POLYPHLORETIN PHOSPHATE (PPP) ANTAGONISTS OF PROSTAGLANDIN ACTION ALSO INHIBIT PROSTAGLANDIN BIOSYNTHESIS INVITRO

被引:3
作者
CURTISPRIOR, PB
OBLIN, AR
BENNETT, A
PARKINSON, NA
ORLOFF, AM
机构
[1] SYNTHELABO LERS,BAGNEUX,FRANCE
[2] UNIV LONDON KINGS COLL,SCH MED & DENT,DEPT SURG,LONDON WC2R 2LS,ENGLAND
关键词
D O I
10.1111/j.2042-7158.1990.tb06628.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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. 1990 Royal Pharmaceutical Society of Great Britain
引用
收藏
页码:660 / 662
页数:3
相关论文
共 21 条
[11]  
CURTISPRIOR PB, 1979, PROSTAGLANDINS MED, V2, P314
[12]  
CURTISPRIOR PB, 1974, ADV EXP MED BIOL, V63, P43
[13]   SYNTHETIC HIGH MOLECULAR WEIGHT ENZYME INHIBITORS .1. POLYMERIC PHOSPHATES OF PHLORETIN AND RELATED COMPOUNDS [J].
DICZFALUSY, E ;
FERNO, O ;
FEX, H ;
HOGBERG, B ;
LINDEROT, T ;
ROSENBERG, T .
ACTA CHEMICA SCANDINAVICA, 1953, 7 (06) :913-920
[15]   POLYPHLORETIN PHOSPHATE - A SELECTIVE ANTAGONIST FOR PROSTAGLANDINS F1ALPHA AND F2ALPHA [J].
EAKINS, KE ;
KARIM, SMM .
LIFE SCIENCES, 1970, 9 (1P1) :1-&
[16]  
GIESSLER C, 1977, PHARMACOL RES COMMUN, V9, P117
[17]   POLYPHLORETIN PHOSPHATE REDUCES ALGESIC ACTION OF BRADYKININ BY INTERFERING WITH E-TYPE PROSTAGLANDINS [J].
JUAN, H ;
LEMBECK, F .
AGENTS AND ACTIONS, 1976, 6 (05) :646-650
[18]   PROPERTIES OF 15-HYDROXY PROSTAGLANDIN DEHYDROGENASE - STRUCTURAL REQUIREMENTS FOR SUBSTRATE BINDING [J].
MARRAZZI, MA ;
MATSCHINSKY, FM .
PROSTAGLANDINS, 1972, 1 (05) :373-+
[19]  
SANNER J, 1988, PROSTAGLANDINS BIOL, P179
[20]  
SANNER JH, 1976, ADV PROSTAGLANDINS, V2, P139