title: Polyphloretin phosphate (PPP) antagonists of prostaglandin action also inhibit prostaglandin biosynthesis in-vitro.
abstract: Several polyphloretin phosphate (PPP) fractions (low mol. wt LC1259; high mol. wt LC1261; crude mixture, LC101) were confirmed in their established property as antagonists of the pharmacological actions of prostaglandins in a preparation of guinea-pig isolated ileum stimulated by prostaglandin (PG)E2. Further samples of the same material were then compared in-vitro with indomethacin in their ability to inhibit prostaglandin biosynthesis from arachidonic acid by a microsomal enzyme preparation. All three PPP fractions potently inhibited prostaglandin generation, with the rank order of potency LC1259 = LC101 = indomethacin greater than LC1261. The oral LD50 in mice was 25 mg kg-1 for indomethacin and greater than 1 g kg-1 for LC101. PPP fractions (especially LC101) may therefore have therapeutic potential as anti-inflammatory agents.
authors.affiliation: Cambridge Research Institute, Histon, UK.
authors.forename: P B
authors.initials: PB
authors.lastname: Curtis-Prior
authors.forename: A R
authors.initials: AR
authors.lastname: Oblin
authors.forename: A
authors.initials: A
authors.lastname: Bennett
authors.forename: N A
authors.initials: NA
authors.lastname: Parkinson
authors.forename: A M
authors.initials: AM
authors.lastname: Orloff
mesh_terms: D000818:Animals; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000378:metabolism; D002417:Cattle; D015232:Dinoprostone / Q000096:biosynthesis; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008970:Molecular Weight; D011121:Polyphloretin Phosphate / Q000494:pharmacology* / Q000633:toxicity; D011448:Prostaglandin Antagonists; D011453:Prostaglandins / Q000096:biosynthesis*
chemical_list: D001095:Arachidonic Acids; D011448:Prostaglandin Antagonists; D011453:Prostaglandins; D016718:Arachidonic Acid; D011121:Polyphloretin Phosphate; D015232:Dinoprostone