Analogues of anthracene, phenanthrene, and benzoflavone inhibit prostaglandin biosynthesis by cells in culture.
Prostaglandin production by methylcholanthrene-transformed 3T3 mouse fibroblasts (MC5-5), human normal fibroblasts (D550), and canine kidney (MDCK) cells was inhibited by several analogues of anthracene, phenanthrene, and benzoflavone. Among the most effective inhibitors of MC5-5's prostaglandin production were anthracene (ID50=1.7 micrometer), 9,10-diaminophenanthrene (ID50=0.48 micrometer), and 7,8-benzoflavone (ID50=0.55 micrometer). Under identical conditions, the ID50's for indomethacin and aspirin were 0.049 and 8.9 micrometer respectively. Production of radioactive prostaglandins by MC5-5 cells from tritiated phospholipids was blocked by 7,8-benzoflavone, but not the release of radioactive arachidonic acid.
D000818:Animals; D000873:Anthracenes / Q000494:pharmacology*; D001241:Aspirin / Q000494:pharmacology; D002478:Cells, Cultured; D004285:Dogs; D005347:Fibroblasts / Q000378:metabolism; D005419:Flavonoids / Q000494:pharmacology*; D006801:Humans; D007213:Indomethacin / Q000494:pharmacology; D051379:Mice; D008968:Molecular Conformation; D010616:Phenanthrenes / Q000494:pharmacology*; D011448:Prostaglandin Antagonists / Q000494:pharmacology*; D011458:Prostaglandins E / Q000096:biosynthesis*; D011460:Prostaglandins F / Q000096:biosynthesis*
D000873:Anthracenes; D005419:Flavonoids; D010616:Phenanthrenes; D011448:Prostaglandin Antagonists; D011458:Prostaglandins E; D011460:Prostaglandins F; D001241:Aspirin; D007213:Indomethacin