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WIN-34B,一种新型草药,通过使成纤维样滑膜细胞中的 IκB-α 磷酸化和丝裂原活化蛋白激酶途径失活来抑制炎症反应。

WIN-34B, a new herbal medicine, inhibits the inflammatory response by inactivating IκB-α phosphorylation and mitogen activated protein kinase pathways in fibroblast-like synoviocytes.

机构信息

Oriental Medicine Research Center for Bone and Joint Disease, East-West Bone and Joint Research Institute, Kyung Hee University, 149 Sangil-dong, Gangdong-gu, Seoul 134-727, Republic of Korea.

出版信息

J Ethnopharmacol. 2012 Oct 11;143(3):779-86. doi: 10.1016/j.jep.2012.06.041. Epub 2012 Aug 1.

DOI:10.1016/j.jep.2012.06.041
PMID:22885131
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

The dried flowers of Lonicera japonica Thunb and dried roots of Anemarrhena asphodeloides BUNGE have been used for the treatment of a variety of inflammatory diseases in traditional Korean medicine.

OBJECTIVE

The aim of the study is to evaluate the anti-inflammatory effects of WIN-34B, a new herbal medicine, in fibroblast-like synoviocytes (FLS) obtained from patients with osteoarthritis (OA).

MATERIALS AND METHODS

WIN-34B is isolated from the n-butanol fraction of dried flowers of L. japonica and dried roots of A. asphodeloides. The anti-inflammatory effects of WIN-34B on cell viability, the production and release of inflammatory mediators, matrix metalloproteinases (MMPs), aggrecanases, tissue inhibitor of matrix proteinases (TIMP) is compared with celecoxib in IL-1β-stimulated human OA FLS. Furthermore, the effect of WIN-34B on inhibitory kappa B-α (IκB-α) phosphorylation and mitogen-activated protein kinases (MAPK) in the IL-1β-stimulated OA FLS was also evaluated.

RESULTS

WIN-34B significantly inhibited the IL-1β-induced cell viability in human OA FLS without cytotoxicity. Compared to celecoxib, WIN-34B exhibited similar or better anti-inflammatory effects through significant suppression of inflammatory mediators (IL-1β, TNF-α, PGE2 and NO), MMPs (MMP-1, MMP-3 and MMP-13) and aggrecanases (ADAMTS-4 and ADAMTS-5), and enhancement of TIMPs (TIMP-1 and TIMP-3). Moreover, WIN-34B reduced the phosphorylation of IκB-α, ERK1/2, p38 and JNK1/2 in IL-1β-stimulated OA FLS.

CONCLUSIONS

WIN-34B exhibited similar or better anti-inflammatory properties in IL-1β-stimulated OA FLS compared to celecoxib. The anti-inflammatory effects of WIN-34B are due to inhibition of inflammatory mediators (IL-1β, TNF-α, PGE2 and NO) and regulation of MMPs, ADAMTSs and TIMPs via the inhibition of IκB-α and MAPK phosphorylation in IL-1β-stimulated OA FLS.

摘要

民族药理学相关性

忍冬的干燥花和知母的干燥根在传统的韩国医学中被用于治疗各种炎症性疾病。

目的

本研究的目的是评估 WIN-34B,一种新型草药,在骨关节炎(OA)患者成纤维样滑膜细胞(FLS)中的抗炎作用。

材料和方法

WIN-34B 是从忍冬干燥花的正丁醇部分和知母干燥根中分离得到的。将 WIN-34B 的抗炎作用与塞来昔布在白细胞介素-1β(IL-1β)刺激的人 OA FLS 中对细胞活力、炎症介质、基质金属蛋白酶(MMPs)、聚集素酶、基质金属蛋白酶抑制剂(TIMP)的产生和释放进行比较。此外,还评估了 WIN-34B 对 IL-1β 刺激的 OA FLS 中抑制性κB-α(IκB-α)磷酸化和丝裂原活化蛋白激酶(MAPK)的影响。

结果

WIN-34B 可显著抑制 IL-1β诱导的人 OA FLS 活力,且无细胞毒性。与塞来昔布相比,WIN-34B 通过显著抑制炎症介质(IL-1β、TNF-α、PGE2 和 NO)、MMPs(MMP-1、MMP-3 和 MMP-13)和聚集素酶(ADAMTS-4 和 ADAMTS-5),增强 TIMPs(TIMP-1 和 TIMP-3),显示出相似或更好的抗炎作用。此外,WIN-34B 可降低 IL-1β 刺激的 OA FLS 中 IκB-α、ERK1/2、p38 和 JNK1/2 的磷酸化。

结论

与塞来昔布相比,WIN-34B 在 IL-1β 刺激的 OA FLS 中显示出相似或更好的抗炎特性。WIN-34B 的抗炎作用是通过抑制炎症介质(IL-1β、TNF-α、PGE2 和 NO)和调节 MMPs、ADAMTSs 和 TIMPs,通过抑制 IL-1β 刺激的 OA FLS 中的 IκB-α 和 MAPK 磷酸化来实现的。

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