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Food Bioscience · 2024 · IF 4.8

Punicalagin ameliorates DSS-induced colitis in mice through strengthening gut barrier, decreasing oxidative stress and downregulating inflammation via AMPK–NF–κB-STAT3 pathway

Huanhuan Liu,Jiahui Li,Chunhong Yan,Jiaxiu Liu,Dongyun Zhao,Shugang Li,Xiaodong Xia

Inflammatory bowel disease is characterized by compromised epithelium barrier function and hyperactive intestinal inflammation. This study aims to investigate the effects of punicalagin, a bioactive ellagitannin in pomegranate, on dextran-sodium sulfate (DSS) - induced colitis in mice and to examine the underlying mechanisms involved. Oral administration of punicalagin (100 mg/kg/day) effectively mitigated the severity of experimental colitis in mice, evidenced by increased colon length, improved intestinal permeability, and decreased histological scores. Punicalagin up-regulated the mRNA expression level of Muc2 in and the protein expression of zonula occludens-1 (ZO-1) and Occludin in colitic mice. Moreover, punicalagin effectively decreased reactive oxygen species (ROS) levels in the colon, and in Caco-2 cells exposed to H 2 O 2 in vitro . Mechanistically, punicalagin attenuated inflammation by inhibiting the secretion of interleukin-6 (IL-6) and the phosphorylation of the NF-κB/STAT3 pathway. In addition, punicalagin increased adenosine monophosphate activated protein kinase (AMPK) phosphorylation in the colon of DSS-treated mice and lipopolysaccharide (LPS) -induced RAW 264.7 macrophages. Knocking down AMPKα by siRNA diminished punicalagin's anti-inflammatory function in RAW 264.7 macrophages exposed to LPS. Furthermore , molecular docking analysis, cellular thermal shift assay (CETSA), and drug affinity responsive target stability (DARTS) analysis supported the direct interaction between punicalagin and AMPK. In conclusion, punicalagin could mitigate DSS-induced colitis through enhancing intestinal epithelial barrier, alleviating oxidative stress, and attenuating inflammation partly through modulation of AMPK–NF–κB-STAT3 pathway.

研究领域: 药理学 · 免疫学 · 胃肠病学
✓ 已验证 DOI 高影响因子
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FOOD AND BIOPRODUCTS PROCESSING · 2024 · IF 3.5

Improving the functional components and biological activities of navel orange juice through fermentation with an autochthonous strain Lactiplantibacillus paraplantarum M23

Meiling Huang,Chunling Lai,Yan Liang,Qin Xiong,Chaoyun Chen,Zhiran Ju,Yueming Jiang,Jun Zhang

The fermentation of navel orange juice with lactic acid bacteria (LAB) has rarely been investigated. In this study, an autochthonous LAB strain isolated from navel orange, Lactiplantibacillus paraplantarum M23, was found to effectively ferment navel orange juice, producing a juice with enhanced functional activities and organoleptic quality. The viable bacterial count in the fermented orange juice remained consistently above 8.51 log CFU/mL throughout the entire 7-day fermentation period. The content of vitamin C (VC), total phenolic content (TPC), total flavonoid content (TFC), and hesperidin in the fermented orange juice increased by a maximum of 28.88, 1.21, 1.13, and 1.16 times, respectively, compared to the unfermented orange juice. The fermented juice exhibited significantly higher antioxidant activity than the unfermented juice, with an increase of up to 255 % and 347 % based on 1,1-diphenyl-2-picrylhydrazyl (DPPH) and ferric ion reducing antioxidant power (FRAP) assays, respectively. This may be attributed to the increase in VC and flavonoids, as demonstrated by Pearson's correlation analysis. Additionally, the fermented orange juice demonstrated improved α-glucosidase inhibition, anti-MRSA, and anti-glycation activities compared to the unfermented juice. Furthermore, the fermented juice notably reduced the levels of NO and ROS in Raw 264.7 cells without any negative impact on cell viability. The findings of this study may help in the development of nutritious and healthy fermented navel orange juice products, and serve as a reference for the production of fermented beverages from other fruits using autochthonous strains.

