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Identification of Salicylates in Willow Bark (Salix Cortex) for Targeting Peripheral Inflammation.

ABSTRACT: Salix cortex-containing medicine is used against pain conditions, fever, headaches, and inflammation, which are partly mediated via arachidonic acid-derived prostaglandins (PGs). We used an activity-guided fractionation strategy, followed by structure elucidation experiments using LC-MS/MS, CD-spectroscopy, and 1D/2D NMR techniques, to identify the compounds relevant for the inhibition of PGE2 release from activated human peripheral blood mononuclear cells. Subsequent compound purification by means of preparative and semipreparative HPLC revealed 2'-O-acetylsalicortin (1), 3'-O-acetylsalicortin (2), 2'-O-acetylsalicin (3), 2',6'-O-diacetylsalicortin (4), lasiandrin (5), tremulacin (6), and cinnamrutinose A (7). In contrast to 3 and 7, compounds 1, 2, 4, 5, and 6 showed inhibitory activity against PGE2 release with different potencies. Polyphenols were not relevant for the bioactivity of the Salix extract but salicylates, which degrade to, e.g., catechol, salicylic acid, salicin, and/or 1-hydroxy-6-oxo-2-cycohexenecarboxylate. Inflammation presents an important therapeutic target for pharmacological interventions; thus, the identification of relevant key drugs in Salix could provide new prospects for the improvement and standardization of existing clinical medicine.

SUBMITTER: Antoniadou K

PROVIDER: S-EPMC8540557 | biostudies-literature | 2021 Oct

REPOSITORIES: biostudies-literature

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Identification of Salicylates in Willow Bark (Salix Cortex) for Targeting Peripheral Inflammation.

Antoniadou Kyriaki K Herz Corinna C Le Nguyen Phan Khoi NPK Mittermeier-Kleßinger Verena Karolin VK Förster Nadja N Zander Matthias M Ulrichs Christian C Mewis Inga I Hofmann Thomas T Dawid Corinna C Lamy Evelyn E

International journal of molecular sciences 20211015 20

Salix cortex-containing medicine is used against pain conditions, fever, headaches, and inflammation, which are partly mediated via arachidonic acid-derived prostaglandins (PGs). We used an activity-guided fractionation strategy, followed by structure elucidation experiments using LC-MS/MS, CD-spectroscopy, and 1D/2D NMR techniques, to identify the compounds relevant for the inhibition of PGE2 release from activated human peripheral blood mononuclear cells. Subsequent compound ...[more]

PMID: 34681798

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Project description:IntroductionRecurring viral outbreaks have a significant negative impact on society. This creates a need to develop novel strategies to complement the existing antiviral approaches. There is a need for safe and sustainable antiviral solutions derived from nature.ObjectiveThis study aimed to investigate the antiviral potential of willow (Salix spp.) bark hot water extracts against coronaviruses and enteroviruses. Willow bark has long been recognized for its medicinal properties and has been used in traditional medicines. However, its potential as a broad-spectrum antiviral agent remains relatively unexplored.MethodsCytopathic effect inhibition assay and virucidal and qPCR-based assays were used to evaluate the antiviral potential of the bark extracts. The mechanism of action was investigated using time-of-addition assay, confocal microscopy, TEM, thermal, and binding assays. Extracts were fractionated and screened for their chemical composition using high-resolution LC-MS.ResultsThe native Salix samples demonstrated their excellent antiviral potential against the non-enveloped enteroviruses even at room temperature and after 45 s. They were equally effective against the seasonal and pandemic coronaviruses. Confocal microscopy verified the loss of infection capacity by negligible staining of the newly synthesized capsid or spike proteins. Time-of-addition studies demonstrated that Salix bark extract had a direct effect on the virus particles but not through cellular targets. Negative stain TEM and thermal assay showed that antiviral action on enteroviruses was based on the added stability of the virions. In contrast, Salix bark extract caused visible changes in the coronavirus structure, which was demonstrated by the negative stain TEM. However, the binding to the cells was not affected, as verified by the qPCR study. Furthermore, coronavirus accumulated in the cellular endosomes and did not proceed after this stage, based on the confocal studies. None of the tested commercial reference samples, such as salicin, salicylic acid, picein, and triandrin, had any antiviral activity. Fractionation of the extract and subsequent MS analysis revealed that most of the separated fractions were very effective against enteroviruses and contained several different chemical groups such as hydroxycinnamic acid derivatives, flavonoids, and procyanidins.ConclusionSalix spp. bark extracts contain several virucidal agents that are likely to act synergistically and directly on the viruses.

