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Literature DB >> 7378071

Inhibition of highly purified mammalian phospholipases A2 by non-steroidal anti-inflammatory agents. Modulation by calcium ions.

Abstract

Highly purified Ca2+-dependent phospholipases A2 that were isolated from human platelets, rabbit alveolar macrophages and peritoneal polymorphonuclear leucocytes and were active in the neutral-to-alkaline pH range were inhibited 50% by 75 microM-indomethacin in the presence of 5.0 mM added Ca2+. Sodium meclofenamate and sodium flufenamate were also inhibitory; the sensitivity to inhibition was a function of Ca2+ concentration. The dose for 50% inhibition (ID50) with meclofenamate was 0.4 mM in the presence of 2.5 mM added Ca2+, but 50nM in the presence of 0.5 mM added Ca2+. Thus, inhibition of phospholipase A2 activity by non-steroidal anti-inflammatory agents via Ca2+ antagonism may significantly contribute to the mechanism of drug action.

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Year: 1980 PMID： 7378071 PMCID： PMC1161621 DOI： 10.1042/bj1860633

Source DB: PubMed Journal: Biochem J ISSN： 0264-6021 Impact factor: 3.857

11 in total

1. Relation between calcium requirement, substrate charge, and rabbit polymorphonuclear leukocyte phospholipase A2 activity.

Authors: R Franson; M Waite
Journal: Biochemistry Date: 1978-09-19 Impact factor: 3.162

2. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding.

Authors: M M Bradford
Journal: Anal Biochem Date: 1976-05-07 Impact factor: 3.365

3. Mobilization of arachidonic acid in human platelets. Kinetics and Ca2+ dependency.

Authors: S Rittenhouse-Simmons; F A Russell; D Deykin
Journal: Biochim Biophys Acta Date: 1977-09-28

4. Low concentrations of indomethacin inhibit phospholipase A2 of rabbit polymorphonuclear leukocytes.

Authors: L Kaplan; J Weiss; P Elsbach
Journal: Proc Natl Acad Sci U S A Date: 1978-06 Impact factor: 11.205

Review 5. Indomethacin--a calcium antagonist.

Authors: B J Northover
Journal: Gen Pharmacol Date: 1977

6. The effect of ACTH on calcium distribution in the perfused cat adrenal gland.

Authors: S D Jaanus; R P Rubin
Journal: J Physiol Date: 1971-03 Impact factor: 5.182

7. Inhibition of prostaglandin synthesis as a mechanism of action for aspirin-like drugs.

Authors: J R Vane
Journal: Nat New Biol Date: 1971-06-23

8. Macrophages synthesis and release prostaglandins in response to inflammatory stimuli.

Authors: J L Humes; R J Bonney; L Pelus; M E Dahlgren; S J Sadowski; F A Kuehl; P Davies
Journal: Nature Date: 1977-09-08 Impact factor: 49.962

9. Interaction of phospholipase A2 with lipid-water interfaces.

Authors: G H de Haas; A J Slotboom; H M Verheij; E H Jansen; P S de Araujo; J C Vidal
Journal: Adv Prostaglandin Thromboxane Res Date: 1978

10. Partial characterization and purification of a rabbit granulocyte factor that increases permeability of Escherichia coli.

Authors: J Weiss; R C Franson; S Beckerdite; K Schmeidler; P Elsbach
Journal: J Clin Invest Date: 1975-01 Impact factor: 14.808

19 in total

9. Anti-inflammatory effects of polyamines in serotonin and carrageenan paw edemata - possible mechanism to increase vascular permeability inhibitory protein level which is regulated by glucocorticoids and superoxide radical.

Authors: Y Oyanagui
Journal: Agents Actions Date: 1984-02

10. Protein synthesis in isolated rabbit forelimb muscles. The possible role of metabolites of arachidonic acid in the response to intermittent stretching.

Authors: R H Smith; R M Palmer; P J Reeds
Journal: Biochem J Date: 1983-07-15 Impact factor: 3.857

Inhibition of highly purified mammalian phospholipases A2 by non-steroidal anti-inflammatory agents. Modulation by calcium ions.

1. Relation between calcium requirement, substrate charge, and rabbit polymorphonuclear leukocyte phospholipase A2 activity.

2. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding.

3. Mobilization of arachidonic acid in human platelets. Kinetics and Ca2+ dependency.

4. Low concentrations of indomethacin inhibit phospholipase A2 of rabbit polymorphonuclear leukocytes.

Review 5. Indomethacin--a calcium antagonist.

6. The effect of ACTH on calcium distribution in the perfused cat adrenal gland.

7. Inhibition of prostaglandin synthesis as a mechanism of action for aspirin-like drugs.

8. Macrophages synthesis and release prostaglandins in response to inflammatory stimuli.

9. Interaction of phospholipase A2 with lipid-water interfaces.

10. Partial characterization and purification of a rabbit granulocyte factor that increases permeability of Escherichia coli.

Review 1. Synovial fluid phospholipase A2s and inflammation.

2. Enhancement of endotoxin-induced isolated renal tubular cell injury by toxic shock syndrome toxin 1.

3. The possible role of phospholipase A2 in cardiac membrane destabilization under calcium overload conditions.

Review 4. How is the level of free arachidonic acid controlled in mammalian cells?

5. Isolation and characterization of a membrane-associated, calcium-dependent phospholipase A2 from rabbit lung.

6. Hydrogen peroxide-induced alterations in prostaglandin secretion in the rat colon in vitro.

7. Effects of Ca2+ on phosphoinositide breakdown in exocrine pancreas.

8. Constant turnover of arachidonic acid and inhibition of a potassium current in Aplysia giant neurons.

9. Anti-inflammatory effects of polyamines in serotonin and carrageenan paw edemata - possible mechanism to increase vascular permeability inhibitory protein level which is regulated by glucocorticoids and superoxide radical.

10. Protein synthesis in isolated rabbit forelimb muscles. The possible role of metabolites of arachidonic acid in the response to intermittent stretching.