Rainsford K D
Anti-inflammatory Research Unit, Strangeways Research Laboratory, Cambridge, UK.
J Pharm Pharmacol. 1989 Feb;41(2):112-7. doi: 10.1111/j.2042-7158.1989.tb06404.x.
A range of anti-inflammatory drugs having varying effects on eicosanoid metabolism and other actions was studied for their potential to inhibit alpha-interleukin 1 (IL-1)-induced cartilage proteoglycan resorption in-vitro. No significant effects on resorption were observed with inhibitors of cyclo-oxygenase, lipoxygenase or mixed inhibitors of both these enzymes, and no influence on IL-1 effects was observed with added eicosanoids. Among the clinically used disease modifying anti-arthritic agents, only auranofin and the immunoregulatory agent, tilomisole, were found effective in inhibiting resorption. Some auranofin analogues having chloride or nitrate leaving groups that inhibit DNA polymerase-alpha were found to be potent inhibitors of IL-1 induced resorption.
研究了一系列对类花生酸代谢及其他作用有不同影响的抗炎药物在体外抑制α-白细胞介素1(IL-1)诱导的软骨蛋白聚糖吸收的潜力。环氧合酶抑制剂、脂氧合酶抑制剂或这两种酶的混合抑制剂对吸收均无显著影响,添加类花生酸后对IL-1的作用也无影响。在临床使用的改善病情抗风湿药中,仅发现金诺芬和免疫调节剂替洛米唑可有效抑制吸收。一些具有抑制DNA聚合酶α的氯或硝酸离去基团的金诺芬类似物被发现是IL-1诱导吸收的有效抑制剂。