Haynes D R, Wright P F, Gadd S J, Whitehouse M W, Vernon-Roberts B
Department of Pathology, University of Adelaide, South Australia.
Agents Actions. 1993 May;39(1-2):49-58. doi: 10.1007/BF01975714.
Aspirin and salicylate are transformed by stimulated human polymorphonuclear leucocytes (PMN), likely to be found at inflammatory sites, into both 2,3- and 2,5-dihydroxybenzoates (DHB). These DHB inhibit both the production of hydrogen peroxide by stimulated human PMN and prostaglandin (PG) E2 by activated rat macrophages. In contrast, DHB stimulated production of interleukin (IL)-1 and tumour necrosis factor (TNF) but inhibited IL-6 production by rat macrophages. These effects were probably a consequence of PGE2 inhibition. Gentisate (2,5-DHB) and homogentisate (a tyrosine metabolite) inhibited the lymphoproliferative action of IL-1. Some related phenols, e.g. 5-aminosalicylate, inhibited H2O2 production but had little effect on PGE2 production. These findings suggest that the local synthesis of DHB may contribute to the overall anti-inflammatory activity of salicylate, which (unlike aspirin) has little direct effect on PG production.
阿司匹林和水杨酸盐可被受刺激的人多形核白细胞（PMN，可能存在于炎症部位）转化为2,3-二羟基苯甲酸酯和2,5-二羟基苯甲酸酯（DHB）。这些DHB既能抑制受刺激的人PMN产生过氧化氢，也能抑制活化的大鼠巨噬细胞产生前列腺素（PG）E2。相反，DHB刺激大鼠巨噬细胞产生白细胞介素（IL）-1和肿瘤坏死因子（TNF），但抑制其产生IL-6。这些作用可能是PGE2受到抑制的结果。龙胆酸盐（2,5-DHB）和尿黑酸盐（一种酪氨酸代谢产物）抑制IL-1的淋巴细胞增殖作用。一些相关酚类，如5-氨基水杨酸盐，可抑制H2O2的产生，但对PGE2的产生影响很小。这些发现表明，DHB的局部合成可能有助于水杨酸盐的整体抗炎活性，水杨酸盐（与阿司匹林不同）对PG的产生几乎没有直接影响。
