Bray M A
Eur J Pharmacol. 1984 Feb 10;98(1):61-7. doi: 10.1016/0014-2999(84)90109-2.
Several retinoids (tretinoin, retinol, retinal, retinyl acetate, etretinate and RO 10-1670) were tested in vitro for their ability to inhibit the generation of the leukocyte chemotactic factor leukotriene B4 (LTB4) from calcium ionophore-stimulated rat PMN in vitro. LTB4 activity was measured in vitro via bioassay using rat PMN aggregation and chemokinesis. Tretinoin, retinol, RO 10-1670 and retinal were active inhibitors of LTB4 generation with ID50S (microM) of 0.55-1.5, 5.9-6.5, 4.8-5.9 and 19-28.4 respectively whilst retinyl acetate and etretinate were inactive. Inhibition of the generation of LTB4 by tretinoin was confirmed by reverse phase-high pressure liquid chromatography. These results are discussed in the context of retinoid treatment of skin diseases such as psoriasis where inhibition of neutrophil accumulation during retinoid treatment has been reported.
对几种维甲酸(维甲酸、视黄醇、视黄醛、醋酸视黄酯、依曲替酯和RO 10-1670)进行了体外测试,以检测它们抑制钙离子载体刺激的大鼠多形核白细胞(PMN)体外生成白细胞趋化因子白三烯B4(LTB4)的能力。通过使用大鼠PMN聚集和趋化运动的生物测定法在体外测量LTB4活性。维甲酸、视黄醇、RO 10-1670和视黄醛是LTB4生成的活性抑制剂,其半数抑制浓度(ID50,微摩尔)分别为0.55 - 1.5、5.9 - 6.5、4.8 - 5.9和19 - 28.4,而醋酸视黄酯和依曲替酯无活性。通过反相高压液相色谱法证实了维甲酸对LTB4生成的抑制作用。在类维生素A治疗诸如牛皮癣等皮肤病的背景下讨论了这些结果,在类维生素A治疗期间已报道有中性粒细胞聚集的抑制作用。