Polyphloretin phosphate (PPP) antagonists of prostaglandin action also inhibit prostaglandin biosynthesis in-vitro.
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.
Curtis-Prior
P B
PB
Cambridge Research Institute, Histon, UK.
Oblin
A R
AR
Bennett
A
A
Parkinson
N A
NA
Orloff
A M
AM
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*
D001095:Arachidonic Acids; D011448:Prostaglandin Antagonists; D011453:Prostaglandins; D016718:Arachidonic Acid; D011121:Polyphloretin Phosphate; D015232:Dinoprostone