•Four new compounds were isolated from M. oleifera seeds.•Their structures were determined using comprehensive spectroscopic methods.•Comprehensive spectroscopic methods including HR-ESIMS, ECD, 1D ...and 2D NMR experiments.•Compounds 1–3 showed moderate anti-inflammatory activities.•Anti-inflammatory mechanisms were revealed by targets prediction and molecular docking.
Moringa oleifera seeds had shown multiple pharmacological properties and contained various chemical constituents. In a study focusing on the investigation of active compounds in M. oleifera seeds, four new compounds were isolated, including three benzyl alcohol compounds (1–3), and one benzyl thiocarbamate (4). Their structures were determined using comprehensive spectroscopic methods, such as ECD, 1D and 2D NMR experiments. The inhibitory activities of these compounds against lipopolysaccharide (LPS)-activated nitric oxide (NO) production in RAW 264.7 were evaluated in vitro. Compounds 1–3 demonstrated moderate inhibitory activities against LPS-activated NO production in RAW 264.7 cells. Furthermore, the potential anti-inflammatory mechanisms of compounds 1–3 were elucidated through target prediction and molecular docking analyses. Molecular docking analysis revealed that these compounds exhibited anti-inflammatory activity by antagonizing the MMP-9 receptor. This study offers new insights for the development and utilization of M. oleifera seeds.
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•PLLA/CS micro/nano-fibrous scaffold was prepared by 3D printing and TIPS method.•3D CS nanofibers favor cell growth and adhesion into the interior of the scaffold.•Qu, a drug, was ...first fixed on the scaffold surface and released continuously.•The PLLA/CS-D/Qu scaffold has excellent osteogenic and anti-inflammatory activity.•The as-prepared PLLA/CS-D/Qu scaffold has potential as a bone repair material.
We present here a porous poly (L-lactide)/chitosan (PLLA/CS) composite scaffold with micro/nano-fiber hierarchical structure that was innovatively fabricated by combining 3D printing and thermally induced phase separation technology. Moreover, bioactive quercetin (Qu) was chosen to further functionalize the PLLA/CS scaffold with polydopamine (PDA) layer. The final results showed that the hydrophilicity and mechanical properties of the resulting PLLA/CS-D/Qu scaffold were obviously superior to those of the pure 3D printing PLLA scaffold. In vitro MC3T3-E1 cell experiments suggested that the introducing CS nanofiber network helped cells grow into the interior of the scaffold and promoted cell adhesion and proliferation. More importantly, the synergistic effect of the CS nanofiber network, PDA layer and especially sustain-released Qu, can endow the PLLA/CS-D/Qu scaffolds with not only excellent cell affinity and osteogenic activity, but also good anti-inflammatory property. Thus, the PLLA/CS-D/Qu scaffolds are expected to have good application prospects in the field of bone tissue engineering.
In the present study, crude polysaccharides were extracted from Gelidium pacificum Okamura, and further purified to obtain the sulfated polysaccharide with molecular weight of 28,807 Da. Its ...monosaccharide composition mainly consisted of xylose (7.1%), galactose (59.7%) and galacturonic acid (19.76%). And the sulfate ester content of the sulfated polysaccharide was estimated as 8.8%. Structure analysis showed that the sulfated polysaccharide comprised of 1,4-linked-α-D-Galp3S, 1,2-linked-α-D-Xylp and 1,3-linked-β-D-GalpA residues, respectively. Its anti-inflammatory effects were investigated in LPS-stimulated human monocytic (THP-1) cells. The sulfated polysaccharide at a concentration of 5 μg/mL fully protected the THP-1 cells against LPS-stimulated cytotoxicity. Furthermore, the addition of sulfated polysaccharide resulted in a significant reduction of NO production in LPS-treated cells, and this effect appeared to be dose-related. The sulfated polysaccharide (5 μg/mL) significantly suppressed the mRNA and protein expression of toll-like receptor-4 (TLR-4), myeloid differentiation factor (MyD88) and tumor necrosis factor receptor-associated factor-6 (TRAF-6) in LPS-stimulated THP-1 cells. These results showed the sulfated polysaccharide not only provided a good protection against LPS-induced cell toxicity, but also exerted an anti-inflammatory effect via the TLR4 signaling pathway.
