Wojtecka-Lukasik E, Sopata I, Maśliński S
Agents Actions. 1986 Apr;18(1-2):68-70. doi: 10.1007/BF01987985.
Auranofin, an orally gold preparation, effective in the treatment of rheumatoid arthritis, was found to be a potent noncytotoxic inhibitor of histamine and collagenase release from mast cells and polymorphonuclear (PMN) leukocytes respectively. Histamine release has been inhibited by auranofin in dose-dependent fashion. Auranofin at concentration of 10(-5) M inhibited 100% of the release, lower concentration 10(-6) M and 10(-7) M produced 80 and 40% decrease. The exposure of PMN-leukocytes to auranofin caused also dose-dependent inhibition of collagenase release. Auranofin at a concentration of 10(-4) M produced a marked reduction (75-100%) of enzyme release from human and rat blood PMN-leukocytes. The modest inhibition 40 and 15-20% at a concentration of 10(-5) M and 10(-6) M respectively was obtained. Auranofin more significantly suppressed collagenase release from leukocytes isolated from inflammatory exudate. Decrease of 100, 80 and 60% were observed upon addition of 10(-4) M, 10(-5) M and 10(-6) M of auranofin. These results suggest that therapeutic action of auranofin may be caused, at least in part, by the inhibition of cellular release of histamine and collagenase in the course of inflammation.
金诺芬，一种口服金制剂，对类风湿性关节炎有效，被发现是一种强效的非细胞毒性抑制剂，分别可抑制肥大细胞和多形核（PMN）白细胞释放组胺和胶原酶。金诺芬以剂量依赖性方式抑制组胺释放。浓度为10^(-5) M的金诺芬可抑制100%的释放，较低浓度10^(-6) M和10^(-7) M分别使释放减少80%和40%。将PMN白细胞暴露于金诺芬也会导致胶原酶释放的剂量依赖性抑制。浓度为10^(-4) M的金诺芬可使人类和大鼠血液PMN白细胞的酶释放显著减少（75 - 100%）。在浓度为10^(-5) M和10^(-6) M时分别获得适度抑制，抑制率为40%和15 - 20%。金诺芬更显著地抑制从炎性渗出物中分离出的白细胞的胶原酶释放。加入10^(-4) M、10^(-5) M和10^(-6) M的金诺芬后，观察到释放分别减少100%、80%和60%。这些结果表明，金诺芬的治疗作用可能至少部分是由其在炎症过程中抑制组胺和胶原酶的细胞释放引起的。
