Redox-responsive chemosensitive polyspermine delivers ursolic acid targeting to human breast tumor cells: The depletion of intracellular GSH contents arouses chemosensitizing effects

被引：9

作者：

Ji, Xin ^{[1
]}

Tang, Qiao ^{[1
]}

Pang, Peng ^{[4
]}

Wu, Jianping ^{[2
]}

Kirk, Thomas Brett ^{[2
]}

Xu, Jiake ^{[3
]}

Ma, Dong ^{[1
]}

Xue, Wei ^{[1
]}

机构：

[1] Jinan Univ, Dept Biomed Engn, Key Lab Biomat Guangdong Higher Educ Inst, Guangzhou 510632, Guangdong, Peoples R China

[2] Curtin Univ, Dept Mech Engn, Imaging & Bioengn Lab 3D, Bentley, WA, Australia

[3] Univ Western Australia, Sch Pathol & Lab Med, Perth, WA, Australia

[4] Jinan Univ, Coll Tradit Chinese Med, Guangzhou 510632, Guangdong, Peoples R China

来源：

COLLOIDS AND SURFACES B-BIOINTERFACES | 2018年 / 170卷

关键词：

Polymeric prodrug; Chemosensitivity; Ursolic acid; Targeted delivery; Cancer therapy; DRUG-DELIVERY; CANCER-THERAPY; IN-VITRO; CO-DELIVERY; NANOPARTICLES; RESISTANCE; METASTASIS; COPOLYMER; APOPTOSIS; MICELLES;

D O I：

10.1016/j.colsurfb.2018.06.029

中图分类号：

Q6 [生物物理学];

学科分类号：

071011 ;

摘要：

Antitumor efficacy of ursolic acid (UA) is seriously limited due to its low hydrophilicity and needy bioavail-ability. To overcome these obstacles, chemosensitive polyspermine (CPSP) conjugated with UA and folic acid (FA) as a novel targeted prodrug was designed and successfully synthesized in this investigation. This prodrug not only showed high aqueous solubility, GSH-triggered degradation and good biocompatibility, but also exhibited better inhibition effect on the tumor cells proliferation in comparison with free UA. FA-CPSP-UA could down-regulate the generation of GSH and manifest excellent ability in enhancing antitumor efficacy. In addition, FA-CPSP-UA could inhibit the expression of MMP-9, which led to restricting MCF-7 cells migration. Taken together, the results indicated that FA-CPSP-UA, as a carrier, can efficiently deliver UA to folate receptor positive cancer cells and improve tumor therapy of UA by Chemosensitive effect.

引用

页码：293 / 302

页数：10

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