•The isolation and purification of Gelidium pacificum Okamura polysaccharide (sulfated polysaccharide) were first studied.•The structure of the sulfated polysaccharide was analyzed and identified.•The sulfated polysaccharide exhibited a protective effect against LPS-stimulated cell toxicity.•The anti-inflammatory mechanisms of the sulfated polysaccharide were studied.
Phenolics, which are secondary metabolites of plants, exhibit remarkable bioactivities. In this contribution, we have focused on their protective effect against chronic diseases rather than their ...antioxidant activities, which have been widely discussed in the literature. A large body of epidemiological studies has proven the bioactivities of phenolics in both standard compounds and natural extracts: namely, anticancer, anti-inflammatory, and antibacterial activities as well as reducing diabetes, cardiovascular disease, and neurodegenerative disease. Phenolics also display anti-analgesic, anti-allergic, and anti-Alzheimer's properties. Thus, this review provides crucial information for better understanding the bioactivities of phenolics in foods and fills a gap in the existing collective and overall knowledge in the field.
Probiotic bacteria are recognized for their health-promoting properties, including maintenance of gut epithelial integrity and host immune system homeostasis. Taking into account the beneficial ...health-promoting effects of GABA, the presence of the
gene, encoding glutamate decarboxylase that converts L-glutamate to GABA, was analyzed in Lactic Acid Bacteria (LAB) natural isolates from Zlatar cheese. The results revealed that 52% of tested
spp. and 8% of
spp. isolates harbor the
gene. Qualitative and quantitative analysis of GABA production performed by thin-layer chromatography (TLC) and high-performance liquid chromatography (HPLC) revealed the highest GABA production by
BGZLS10-17. Since high GABA-producing LAB natural isolates are the most valuable source of naturally produced GABA, the probiotic properties of BGZLS10-17 were characterized. This study demonstrated high adhesion of BGZLS10-17 strain to Caco-2 cells and the ability to decrease the adhesion of
ATCC25922 and
C29039. Treatment of differentiated Caco-2 cells monolayer with BGZLS10-17 supernatant containing GABA alleviated inflammation (production of IL-8) caused by IL-1β and significantly stimulated the expression of tight junction proteins (zonulin, occludin, and claudin 4), as well as the expression of
cytokine leading to the conclusion that immunosuppression and strengthening the tight junctions can have significant role in the maintenance of intestinal epithelial barrier integrity. Taken together the results obtained in this study support the idea that using of GABA producing BGZLS10-17 probiotic strain could be a good strategy to modulate immunological response in various inflammatory diseases, and at the same time, it could be a good candidate for adjunct starter culture for production of GABA-enriched dairy foods and beverages offering new perspectives in designing the novel functional foods.
Front Cover/Cover Picture. Artemisia annua L. is an annual herb of Asteraceae family, one of the famous traditional Chinese medicines, commonly known as “Qing Hao”. However, in Chongming District of ...Shanghai, it is called “Ku Cao” and has been used for women's post‐natal rehabilitation for a long time. In this study, five new monoterpene glycosides (1–5) and two new sesquiterpenoid glycosides (6 and 7) were isolated from the water extract of the aerial part of A. annua. All the new compounds significantly inhibited the expression of IL‐6 interleukin‐6 in lipopolysaccharide‐stimulated RAW 264.7 macrophages as reported by Q.‐G. Wu et al. in their research article at 10.1002/cbdv.202201237.
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Spinal cord injury (SCI) can cause locomotor dysfunctions and sensory deficits. Evidence shows that functional nanodrugs can regulate macrophage polarization and promote ...anti-inflammatory cytokine expression, which is feasible in SCI immunotherapeutic treatments. Molybdenum disulfide (MoS2) nanomaterials have garnered great attention as potential carriers for therapeutic payload. Herein, we synthesize MoS2@PEG (MoS2 = molybdenum disulfide, PEG = poly (ethylene glycol)) nanoflowers as an effective carrier for loading etanercept (ET) to treat SCI. We characterize drug loading and release properties of MoS2@PEG in vitro and demonstrate that ET-loading MoS2@PEG obviously inhibits the expression of M1-related pro-inflammatory markers (TNF-α, CD86 and iNOS), while promoting M2-related anti-inflammatory markers (Agr1, CD206 and IL-10) levels. In vivo, the mouse model of SCI shows that long-circulating ET-MoS2@PEG nanodrugs can effectively extravasate into the injured spinal cord up to 96 h after SCI, and promote macrophages towards M2 type polarization. As a result, the ET-loading MoS2@PEG administration in mice can protect survival motor neurons, thus, reducing injured areas at central lesion sites, and significantly improving locomotor recovery. This study demonstrates the anti-inflammatory and neuroprotective activities of ET-MoS2@PEG and promising utility of MoS2 nanomaterial-mediated drug delivery.
