Dahboul Fatima, Perrin-Sarrado Caroline, Boudier Ariane, Lartaud Isabelle, Schneider Raphaël, Leroy Pierre
Université de Lorraine, CITHÉFOR - EA 3452, Faculté de Pharmacie, BP 80403, 54001 Nancy Cedex, France.
Université de Lorraine et CNRS, Laboratoire Réactions et Génie des Procédés, UMR 7274, BP 20451, 54001 Nancy Cedex, France.
Eur J Pharmacol. 2014 May 5;730:171-9. doi: 10.1016/j.ejphar.2014.02.034. Epub 2014 Mar 10.
S-nitrosothiols (RSNO) are considered as potential drugs for delivering nitric oxide (NO) or related species in cardiovascular disorders associated with decrease in NO bioavailability. We have synthesized a new RSNO, i.e. S,S'-dinitrosobucillamine (BUC(NO)2), which combines in its structure two S-mononitrosothiols, S-nitroso-N-acetylpenicillamine (SNAP) and S-nitroso-N-acetylcysteine (NACNO). Synthesized BUC(NO)2 was structurally characterized using high-performance liquid chromatography/mass spectrometry (HPLC/MS), (1)H nuclear magnetic resonance ((1)H NMR), infrared (IR) and UV-visible spectroscopies, and thermal analysis; resulting data are consistent with the expected structure. The vasorelaxant effect of BUC(NO)2 was evaluated using isolated rat aortic rings and compared to SNAP, NACNO, and to an equimolar mixture of NACNO plus SNAP in order to mimic the number of NO contained in a BUC(NO)2 molecule. BUC(NO)2 (pD2=7.8±0.1) was more potent in vasorelaxation than NACNO (pD2=6.4±0.2), SNAP (pD2=6.7±0.1) and the mixture of SNAP plus NACNO (pD2=6.7±0.2). The release of NO from BUC(NO)2 was 6-fold that of the basal value and significantly higher than the release of NO from the SNAP plus NACNO mixture (4-fold increase versus basal value). Finally, the role of protein disulfide isomerase (PDI) in BUC(NO)2 metabolism was investigated. Vasorelaxant effect (pD2=6.8±0.2) and NO release decreased in the presence of a PDI inhibitor (both P<0.05 versus BUC(NO)2). In conclusion, BUC(NO)2 releases a larger amount of NO into the aorta, partially through PDI activation, and induces vasorelaxation at lower concentrations than other RSNO previously reported.
S-亚硝基硫醇(RSNO)被认为是在与一氧化氮(NO)生物利用度降低相关的心血管疾病中递送NO或相关物质的潜在药物。我们合成了一种新的RSNO,即S,S'-二亚硝基布西拉明(BUC(NO)2),其结构中结合了两个S-单亚硝基硫醇,S-亚硝基-N-乙酰青霉胺(SNAP)和S-亚硝基-N-乙酰半胱氨酸(NACNO)。使用高效液相色谱/质谱(HPLC/MS)、核磁共振氢谱(¹H NMR)、红外光谱(IR)和紫外可见光谱以及热分析对合成的BUC(NO)2进行结构表征;所得数据与预期结构一致。使用离体大鼠主动脉环评估BUC(NO)2的血管舒张作用,并与SNAP、NACNO以及NACNO加SNAP的等摩尔混合物进行比较,以模拟BUC(NO)2分子中所含NO的数量。BUC(NO)2(pD2 = 7.8±0.1)在血管舒张方面比NACNO(pD2 = 6.4±0.2)、SNAP(pD2 = 6.7±0.1)和SNAP加NACNO的混合物(pD2 = 6.7±0.2)更有效。BUC(NO)2释放的NO是基础值的6倍,并且显著高于SNAP加NACNO混合物释放的NO(相对于基础值增加4倍)。最后,研究了蛋白质二硫键异构酶(PDI)在BUC(NO)2代谢中的作用。在存在PDI抑制剂的情况下,血管舒张作用(pD2 = 6.8±0.2)和NO释放降低(两者与BUC(NO)2相比均P<0.05)。总之,BUC(NO)2向主动脉中释放大量NO,部分通过PDI激活,并且在比先前报道的其他RSNO更低的浓度下诱导血管舒张。