Abstract
The isoquinoline peripheral benzodiazepine receptor ligand PK11195 increased drug (daunomycin)- and fluorochrome (calcein-AM) uptake and induced apoptosis detected by flow cytometry (FCM) technique, DNA electrophoretic analysis and poly(ADP-ribose) polymerase (PARP) cleavage in human multidrug-resistant myeloid leukemia (BL-60/VCR) and ovarian carcinoma (A2780/ADR) cells in vitro. The position of PK11195 with respect to drug-resistance modulator (DRM) efficiency, compared to the reference DRMs with the aid of FCM technique, was as follows: PSC833 > verapamil > PK11195 > vincristine. Our data show up to now not indicated observation that PK11195 possesses multidrug resistance modulating activity.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics
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Antineoplastic Agents / metabolism*
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Antineoplastic Agents / pharmacology*
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Antineoplastic Agents / toxicity
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Apoptosis / drug effects*
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Biological Transport
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Carcinoma / drug therapy
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Carcinoma / metabolism
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Daunorubicin / metabolism*
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Daunorubicin / toxicity
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Drug Resistance, Multiple
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Drug Resistance, Neoplasm
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Drug Synergism
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Female
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Fluoresceins / metabolism
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Fluorescent Dyes / metabolism
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HL-60 Cells
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Humans
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Isoquinolines / metabolism
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Isoquinolines / pharmacology*
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Leukemia, Myeloid / drug therapy*
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Leukemia, Myeloid / metabolism
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Ligands
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Mitochondrial Proteins / metabolism
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Ovarian Neoplasms / drug therapy
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Ovarian Neoplasms / metabolism
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Receptors, GABA-A / metabolism
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Tumor Cells, Cultured
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Antineoplastic Agents
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Fluoresceins
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Fluorescent Dyes
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Isoquinolines
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Ligands
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Mitochondrial Proteins
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Receptors, GABA-A
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calcein AM
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PK 11195
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Daunorubicin