66 research outputs found
Lythrum salicaria Ellagitannins Stimulate IPEC-J2 Cells Monolayer Formation and Inhibit Enteropathogenic Escherichia coli Growth and Adhesion
Lythrum salicaria herb (LSH) was applied in diarrhea therapy since ancient times. Despite empirically referenced therapeutic effects, the bioactivity mechanisms and chemical constituents responsible for pharmacological activity remain not fully resolved. Taking into consideration the historical use of LSH in treatment of diarrhea in humans and farm animals, the aim of the study was to examine in vitro the influence of LSH and its C-glycosylic ellagitannins on processes associated with maintaining intestinal epithelium integrity and enteropathogenic Escherichia coli (EPEC) growth and adhesion. LSH was not only inhibiting EPEC growth in a concentration dependent manner but also its adhesion to IPEC-J2 intestinal epithelial cell monolayers. Inhibitory activity toward EPEC growth was additionally confirmed ex vivo in distal colon samples of postweaning piglets. LSH and its dominating C-glycosylic ellagitannins, castalagin (1), vescalagin (2), and salicarinins A (3) and B (4) were stimulating IPEC-J2 monolayer formation by enhancing claudin 4 production. Parallelly tested gut microbiota metabolites of LSH ellagitannins, urolithin C (5), urolithin A (6), and its glucuronides (7) were inactive. The activities of LSH and the isolated ellagitannins support its purported antidiarrheal properties and indicate potential mechanisms responsible for its beneficial influence on the intestinal epithelium
"Schisandra rubriflora" pllant material and in vitro microshoot cultures as rich sources of natural phenolic antioxidants
Schisandra rubriflora is a dioecious, underestimated medicinal plant species known from
traditional Chinese medicine. The present study was aimed at characterising the polyphenolic
profile composition and the related antioxidant capacity of S. rubriflora fruit, stem and leaf
and in vitro microshoot culture extracts. Separate analyses of material from female and male
specimens were carried out. This study was specifically aimed at detailed characterisation of the
contribution of phenolic compounds to overall antioxidant activity using ultra-high-performance
liquid chromatography with a photodiode array detector coupled to electrospray ionization ion trap
mass spectrometry (UHPLC-DAD-ESI-MS3
) and a high-performance liquid chromatography-diode
array detector (HPLC-DAD). Using UHPLC-DAD-ESI-MS3
, twenty-seven phenolic compounds
from among phenolic acids and flavonoids were identified. Concentrations of three phenolic acids
(neochlorogenic, chlorogenic and cryptochlorogenic acids) and eight flavonoids (hyperoside, rutoside,
isoquercitrin, guaijaverin, trifolin, quercetin, kaempferol, and isorhamnetin) were determined using
HPLC-DAD using reference standards. The highest total phenolic content was confirmed for the
stem and leaf extracts collected in spring. The contents of phenolic compounds of in vitro biomasses
were comparable to that in the fruit extracts. The methanolic extracts from the studied plant
materials were evaluated for their antioxidant properties using various in vitro assays, namely free
radicals scavenging estimation using 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH), ferric-reducing
antioxidant power (FRAP) and cupric-reducing antioxidant capacity (CUPRAC) as well as QUick,
Easy, New, CHEap, and Reproducible CUPRAC (QUENCHER-CUPRAC) assays. A close relationship
between the content of polyphenolic compounds in S. rubriflora and their antioxidant potential has
been documented
Comparative studies of urolithins and their phase II metabolites on macrophage and neutrophil functions
Purpose Ellagitannins are high molecular weight polyphenols present in high quantities in various food products. They are metabolized by human and animal gut microbiota to postbiotic metabolites-urolithins, bioavailable molecules of a low molecular weight. Following absorption in the gut, urolithins rapidly undergo phase II metabolism. Thus, to fully evaluate the mechanisms of their biological activity, the in vitro studies should be conducted for their phase II conjugates, mainly glucuronides. The aim of the study was to comparatively determine the influence of urolithin A, iso-urolithin A, and urolithin B together with their respective glucuronides on processes associated with the inflammatory response. Methods The urolithins obtained by chemical synthesis or isolation from microbiota cultures were tested with their respective glucuronides isolated from human urine towards modulation of inflammatory response in THP-1-derived macrophages, RAW 264.7 macrophages, PBMCs-derived macrophages, and primary neutrophils. Results Urolithin A was confirmed to be the most active metabolite in terms of LPS-induced inflammatory response inhibition (TNF-alpha attenuation, IL-10 induction). The observed strong induction of ERK1/2 phosphorylation has been postulated as the mechanism of its action. None of the tested glucuronide conjugates was active in terms of pro-inflammatory TNF-alpha inhibition and anti-inflammatory IL-10 and TGF-beta 1 induction. Conclusion Comparative studies of the most abundant urolithins and their phase II conjugates conducted on human and murine immune cells unambiguously confirmed urolithin A to be the most active metabolite in terms of inhibition of the inflammatory response. Phase II metabolism was shown to result in the loss of urolithins' pharmacological properties
