| Improved antitumoral properties of pure antiestrogen RU 58668-loaded liposomes in multiple myeloma. | |
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MedLine Citation:
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PMID: 16753295 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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In most of multiple myeloma (MM) cells, the "pure" antiestrogen (AE) RU 58668 (RU) induced either a G1-arrest (LP-1, OPM-2, NCI-H929, U266 cells) or apoptosis (RPMI 8226 cells). In RPMI 8226 cells, RU activates a caspase-dependent cell death pathway leading to the release of cytochrome c, the decrease of the essential MM survival factor Mcl-1, the cleavage of Bid and the activation of caspases-3 and -8. Incorporation of RU in pegylated cholesterol-containing liposomes allowed a controlled RU release, improving its anti-proliferative and apoptotic effects in cells. In RPMI 8226 xenografts, i.v. injected RU-liposomes but not free RU, exhibited antitumor activity. In vivo, RU-liposomes triggered the mitochondrial death pathway, concomitantly with a down-regulation of Mcl-1 and Bid cleavage. The decrease of CD34 immunoreactivity indicated a reduction of angiogenesis. The decrease of VEGF secretion in vitro supported a direct effect of RU on angiogenesis. These pro-apoptotic and antiangiogenic effects were explained by a prolonged exposure to the drug and to the endocytosis capacity of liposomes which might increase RU uptake and bypass a membrane export of free RU. Thus, these combined enhanced activities of RU-liposomes support that such a delivery of an AE may constitute a strategy of benefit for MM treatment. |
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Authors:
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Sébastien Maillard; Juliette Gauduchon; Véronique Marsaud; Fabrice Gouilleux; Elisabeth Connault; Paule Opolon; Elias Fattal; Brigitte Sola; Jack-Michel Renoir |
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Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't Date: 2006-06-05 |
Journal Detail:
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Title: The Journal of steroid biochemistry and molecular biology Volume: 100 ISSN: 0960-0760 ISO Abbreviation: J. Steroid Biochem. Mol. Biol. Publication Date: 2006 Jul |
Date Detail:
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Created Date: 2006-07-24 Completed Date: 2006-09-25 Revised Date: 2008-11-21 |
Medline Journal Info:
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Nlm Unique ID: 9015483 Medline TA: J Steroid Biochem Mol Biol Country: England |
Other Details:
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Languages: eng Pagination: 67-78 Citation Subset: IM |
Affiliation:
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CNRS UMR 8612, Université de Paris-Sud, Châtenay-Malabry, France. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Antineoplastic Agents / isolation & purification, pharmacology* Apoptosis / drug effects B-Lymphocytes / cytology, drug effects Cell Line, Tumor Cell Proliferation / drug effects Cells, Cultured Delayed-Action Preparations Drug Delivery Systems / methods Estradiol / analogs & derivatives*, isolation & purification, pharmacology Estrogen Antagonists / isolation & purification, pharmacology* Estrogen Receptor Modulators / administration & dosage, pharmacology* Female Humans Immunohistochemistry Liposomes* Mice Mice, Nude Models, Biological Multiple Myeloma / drug therapy*, pathology Palatine Tonsil / cytology Xenograft Model Antitumor Assays |
| Chemical | |
Reg. No./Substance:
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0/Antineoplastic Agents; 0/Delayed-Action Preparations; 0/Estrogen Antagonists; 0/Estrogen Receptor Modulators; 0/Liposomes; 151555-47-4/RU 58668; 50-28-2/Estradiol |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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