| Iodination increases the activity of verapamil derivatives in reversing PGP multidrug resistance. | |
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MedLine Citation:
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PMID: 20682982 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Iodinated derivatives of verapamil were synthesized and tested as P-glycoprotein (Pgp)-mediated multidrug resistance (MDR) reversal agents. The ability of these compounds to revert MDR was evaluated on daunorubicin-resistant K562 cells, by measuring the intracellular accumulation of rhodamine 123, a fluorescent probe of Pgp transport activity. One of the investigated compounds (16c) was found to be a more potent MDR reversal agent than verapamil and cyclosporin A, used as reference molecules. Further in vitro studies showed that compound 16c restored daunorubicin activity and, when used alone, did not induce cell death, cell cycle perturbation and modification of calcium channel activity in comparison with verapamil. |
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Authors:
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Regis Barattin; Bastien Gerby; Kevin Bourges; Gaëlle Hardy; Jose Olivares; Jean Boutonnat; Christophe Arnoult; Amaury D U Moulinet D'Hardemare; Xavier Ronot |
Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Anticancer research Volume: 30 ISSN: 1791-7530 ISO Abbreviation: Anticancer Res. Publication Date: 2010 Jul |
Date Detail:
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Created Date: 2010-08-04 Completed Date: 2010-08-30 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8102988 Medline TA: Anticancer Res Country: Greece |
Other Details:
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Languages: eng Pagination: 2553-9 Citation Subset: IM |
Affiliation:
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University of Grenoble I, Department of Molecular Chemistry, UMR CNRS 5250, F-38041, Grenoble Cedex 9, France. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Calcium Channel Blockers / pharmacology Calcium Channels, L-Type / metabolism Cell Cycle / drug effects Cyclosporine / pharmacology Daunorubicin / pharmacology Drug Resistance, Neoplasm Drug Synergism Humans K562 Cells Male Myocytes, Cardiac / drug effects, metabolism P-Glycoprotein / antagonists & inhibitors*, metabolism Rats Rats, Wistar Rhodamine 123 / pharmacokinetics Verapamil / analogs & derivatives*, pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Calcium Channel Blockers; 0/Calcium Channels, L-Type; 0/P-Glycoprotein; 20830-81-3/Daunorubicin; 52-53-9/Verapamil; 59865-13-3/Cyclosporine; 62669-70-9/Rhodamine 123 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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