6533b86ffe1ef96bd12cd4f9
RESEARCH PRODUCT
Cytotoxicity and chemosensitizing activity of amphiphilic poly(glycerol)-poly(alkylene oxide) block copolymers.
Nikolay S. Melik-nubarovHolger FreyT. V. DeminaGennadii A. BadunJörg NieberleSophie S. MüllerOlga A. BudkinaI. D. Grozdovasubject
GlycerolPolymers and PlasticsCell SurvivalPolymersBioengineeringAntineoplastic AgentsMicellePolyethylene GlycolsBiomaterialschemistry.chemical_compoundInhibitory Concentration 50Polymer chemistryAmphiphilePEG ratioMaterials ChemistryCopolymerHumansATP Binding Cassette Transporter Subfamily B Member 1CytotoxicityMicelleschemistry.chemical_classificationDrug SynergismPolymerPoloxamerDrug Resistance MultiplechemistryDoxorubicinDrug Resistance NeoplasmMCF-7 CellsDrug Screening Assays AntitumorK562 CellsEthylene glycolHydrophobic and Hydrophilic Interactionsdescription
All polymeric chemosensitizers proposed thus far have a linear poly(ethylene glycol) (PEG) hydrophilic block. To testify whether precisely this chemical structure and architecture of the hydrophilic block is a prerequisite for chemosensitization, we tested a series of novel block copolymers containing a hyperbranched polyglycerol segment as a hydrophilic block (PPO-NG copolymers) on multi-drug-resistant (MDR) tumor cells in culture. PPO-NG copolymers inhibited MDR of three cell lines, indicating that the linear PEG can be substituted for a hyperbranched polyglycerol block without loss of the polymers' chemosensitizing activity. The extent of MDR reversal increased with the polymers affinity toward the cells and the expression level of P-glycoprotein. In contrast with Pluronic L61, which increases viability of tumor cells in the absence of drugs, PPO-NG chemosensitizers are completely devoid of this property undesired in cancer therapy, making them promising candidates for application as novel MDR reversal agents.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2014-06-14 | Biomacromolecules |