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  • Polymer and Materials Science  (2)
  • cancer  (1)
  • 1
    ISSN: 1573-904X
    Keywords: block copolymer ; cancer ; multidrug resistance ; Pluronic
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. Using monolayers of human pancreatic adenocarcinoma cells (Panc-1) that express multidrug resistance-associated protein (MRP), the present work investigates the effects of Pluronic block copolymers on the functional activity of MRP. Methods. The studies examined the accumulation and efflux of the MRP selective probe fluorescein (FLU) in Panc-1 cell monolayers with and without Pluronic P85 (P85), Pluronic L81 (L81) and Pluronic F108 (F108). Results. Treatment of Panc-1 cells with P85 resulted in concentration-dependent increases in FLU accumulation and elimination of FLU sequestration in vesicular compartments in these cells. The effects of P85 were selective for FLU in the Panc-1 cell monolayers. Inhibition of MRP-mediated transport was dependent on the composition of Pluronic block copolymer: the more hydrophobic copolymer had the greater effect on FLU uptake in Panc-1 monolayers (L81 〉 P85 〉 F108). Conclusions. This paper demonstrates for the first time that Pluronic block copolymers inhibit multidrug resistance-associated protein (MRP). The similarities in the effects of Pluronic block copolymers on MRP and P-glycoprotein drug efflux systems suggest that a single unifying mechanism may explain the inhibition observed.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    New York : Wiley-Blackwell
    Die Makromolekulare Chemie 191 (1990), S. 2801-2814 
    ISSN: 0025-116X
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Physics
    Notes: Being solubilized in systems of reversed micelles of a surfactant, the macromolecules incorporate into the inner cavities of the micelles, whose size can be changed by varying the degree of hydration, w0 = [H2O]/[surfactant]. The conjugates of proteins (α-chymotrypsin, bovine serum albumin (BSA), monoclonal antibodies to insulin) with linear polyelectrolytes (poly(methacrylic acid), quaternized poly(4-vinylpyridine)) are synthesized in reversed micelles of Aerosol OT (sodium bis(2-ethylhexyl)sulfosuccinate) in the octane with 100% yield. The yield critically depends on the degree of hydration: the reaction does not proceed at low w0, but if w0 exceeds a threshold value (which differs for various macromolecules) the yield increases sharply and reaches 100%. Using the ultracentrifugation it was demonstrated that at low w0 the polyelectrolyte represents a compact globule compressed by the micellar matrix in the inner cavity of a micelle. Under these conditions, there is no space for the protein in a micelle which contains polyelectrolyte, and therefore reaction does not proceed. If w0 exceeds a threshold value the micelles become large enough to entrap the conjugated macromolecules simultaneously. The possibility of regulation of the conjugate composition by variation of w0 (via the size of the micellar matrix) was demonstrated by a conjugate of BSA with quaternized poly(4-vinylpyridine).
    Additional Material: 7 Ill.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 0006-3525
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: A tool was developed for enhancement of plasmid penetration into an intact cell, based on increasing DNA hydrophobicity via inclusion into a soluble interpolyelectrolyte complex (IPC) with polycations. The characteristics of formation of DNA IPC with synthetic polycations [poly(N-ethyl-4-vinylpyridinium)bromide (PVP) and PVP modified with 3% of N-cetyl-4-vinylpyridinium units (PVP-C)] were studied using ultracentrifugation and polyacrylamide gel electrophoresis methods. The conditions were established under which the mixing of DNA and polycation aqueous solutions results in the selfassembly of soluble IPC species. Incorporation of DNA into IPC results in the enhancement of DNA binding with isolated Bacillus subtilis membranes. A considerable increase in the efficiency of transformation of B. subtilis cells with pBC16 plasmid resulted from incorporation of the plasmid into the IPC with PVP and CVP.
    Additional Material: 6 Ill.
    Type of Medium: Electronic Resource
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