Sinclair R, Eriksson A S, Gretzer C, Cassuto J, Thomsen P
Department of Anaesthesiology, Central Hospital, Mölndal, Sweden.
Acta Anaesthesiol Scand. 1993 Feb;37(2):159-65. doi: 10.1111/j.1399-6576.1993.tb03693.x.
The anti-inflammatory effects of the amide local anaesthetics lidocaine and bupivacaine were evaluated in vitro by examination of the metabolic activation and secretory responses of human polymorphonuclear granulocytes (PMNGs) and mononuclear cells. Pretreatment with lidocaine or bupivacaine had a dose-dependent inhibitory effect on PMNG luminol-amplified chemiluminescence stimulated by bovine serum albumin (BSA)/anti-BSA immune complexes (IC) or by serum-opsonized zymosan (SOZ) particles. Both lidocaine and bupivacaine inhibited the release of the inflammatory mediators leukotriene B4 (LTB4) and interleukin-1 (IL-1) evaluated by radioimmunoassay (RIA). Pretreatment of suspended PMNGs and monocytes with the anaesthetics caused a marked inhibition of LTB4 release when the cells were stimulated with SOZ. In short-term (24 h) cultures of mononuclear cells the addition of lidocaine or bupivacaine reduced, in a dose-dependent manner, the level of IL-1 detected after stimulation with lipopolysaccharide (LPS). In all three assays (chemiluminescence, LTB4 and IL-1 RIA) bupivacaine was found to be more potent than lidocaine. The present results show that amide local anaesthetics have marked suppressive effects on the metabolic activation and secretory functions of leukocytes stimulated by different agonists. Although the detailed mechanisms for these effects are not known, they may explain part of the potent anti-inflammatory actions of local anaesthetics previously described in vivo.
通过检测人多形核粒细胞（PMNGs）和单核细胞的代谢激活及分泌反应，在体外评估了酰胺类局部麻醉药利多卡因和布比卡因的抗炎作用。用利多卡因或布比卡因预处理对牛血清白蛋白（BSA）/抗BSA免疫复合物（IC）或血清调理酵母聚糖（SOZ）颗粒刺激的PMNG鲁米诺增强化学发光具有剂量依赖性抑制作用。利多卡因和布比卡因均抑制通过放射免疫测定（RIA）评估的炎症介质白三烯B4（LTB4）和白细胞介素-1（IL-1）的释放。当用SOZ刺激细胞时，用麻醉药预处理悬浮的PMNG和单核细胞可显著抑制LTB4的释放。在单核细胞的短期（24小时）培养中，添加利多卡因或布比卡因以剂量依赖性方式降低了用脂多糖（LPS）刺激后检测到的IL-1水平。在所有三种测定（化学发光、LTB4和IL-1 RIA）中，发现布比卡因比利多卡因更有效。目前的结果表明，酰胺类局部麻醉药对不同激动剂刺激的白细胞的代谢激活和分泌功能具有显著的抑制作用。尽管这些作用的详细机制尚不清楚，但它们可能部分解释了先前在体内描述的局部麻醉药强大的抗炎作用。
