前列腺素作用的多聚根皮素磷酸酯（PPP）拮抗剂在体外也能抑制前列腺素的生物合成。
Polyphloretin phosphate (PPP) antagonists of prostaglandin action also inhibit prostaglandin biosynthesis in-vitro.
作者信息
Curtis-Prior P B, Oblin A R, Bennett A, Parkinson N A, Orloff A M
机构信息
Cambridge Research Institute, Histon, UK.
出版信息
J Pharm Pharmacol. 1990 Sep;42(9):660-2. doi: 10.1111/j.2042-7158.1990.tb06628.x.
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.
在前列腺素（PG）E2刺激的豚鼠离体回肠制备物中，已证实几种聚磷酸根皮素（PPP）组分（低分子量的LC1259；高分子量的LC1261；粗混合物，LC101）具有作为前列腺素药理作用拮抗剂的既定特性。然后，将相同材料的进一步样品在体外与吲哚美辛比较，以评估它们通过微粒体酶制剂抑制花生四烯酸合成前列腺素的能力。所有三种PPP组分均能有效抑制前列腺素的生成，效力顺序为LC1259 = LC101 = 吲哚美辛＞LC1261。吲哚美辛对小鼠的口服半数致死量为25 mg kg-1，而LC101大于1 g kg-1。因此，PPP组分（尤其是LC101）可能具有作为抗炎剂的治疗潜力。
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