柳皮提取物 STW 33-I（Proaktiv(®)）对脂多糖激活的人单核细胞和分化的巨噬细胞的抗炎作用。

Anti-inflammatory effects of the willow bark extract STW 33-I (Proaktiv(®)) in LPS-activated human monocytes and differentiated macrophages.

机构信息

Anatomy and Cell Biology, Department of Medical Cell Biology, University of Marburg, Robert-Koch-Str. 8, 35032 Marburg, Germany.

出版信息

Phytomedicine. 2010 Dec 1;17(14):1106-13. doi: 10.1016/j.phymed.2010.03.022. Epub 2010 May 31.

DOI:10.1016/j.phymed.2010.03.022

PMID:20570123

Abstract

INTRODUCTION

Willow bark extract is frequently used in the treatment of painful rheumatological diseases, such as arthritis and back pain. Its effect has been attributed to its main component salicin, but pharmacological studies have shown that the clinical efficacy of the willow bark extract cannot be explained by its salicin content alone. Therefore different modes of action have been suggested for the anti-inflammatory effect of willow bark extract. Here, we report in vitro data revelling the effect and mode of action of the aqueous willow bark extract STW 33-I as well as a water-soluble fraction (fraction E [Fr E]) in comparison with well-known non-steroidal anti-inflammatory drugs (NSAIDs) like aspirin (ASA) and diclofenac (Diclo) on pro-inflammatorily activated human monocytes and differentiated macrophages.

RESULTS

STW 33-I and the water-soluble Fr E showed concentration-dependent and significant anti-inflammatory effects in lipopolysaccharide-activated monocytes. Both inhibited the intracellular protein expression of tumour necrosis factor-alpha (TNFα) as well as the mRNA expression of TNFα and cyclooxygenase 2 (COX-2), and the release of nitric oxide (NO). In addition, apoptosis of pro-inflammatorily activated monocytes was induced. Furthermore, treatment of activated macrophages with STW 33-I inhibited the nuclear translocation of the p65 subunit of the nuclear transcription factor-kappa B (NF-κB p65).

CONCLUSIONS

The present in vitro investigations suggest a significant anti-inflammatory activity of willow bark water extract STW 33-1 and of its water-soluble fraction by inhibiting pro-inflammatory cytokines (TNFα), COX-2 and nuclear translocation of the transcription factor NF-κB in pro-inflammatorily activated monocytes. Our results provide further evidence for the therapeutic use of STW 33-I in inflammation-related disorders.

摘要

简介

柳树皮提取物常用于治疗疼痛性风湿性疾病，如关节炎和背痛。其疗效归因于其主要成分水杨酸，但药理学研究表明，柳树皮提取物的临床疗效不能仅用其水杨酸含量来解释。因此，不同的作用模式被认为是柳树皮提取物抗炎作用的机制。在这里，我们报告了水提柳树皮提取物 STW 33-I 及其水溶性部分（Fr E）的体外数据，与阿司匹林（ASA）和双氯芬酸（Diclo）等知名非甾体抗炎药（NSAIDs）比较，其对脂多糖激活的人单核细胞和分化的巨噬细胞的作用和作用模式。

结果

STW 33-I 和水溶性 Fr E 在脂多糖激活的单核细胞中表现出浓度依赖性和显著的抗炎作用。两者均抑制肿瘤坏死因子-α（TNFα）的细胞内蛋白表达以及 TNFα和环氧化酶 2（COX-2）的 mRNA 表达，并抑制一氧化氮（NO）的释放。此外，还诱导了促炎激活的单核细胞凋亡。此外，STW 33-I 处理激活的巨噬细胞抑制核转录因子-κB（NF-κB p65）的 p65 亚基的核易位。