Polyphloretin phosphate (PPP) antagonists of prostaglandin action also inhibit prostaglandin biosynthesis in-vitro

Author:

Curtis-Prior P B1,Oblin A R21,Bennett A13,Parkinson N A31,Orloff A M21

Affiliation:

1. Cambridge Research Institute, Histon, Cambridge, UK

2. Synthelabo-LERS, Bagneux, France

3. Department of Surgery, King's College School of Medicine and Dentistry, London, UK

Abstract

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 > LC1261. The oral LD50 in mice was 25 mg kg−1 for indomethacin and > 1 g kg−1 for LC101. PPP fractions (especially LC101) may therefore have therapeutic potential as anti-inflammatory agents.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

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