Gibert C, Vila L, Puig L, Solá J, Moragas J M
Unitat de Recerca Biomédica (Eicosanoids Laboratory), Hospital de la Santa Creu i Sant Pau, Barcelona, Spain.
Skin Pharmacol. 1989;2(2):86-92. doi: 10.1159/000210805.
Lonapalene was studied as a topical antipsoriatic agent on the basis of its inhibitory effect on 5-lipoxygenase. We studied the effect of lonapalene on the metabolism of exogenous arachidonic acid in washed platelet suspensions by RP-HPLC. Lonapalene was shown to inhibit platelet cyclooxygenase, with substrate diversion towards 12-HETE production. The pattern of inhibition was similar to that of indometacin, although lonapalene was about 1,000 times weaker. The dual inhibition of lonapalene and concomitant deviation of arachidonic acid metabolism may have potential implications, with regard to therapeutic indications and side effects, which deserve further study.
基于洛那帕林对5-脂氧合酶的抑制作用，对其作为一种外用抗银屑病药物进行了研究。我们通过反相高效液相色谱法研究了洛那帕林对洗涤过的血小板悬浮液中外源性花生四烯酸代谢的影响。结果表明，洛那帕林可抑制血小板环氧化酶，使底物转向生成12-羟基二十碳四烯酸（12-HETE）。尽管洛那帕林的抑制作用比吲哚美辛弱约1000倍，但其抑制模式与吲哚美辛相似。洛那帕林的双重抑制作用以及花生四烯酸代谢的伴随偏差，在治疗适应症和副作用方面可能具有潜在意义，值得进一步研究。
