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 journalArticle

39 Citations (Scopus)

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 languageEnglish (US)
Article numbere0136649.
JournalPloS one
Volume10
Issue number8
DOIs
StatePublished - Aug 26 2015
Externally publishedYes

Fingerprint

isoquinolines
antineoplastic agents
transferrin
Transferrin
Liposomes
Antineoplastic Agents
Tumors
chemical derivatives
Cells
Derivatives
Danazol
Neoplasms
HEK293 Cells
Drug and Narcotic Control
Cytotoxicity
bromides
Bromides
cytotoxicity
Assays
drugs

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Agricultural and Biological Sciences(all)

Cite this

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.

In: PloS one, Vol. 10, No. 8, e0136649., 26.08.2015.

Research output: Contribution to journalArticle

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. In: PloS one. 2015 ; Vol. 10, No. 8.
@article{3af000c417e04340acd16e161e08fb22,
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",
year = "2015",
month = "8",
day = "26",
doi = "10.1371/journal.pone.0136649",
language = "English (US)",
volume = "10",
journal = "PLoS One",
issn = "1932-6203",
publisher = "Public Library of Science",
number = "8",

}

TY - JOUR

T1 - A novel isoquinoline derivative anticancer agent and its targeted delivery to tumor cells using transferrin-conjugated liposomes

AU - Yang, Xuewei

AU - Yang, Shuang

AU - Chai, Hongyu

AU - Yang, Zhaogang

AU - Lee, Robert J.

AU - Liao, Weiwei

AU - Teng, Lesheng

PY - 2015/8/26

Y1 - 2015/8/26

N2 - 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.

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.

UR - http://www.scopus.com/inward/record.url?scp=84943328017&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84943328017&partnerID=8YFLogxK

U2 - 10.1371/journal.pone.0136649

DO - 10.1371/journal.pone.0136649

M3 - Article

C2 - 26309138

AN - SCOPUS:84943328017

VL - 10

JO - PLoS One

JF - PLoS One

SN - 1932-6203

IS - 8

M1 - e0136649.

ER -