Lanni C, Becker E L
Int Arch Allergy Appl Immunol. 1985;76(3):214-7. doi: 10.1159/000233694.
The lipoxygenase and/or cyclooxygenase inhibitors nordihydroguaiaretic acid (NDGA), 4,8,11,14-eicosatetraynoic acid (ETYA) and the bioflavonoid, quercetin, also inhibit phospholipase A2 (phosphatidase 2-acyl hydrolase; EC 3.1.1.4) activity of neutrophil acid extracts and sonicates. The IC50 are 13 microM for NDGA, 22 microM for ETYA, and 100 microM for quercetin when measured on the neutrophil acid extracts; the IC50 obtained with the sonicates are 11 microM, 12 microM and 57 microM, respectively. p-Bromophenylacyl bromide (BPB) inhibits the phospholipase A2 activity of neutrophil acid extracts with an IC50 of 10 microM. In contrast, intact neutrophils incubated for up to 1 h with BPB, washed to remove the drug, and sonicated to expose the phospholipase A2, lose less than 20% of their activity. This strongly suggests that BPB does not inhibit neutrophil function by preventing phospholipase action.
脂氧合酶和/或环氧化酶抑制剂去甲二氢愈创木酸（NDGA）、4,8,11,14-二十碳四炔酸（ETYA）以及生物类黄酮槲皮素，也能抑制中性粒细胞酸性提取物和超声破碎物的磷脂酶A2（磷脂酶2-酰基水解酶；EC 3.1.1.4）活性。以中性粒细胞酸性提取物进行测定时，NDGA的半数抑制浓度（IC50）为13微摩尔，ETYA为22微摩尔，槲皮素为100微摩尔；用超声破碎物测得的IC50分别为11微摩尔、12微摩尔和57微摩尔。对溴苯甲酰溴（BPB）抑制中性粒细胞酸性提取物的磷脂酶A2活性，IC50为10微摩尔。相比之下，完整的中性粒细胞与BPB孵育长达1小时，经洗涤以去除药物，然后超声破碎以暴露磷脂酶A2，其活性损失不到20%。这有力地表明，BPB并非通过阻止磷脂酶作用来抑制中性粒细胞功能。
