.nih.gov/pubmed/32545770
http://dx.doi.org/10.3390/ijms21124218
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