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Titolo:
A comparison of the effects of olopatadine and ketotifen on model membranes
Autore:
Brockman, H; Graff, G; Spellman, J; Yanni, J;
Indirizzi:
Alcon Res Ltd, Ophthalmol Res, Ft Worth, TX 76134 USA Alcon Res Ltd Ft Worth TX USA 76134 phthalmol Res, Ft Worth, TX 76134 USA Univ Minnesota, Hormel Inst, Austin, MN 55912 USA Univ Minnesota Austin MN USA 55912 ota, Hormel Inst, Austin, MN 55912 USA
Titolo Testata:
ACTA OPHTHALMOLOGICA SCANDINAVICA
, volume: 78, anno: 2000, supplemento:, 230
pagine: 10 - 15
SICI:
1395-3907(200006)78:<10:ACOTEO>2.0.ZU;2-5
Fonte:
ISI
Lingua:
ENG
Soggetto:
MAST-CELLS; HUMAN-LUNG; HISTAMINE-RELEASE; IN-VITRO; ANTIHISTAMINES; AL-4943A; MONOLAYERS; INHIBITION; TENSION; DRUGS;
Keywords:
olopatadine; ketotifen; erythrocyte membranes; phospholipid monolayers;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Citazioni:
29
Recensione:
Indirizzi per estratti:
Indirizzo: Yanni, J Alcon Res Ltd, Ophthalmol Res, 6201 S Freeway, Ft Worth, TX 76134USA Alcon Res Ltd 6201 S Freeway Ft Worth TX USA 76134 , TX 76134 USA
Citazione:
H. Brockman et al., "A comparison of the effects of olopatadine and ketotifen on model membranes", ACT OPHTH S, 78, 2000, pp. 10-15

Abstract

Olopatadine is a human conjunctival mast cell stabilizer with antihistaminic activity. Ketotifen is an older molecule that possesses antihistaminic activity and is reported to have additional pharmacological properties. The interactions of these two compounds with model membranes (i.e., monolayers of 1-stearoyl-2-oleoyl-sn-glycerophosphocholine at the argon-buffer interface), and natural (i.e., erythrocyte) membranes were compared in an effort to understand the differences in their biological activities, Drug-lipid interaction with monolayers was determined by monitoring the surface pressure as a function of the drug concentration in the aqueous phase supporting themonolayer, Drug interaction with erythrocyte membranes was determined by monitoring changes in the permeability of the membranes to hemoglobin and 6-carboxyfluorescein as a function of drug concentration in the medium. Olopatadine and ketotifen are both intrinsically surface active and both interact with phospholipid monolayers, However, in both the presence and absence of lipid monolayers, the changes in surface pressure induced by olopatadine are lower than those caused by ketotifen, The effects of these two drugs oncell membranes were dramatically different. Exposure of bovine erythrocytes to increasing concentrations of ketotifen (1-10 mM) resulted in complete hemolysis of the cells, whereas olopatadine (1-10 mM) caused only minimal hemolysis (<8%), Consistent results mere obtained in experiments measuring the leakage of 6-carboxyfluorescein from erythrocyte ghosts as a more sensitive marker of membrane perturbation, Olopatadine treatment (0.1-10 mM) minimally perturbed the cell membrane while ketotifen (1-10 mM) caused a concentration dependent release of the fluorescent marker. These data demonstratefundamental differences between the two drugs in their effects on cell membranes, Moreover, the differences are consistent with the surface activities of the two compounds measured in monolayers and with reported differencesin their pharmacological activities. These findings offer an explanation for the biphasic non-specific cytotoxic effect of ketotifen on histamine release from mast cells and may account for the nonlytic mast cell stabilizingactivity of olopatadine.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/03/20 alle ore 23:10:06