A rapid synthetic route to a nontoxic fluorescently labeled water-soluble calixarene has been developed. Investigation of the cellular uptake of the labeled calixarene, via confocal microscopy, through coincubation with uptake inhibitors demonstrates that uptake is not through the common clathrin coated pits or caveolae (lipid raft) endocytic pathways and that the calixarene derivative localizes within the cytoplasm and does not enter the nucleus. The study demonstrates the power of fluorescent labeling for investigation of interactions between calixarenes and biological systems and the potential for calixarene based intracellular imaging agents
Vanadyl bearing calix[4]arene ligands have undergone evaluation against several cell lines, and show varying degrees of toxicity. For vanadyl complexed to a sulfonylcalix[4]arene, monitoring of the strong blue fluorescence revealed slow uptake kinetics. The complex is exclusively found in the cytoplasm of the cells and uptake is not due to active endocytotic mechanisms.
Summary Pleural effusion samples were obtained from 55 patients with malignant disease, including patients with primary lung cancers and those with a variety of other tumours metastatic to the pleura. The effusions were assayed for the presence of hepatocyte growth factor/scatter factor (HGF/SF), by both ELISA and bioassay. The presence of malignant cells in the effusions was also assessed. Detectable amounts of the factor, as judged by both criteria, were found in over 90% of all the effusions, including those from patients with a wide variety of carcinomas and also lymphomas. A wide range of HGF/SF levels were found for all tumour classes, some effusions containing high levels above 4 ng ml-. It is concluded that tumours within the pleura and adjacent lung tissue are usually exposed to biologically significant levels of HGF/SF.
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