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青藤碱可减轻实验性诱导的类风湿性关节炎小鼠的机械性超敏反应。

Sinomenine alleviates mechanical hypersensitivity in mice with experimentally induced rheumatoid arthritis.

作者信息

Gao Tianle, Shi Tiansheng, Wiesenfeld-Hallin Zsuzsanna, Svensson Camilla I, Xu Xiao-Jun

机构信息

Department of Physiology and Pharmacology, Section of Integrative Pain Research, Karolinska Institutet, Stockholm, Sweden.

Department of Physiology and Pharmacology, Section of Molecular Pain Research, Karolinska Institutet, Stockholm, Sweden.

出版信息

Scand J Pain. 2015 Apr 1;7(1):9-14. doi: 10.1016/j.sjpain.2014.12.003.

Abstract

Background and aims We have previously reported that sinomenine, an alkaloid isolated from the root of the plant Sinomenium acutum, had antinociceptive effect in rodent models of acute inflammatory or neuropathic pain. As a traditional medicine, sinomenine is used in China to treat rheumatoid arthritis (RA). Methods In the present study, we evaluated the potential antinociceptive effect of sinomenine in a mouse model of RA, collagen type II antibody (CII Ab) induced arthritis (CAIA) after acute and chronic administration. Results As single administration, sinomenine at 40 or 80 mg/kg significantly reduced mechanical hypersensitivity both at the time of peak joint inflammation (days 11-19 after CII Ab injection) or during the post-inflammatory phase (days 35-54). No tolerance to the effect of 80 mg/kg sinomenine was observed during repeated injection twice a day for 5 days from day 11 to day 19 or from day 49 to day 53 after CII Ab injection in CAIA mice. Conclusions We have shown that sinomenine is effective in alleviating localized and spread hypersensitivities in CAIA mice both during acute inflammation and in post-inflammatory phase. Further, repeated sinomenine administration has elevated the baseline mechanical threshold without producing tolerance. Implications Sinomenine may be clinically useful to treat chronic pain in RA, including wide-spread pain which appears to be a difficult clinical problem despite the improvement in the acute treatment of RA by disease modifying agents.

摘要

背景与目的 我们之前报道过,从青藤属植物根中分离出的生物碱青藤碱在急性炎症或神经性疼痛的啮齿动物模型中具有抗伤害感受作用。作为一种传统药物,青藤碱在中国用于治疗类风湿关节炎(RA)。方法 在本研究中,我们评估了青藤碱在类风湿关节炎小鼠模型(II型胶原抗体(CII Ab)诱导的关节炎(CAIA))急性和慢性给药后的潜在抗伤害感受作用。结果 单次给药时,40或80mg/kg的青藤碱在关节炎症高峰期(CII Ab注射后第11 - 19天)或炎症后期(第35 - 54天)均显著降低机械性超敏反应。在CAIA小鼠中,从CII Ab注射后第11天至第19天或第49天至第53天每天两次重复注射80mg/kg青藤碱期间,未观察到对其作用的耐受性。结论 我们已表明,青藤碱在CAIA小鼠的急性炎症期和炎症后期均能有效减轻局部和扩散的超敏反应。此外,重复给予青藤碱可提高基线机械阈值且不会产生耐受性。意义 青藤碱在临床上可能有助于治疗类风湿关节炎的慢性疼痛,包括广泛疼痛,尽管疾病改善药物在类风湿关节炎的急性治疗中有所改善,但广泛疼痛似乎仍是一个棘手的临床问题。

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