研究领域: 食品科学 · 微生物学 · 营养学 · 生物化学
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2019 · IF 3.571

Transglycosylation Improved Caffeic Acid Phenethyl Ester Anti-Inflammatory Activity and Water Solubility by Leuconostoc mesenteroides Dextransucrase

Yao Li,Lan-hua Liu,Xiao-qin Yu,Yu-xin Zhang,Jing-wen Yang,Xue-qin Hu,Hong-bin Zhang

Bioglycosylation is an efficient strategy to improve the biological activity and physicochemical properties of natural compounds for therapeutic drug development. In this study, two caffeic acid phenethyl ester (CAPE) glucosides (G-CAPE and 2G-CAPE) were synthesized by transglycosylation with dextransucrase from Leuconostoc mesenteroides 0326 with CAPE as an acceptor and sucrose as a donor. The products were purified and the structures were characterized. The physicochemical properties, anti-inflammatory activity, and cytotoxicity of the two CAPE glucosides were measured. The water solubility of G-CAPE and 2G-CAPE is 35 and 90 times higher, respectively, than that of CAPE. Compared to CAPE, the monoglycoside product showed superior anti-inflammatory effects, and its inhibition rate of NO, IF-6, and TNF-α is 93.4%, 76.81%, and 56.58% in RAW 264.7 macrophages, respectively, at 20 μM. Also, the cytotoxicity of both products was significantly improved. These glycosylation-modified CAPEs circumvent some of the flaws in CAPE application in anti-inflammatory drugs.

CAS / MDL: 75-05-8 7732-18-5
研究领域: 药学化学 · 生物化学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOORGANIC CHEMISTRY · 2022 · IF 5.307

Twelve novel sesquiterpenes with anti-inflammatory and cholesterol-lowering activities from burdock leaves

Hanjing Liang,Qingmei Feng,Hui Guo,Jiangnan Lv,Lingxia Zhang,Qingxia Li,Jun Chi,Qiuyan Liu,Zhimin Wang,Liping Dai

Nine new cadinane-type sesquiterpenoids ( 1 – 9 ) and three new eucalyptane -type sesquiterpenes ( 10 – 12 ) were isolated from the ethyl acetate extract of Burdock leaves, which were commonly used for preventing or treating atherosclerosis in China. Their structures were confirmed by extensive spectroscopic analysis, single-crystal X-ray diffraction analysis and ECD calculations. Compound 1 possessed the rare large conjugated skeleton. All the isolates were evaluated for anti-inflammatory and cholesterol-lowering activities by the LPS- and oxidized-low-density-lipoprotein-stimulated RAW 264.7 cells, respectively. As the results, all isolates could decrease the productions of NO, and down-regulate the accumulation of cholesterol. Among them, 4 showed the most potent cholesterol-lowering effect. For the high content of 4 in the herb, mechanistic study of 4 was performed and the results showed that 4 markedly reduced the release of pro-inflammatory mediators which was probably associated with inhibition of the PI3K/Akt and 5-LOX signaling pathways. The findings of this study demonstrated the anti-inflammatory/cholesterol-lowering effects of the new sesquiterpenes from burdock leaves, which provides chemical basis and scientific evidence for the herb used as anti-atherosclerosis agents for the further study. The sesquiterpene lactones of burdock leaves are expected to become new small molecule inhibitors for the treatment of AS .

