Phellinus baumii is used to treat inflammatory bowel disease (IBD) and gastroenteritis. In this study, a 46 kDa heteropolysaccharide SHPS-1 was isolated from fruiting bodies of P. baumii. SHPS-1 ...consisted of arabinose, mannose, glucose, and galactose at a molar ratio of 2.2:15.7:49.3:32.8. SHPS-1 had a backbone containing 1,3-linked β-D-Glcp and 1,6-linked α-D-Galp residues, and Araf, Manp and Galp units were attached as oligosaccharidic side chains to the backbone at C-6 of some glucopyranoses. SHPS-1 decreased phosphorylation level of STAT-1 and expression levels of STAT-1 targeted genes such as iNOS and TNF-α in lipopolysaccharide-stimulated macrophage RAW 264.7 cells. Furthermore, SHPS-1 promoted the expression of IL-10 and macrophage mannose receptor CD 206, markers of tissue repairing macrophages. SHPS-1 alleviated ulcerative colitis in mice by decreasing pro-inflammatory genes and increasing anti-inflammatory and tissue repairing genes. Collectively, SHPS-1 polysaccharide from P. baumii had anti-inflammatory activity and can potentially treat IBD.
•Polysaccharide SHPS-1 was isolated from fruiting bodies of mushroom Phellinus baumii.•SHPS-1 contains 1,3-linked β-D-Glcp and 1,6-linked α-D-Galp units in backbone.•Araf, Manp and Galp units are attached as side chains to the backbone at C-6 of glucopyranoses.•SHPS-1 is anti-inflammatory and can potentially treat inflammatory bowel disease.•SHPS-1 decreased STAT-1 phosphorylation and stimulated macrophage mannose receptor.
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Berberine (Ber), an isoquinoline alkaloid, is a potential drug therapy for ulcerative colitis (UC) because of its anti-inflammatory activity, high biological safety, and few side ...effects. Nevertheless, its clinical application is hindered by its limited water solubility and low bioavailability. Currently, compared to synthetic nanocarriers, exosomes as carriers possess advantages such as low toxicity, high stability, and high specificity. Human placental mesenchymal stem cell-derived exosomes (HplMSC-Exos) have emerged as a promising drug delivery system, offering intrinsic anti-inflammatory and antioxidant activities. Therefore, we engineered MSC-Exos loaded with Ber (Exos-Ber) to enhance the solubility and bioavailability of Ber and for colon targeting, revealing a novel approach for treating UC with natural compounds. Structurally and functionally, Exos-Ber closely resembled unmodified Exos. Both in vitro and in vivo investigations confirmed the antioxidant and anti-inflammatory properties of Exos-Ber. Notably, Exos-Ber exhibited reparative effects on injured epithelial cells and reduced cellular apoptosis. Furthermore, Exos-Ber concurrently demonstrated anti-inflammatory and antioxidant activities, contributing to the mitigation of UC, possibly through its modulation of the MAPK signaling pathway. Overall, our findings demonstrate the potential of Exos-Ber as a promising therapeutic option for alleviating UC, highlighting its capacity to enhance the clinical applicability of Ber.
Fourteen undescribed nitrogenous merosesquiterpenoids, purpurols A−D (1–4) and puraminones A−J (5–14), along with three known related compounds (15–17) were isolated from the sponge Pseudoceratina ...purpurea collected in the South China Sea. Their structures and absolute configurations were unambiguously elucidated by a combination of spectroscopic data, X-ray diffraction analysis, electronic circular dichroism calculations, and chemical derivatization. Purpurols A−D (1–4) incorporated nitrogenous heterocycles, compounds 1 and 2 feature an unusual benzothiazole ring, while 3 and 4 feature benzoxazole ring. Puraminones A−J (5–14) represent sesquiterpenoid aminoquinones with different amine and amino acid side chains at C-20. Additionally, twenty unreported sesquiterpenoid aminoquinone analogues were obtained through chemical derivatization. It is worth noting that all compounds are featured with unusual rearranged 4,9-friedodrimane subunit. In the bioassays, purpurols A and B showed weak anti-inflammation in zebrafish, as well as some compounds showed activities against tumor cells, therefore, preliminary structure–cytotoxicity relationships are also discussed.
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•Fourteen undescribed nitrogenous merosesquiterpenoids were reported.•Their structures were elucidated by NMR, ECD, chemical derivatization, and X-ray diffraction.•Compounds 1 and 2 showed weak anti-inflammation in zebrafish.•Compounds 5, 9, 10, and 14 showed moderate cytotoxicity against K562 cell lines.
