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关节内注射分子 14G1862 系统:在骨关节炎大鼠模型中的镇痛和保护作用。

Intra-Articular Route for the System of Molecules 14G1862 from : Pain Relieving and Protective Effects in a Rat Model of Osteoarthritis.

机构信息

Department of Neuroscience, Psychology, Drug Research and Child Health-NEUROFARBA-Pharmacology and Toxicology Section, University of Florence, Viale Gaetano Pieraccini 6, 50139 Florence, Italy.

Aboca SpA Società Agricola, Innovation & Medical Science Division, Loc. Aboca 20, 52037 Sansepolcro, Italy.

出版信息

Nutrients. 2020 May 31;12(6):1618. doi: 10.3390/nu12061618.

Abstract

Current pharmacological therapies for the management of chronic articular diseases are far from being satisfactory, so new strategies need to be investigated. We tested the intra-articular pain relieving properties of a system of molecules from a characterized extract (14G1862) in a rat model of osteoarthritis induced by monoiodoacetate (MIA). 14G1862 (0.2-2 mg mL) was intra-articularly (i.a.) injected 7 days after MIA, behavioural and histological evaluations were performed 14, 30 and 60 days after treatments. Moreover, the effect of 14G1862 on nitrate production and iNOS expression in RAW 264.7 macrophages stimulated with LPS was assessed. , 14G1862 treatment attenuated LPS-induced NO production and iNOS expression in a comparable manner to celecoxib. , 14G1862 significantly reduced mechanical allodynia and hyperalgesia, spontaneous pain and motor alterations starting on day 14 up to day 60. The efficacy was higher or comparable to that evoked by triamcinolone acetonide (100 μg i.a.) used as reference drug. Histological evaluation highlighted the improvement of several morphological parameters in MIA + 14G1862-treated animals with particularly benefic effects on joint space and fibrin deposition. In conclusion, i.a. treatment with is a candidate to be a novel effective approach for osteoarthritis therapy.

摘要

当前用于治疗慢性关节疾病的药物疗法远不能令人满意,因此需要研究新的策略。我们在碘乙酸(MIA)诱导的骨关节炎大鼠模型中测试了一种特征性提取物(14G1862)的分子系统的关节内止痛特性。在 MIA 后 7 天,将 14G1862(0.2-2 mg mL)关节内注射,在治疗后 14、30 和 60 天进行行为和组织学评估。此外,还评估了 14G1862 对 LPS 刺激的 RAW 264.7 巨噬细胞中硝酸盐产生和 iNOS 表达的影响。结果表明,14G1862 以与塞来昔布相当的方式减弱了 LPS 诱导的 NO 产生和 iNOS 表达。结果表明,14G1862 从第 14 天开始显著减轻机械性痛觉过敏和痛觉过敏、自发性疼痛和运动改变,直至第 60 天。疗效高于或相当于作为参考药物的曲安奈德(100 μg 关节内注射)。组织学评估突出了 MIA + 14G1862 治疗动物的几种形态参数的改善,特别是对关节间隙和纤维蛋白沉积有有益的影响。总之,关节内治疗是治疗骨关节炎的一种有前途的新方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c571/7352185/55f7c8d34799/nutrients-12-01618-g001.jpg

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