研究领域: 药理学 · 化学 · 分子生物学 · 植物科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF FOOD SCIENCE · 2022 ·Vol. 87 ·期 7 ·3223-3234 · IF 3.693

Digestion behavior of a polysaccharide from Cyclina sinensis: An explanation for the discrepancy in its immunostimulatory activities in vitro and in vivo

Youxian Zhou,Yue Gong,Zhengqi Liu,Lilong Wang,Chunqing Ai,Chengrong Wen,Taihai Zhu,Shuang Song

Although numerous polysaccharides have demonstrated potential immunostimulatory activities in in vitro models, only a few of them successfully stimulate the immune system in vivo. In order to explore the possible reasons for the activity loss of polysaccharides in in vivo models, the immunostimulatory activities in vitro and in vivo and the digestion behavior of a polysaccharide from Cyclina sinensis (CSP) were investigated in the present study. CSP showed obvious immunostimulatory activity in a RAW 264.7 cell model. In in vitro experiment, CSP did not exhibit cytotoxicity at concentrations of ≤10 µg/ml, and significantly increased NO production at concentrations of 0.4–10 µg/ml, suggesting CSP processes immunostimulatory activity in vitro. Further investigation using simulated digestion model indicated that CSP could bind with the protein in the digestive fluids to form precipitate in both the stomach and small intestine, and it could be seriously degraded by amylase during the digestion in the small intestine. Furthermore, the in vivo immunostimulatory activity evaluation demonstrated CSP had no effect on immunosuppressed mice as indicated by the body weight, thymus and spleen indexes, and TNF-α, IL-1β, IL-6, and IL-10 mRNA expression. Thus, the present study indicates that the degradation and precipitation of CSP in the digestive tract are the possible reasons for the activity loss of CSP after digestion. Practical Application Cyclina sinensis is the common aquatic shellfish in China and plays an important role in the marine aquaculture industry. Cyclina sinensis polysaccharide (CSP) is the main active component of C. sinensis . The structure characterization and immunostimulatory activity of a purified fraction of CSP (CSP-1) and the effect of digestion on CSP and its immunostimulatory activity were studied. The result of this study promotes the understanding of the nutritional function effects and provides a scientific reference for the rational development and high-value utilization of C. sinensis .

CAS / MDL: 67-68-5
研究领域: 免疫学 · 营养科学 · 海洋生物学 · 药学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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FOOD RESEARCH INTERNATIONAL · 2023 · IF 8.1

Microfluidic fabrication of size-controlled nanocarriers with improved stability and biocompatibility for astaxanthin delivery

Meng Guo,Weina Cui,Yuanchao Li,Siyuan Fei,Chaofan Sun,Mingqian Tan,Wentao Su

Improving the stability of astaxanthin (AST) is a vital way to enhance its oral bioavailability. In this study, a microfluidic strategy for the preparation of astaxanthin nano-encapsulation system was proposed. Thanks to the precise control of microfluidic and the rapid preparation ability of the Mannich reaction, the resulting astaxanthin nano-encapsulation system (AST-ACNs-NPs) was obtained with average sizes of 200 nm, uniform spherical shape and high encapsulation rate of 75%. AST was successfully doped into the nanocarriers, according to the findings of the DFT calculation, fluorescence spectrum, Fourier transform spectroscopy, and UV–vis absorption spectroscopy. Compared with free AST, AST-ACNs-NPs showed better stability under the conditions of high temperature, pH and UV light with<20% activity loss rate. The nano-encapsulation system containing AST could significantly reduce the hydrogen peroxide produced by reactive oxygen species, keep the potential of the mitochondrial membrane at a healthy level, and improve the antioxidant ability of H 2 O 2 -induced RAW 264.7 cells. These results indicated that microfluidics-based astaxanthin delivery system is an effective solution to improve the bioaccessibility of bioactive substances and has potential application value in food industry.

