A novel isoquinoline derivative anticancer agent and its targeted delivery to tumor cells using transferrin-conjugated liposomes

Xuewei Yang; Shuang Yang; Hongyu Chai; Zhaogang Yang; Robert J. Lee; Weiwei Liao; Lesheng Teng

doi:10.1371/journal.pone.0136649

A novel isoquinoline derivative anticancer agent and its targeted delivery to tumor cells using transferrin-conjugated liposomes

Xuewei Yang, Shuang Yang, Hongyu Chai, Zhaogang Yang, Robert J. Lee, Weiwei Liao, Lesheng Teng

Research output: Contribution to journal › Article › peer-review

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Abstract

We have screened 11 isoquinoline derivatives and α-methylene-?-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.

Original language	English (US)
Article number	e0136649.
Journal	PloS one
Volume	10
Issue number	8
DOIs	https://doi.org/10.1371/journal.pone.0136649
State	Published - Aug 26 2015
Externally published	Yes

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title = "A novel isoquinoline derivative anticancer agent and its targeted delivery to tumor cells using transferrin-conjugated liposomes",

abstract = "We have screened 11 isoquinoline derivatives and α-methylene-?-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.",

author = "Xuewei Yang and Shuang Yang and Hongyu Chai and Zhaogang Yang and Lee, {Robert J.} and Weiwei Liao and Lesheng Teng",

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AU - Yang, Xuewei

AU - Yang, Shuang

AU - Chai, Hongyu

AU - Yang, Zhaogang

AU - Lee, Robert J.

AU - Liao, Weiwei

AU - Teng, Lesheng

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AB - We have screened 11 isoquinoline derivatives and α-methylene-?-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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A novel isoquinoline derivative anticancer agent and its targeted delivery to tumor cells using transferrin-conjugated liposomes

Abstract

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