Mühl H, Pfeilschifter J
Department of Pharmacology, University of Basel, Switzerland.
Biochem J. 1994 Oct 15;303 ( Pt 2)(Pt 2):607-12. doi: 10.1042/bj3030607.
In cultured glomerular mesangial cells, interleukin 1 beta (IL-1 beta) has been shown to induce a dose- and time-dependent accumulation of nitrite, a stable metabolite of nitric oxide (NO). In parallel, increased levels of mRNA of an inducible macrophage-type of nitric oxide synthase (iNOS) were observed after incubating mesangial cells with IL-1 beta. Here we report that addition of the biologically active phorbol esters, phorbol 12-myristate 13-acetate (PMA) and phorbol 12,13-dibutyrate (PDBu), dose-dependently inhibited the IL-1 beta-stimulated increase in iNOS mRNA levels and nitrite production. In contrast, the biologically inactive phorbol ester 4 alpha-phorbol 12,13-didecanoate, had no effect on cytokine induction of iNOS and nitrite formation. Incubation of mesangial cells with PMA or PDBu alone, in the absence of IL-1 beta, did not trigger any iNOS expression. Time-course studies indicated that phorbol ester needs to be added for only 1 h in order to maximally inhibit cytokine-induced nitrite production. Down-regulation of protein kinase C (PKC)-alpha and -delta isoenzymes by 8 h PMA or PDBu treatment before stimulation with IL-1 beta still resulted in full inhibition of iNOS induction. In contrast, a 24 h treatment of mesangial cells with PMA or PDBu, a regimen that also causes depletion of PKC-epsilon, abolished inhibition of IL-1 beta-induced iNOS expression and nitrite production. In addition, the selective PKC inhibitor calphostin C potentiated IL-1 beta induction of iNOS activity. In summary these data suggest that IL-1 beta induction of iNOS expression is tonically suppressed by PKC and the epsilon-isoenzyme is the most likely candidate mediating this effect.
在培养的肾小球系膜细胞中,白细胞介素1β(IL-1β)已被证明可诱导亚硝酸盐呈剂量和时间依赖性积累,亚硝酸盐是一氧化氮(NO)的一种稳定代谢产物。同时,在用IL-1β孵育系膜细胞后,观察到诱导型巨噬细胞一氧化氮合酶(iNOS)的mRNA水平升高。在此我们报告,添加具有生物活性的佛波酯、佛波醇12-肉豆蔻酸酯13-乙酸酯(PMA)和佛波醇12,13-二丁酸酯(PDBu),可剂量依赖性地抑制IL-1β刺激引起的iNOS mRNA水平升高和亚硝酸盐产生。相反,无生物活性的佛波酯4α-佛波醇12,13-二癸酸酯对iNOS的细胞因子诱导和亚硝酸盐形成没有影响。在无IL-1β的情况下,单独用PMA或PDBu孵育系膜细胞不会触发任何iNOS表达。时间进程研究表明,佛波酯只需添加1小时就能最大程度地抑制细胞因子诱导的亚硝酸盐产生。在用IL-1β刺激前,用PMA或PDBu处理8小时使蛋白激酶C(PKC)-α和-δ同工酶下调,仍能完全抑制iNOS诱导。相反,用PMA或PDBu对系膜细胞进行24小时处理(该方案也会导致PKC-ε耗竭),则消除了对IL-1β诱导的iNOS表达和亚硝酸盐产生的抑制作用。此外,选择性PKC抑制剂钙泊三醇增强了IL-1β对iNOS活性的诱导。总之,这些数据表明,PKC对IL-1β诱导的iNOS表达有持续性抑制作用,而ε同工酶最有可能介导这种效应。