| Inhibition of P-glycoprotein-dependent multidrug resistance by an isoquinolinesulfonamide compound H-87 in rat ascites hepatoma AH66 cells. | |
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MedLine Citation:
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PMID: 8799494 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The effects of an isoquinolinesulfonamide compound, H-87, on naturally acquired multidrug-resistance (MDR) in rat hepatoma AH66 cells were examined. AH66 cells were highly resistant to vinblastine, SN-38, an active camptothecin analog, adriamycin, and etoposide, compared with the sensitive variant AH66F cells. Although H-87 hardly affected the sensitivities to antitumor agents of AH66F cells, this compound completely inhibited the resistance to vinblastine, moderately inhibited the resistance to SN-38 and adriamycin and had little effect on etoposide, mitomycin C, cisplatin, and 5-fluorouracil. H-87 significantly decreased the efflux of vinblastine from the resistant cells and increased the drug accumulation. SN-38 and adriamycin also exhibited a weak but significant increase in vinblastine accumulation in AH66 cells. H-87 inhibited [3H]azidopine-photolabeling to 160 kDa P-glycoprotein in the plasma membrane of AH66 cells, as reported in acquired MDR leukemic cells. Consequently, the MDR-overcoming effect of H-87 seems to be due to its direct inhibition of the binding of antitumor agents on P-glycoprotein in the plasma membrane. |
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Authors:
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S Nakamura; T Minamino; M Nomura; S Wakusawa; K Miyamoto; H Hidaka |
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Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Biological & pharmaceutical bulletin Volume: 19 ISSN: 0918-6158 ISO Abbreviation: Biol. Pharm. Bull. Publication Date: 1996 Jun |
Date Detail:
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Created Date: 1997-01-02 Completed Date: 1997-01-02 Revised Date: 2007-09-25 |
Medline Journal Info:
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Nlm Unique ID: 9311984 Medline TA: Biol Pharm Bull Country: JAPAN |
Other Details:
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Languages: eng Pagination: 886-9 Citation Subset: IM |
Affiliation:
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Fujiyakuhin Co., Ltd., Ohmiya, Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Affinity Labels Animals Antineoplastic Agents / pharmacology Azides / metabolism Camptothecin / analogs & derivatives, pharmacology Dihydropyridines / metabolism Doxorubicin / pharmacology Drug Resistance, Multiple* Drug Resistance, Neoplasm* Etoposide / pharmacology Female Isoquinolines / pharmacology* P-Glycoprotein / antagonists & inhibitors Protein Binding / drug effects Protein Kinase Inhibitors Rats Sulfonamides* Tritium Tumor Cells, Cultured Vinblastine / pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Affinity Labels; 0/Antineoplastic Agents; 0/Azides; 0/Dihydropyridines; 0/Isoquinolines; 0/P-Glycoprotein; 0/Protein Kinase Inhibitors; 0/Sulfonamides; 10028-17-8/Tritium; 100286-90-6/irinotecan; 127243-85-0/H 89; 23214-92-8/Doxorubicin; 33419-42-0/Etoposide; 7689-03-4/Camptothecin; 865-21-4/Vinblastine; 90523-31-2/azidopine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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