A Novel Isoquinoline Derivative Anticancer Agent and Its Targeted Delivery to Tumor Cells Using Transferrin-Conjugated Liposomes

We have screened 11 isoquinoline derivatives and α-methylene-γ-butyrolactones using the 3-(4,5-dimethylthi-azol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay in HeLa and HEK-293T cells. Compound 2 was identified as potential anticancer agent. To further improve its therapeutic poten...

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Detalles Bibliográficos
Autores principales: Yang, Xuewei, Yang, Shuang, Chai, Hongyu, Yang, Zhaogang, Lee, Robert J., Liao, Weiwei, Teng, Lesheng
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2015
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4550422/
https://www.ncbi.nlm.nih.gov/pubmed/26309138
http://dx.doi.org/10.1371/journal.pone.0136649
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author Yang, Xuewei
Yang, Shuang
Chai, Hongyu
Yang, Zhaogang
Lee, Robert J.
Liao, Weiwei
Teng, Lesheng
author_facet Yang, Xuewei
Yang, Shuang
Chai, Hongyu
Yang, Zhaogang
Lee, Robert J.
Liao, Weiwei
Teng, Lesheng
author_sort Yang, Xuewei
collection PubMed
description We have screened 11 isoquinoline derivatives and α-methylene-γ-butyrolactones using the 3-(4,5-dimethylthi-azol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay in HeLa and HEK-293T cells. Compound 2 was identified as potential anticancer agent. To further improve its therapeutic potential, this agent was incorporated into transferrin (Tf)-conjugated liposomes (LPs) for targeted delivery to tumor cells. We have demonstrated Tf-LP-Compound 2 have superior antitumor activity compared to non-targeted controls and the free drug. These data show Tf-LP-Compound 2 to be a promising agent that warrants further evaluation.
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spelling pubmed-45504222015-09-01 A Novel Isoquinoline Derivative Anticancer Agent and Its Targeted Delivery to Tumor Cells Using Transferrin-Conjugated Liposomes Yang, Xuewei Yang, Shuang Chai, Hongyu Yang, Zhaogang Lee, Robert J. Liao, Weiwei Teng, Lesheng PLoS One Research Article We have screened 11 isoquinoline derivatives and α-methylene-γ-butyrolactones using the 3-(4,5-dimethylthi-azol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay in HeLa and HEK-293T cells. Compound 2 was identified as potential anticancer agent. To further improve its therapeutic potential, this agent was incorporated into transferrin (Tf)-conjugated liposomes (LPs) for targeted delivery to tumor cells. We have demonstrated Tf-LP-Compound 2 have superior antitumor activity compared to non-targeted controls and the free drug. These data show Tf-LP-Compound 2 to be a promising agent that warrants further evaluation. Public Library of Science 2015-08-26 /pmc/articles/PMC4550422/ /pubmed/26309138 http://dx.doi.org/10.1371/journal.pone.0136649 Text en © 2015 Yang et al http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are properly credited.
spellingShingle Research Article
Yang, Xuewei
Yang, Shuang
Chai, Hongyu
Yang, Zhaogang
Lee, Robert J.
Liao, Weiwei
Teng, Lesheng
A Novel Isoquinoline Derivative Anticancer Agent and Its Targeted Delivery to Tumor Cells Using Transferrin-Conjugated Liposomes
title A Novel Isoquinoline Derivative Anticancer Agent and Its Targeted Delivery to Tumor Cells Using Transferrin-Conjugated Liposomes
title_full A Novel Isoquinoline Derivative Anticancer Agent and Its Targeted Delivery to Tumor Cells Using Transferrin-Conjugated Liposomes
title_fullStr A Novel Isoquinoline Derivative Anticancer Agent and Its Targeted Delivery to Tumor Cells Using Transferrin-Conjugated Liposomes
title_full_unstemmed A Novel Isoquinoline Derivative Anticancer Agent and Its Targeted Delivery to Tumor Cells Using Transferrin-Conjugated Liposomes
title_short A Novel Isoquinoline Derivative Anticancer Agent and Its Targeted Delivery to Tumor Cells Using Transferrin-Conjugated Liposomes
title_sort novel isoquinoline derivative anticancer agent and its targeted delivery to tumor cells using transferrin-conjugated liposomes
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4550422/
https://www.ncbi.nlm.nih.gov/pubmed/26309138
http://dx.doi.org/10.1371/journal.pone.0136649
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