Schwalm S F, Lewis A J, Hand J M
Prostaglandins. 1987 Jan;33(1):113-9. doi: 10.1016/0090-6980(87)90309-1.
The effects of the 5-lipoxygenase inhibitors nordihydroguiaretic acid (NDGA), 5, 8, 11, 14-eicosatetraynoic acid (ETYA), 1-phenyl-3-pyrazolidone (phenidone) and BW-755c, on the contractile response to LTC4 or LTD4 were examined on the isolated guinea pig trachea. Responses to either LTC4 or LTD4 were obtained on indomethacin treated tissues, in the presence of either L-serine-borate complex or L-cysteine, respectively, to inhibit metabolic conversion of the leukotrienes. NDGA (30 microM) and ETYA (100 microM) produced a selective competitive antagonism of LTD4-induced contractions, while phenidone antagonized both LTC4- and LTD4-induced responses in a non-competitive manner. In contrast, BW-755c (30 microM) did not significantly antagonize LTC4 or LTD4 concentration-response curves. The results suggest that leukotriene antagonism may be produced by large concentrations of some 5-lipoxygenase inhibitors.
在离体豚鼠气管上研究了5-脂氧合酶抑制剂去甲二氢愈创木酸（NDGA）、5,8,11,14-二十碳四炔酸（ETYA）、1-苯基-3-吡唑烷酮（非那宗）和BW-755c对LTC4或LTD4收缩反应的影响。在吲哚美辛处理的组织上分别在L-丝氨酸-硼酸盐复合物或L-半胱氨酸存在的情况下获得对LTC4或LTD4的反应，以抑制白三烯的代谢转化。NDGA（30μM）和ETYA（100μM）对LTD4诱导的收缩产生选择性竞争性拮抗作用，而非那宗以非竞争性方式拮抗LTC4和LTD4诱导的反应。相比之下，BW-755c（30μM）并未显著拮抗LTC4或LTD4的浓度-反应曲线。结果表明，某些5-脂氧合酶抑制剂的高浓度可能产生白三烯拮抗作用。
