Department of Pharmacology, Ribeirao Preto Medical School, University of São Paulo Av. Bandeirantes 3900, 14049-900, Ribeirao Preto, SP, Brazil.
Department of Physiology, Pharmacology and Neuroscience, Sophie Davis School of Biomedical Education, City University of New York Medical School New York, NY, 10031 ; Avicenna Pharmaceuticals Inc. New York, NY, 10019.
Pharmacol Res Perspect. 2015 Jun;3(3):e00133. doi: 10.1002/prp2.133. Epub 2015 May 8.
The development of nitric oxide (NO)- and hydrogen sulfide (H2S)-releasing nonsteroidal anti-inflammatory drugs (NSAIDs) has generated more potent anti-inflammatory drugs with increased safety profiles. A new hybrid molecule incorporating both NO and H2S donors into aspirin (NOSH-aspirin) was recently developed. In the present study, the antinociceptive activity of this novel molecule was compared with aspirin in different models of inflammatory pain. It was found that NOSH-aspirin inhibits acetic acid-induced writhing response and carrageenan (Cg)-induced inflammatory hyperalgesia in a dose-dependent (5-150 μmol/kg, v.o.) manner, which was superior to the effect of the same doses of aspirin. NOSH-aspirin's antinociceptive effect was also greater and longer compared to aspirin upon complete Freund's adjuvant (CFA)-induced inflammatory hyperalgesia. Mechanistically, NOSH-aspirin, but not aspirin, was able to reduce the production/release of interleukin-1 beta (IL-1β) during Cg-induced paw inflammation. Furthermore, NOSH-aspirin, but not aspirin, reduced prostaglandin E2-induced hyperalgesia, which was prevented by treatment with a ATP-sensitive potassium channel (KATP) blocker (glibenclamide; glib.). Noteworthy, the antinociceptive effect of NOSH-aspirin was not associated with motor impairment. The present results indicate that NOSH-aspirin seems to present greater potency than aspirin to reduce inflammatory pain in several models. The enhanced effects of NOSH-aspirin seems to be due to its ability to reduce the production of pronociceptive cytokines such as IL-1 β and directly block hyperalgesia caused by a directly acting hyperalgesic mediator in a mechanism dependent on modulation of KATP channels. In conclusion, we would like to suggest that NOSH-aspirin represents a prototype of a new class of analgesic drugs with more potent effects than the traditional NSAID, aspirin.
一氧化氮(NO)和硫化氢(H2S)释放型非甾体抗炎药(NSAIDs)的发展产生了更有效的抗炎药物,具有更高的安全性。最近开发了一种将NO 和 H2S 供体结合到阿司匹林(NOSH-aspirin)中的新型混合分子。在本研究中,与阿司匹林相比,比较了这种新型分子在不同炎症性疼痛模型中的镇痛活性。结果发现,NOSH-aspirin 以剂量依赖性方式(5-150 μmol/kg,口服)抑制乙酸引起的扭体反应和角叉菜胶(Cg)诱导的炎症性痛觉过敏,效果优于相同剂量的阿司匹林。与完全弗氏佐剂(CFA)诱导的炎症性痛觉过敏相比,NOSH-aspirin 的镇痛作用也更大且持续时间更长。从机制上讲,NOSH-aspirin 可减少 Cg 诱导的爪炎症期间白细胞介素-1β(IL-1β)的产生/释放,而阿司匹林则不能。此外,NOSH-aspirin 可减少前列腺素 E2 引起的痛觉过敏,而这种作用可被 ATP 敏感性钾通道(KATP)阻断剂(格列本脲;glib.)所阻断。值得注意的是,NOSH-aspirin 的镇痛作用与运动障碍无关。本研究结果表明,NOSH-aspirin 似乎比阿司匹林更有效地减轻几种模型中的炎症性疼痛。NOSH-aspirin 增强的作用似乎是由于其减少致痛细胞因子(如 IL-1β)产生的能力以及直接阻断直接作用的致痛介质引起的痛觉过敏的能力,该作用机制依赖于 KATP 通道的调节。总之,我们建议 NOSH-aspirin 代表一类新型镇痛药的原型,其作用比传统 NSAID 阿司匹林更强。