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一种新型香豆素衍生物,8-甲氧基色原酮-2-酮通过下调一氧化氮、核因子κB和促炎细胞因子来减轻胶原诱导的关节炎。

A novel coumarin derivative, 8-methoxy chromen-2-one alleviates collagen induced arthritis by down regulating nitric oxide, NFκB and proinflammatory cytokines.

作者信息

Sahu Debasis, Raghav Sunil Kumar, Gautam Hemlata, Das Hasi R

机构信息

Genomics and Molecular Medicine, CSIR - Institute of Genomics and Integrative Biology, Mall Road, Delhi 110 007, India; Product Development Cell-II, DBT-National Institute of Immunology, New Delhi - 110067, India.

Genomics and Molecular Medicine, CSIR - Institute of Genomics and Integrative Biology, Mall Road, Delhi 110 007, India; Immuno-Genomics and Systems Biology, DBT-Institute of Life Sciences, Nalco Nagar Road, Chandrasekharpur, Bhubaneshwar, Odisha, India.

出版信息

Int Immunopharmacol. 2015 Dec;29(2):891-900. doi: 10.1016/j.intimp.2015.08.012. Epub 2015 Oct 2.

Abstract

Ruta graveolens (Rue) is a well-known medicinal plant having anti-inflammatory and other healing properties. This contains many active phytochemicals such as coumarins which possess anti-inflammatory and anti-cancer activities. The present study was carried out to evaluate the therapeutic potential of a newly isolated coumarin derivative from rue plant, 8-methoxy-chromen-2-one (MCO) in the collagen induced arthritic (CIA) rat model. MCO showed inhibition of cytokines and NF-κB in LPS stimulated J774 cells which prompted its possible use in animal. In CIA, arthritic index and arthritic score reduced markedly within 15days of MCO treatment at doses of 2mg and 20mg per kg body weight. Alleviation of joint damage in CIA animals on treatment with MCO was evident from radiographic and histological data. Behavioral studies by open field tests also showed convalescence in the MCO treated CIA rats. Further, escalated plasma levels of pro-inflammatory cytokines TNF-α, IL-1β and IL-6, and also nitric oxide reduced significantly with the treatment. All these results indicate the therapeutic efficacy of MCO and its possible use as an anti-arthritic drug.

摘要

芸香是一种著名的药用植物,具有抗炎和其他愈合特性。它含有许多活性植物化学物质,如具有抗炎和抗癌活性的香豆素。本研究旨在评估从芸香植物中新分离出的香豆素衍生物8-甲氧基-色原酮-2-酮(MCO)在胶原诱导性关节炎(CIA)大鼠模型中的治疗潜力。MCO在脂多糖刺激的J774细胞中显示出对细胞因子和核因子-κB的抑制作用,这促使其可能用于动物实验。在CIA模型中,给予每千克体重2毫克和20毫克剂量的MCO治疗15天内,关节炎指数和关节炎评分显著降低。从影像学和组织学数据可以明显看出,MCO治疗的CIA动物关节损伤得到缓解。通过旷场试验进行的行为学研究也表明,MCO治疗的CIA大鼠病情有所好转。此外,治疗后促炎细胞因子肿瘤坏死因子-α、白细胞介素-1β和白细胞介素-6以及一氧化氮的血浆水平显著降低。所有这些结果表明MCO具有治疗效果,并可能用作抗关节炎药物。

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