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

Anatomy and Cell Biology, Department of Medical Cell Biology, University of Marburg, Robert-Koch-Str. 8, 35032 Marburg, Germany.
Phytomedicine: international journal of phytotherapy and phytopharmacology (Impact Factor: 3.13). 12/2010; 17(14):1106-13. DOI: 10.1016/j.phymed.2010.03.022
Source: PubMed


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.
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).
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.

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    • "However, authentic naringenin-7- O-glucoside (with a retention time of 34.5 min) was not cleaved during thiolysis. Given that naringenin, naringenin-7-O-glucoside and (±)-naringenin-5-O-glucoside (as two peaks) were previously detected in willow bark[10], we propose that, surprisingly, (±)- naringenin-5-O-glucoside was degraded under the relatively mild conditions of this thiolysis reaction. "

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    • "DHA has been reported to significantly reduce the expression of p65 and its nuclear binding [39]. Bonaterra et al. [40] explained similar effects on NF-κB translocation using willow bark extract, aspirin and diclofenac. The studies with various pharmaceutical medicines have indicated that therapeutics blocking NF-κB translocation might be an effective treatment for inflammatory disease [41]. "
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    ABSTRACT: Phloridzin or phlorizin (PZ) is a predominant phenolic compound found in apple and also used in various natural health products. Phloridzin shows poor absorption and cellular uptake due to its hydrophilic nature. The aim was to investigate and compare the effect of docosahexaenoic acid (DHA) ester of PZ (PZ-DHA) and its parent compounds (phloridzin and DHA), phloretin (the aglycone of PZ) and cyclooxygenase inhibitory drugs (diclofenac and nimesulide) on production of pro-inflammatory biomarkers in inflammation-induced macrophages by lipopolysaccharide (LPS)-stimulation. Human THP-1 monocytes were seeded in 24-well plates (5×10(5)/well) and treated with phorbol 12-myristate 13-acetate (PMA, 0.1μg/mL) for 48h to induce macrophage differentiation. After 48h, the differentiated macrophages were washed with Hank's buffer and treated with various concentrations of test compounds for 4h, followed by the LPS-stimulation (18h). Pre-exposure of PZ-DHA ester was more effective in reducing tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6) and cyclooxygenase-2 (COX-2) protein levels compared to DHA and nimesulide. However, diclofenac was the most effective in reducing prostaglandin (PGE2) level by depicting a dose-dependent response. However, PZ-DHA ester and DHA were the most effective in inhibiting the activation of nuclear factor-kappa B (NF-κB) among other test compounds. Our results suggest that PZ-DHA ester might possess potential therapeutic activity to treat inflammation related disorders such as type 2 diabetes, asthma, atherosclerosis and inflammatory bowel disease. Copyright © 2015. Published by Elsevier B.V.
    Full-text · Article · Jan 2015 · International immunopharmacology
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    • "Therefore, COX-inhibition was first regarded the main mechanism of the anti-inflammatory activity of WB. In the meanwhile it was shown that WB can also modulate relevant pro-and anti-inflammatory cytokines like TNF-␣, IL-6, IL-1, IL-10, and IL-8 (Bonaterra et al. 2009; Fiebich et al. 2005; Fiebich and Chrubasik 2004) and that not only salicyl alcohol derivatives, but also the polyphenols of WB contribute to this modulation (Khayyal et al. 2005; Nahrstedt et al. 2007). In addition, polyphenols are known to possess antioxidant and neuroprotective effects which can also interfere with inflammatory events (Kannappan et al. 2011). "
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    ABSTRACT: Inflammatory processes are increasingly recognised to contribute to neurological and neuropsychatric disorders such as depression. Thus we investigated whether a standardized willow bark preparation (WB) which contains among other constituents salicin, the forerunner of non-steroidal antiphlogistic drugs, would have an effect in a standard model of depression, the forced swimming test (FST), compared to the antidepressant imipramine. Studies were accompanied by gene expression analyses. In order to allocate potential effects to the different constituents of WB, fractions of the extract with different compositions of salicyl alcohol derivative and polyphenols were also investigated.
    Full-text · Article · Jun 2012 · Phytomedicine: international journal of phytotherapy and phytopharmacology
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