Otomo S, Higuchi S, Tanaka M, Gotoh Y, Osada Y, Ohzeki M
Nihon Yakurigaku Zasshi. 1981 Sep;78(3):185-90.
The inhibitory effects of anti-inflammatory drugs on th erythema induced by arachidonic acid in guinea pigs were studied. Values of ED50 (mg/kg, p.o.) were; diclofenac sodium (19.9), indomethacin (28.1), naproxen (52.4), phenylbutazone (67.1), ibuprofen (81.3), aspirin (92.6). These drugs, however, were ineffective on the erythema induced by prostaglandin E2. Basic nonsteroidal and steroidal anti-inflammatory drugs and anti-oxidants were negative in the inhibition of arachidonic acid-induced erythema. Cyproheptadine as an anti-histamine and -serotonin agent and morphine as a CNS acting agent were also negative. Erythema did not occur following treatment with linoleic acid, linolenic acid and gamma-linolenic acid. Bishomo-gamma-linolenic acid-induced erythema was inhibited by diclofenac sodium. The inhibition of acidic nonsteroidal anti-inflammatory drugs in this system seemed to be the result of a block of the enzymatic conversion of arachidonic acid to prostaglandins. The arachidonic acid-induced erythema in guinea pigs can serve as a new animal model for evaluating prostaglandins biosynthesis inhibitors such as anti-inflammatory drugs.
研究了抗炎药对豚鼠花生四烯酸诱导的红斑的抑制作用。口服半数有效剂量(ED50,mg/kg)的值分别为:双氯芬酸钠(19.9)、吲哚美辛(28.1)、萘普生(52.4)、保泰松(67.1)、布洛芬(81.3)、阿司匹林(92.6)。然而,这些药物对前列腺素E2诱导的红斑无效。碱性非甾体和甾体抗炎药以及抗氧化剂对花生四烯酸诱导的红斑无抑制作用。作为抗组胺和抗5-羟色胺剂的赛庚啶以及作为中枢神经系统作用剂的吗啡也无抑制作用。用亚油酸、亚麻酸和γ-亚麻酸处理后未出现红斑。双氯芬酸钠可抑制二高-γ-亚麻酸诱导的红斑。该系统中酸性非甾体抗炎药的抑制作用似乎是由于花生四烯酸向前列腺素的酶促转化受阻。豚鼠花生四烯酸诱导的红斑可作为一种新的动物模型,用于评估前列腺素生物合成抑制剂,如抗炎药。