Price G H
Clin Chim Acta. 1979 Jun 15;94(3):211-7. doi: 10.1016/0009-8981(79)90067-6.
Several sulfonamides used as antibacterial or diuretic drugs are potent alkaline phosphatase inhibitors. The mechanism of inhibition may involve binding of the zinc in the active site of the enzyme by the unbonded electron pair on the sulfonamide group nitrogen atom as well as binding of the drug to a second site. Addition of progressively larger groups to this nitrogen leads to an increasing loss of inhibitory capability. Isoenzymes from human liver, bone, kidney, granulation tissue and intestine are inhibited to a similar extent while the placenta isoenzyme is more resistant. It is suggested that some pharmacologic actions of sulfonamides may be due to inhibition of alkaline phosphatase, rather than carbonic anhydrase.
几种用作抗菌或利尿药物的磺胺类药物是强效碱性磷酸酶抑制剂。抑制机制可能涉及磺胺基团氮原子上未键合的电子对与酶活性位点中的锌结合，以及药物与第二个位点的结合。向该氮原子添加逐渐增大的基团会导致抑制能力逐渐丧失。来自人肝脏、骨骼、肾脏、肉芽组织和肠道的同工酶受到的抑制程度相似，而胎盘同工酶更具抗性。有人提出，磺胺类药物的某些药理作用可能是由于抑制碱性磷酸酶，而非碳酸酐酶。
