Shen Zhen, Guo Yun-Dan, Tang Ming-Ze, Zhou Ping, Su Yu-Xin, Shen Hao-Ran, Li Tao, Jiang Wei, Han Yan-Xing, Tie Cai, Cui Jing-Jing, Gao Tian-Le, Jiang Jian-Dong
Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.
Heart Failure Center, Fuwai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100037, China.
Antioxidants (Basel). 2024 Jul 2;13(7):803. doi: 10.3390/antiox13070803.
Pregabalin is a medication primarily used in the treatment of neuropathic pain and anxiety disorders, owing to its gabapentinoid properties. Pregabalin monotherapy faces limitations due to its variable efficacy and dose-dependent adverse reactions. In this study, we conducted a comprehensive investigation into the potentiation of pregabalin's analgesic effects by dexborneol, a neuroprotective bicyclic monoterpenoid compound. We performed animal experiments where pain models were induced using two methods: peripheral nerve injury, involving axotomy and ligation of the tibial and common peroneal nerves, and incisional pain through a longitudinal incision in the hind paw, while employing a multifaceted methodology that integrates behavioral pharmacology, molecular biology, neuromorphology, and lipidomics to delve into the mechanisms behind this potentiation. Dexborneol was found to enhance pregabalin's efficacy by promoting its transportation to the central nervous system, disrupting self-amplifying vicious cycles via the reduction of HMGB1 and ATP release, and exerting significant anti-oxidative effects through modulation of central lipid metabolism. This combination therapy not only boosted pregabalin's analgesic property but also notably decreased its side effects. Moreover, this therapeutic cocktail exceeded basic pain relief, effectively reducing neuroinflammation and glial cell activation-key factors contributing to persistent and chronic pain. This study paves the way for more tolerable and effective analgesic options, highlighting the potential of dexborneol as an adjuvant to pregabalin therapy.
普瑞巴林是一种主要用于治疗神经性疼痛和焦虑症的药物,因其具有加巴喷丁类药物的特性。普瑞巴林单一疗法由于其疗效可变和剂量依赖性不良反应而面临局限性。在本研究中,我们对右旋龙脑(一种具有神经保护作用的双环单萜类化合物)增强普瑞巴林镇痛效果进行了全面研究。我们进行了动物实验,采用两种方法诱导疼痛模型:外周神经损伤,包括切断和结扎胫神经和腓总神经,以及通过后爪纵向切口造成切口疼痛,同时采用行为药理学、分子生物学、神经形态学和脂质组学等多方面方法来深入探究这种增强作用背后的机制。结果发现,右旋龙脑通过促进普瑞巴林向中枢神经系统的转运、通过减少HMGB1和ATP释放来打破自我放大的恶性循环以及通过调节中枢脂质代谢发挥显著的抗氧化作用,从而增强普瑞巴林的疗效。这种联合疗法不仅增强了普瑞巴林的镇痛特性,还显著降低了其副作用。此外,这种治疗组合超出了基本的疼痛缓解效果,有效减轻了神经炎症和神经胶质细胞活化,而神经炎症和神经胶质细胞活化是导致持续性和慢性疼痛的关键因素。这项研究为更可耐受和有效的镇痛选择铺平了道路,突出了右旋龙脑作为普瑞巴林治疗辅助药物的潜力。