Piller N B
Br J Exp Pathol. 1976 Jun;57(3):266-73.
A very strong correlation has been shown to exist between acid and neutral protease activity levels in the skin, the acid protease activity level of the oedema fluid, and the oedema-reducing ability of the benzo-pyrones and related drugs. Macrophages, which are believed to be the main cells affected by the drugs, are very common in thermally injured tissues. Their lysosomal enzymes work at an acid pH. Since the main acid protease is cathepsin D, the overall acid protease levels are representative of changes in cathepsin D levels. Elevated levels are concomitant with more complete and rapid digestion of accumulated protein. The resulting fragments then can rapidly leave the injured tissues, freeing the oedema fluid. This form of proteolysis is very much different from that which is used by pharmacologists as a measure of inflammation. Normal proteolysis in inflammation represents an estimate of tissue derangement, but the proteolysis induced by drugs such as the benzo-pyrones represents a means of lessening some of the more injurious effects of this derangement. The results presented here strongly confirm this.
皮肤中的酸性和中性蛋白酶活性水平、水肿液的酸性蛋白酶活性水平与苯并吡喃及相关药物的消肿能力之间已显示出很强的相关性。巨噬细胞被认为是受这些药物影响的主要细胞，在热损伤组织中非常常见。它们的溶酶体酶在酸性pH值下起作用。由于主要的酸性蛋白酶是组织蛋白酶D，总的酸性蛋白酶水平代表了组织蛋白酶D水平的变化。水平升高伴随着积累蛋白质更完全和快速的消化。产生的片段随后可以迅速离开受伤组织，释放水肿液。这种蛋白水解形式与药理学家用作炎症指标的形式非常不同。炎症中的正常蛋白水解代表了组织紊乱的一种估计，但苯并吡喃等药物诱导的蛋白水解代表了减轻这种紊乱一些更有害影响的一种手段。这里给出的结果有力地证实了这一点。
