Uptake of the carborane derivative of cholesteryl ester by glioma cancer cells is mediated through LDL receptors

This study was to elucidate the mechanism of cellular uptake of cholesteryl 1,12-dicarba-closo-dodecaboranel-carboxylate (BCH), a new anti-cancer carborane derivative of cholesteryl ester, by glioma cancer cells. BCH (solubilized with liposomal formulation) was incubated with SF-763 and SF-767 gliom...

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Veröffentlicht in:Pharmaceutical research 2004-07, Vol.21 (7), p.1257-1262
Hauptverfasser: Pan, Guangliang, Oie, Svein, Lu, D Robert
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Oie, Svein
Lu, D Robert
description This study was to elucidate the mechanism of cellular uptake of cholesteryl 1,12-dicarba-closo-dodecaboranel-carboxylate (BCH), a new anti-cancer carborane derivative of cholesteryl ester, by glioma cancer cells. BCH (solubilized with liposomal formulation) was incubated with SF-763 and SF-767 glioma cell lines in the presence of different amounts of monoclonal anti-LDL receptor antibody for cellular uptake studies. Various amounts of lipoprotein deficient serum (LPDS) were also used during the uptake. The effect of calcium ion and low temperature on BCH uptake were investigated. In addition, the transfer of BCH from liposomes to low-density lipoprotein (LDL) particles was determined through gradient ultracentrifugation. BCH uptake by these glioma cells was significantly inhibited by the monoclonal antibody. The uptake by both cell lines was reversely correlated with the amount of LPDS. The presence of calcium ion promoted the BCH uptake, whereas the low temperature decreased the BCH uptake. After 16 h incubation, about 46% of BCH was transferred from liposomes to LDL particles. These results strongly suggested that the cellular uptake of BCH (in liposomal formulation) by SF-763 and SF-767 glioma cell lines is mediated through LDL receptors.
doi_str_mv 10.1023/b:pham.0000033014.04820.a7
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source MEDLINE; Springer Nature - Complete Springer Journals
subjects Antibodies
Antibodies, Monoclonal - isolation & purification
Antibodies, Monoclonal - pharmacology
Boron Compounds - administration & dosage
Boron Compounds - pharmacokinetics
Brain cancer
Calcium - metabolism
Cancer therapies
Cell culture
Cell growth
Cell Line, Tumor
Cholesterol
Cholesterol Esters - administration & dosage
Cholesterol Esters - pharmacokinetics
Chromatography, High Pressure Liquid
Cold Temperature
Dose-Response Relationship, Drug
Electrophoresis, Polyacrylamide Gel
Glioma
Humans
Laboratories
Ligands
Lipoproteins
Lipoproteins, LDL - metabolism
Liposomes
Low density lipoprotein receptors
Receptors, LDL - antagonists & inhibitors
Receptors, LDL - physiology
title Uptake of the carborane derivative of cholesteryl ester by glioma cancer cells is mediated through LDL receptors
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