The in vitro effect of primaquine on red cell phospholipid metabolism. 1976

A Miller, and H C Smith

Primaquine converts erythrocytes into osmotically fragile spherocytes. Since primaquine increased the rate of acylation of erythrocyte lysophosphatidylcholine (LPC), it has been suggested that a deficiency of LPC is responsible for its hemolytic action. We have examined the validity of this hypothesis. In the absence of added lysophosphatides, primaquine slightly decreased the incorporation of albumin-bound palmitic acid-14C into phosphatidylcholine (PC) whereas that into phosphatidylethanolamine (PE) was more depressed. When unbound dispersions of fatty acid were used, red cells exposed to primaquine manifested a slight increase in palmitic acid-14C incorporation into PC whereas that into PE remained decreased. In the presence of exogenous LPC, control cells increased their incorporation of bound palmitic acid-14C into PC while decreasing it into PE. In these same experiments, red cells incubated with primaquine demonstrated a much greater enhancement of LPC acylation than control cells. Lysophosphatidylethanolamine acylation, while depressed, was still slightly greater than that of cells incubated with drug alone. The concentration of LPC in control and primaquine-treated erythrocytes incubated with exogenous LPC was comparable and was approximately five times that of cells not incubated with LPC. The osmotic fragility of erythrocytes correlated poorly with their concentration of LPC. The effect of primaquine on the incorporation of bound palmitic acid into erythrocyte PC was influenced by exogenous LPC with the reaction markedly increased in its presence but slightly depressed in its absence. The proposal that the hemolytic action of primaquine is due to a decrease in red cell LPC is not supported by the data.

UI MeSH Term Description Entries
D008244 Lysophosphatidylcholines Derivatives of PHOSPHATIDYLCHOLINES obtained by their partial hydrolysis which removes one of the fatty acid moieties. Lysolecithin,Lysolecithins,Lysophosphatidylcholine
D009996 Osmotic Fragility RED BLOOD CELL sensitivity to change in OSMOTIC PRESSURE. When exposed to a hypotonic concentration of sodium in a solution, red cells take in more water, swell until the capacity of the cell membrane is exceeded, and burst. Saline Fragility,Fragility, Osmotic,Fragility, Saline
D010169 Palmitic Acids A group of 16-carbon fatty acids that contain no double bonds. Acids, Palmitic
D010743 Phospholipids Lipids containing one or more phosphate groups, particularly those derived from either glycerol (phosphoglycerides see GLYCEROPHOSPHOLIPIDS) or sphingosine (SPHINGOLIPIDS). They are polar lipids that are of great importance for the structure and function of cell membranes and are the most abundant of membrane lipids, although not stored in large amounts in the system. Phosphatides,Phospholipid
D011319 Primaquine An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404) Primacin,Primaquine Diphosphate,Primaquine Phosphate,Diphosphate, Primaquine,Phosphate, Primaquine
D011485 Protein Binding The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments. Plasma Protein Binding Capacity,Binding, Protein
D002463 Cell Membrane Permeability A quality of cell membranes which permits the passage of solvents and solutes into and out of cells. Permeability, Cell Membrane
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004912 Erythrocytes Red blood cells. Mature erythrocytes are non-nucleated, biconcave disks containing HEMOGLOBIN whose function is to transport OXYGEN. Blood Cells, Red,Blood Corpuscles, Red,Red Blood Cells,Red Blood Corpuscles,Blood Cell, Red,Blood Corpuscle, Red,Erythrocyte,Red Blood Cell,Red Blood Corpuscle
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man

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