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Inhibition of prostanoid formation in intact cells by 2,5‐di‐( tert ‐butyl)‐1,4‐benzohydroquinone, a blocker of Ca 2+ ‐ATPases
Author(s) -
Leis Hans J.,
Zach Doris,
Huber Evelyn,
Ziermann Laszlo,
Gleispach Helmut,
Windischhofer W.
Publication year - 1996
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1996.tb15224.x
Subject(s) - prostanoid , chemistry , atpase , pharmacology , microbiology and biotechnology , biochemistry , medicine , biology , receptor , enzyme
1 The blocker of endoplasmic reticulum Ca 2+ ‐ATPase, 2,5‐di‐( tert ‐butyl)‐1,4‐benzohydroquinone (BHQ) was shown to inhibit formation of prostaglandin E 2 and prostacyclin in the osteoblast‐like cell lines, MC3T3‐E1 and ROS 17/2.8, respectively, in a dose‐dependent manner with an IC 50 of 0.5‐1 μ m . Inhibition was observed with various stimuli (arachidonic acid, bradykinin, melittin and calcium ionophore, A23187). 2 This effect was also observed in human platelets, where BHQ dose‐dependently blocked thromboxane biosynthesis and formation of 12‐hydroxy‐heptadecatrienoic acid after stimulation with arachidonic acid, but not formation of 12‐hydroxy‐eicosatetraenoic acid. 3 Inhibition of prostaglandin E 2 formation in MC3T3‐E1 cells was not observed with thapsigargin after stimulation with arachidonic acid, A23187 or melittin, whereas bradykinin‐induced prostaglandin E 2 biosynthesis was blocked. 4 Taken together, the results suggest a direct inhibitory action of BHQ on the cyclo‐oxygenase in these three cell systems.