Herein, 17 previously undescribed polyacetylenes and 9 known ones were isolated from Tridax procumbens L. Their structures were identified using spectroscopic techniques (NMR, UV, IR, MS and optical ...rotation), the modified Mosher method, electronic circular dichroism (ECD) data and ECD calculation. The cytotoxicity of polyacetylenes on six human tumour cell lines (K562, K562/ADR, AGS, MGC-803, SPC-A-1 and MDA-MB-231) was evaluated. (3S,10R)-tridaxin B (2a), (3S,10S)-tridaxin B (2b) and tridaxin F (8) demonstrated substantial cytotoxic effects against the K562 cell line, with half-maximal inhibitory concentration (IC50) values of 2.62, 14.43 and 17.91 μM, respectively. Cell and nucleus morphology assessments and Western blot analysis confirmed that the cytotoxicity of the three polyacetylenes on K562 cells was mediated through a dose-dependent apoptosis pathway. Furthermore, (3S,10R)-tridaxin A (1a) and tridaxin G (9) exhibited considerable inhibitory effects on lipopolysaccharide-stimulated nitric oxide production in RAW 264.7 macrophages, with IC50 values of 15.92 and 20.35 μM, respectively. Further investigations revealed that 9 exerted anti-inflammatory activities by impeding the nuclear translocation of NF-κB and down-regulating the expression of pro-inflammatory factors, including those of iNOS, COX-2, IL-1β and IL-6, in a concentration-dependent manner. The study provides evidence that polyacetylenes from T. procumbens may serve as a potential source of anti-tumour or anti-inflammatory agents for treating related diseases.
Twenty-six polyacetylenes, including seventeen previously undescribed compounds, were isolated from Tridax procumbens L. Display omitted
•Seventeen previously undescribed polyacetylenes were isolated from Tridax procumbens.•Cytotoxic and anti-inflammatory activities of these polyacetylenes were investigated.•Polyacetylenes from T. procumbens may serve as anti-tumor or anti-inflammatory agent.
Meliasanines A–L, twelve previously unreported tirucallane-type triterpenoids, together with fifteen known ones, have been isolated from the stem bark of Melia toosendan. Their structures and ...absolute configurations were determined based on HRESIMS, and NMR, combined with calculated ECD and single-crystal X-ray diffraction analyses. Subsequently, all compounds except 10 were evaluated for their inhibitory effect on the production of nitric oxide induced by lipopolysaccharide in RAW264.7 macrophage cells. The results indicated that seven compounds (1, 13, 14, 16, 20, 22, and 23) exhibited significant NO inhibitory effects, with IC50 values ranging from 1.35 to 5.93 μM, which were more effective than the positive control indomethacin (IC50 = 13.18 μM). Moreover, the corresponding results of Western blot analysis revealed that meliasanine A (1) can significantly suppress the protein expression of inducible nitric oxide synthase and cyclooxygenase 2 in a concentration-dependent manner. The mechanism study suggested that meliasanine A exerts an anti-inflammatory effect via the nuclear factor-κB signaling pathway by suppressing phosphorylation of P65 and IκBα.
Twelve undescribed tirucallane-type triterpenoids were isolated from the stem bark of Melia toosendan. The compound 1 showed a significant anti-inflammatory effect via NF-κB signaling pathway. Display omitted
•Twelve undescribed tirucallane-type triterpenoids were isolated from M. toosendan.•The absolute configurations of 1 and 5 were elucidated by X-ray crystallographic.•Seven compounds exhibited significant NO inhibitory effects with IC50 1.35–5.93 μM.•Meliasanine A exerts an anti-inflammatory effect via NF-κB signaling pathway.
Objective:To evaluate and compare the antioxidant potential and anti-inflammatory activity of ethanolic extract of flowers of Moringa oleifera(M.oleifera)grown in Oman.Methods:Flowers of ...M.oleiferawere collected in the month of December 2012 and identified by a botanist.Alcoholic extract of the dry pulverized flowers ofM.oleiferawere obtained by cold maceration method.The ethanolic flower extract was subjected to preliminary phytochemical screening as the reported methods.Folin-Ciocalteu reagent was used to estimate total phenolic content.DPPH was used to determinein-vitroantioxidant activity and anti-inflammatory activity of flowers was investigated by protein denaturation method.Results:Phytochemical analysis of extract showed presence of major classes of phytochemicals such as tannins,alkaloids,flavonoids,cardiac glycosidesetc.M.oleiferaflowers were found to contain 19.31 mg/g of gallic acid equivalent of total phenolics in dry extract but exhibited moderate antioxidant activity.The anti-inflammatory activity of plant extract was significant and comparable with the standard drug diclofenac sodium.Conclusions:The results of our study suggest that flowers ofM.oleiferapossess potent anti-inflammatory activity and are also a good source of natural antioxidants.Further study is needed to identify the chemical compounds responsible for their anti-inflammatory activity.