Project description:BACKGROUND:Willows (Salix spp.) are ecosystem "foundation species" that are hosts to large numbers of associated insects. Determining their patterns of distribution across Europe is therefore of interest for understanding the spatial distribution of associated fauna. The aim of this study was to record species composition at multiple sites on a long latitudinal gradient (megatransect) across Europe as a baseline for the future detailed analysis of insect fauna at these sites. In this way we used willow stands as comparable mesocosms in which to study floristic and faunistic changes with latitude across Europe. NEW INFORMATION:To determine spatial patterning of an ecologically important group on a latitudinal gradient across Europe, we sampled willows at the stand level in 42 sites, approximately 100 km apart, from the Aegean (38.8°N) to the Arctic Ocean (70.6°N), but at a similar longitude (21.2 to 26.1°E). The sites were predominantly lowland (elevations 1 to 556 metres amsl, median = 95 m) and wet (associated with rivers, lakes, drainage ditches or wet meadows). The median number of willow taxa (species and hybrids) per stand was four, and varied from one to nine. There is a progressive increase in willow diversity from south to north with the median number of taxa per stand in southern Europe being three, and in northern Europe six. A total of 20 willow species were recorded, along with 12 hybrids. The most widespread willow in the transect was Salix alba L. (occurring in 20 sites out of 42) followed by S. triandra L. (15 sites), S. caprea L., S. phylicifolia L. (14 sites) and S. myrsinifolia Salisb., Salix ×fragilis L. (13 sites). Voucher specimens from this study are deposited in the herbaria of the Natural History Museum (BM) and the Royal Botanic Gardens Kew (K). These samples provide a "snapshot" of willow diversity along a latitudinal gradient and an indication of the geographically changing taxonomic diversity that is presented to willow-feeding herbivores across Europe. It is anticipated that further papers will examine the insect fauna collected from these sites as part of this study.

Project description:BackgroundInflammatory bowel diseases are the most common chronic intestinal inflammatory conditions, and their incidence has shown a dramatic increase in recent decades. Limited efficacy and questionable safety profiles with existing therapies suggest the need for better targeting of therapeutic strategies. Adenosine monophosphate-activated protein kinase (AMPK) is a key regulator of cellular metabolism and has been implicated in intestinal inflammation. Macrophages execute an important role in the generation of intestinal inflammation. Impaired AMPK in macrophages has been shown to be associated with higher production of proinflammatory cytokines; however, the role of macrophage AMPK in intestinal inflammation and the mechanism by which it regulates inflammation remain to be determined. In this study, we investigated the role of AMPK with a specific focus on macrophages in the pathogenesis of intestinal inflammation.MethodsA dextran sodium sulfate-induced colitis model was used to assess the disease activity index, histological scores, macroscopic scores, and myeloperoxidase level. Proinflammatory cytokines such as tumor necrosis factor-α, interleukin-6, and interleukin-1β were measured by enzyme-linked immunosorbent assay. Transient transfection of AMPKβ1 and LC3-II siRNA in RAW 264.7 cells was performed to elucidate the regulation of autophagy by AMPK. The expression of p-AMPK, AMPK, and autophagy markers (eg, LC3-II, p62, Beclin-1, and Atg-12) was analyzed by Western blot.ResultsGenetic deletion of AMPKβ1 in macrophages upregulated the production of proinflammatory cytokines, aggravated the severity of dextran sodium sulfate-induced colitis in mice, which was associated with an increased nuclear translocation of nuclear factor-κB, and impaired autophagy both in vitro and in vivo. Notably, the commonly used anti-inflammatory 5-aminosalicylic acid (ie, mesalazine) and sodium salicylate ameliorated dextran sodium sulfate-induced colitis through the activation of macrophage AMPK targeting the β1 subunit.ConclusionsTogether, these data suggest that the development of therapeutic agents targeting AMPKβ1 may be effective in the treatment of intestinal inflammatory conditions including inflammatory bowel disease.

Dataset Information

Identification of Salicylates in Willow Bark (Salix Cortex) for Targeting Peripheral Inflammation.

Publications

Identification of Salicylates in Willow Bark (<i>Salix</i> Cortex) for Targeting Peripheral Inflammation.

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