Abstract：
:Membrane damage caused by phospholipase A action is thought to be an important factor in ischemic myocardial injury. Propranolol has been shown previously to have beneficial effects in both animal experiments and clinical trials, and it has membrane-stabilizing properties in vitro. To investigate the possibility that these effects might be due, in part, to effects on phospholipases, we determined the effects of propranolol on rat heart phospholipases A at physiological pH using small unilamellar liposomes of di[1-14C]oleoylphosphatidylcholine as substrate. Propranolol inhibited heart phospholipases A in vitro. The concentration required to give 50% inhibition was 0.2 mM for the mitochondrial and cytosolic phospholipases A and 2.9 mM for sarcoplasmic reticulum phospholipase A. The binding of [4-3H]propranolol to fresh membrane preparations was studied using an ultracentrifugation method. Propranolol bound readily to both membrane fractions in vitro with no significant difference in the saturation number (0.20 to 0.28 mol drug per mol phospholipid) but the association constant, KA, was higher for mitochondrial membranes (3760 +/- 350) than for the sarcoplasmic reticulum (2190 +/- 390). Our results show that propranolol inhibited heart phospholipases A in vitro at physiological pH. The mitochondrial and cytosolic phospholipases A were more susceptible to inhibition than the phospholipase A of sarcoplasmic reticulum. Propranolol bound to mitochondria and sarcoplasmic reticulum in vitro, suggesting the possibility that propranolol binding to heart membranes in vivo could result in drug concentrations in these membranes high enough to inhibit phospholipase A. This could represent an additional mechanism by which propranolol exerts beneficial effects in myocardial ischemia.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Trotz M,Jellison EJ,Hostetler KYdoi
10.1016/0006-2952(87)90666-6subject
Has Abstractpub_date
1987-12-15 00:00:00pages
4251-6issue
24eissn
0006-2952issn
1873-2968pii
0006-2952(87)90666-6journal_volume
36pub_type
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