Hiroi J, Ohara K, Fujitsu T, Hirai O, Satoh S, Ochi T, Senoh H, Mori J, Kikuchi H
Nihon Yakurigaku Zasshi. 1985 Dec;86(6):441-55. doi: 10.1254/fpj.86.441.
The anti-inflammatory effects of auranofin were studied and compared with those of indomethacin, gold sodium thiomalate (GST) and D-penicillamine. Auranofin was active as indomethacin in inhibiting carrageenan induced paw edema in rats, but was less potent than indomethacin in inhibiting UV-induced erythema in guinea pigs. Auranofin inhibited Arthus type paw edema and reverse PCA reaction in rats, on which indomethacin was ineffective. The inhibitory activity of auranofin on adjuvant arthritis was weaker than that of indomethacin. In in vitro experiments, auranofin did not show any suppression of cyclooxygenase activity, but was capable of suppression of lysosomal enzyme release and chemotaxis of neutrophils and macrophages. In addition to these anti-inflammatory activities, auranofin had almost equal anti-analgesic and anti-pyretic activity to that of indomethacin. The above results indicated that the anti-inflammatory profiles of auranofin and indomethacin differ, so we can expect new therapeutic activities of auranofin. GST had similar anti-inflammatory and anti-analgesic profiles to those of auranofin; however, the activities were less potent than auranofin and devoid of anti-pyretic activity. D-penicillamine did not show any anti-inflammatory, anti-analgesic or anti-pyretic activity.
研究了金诺芬的抗炎作用,并将其与吲哚美辛、硫代苹果酸金钠(GST)和D-青霉胺进行比较。金诺芬在抑制角叉菜胶诱导的大鼠足爪肿胀方面与吲哚美辛活性相当,但在抑制豚鼠紫外线诱导的红斑方面比吲哚美辛效力弱。金诺芬能抑制大鼠的阿瑟斯型足爪肿胀和逆转被动皮肤过敏反应,而吲哚美辛对此无效。金诺芬对佐剂性关节炎的抑制活性比吲哚美辛弱。在体外实验中,金诺芬未显示出对环氧化酶活性的任何抑制作用,但能够抑制溶酶体酶释放以及中性粒细胞和巨噬细胞的趋化性。除了这些抗炎活性外,金诺芬的抗镇痛和退热活性与吲哚美辛几乎相当。上述结果表明金诺芬和吲哚美辛的抗炎特性不同,因此我们可以期待金诺芬有新的治疗活性。GST具有与金诺芬相似的抗炎和抗镇痛特性;然而,其活性比金诺芬弱且没有退热活性。D-青霉胺未显示出任何抗炎、抗镇痛或退热活性。