[Utilization of purified myometrium cell plasma membrane Ca2+, Mg2+-ATPase for comparative estimation of the efficiency of energy-dependent Ca2+-transport inhibitors].
With the aim of comparative estimation of efficacy of well-known inhibitors of energy-dependent Ca(2+)-transporting systems their effects were investigated on the activity of purified Ca2+, Mg(2+)-ATPase of the myometrium cell plasma membranes. From the approved inhibitors (eosin Y, o-vanadate, thapsigargin, cyclopiazonic acid, ruthenium red, sodium azide) only eosin Y and o-vanadate are potent inhibitors of myometrium sarcolemma Ca(2+)-pump: the values of Ki equal 0.8 and 4.7 microM, respectively. Thapsigargin and cyclopiazonic acid as well as ruthenium red in concentrations inhibiting, respectively, endo(sarco)plasmic reticulum Ca(2+)-pump and energy-dependent Ca(2+)-transport in mitochondria had no effect on the Ca2+, Mg(2+)-ATPase of the uterus smooth muscle cell plasma membrane. Sodium azide (10 mM) blocking completely Ca(2+)-transport in mitochondria inhibited activity of the plasma membrane Ca(2+)-transporting ATPase by 14%.
Palladin Institute of Biochemistry, National Academy of Sciences of Ukraine, Kyiv. slinchenko@biochem.kiev.ua
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Slinchenko
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Chernysh
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Kosterin
D000818:Animals; D001692:Biological Transport; D017301:Ca(2+) Mg(2+)-ATPase / Q000378:metabolism*; D002118:Calcium / Q000378:metabolism*; D000252:Calcium-Transporting ATPases / Q000037:antagonists & inhibitors* / Q000187:drug effects / Q000378:metabolism; D002462:Cell Membrane / Q000201:enzymology; D004734:Energy Metabolism / Q000187:drug effects*; D004791:Enzyme Inhibitors / Q000494:pharmacology; D004801:Eosine Yellowish-(YS) / Q000494:pharmacology; D005260:Female; D007211:Indoles / Q000494:pharmacology; D008931:Mitochondria, Muscle / Q000187:drug effects / Q000378:metabolism; D009130:Muscle, Smooth / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism; D009215:Myometrium / Q000378:metabolism*; D012430:Ruthenium Red / Q000494:pharmacology; D019810:Sodium Azide / Q000494:pharmacology; D013552:Swine; D019284:Thapsigargin / Q000494:pharmacology; D014638:Vanadates / Q000494:pharmacology
D004791:Enzyme Inhibitors; D007211:Indoles; D012430:Ruthenium Red; D014638:Vanadates; D019284:Thapsigargin; D019810:Sodium Azide; D017301:Ca(2+) Mg(2+)-ATPase; D000252:Calcium-Transporting ATPases; D002118:Calcium; D004801:Eosine Yellowish-(YS); C000543:cyclopiazonic acid