ETHNOPHARMACOLOGICAL RELEVANCEThe fruits of wampee (Clausena lansium (Lour.) Skeels), which contain significant amounts of phenolics, are frequently applied as traditional medications to prevent or ...relieve inflammatory symptoms. Green honey wampee (GHW) is a local cultivar specially cultivated in Lianjiang City, Guangdong Province.AIM OF THE STUDYThis study aimed to investigate phenolic distribution profiles in the peels, seeds and pulp of GHW as well as elucidate the underlying molecular mechanisms of the effective compounds for anti-inflammatory activity.MATERIALS AND METHODPhenolic compounds in the extract were identified through UPLC-MS/MS and their ability to alleviate inflammation was assessed using RAW 264.7 macrophages exposed to lipopolysaccharide.RESULTSAmong the three parts of GHW fruits, the total phenolic contents followed a descending order of peels > pulp > seeds. Additionally, eighty-six phenols were tentatively determined from the three parts, of which flavonoids accounted for the highest proportion. Furthermore, the phenolic extract of peels, seeds and pulp exhibited potential anti-inflammatory activity through the suppression effect on different pro-inflammatory mediators (NO, IL-6 and TNF-α). Among the three principal phenolic compounds (rutin, quercitrin, isorhamnetin-3-O-neohesperidoside) detected in GHW fruits, quercitrin was proved to be a more important anti-inflammatory compound inhibiting the iNOS and TNF-α mRNA expressions through the suppression effect on the phosphorylation of IκBα and ERK, belonging to the NF-κB and MAPK signaling pathway respectively.CONCLUSIONSNot only wampee pulp but also its by-products like peels and seeds are able to be comprehensively utilized as immunomodulatory supplements for daily diets due to their rich phenolic contents.
Twenty target compounds were designed, synthesized and evaluated in terms of their biological activity.
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Twenty benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety were ...synthesized and evaluated for their anti-oxidant and anti-inflammatory activities. Among these compounds, 8h and 8l were appeared to have high radical scavenging efficacies as 0.05 ± 0.02 and 0.07 ± 0.03 mmol/L of IC50 values in ABTS+ bioassay, respectively. In anti-inflammatory tests, compound 8h displayed good activity with 57.35% inhibition after intraperitoneal administration, which was more potent than the reference drug (indomethacin). Molecular modeling studies were performed to investigate the binding mode of the representative compound 8h into COX-2 enzyme. In vitro enzyme study implied that compound 8h exerted its anti-inflammatory activity through COX-2 inhibition.
Periplaneta americana is a medicinal insect that has been applied to promote blood circulation and remove blood stasis based on traditional Chinese medicine (TCM) for a long time. Its modern ...preparation, Xinmailong injection, was adopted for the treatment of congestive heart failure (CHF). The bioactive constituents of P. americana and their correlation with its traditional uses need further investigation.
This study aimed to elucidate the N-acetyldopamine (NADA) oligomers from P. american, determine their spatial distribution, and investigate their anti-inflammatory and vasorelaxant effects to provide scientific evidence supporting the clinical use of this medicinal insect.
NADA oligomers were isolated from the CH2Cl2: CH3OH (2:1) extract of P. americana, through sequential chromatographic methods including silica gel, Sephadex LH-20, preparative HPLC, and chiral-phase separation. Their structures were determined by HRESIMS, 1D and 2D NMR spectroscopic analysis, chiral resolution, and calculated electronic circular dichroism analysis. With the aid of atmospheric pressure scanning matrix-assisted laser desorption/ionization mass spectrometry imaging (AP-SMALDI MSI), the isolated compounds in a spatial profile within P. americana were identified. NO production was measured to assess anti-inflammatory activity. Vasorelaxant activity assessments were performed on the norepinephrine-precontracted 3rd-order mesenteric arteries.
Seven new NADA trimers, peridopamines A−G (1−7), two new NADA dimers, peridopamines H and I (8 and 9), and six known NADA derivatives (10−15), were obtained from P. americana. The trimers and dimers were detected and showed similar pattern of distribution with accumulation in peripheral and rigid parts of P. americana, based on quasimolecular ion AP-SMALDI MS images of sections from the whole body and dissected areas of the insect. Furthermore, the anti-inflammatory and vasorelaxant effects of isolated compounds were investigated. Compounds 8 and 9 presented significant and moderate anti-inflammatory potentials, respectively. Compounds 8, 10, 12 and 15 possess significant vasorelaxant potentials at concentrations correlated with EC50 values of 6.7–23.7 μM.
Fifteen NADA oligomers were isolated from P. americana. The distribution of these compounds was visualized by AP-SMALDI imaging experiments and NADA oligomers were mainly observed in peripheral parts. Bioassays showed that the tested compounds had anti-inflammatory and vasorelaxant activities, which indicated that NADA oligomers are active ingredients of this insect-based TCM and have potential for the treatment of cardiovascular disease.
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•Nine new N-acetyldopamine (NADA) oligomers, and six known ones were obtained from Periplaneta americana.•Isolated NADA Oligomers exhibited anti-inflammatory and vasorelaxant activities.•This paper provided a rapid and visualized analytical strategy for bioactive constituents research of insect-based TCM.
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