Ulcerative colitis is a chronic inflammatory disease with a remitting-relapsing clinical course, it has evolved into a global burden given its high incidence worldwide. Cantharidin (CTD) derivatives ...are a class of compounds whose structures characterized with a 7-oxabicyclo 2.2.1heptane core. Though potent cytotoxicity CTD and its derivatives showed, their clinical usage as anti-cancer drugs was limited by the toxicity in organs. In order to find new CTD analogues with good activity and lower toxicity, 21 CTD analogues with or without alkynyl substitution at C5 position of 7-oxabicyclo 2.2.1heptane core were synthesized, some compounds showed better in vitro anti-inflammatory activity compared to CTD and norcantharidin (NCTD). Based on the structure-activity relationship results of in vitro experiment, analogue 3i was chosen for further study. Results from the acute toxicity in mice showed that 3i was hypotoxic with the single-dose MTD (maximum tolerated dose) for oral administration is over 1852 mg/kg, at least 35-fold lower than that of NCTD. Mechanism study indicated that 3i could potently inhibit TNF-α induced activation of NF-κB signaling by down-regulation the expression levels of phosphor- IKK, IκBα, and NF-κB p65, and alleviated dextran sulfate sodium-induced colitis in mice. This study indicated that CTD analogues with alkynyl substitution at C5 position of 7-oxabicyclo 2.2.1heptane core is a kind of new compounds with good anti-inflammatory activity and lower toxicity in vivo, and might be used as therapeutic agents for inflammatory diseases.
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•Fourteen cantharidin analogues were synthesized by iridium-catalyzed asymmetric hydroalkynylation reactions.•Cantharidin analogues with alkynyl substitution showed good in vitro anti-inflammatory activities.•Cantharidin analogue 3i inhibited TNF-α induced activation of NF-κB pathway.•Cantharidin analogue 3i showed weak in vivo toxicity and attenuated DSS-induced colitis in mice.
•Three fucosylated chondroitin sulfate were obtained from three edible sea cucumbers.•The detailed structures of fCSs, particularly the fucose branches, were investigated and compared.•Antioxidant ...and anti-inflammatory properties of the three fCS were evaluated.•O-4 sulfation is particularly important for the antioxidant activities.
Three fucosylated chondroitin sulfate (fCS) were obtained from edible sea cucumbers Apostichopus japonicus, Stichopus chloronotus and Acaudina molpadioidea collected from China. fCS from Stichopus chloronotus was firstly reported. The detailed structures of fCSs, particularly the fucose branches, were investigated and compared. 1H and 13C NMR of the polysaccharide identified three sulfation patterns of fucose branches: 4-O-, 2,4-di-O, and 3,4-di-O-sulfation variously existed in different fCSs. The backbone structure was confirmed by the monosaccharide composition and two-dimensional NMR. Antioxidant properties of fCSs were evaluated by the scavenging abilities on 1,1-diphenyl-2-picrylhydrazyl, nitric oxide radicals and inhibition of lipid peroxidation. The results showed that their activities could be affected by the sulfation patterns of the fucose branches, and O-4 sulfation is particularly important for its activities. The anti-inflammatory assays of fCS-Am showed significant reduction of the carrageenan induced edema in a dose depended manner, which could be used as a potential antiallergic agent.
Two unprecedented aconitine-type C19-diterpenoid alkaloids, refractines A-B (1-2), along with 12 known compounds (3-14) were isolated from the roots of Aconitum refractum (Finet et Gagnep.) Hand. ...-Mazz. Their structures were elucidated based on extensive spectroscopic analyses, including 1D and 2D NMR, IR, and HR-ESI-MS data. All compounds were tested for inhibitory activities against NO production in LPS induced RAW 264.7 macrophages, compounds 10 and 14 had slight inhibited NO production with rate of 29.4% and 22.1% at the concentration of 30 μM, respectively.
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