ChloroquineV1, Main, Exploration, bibRecord, 003010

Reversal of drug-resistant falciparum malaria by calcium antagonists: Potential for host cell toxicity

Identifieur interne : 003010 ( Main/Exploration ); précédent : 003009; suivant : 003011

Reversal of drug-resistant falciparum malaria by calcium antagonists: Potential for host cell toxicity

Auteurs : George Watt [États-Unis] ; Gary W. Long [États-Unis] ; Max Grogl [États-Unis] ; Samuel K. Martin [États-Unis]

Source :

Transactions of The Royal Society of Tropical Medicine and Hygiene [ 0035-9203 ] ; 1990.

RBID : ISTEX:961110AADFC63244EE63ECDDBF963F756AB658B3

English descriptors

Teeft :
- Annual subscription, Calcium antagonists, Cell line, Cell lines, Chloroquine, Chloroquine resistance, Culture medium, Cytoplasmic domain, Desipramine, Drug accumulation, Excretory function, Gottesman, Hepatocytes, Human cells, Iatrogenic toxicity, Lung cells, Microtitre plates, Monoclonal antibodies, Mouse hepatocytes, Multidrug resistance, National academy, Normal cells, Pastan, Positive control cells, Primary mouse hepatocytes, Reversal, Royal society, Second antibody, Supraphysiological concentrations, Toxicity, Tropical medicine, Verapamil, Walter reed army institute.

Abstract

Agents capable of reversing multidrug resistance (mdr) in falciparum malaria were investigated for potentiation of chloroquine accumulation and toxicity in a cell culture system. Verapamil, its analog RO11-2933, and desipramine caused a dose-dependent increase in the accumulation of chloroquine (CQ) within human and mouse hepatocytes but not human lung cells. Only those cells in which drug accumulation was enhanced by reversing agents reacted positively for P-glycoprotein (PgP)—the putative mediator of the enhanced drug efflux characteristic of mdr. Clinically achievable concentrations of verapamil (0·4 μM) and desipramine (1 μm) increased CQ accumulation within primary mouse hepatocytes by more than 50%. A well-differentiated normal human cell line (Hep-G2) was killed in media containing a combination of supraphysiological concentrations of CQ and verapamil but survived the same concentrations of either drug alone. Reversing agents may block PgP-mediated drug export from normal tissues as well as from MDR cells. Iatrogenic toxicity resulting from this accumulation of potentially toxic drugs such as CQ within normal cells could complicate the reversal of mdr in vivo.

Url:

DOI: 10.1016/0035-9203(90)90248-D

Affiliations:

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<front><div type="abstract">Agents capable of reversing multidrug resistance (mdr) in falciparum malaria were investigated for potentiation of chloroquine accumulation and toxicity in a cell culture system. Verapamil, its analog RO11-2933, and desipramine caused a dose-dependent increase in the accumulation of chloroquine (CQ) within human and mouse hepatocytes but not human lung cells. Only those cells in which drug accumulation was enhanced by reversing agents reacted positively for P-glycoprotein (PgP)—the putative mediator of the enhanced drug efflux characteristic of mdr. Clinically achievable concentrations of verapamil (0·4 μM) and desipramine (1 μm) increased CQ accumulation within primary mouse hepatocytes by more than 50%. A well-differentiated normal human cell line (Hep-G2) was killed in media containing a combination of supraphysiological concentrations of CQ and verapamil but survived the same concentrations of either drug alone. Reversing agents may block PgP-mediated drug export from normal tissues as well as from MDR cells. Iatrogenic toxicity resulting from this accumulation of potentially toxic drugs such as CQ within normal cells could complicate the reversal of mdr in vivo.</div>
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Reversal of drug-resistant falciparum malaria by calcium antagonists: Potential for host cell toxicity

Reversal of drug-resistant falciparum malaria by calcium antagonists: Potential for host cell toxicity

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