脂质调节剂Resolvins是新近发现的一系列由奥米伽-3脂肪酸释放的天然小分子,对一系列急性慢性疾病具有治疗潜力,特别是在消除感染和恢复免疫稳态方面。
如今,研究人员在4月在线出版的《自然—医学》期刊上报告,Resolvins有可能是一种治疗炎症疼痛的新型镇痛药,可以缓解炎症带的疼痛,并作用于脊柱以预防慢性疼痛。
关节炎和术后痛等是一种因组织损伤所引发的炎症疼痛,组织损伤所释放的物质会增强炎症并在脊柱中发生作用导致慢性疼痛。
Ru-RongJi和同事发现,由某种奥米伽-3脂肪酸所产生的两种脂质调节剂RvE1和RvD1能缓解小鼠的疼痛症状。他们指出,在缓解疼痛方面,RvE1是它的父辈化合物力量的1万倍,而且,一种人工合成的化合物Chemerin所需要结合的受体与RvE1和RvD1一样,这种人工化合物也能明显降低疼痛症状。除了抗炎症效用之外,他们还发现RvE1可作用于脊柱以预防因神经元活动所导致的永久性慢性疼痛。而且,这种止痛作用并不会影响正常的疼痛反应。(生物谷Bioon.com)
生物谷推荐原始出处:
Nature Medicine Published online: 11 April 2010 | doi:10.1038/nm.2123
Resolvins RvE1 and RvD1 attenuate inflammatory pain via central and peripheral actions
Zhen-Zhong Xu1,3, Ling Zhang1,3, Tong Liu1, Jong Yeon Park1, Temugin Berta1, Rong Yang2, Charles N Serhan2,3 & Ru-Rong Ji1,3
AbstractInflammatory pain, such as arthritis pain, is a growing health problem1. Inflammatory pain is generally treated with opioids and cyclooxygenase (COX) inhibitors, but both are limited by side effects. Recently, resolvins, a unique family of lipid mediators, including RvE1 and RvD1 derived from omega-3 polyunsaturated fatty acid, have shown marked potency in treating disease conditions associated with inflammation2, 3. Here we report that peripheral (intraplantar) or spinal (intrathecal) administration of RvE1 or RvD1 in mice potently reduces inflammatory pain behaviors induced by intraplantar injection of formalin, carrageenan or complete Freund's adjuvant (CFA), without affecting basal pain perception. Intrathecal RvE1 injection also inhibits spontaneous pain and heat and mechanical hypersensitivity evoked by intrathecal capsaicin and tumor necrosis factor-α (TNF-α). RvE1 has anti-inflammatory activity by reducing neutrophil infiltration, paw edema and proinflammatory cytokine expression. RvE1 also abolishes transient receptor potential vanilloid subtype-1 (TRPV1)- and TNF-α–induced excitatory postsynaptic current increases and TNF-α–evoked N-methyl-D-aspartic acid (NMDA) receptor hyperactivity in spinal dorsal horn neurons via inhibition of the extracellular signal–regulated kinase (ERK) signaling pathway. Thus, we show a previously unknown role for resolvins in normalizing the spinal synaptic plasticity that has been implicated in generating pain hypersensitivity. Given the potency of resolvins and the well-known side effects of opioids and COX inhibitors, resolvins may represent new analgesics for treating inflammatory pain.