Phytochemical and biological activity studies on Nasturtium officinale (watercress) microshoot cultures grown in RITA temporary immersion systems
The main compounds in both extracts were gluconasturtiin, 4-methoxyglucobrassicin and rutoside, the amounts of which were, respectively, determined as 182.93, 58.86 and 23.24 mg/100 g dry weight (DW) in biomass extracts and 640.94, 23.47 and 7.20 mg/100 g DW in plant herb extracts. The antioxidant potential of all the studied extracts evaluated using CUPRAC (CUPric Reducing Antioxidant Activity), FRAP (Ferric Reducing Ability of Plasma), and DPPH (1,1-diphenyl-2-picrylhydrazyl) assays was comparable. The anti-inflammatory activity of the extracts was tested based on the inhibition of 15-lipoxygenase, cyclooxygenase-1, cyclooxygenase-2 (COX-2), and phospholipase A2. The results demonstrate significantly higher inhibition of COX-2 for in vitro cultured biomass compared with the herb extracts (75.4 and 41.1%, respectively). Moreover, all the studied extracts showed almost similar antibacterial and antifungal potential. Based on these findings, and due to the fact that the growth of in vitro microshoots is independent of environmental conditions and unaffected by environmental pollution, we propose that biomass that can be rapidly grown in RITA® bioreactors can serve as an alternative source of bioactive compounds with valuable biological properties
Therapeutic Effects of Oral Application of Menthol and Extracts from Tormentil (Potentilla erecta), Raspberry Leaves (Rubus idaeus), and Loosestrife (Lythrum salicaria) during Acute Murine Campylobacteriosis
Human food-borne infections with the enteropathogen Campylobacter jejuni are becoming increasingly prevalent worldwide. Since antibiotics are usually not indicated in campylobacteriosis, alternative treatment regimens are important. We here investigated potential disease-alleviating effects of menthol and of extracts from tormentil, raspberry leaves, and loosestrife in acute murine campylobacteriosis. Therefore, C. jejuni-infected microbiota-depleted IL-10−/− mice were orally treated with the compounds alone or all in combination from day 2 until day 6 post-infection. Whereas neither treatment regimen affected gastrointestinal pathogen loads, the combination of compounds alleviated C. jejuni-induced diarrheal symptoms in diseased mice on day 6 post-infection. Furthermore, the therapeutic application of tormentil and menthol alone and the combination of the four compounds resulted in lower colonic T cell numbers in infected mice when compared to placebo counterparts. Notably, pro-inflammatory cytokines measured in mesenteric lymph nodes taken from C. jejuni-infected mice following tormentil, menthol, and combination treatment did not differ from basal concentrations. However, neither treatment regimen could dampen extra-intestinal immune responses, including systemic pro-inflammatory cytokine secretion on day 6 post-infection. In conclusion, the combination of menthol and of extracts from tormentil, raspberry leaves, and loosestrife constitutes an antibiotic-independent approach to alleviate campylobacteriosis symptoms
In Vitro Antiproliferative and Antioxidant Effects of Extracts from Rubus caesius
The present study was performed to evaluate the effect of different extracts and subfractions from Rubus caesius leaves on two human colon cancer cell lines obtained from two stages of the disease progression lines HT29 and SW948. Tested samples inhibited the viability of cells, both HT29 and SW948 lines, in a concentration-dependent manner. The most active was the ethyl acetate fraction which, applied at the highest concentration (250 μg/mL), decreased the viability of cells (HT29 and SW948) below 66%. The extracts and subfractions were also investigated for antioxidant activities on DPPH and FRAP assays. All extracts, with the exception of water extract at a dose of 250 μg/mL, almost totally reduced DPPH. The highest Fe3+ ion reduction was shown for the diethyl and ethyl acetate fractions. It was more than 6.5 times higher (at a dose 250 μg/mL) as compared to the control. The LC-MS studies of the analysed preparations showed that all samples contain a wide variety of polyphenolics, among which ellagitannins turned out to be the main constituents with dominant ellagic acid, sanguiin H-6, and flavonol derivatives
Novel Opioid-Neurotensin-Based Hybrid Peptide with Spinal Long-Lasting Antinociceptive Activity and a Propensity to Delay Tolerance Development
The behavioral responses exerted by spinal administration of the opioid-neurotensin hybrid peptide, PK23, were studied in adult male rats. The antinociceptive effect upon exposure to a thermal stimulus, as well as tolerance development, was assessed in an acute pain model. The PK23 chimera at a dose of 10 nmol/rat produced a potent pain-relieving effect, especially after its intrathecal administration. Compared with intrathecal morphine, this novel compound was found to possess a favourable side effect profile characterized by a reduced scratch reflex, delayed development of analgesic tolerance or an absence of motor impairments when given in the same manner, though some animals died following barrel rotation as a result of its i.c.v. administration (in particular at doses higher than 10 nmol/rat). Nonetheless, these results suggest the potential use of hybrid compounds encompassing both opioid and neurotensin structural fragments in pain management. This highlights the enormous potential of synthetic neurotensin analogues as promising future analgesics
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