Positive cooperativity in the cellular uptake of a boronated porphyrin

The International Journal of Biochemistry & Cell Biology
Sara NovickMichael R Quastel

Abstract

This work was undertaken to assess the kinetics of boronated porphyrin cellular uptake, which has been reported to occur by way of the low-density lipoprotein receptors. Because of current interest in the use of boronated porphyrins in boron neutron capture therapy of tumors, this pathway was investigated for the cellular uptake of a boronated porphyrin (tetrakis-carborane-carboxylate, esters of 2,4-bis (alpha,beta-dihydroxyethyl) deuteroporphyrin IX). Boron uptake occurred even without low-density lipoprotein in the culture medium. Pre-incubation of V-79 Chinese hamster cells for 24 h in medium containing delipidized fetal bovine serum markedly increased the subsequent uptake of boron when compared with cells pre-incubated with medium containing 10% fetal bovine serum. The increased uptake was characterized by greater affinity for boronated porphyrin, compared to cells pre-incubated in 10% fetal bovine serum. Twenty-four hour preincubation of cells with increasing concentrations of LDL added to delipidized medium suppressed the up-regulation of the boron level. In contrast, incubation with added acetylated LDL did not prevent the up-regulation of boron uptake. Positive cooperativity was demonstrated by Hill and Scatchard plots...Continue Reading

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Jan 5, 2008·Photochemistry and Photobiology·Slavka KascakovaDaniel Jancura
Jan 6, 2009·Bioorganic & Medicinal Chemistry·Valentina A Ol'shevskayaAlexander A Shtil

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