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Combretastatin A-4 prodrug: A potent inhibitor of malignant hemangioendothelioma cell proliferation by A.S. Böhle; I. Leuschner; H. Kalthoff; D. Henne-Bruns is a Medicine article available to read on EtoBox.

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Anti-vascular treatment by targeting proliferating endothelial cells has become a promising option in anti-neoplastic therapy. Combretastatin A-4 prodrug (CA-4PD) has been identified as a selective inhibitor of endothelial cell proliferation, acting by the interruption of microtubule assembly. In this study, the effect of CA-4PD on proliferating endothelial cells derived from a primary tumor of the vascular endothelium was investigated in vitro and in vivo. In vitro, CA-4PD was an effective inhibitor of endothelial cell proliferation in a time-and dose-dependent manner, displaying a certain selectivity toward endothelial cells in comparison to proliferating fibroblasts. Analysis of DNA profiles by FACS revealed an increasing proportion of cells arrested in the G 2 cell-cycle phase with correlation to the duration of drug exposure. A decrease in cell viability correlated with duration of drug exposure, whereas FACS analysis, DNA fragmentation assay, and DNA gel electrophoresis failed to demonstrate that DNA fragmentation was indicative of apoptosis up to 48 hr of continued drug exposure. In vivo, CA-4PD induced excessive regressive alterations in experimentally allotransplanted hema

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Author

A.S. Böhle; I. Leuschner; H. Kalthoff; D. Henne-Bruns

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley; Research Square; Test accounts (ISSN 0020-7136)

Published

2000

Language

EN

Field

Medicine (Health Sciences)