Eskandari Nahid, Wickramasinghe Thulani, Peachell Peter T
Academic Unit of Molecular Pharmacology and Pharmacogenetics, University of Sheffield, Royal Hallamshire Hospital (Floor L), Sheffield S10 2JF.
Br J Pharmacol. 2004 Aug;142(8):1265-72. doi: 10.1038/sj.bjp.0705892. Epub 2004 Jul 20.
The aim of the present study was to determine whether inhibition of cyclic nucleotide phosphodiesterase (PDE) modulates the stimulated generation of the cytokines, interleukin-4 (IL-4) and IL-13, from human basophils. This was addressed by evaluating the effects of both nonselective and selective inhibitors of PDEs on the generation of cytokines from basophils. The nonselective PDE inhibitors, isobutyl-methylxanthine (IBMX) and theophylline, attenuated the IgE-mediated generation of IL-4 and IL-13 and, also, the release of histamine from basophils. The effects of the isoform-selective inhibitors, 8-methoxymethyl-IBMX (PDE 1 inhibitor), siguazodan (PDE3 inhibitor), rolipram (PDE4 inhibitor), denbufylline (PDE4 inhibitor), Org 30029 (mixed PDE3 and 4 inhibitor) and zaprinast (PDE5 inhibitor), were studied. Of these selective compounds, only rolipram, denbufylline and Org 30029 inhibited the IgE-dependent generation of IL-4, IL-13 and histamine from basophils to a statistically significant (P<0.05) degree. The effects of isoform-selective inhibitors on basophils activated by IL-3 were evaluated. The IL-3-induced generation of IL-4, IL-13 and histamine was inhibited to a statistically significant (P<0.05) extent, only by compounds that act as inhibitors of PDE4. These data suggest that inhibition of PDE4 can regulate the generation of cytokines from human basophils.
本研究的目的是确定环核苷酸磷酸二酯酶(PDE)的抑制是否会调节人嗜碱性粒细胞受刺激后细胞因子白细胞介素-4(IL-4)和IL-13的生成。通过评估PDE的非选择性和选择性抑制剂对嗜碱性粒细胞细胞因子生成的影响来解决这一问题。非选择性PDE抑制剂异丁基甲基黄嘌呤(IBMX)和茶碱可减弱IgE介导的IL-4和IL-13生成,以及嗜碱性粒细胞中组胺的释放。研究了同工型选择性抑制剂8-甲氧基甲基-IBMX(PDE 1抑制剂)、西呱旦(PDE3抑制剂)、咯利普兰(PDE4抑制剂)、登布茶碱(PDE4抑制剂)、Org 30029(PDE3和4混合抑制剂)和扎普司特(PDE5抑制剂)的作用。在这些选择性化合物中,只有咯利普兰、登布茶碱和Org 30029对嗜碱性粒细胞中IgE依赖的IL-4、IL-13和组胺生成的抑制达到统计学显著(P<0.05)程度。评估了同工型选择性抑制剂对IL-3激活的嗜碱性粒细胞的作用。只有作为PDE4抑制剂的化合物能将IL-3诱导的IL-4、IL-13和组胺生成抑制到统计学显著(P<0.05)程度。这些数据表明,抑制PDE4可调节人嗜碱性粒细胞中细胞因子的生成。