CAS / MDL: 56-87-1
研究领域: 药学 · 纳米技术 · 生物医学工程 · 食品科学 · 化学工程
✓ 已验证 产品关联 DOI PubMed 高影响因子
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FITOTERAPIA · 2018 · IF 2.642

LC-MS guided isolation of gracilistones A and B, a pair of diastereomeric sesquiterpenoids with an unusual tetrahydrofuran-fused tricyclic skeleton from Acanthopanax gracilistylus and their potential anti-inflammatory activities

Hong-Bo Xu,Tong-Hua Yang,Pei Xie,Zhi-Shu Tang,Xiao Song,Huai-Li Xu,Yan-Hong Li,Dong-Bo Zhang,Yan-Ru Liu,Yan-Ni Liang,Yu Zhang,Shi-Jun Liu,Si-Min Wei,Chen Sun,Hong-Bo Liu,Chong Deng,Wei Wang

Gracilistones A ( 1 ) and B ( 2 ), two new eudesmane-type sesquiterpenoids with an unusual tetrahydrofuran-fused 6/6/5 tricyclic ring system, were obtained from Acanthopanax gracilistylus under the guidance of LC-MS investigation. Their structures and absolute configurations were assigned by extensive spectroscopic analyses and quantum calculation methods. Compounds 1 and 2 showed potent inhibitory activity against LPS-induced nitric oxide production in RAW 264.7 macrophages, compared with the positive control L-NMMA. In addition, compounds 1 and 2 were also evaluated for their antioxidant (DPPH • and ABTS •+ ) and xanthine oxidase (XO) inhibitory activities, and they exhibited weak inhibitory effects at 100 μM.

研究领域: 药用植物学 · 药物化学 · 炎症研究 · 天然产物化学
✓ 已验证 DOI PubMed 高影响因子
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ENVIRONMENTAL POLLUTION · 2019 · IF 5.714

Autophagy protects murine macrophages from β-cypermethrin-induced mitochondrial dysfunction and cytotoxicity via the reduction of oxidation stress

Bingnan He,Xia Wang,Jianbo Zhu,Baida Kong,Lai Wei,Yuanxiang Jin,Zhengwei Fu

The immunotoxicity of synthetic pyrethroid (SPs) has garnered much attention, and our previous research demonstrated that β-CYP causes immunotoxicity and oxidative stress in macrophages. Nevertheless, the underlying mechanism remains largely unknown. In this study, the murine macrophage RAW 264.7 cells and murine peritoneal macrophages (PMs) were exposed to β-CYP. The results showed that β-CYP elevated intracellular ROS levels in both RAW 264.7 cells and PMs. Exposure to β-CYP also caused mitochondrial dysfunction with reduced mitochondrial membrane potential (MMP), intracellular ATP level and mitochondrial DNA (mtDNA) content in the two cell types. In addition, exposure of RAW 264.7 cells to β-CYP for 12 h and 24 h enhanced autophagy, with elevated Beclin1, Rab7, Lamp1 and LC3-II expression levels, while 48 h of exposure attenuated autophagy. In contrast, exposure of PMs to β-CYP for 12 h promoted autophagy, whereas exposure for 24 h and 48 h impaired autophagy. Cotreatment with an antioxidant, N-acetyl-L-cysteine (NAC), partially blocked the reduced MMP, intracellular ATP level and autophagy disturbance. Moreover, cotreatment with an autophagy agonist, rapamycin (RAPA), partially blocked mitochondrial dysfunction and oxidative stress in the two cell types, whereas cotreatment with an autophagy inhibitor, 3-methyladenine (3-MA), augmented the abovementioned toxic effects. Furthermore, mitochondrial ROS levels in both RAW 264.7 cells and PMs were elevated by exposure to β-CYP, and molecular docking showed that β-CYP docked with mouse respiratory chain complex I by binding to the ND2, ND4, and ND5 subunits of the protein complex. Taken together, the data obtained in the present study demonstrate that oxidative stress partially mediates mitochondrial dysfunction and autophagy disturbance upon exposure to β-CYP in macrophages, and autophagy plays a protective role against the toxic effects.

研究领域: 免疫毒理学 · 细胞生物学 · 毒理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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FOOD CHEMISTRY · 2024 · IF 8.5

Physicochemical evaluation, structural characterization, in vitro and in vivo bioactivities of water-soluble polysaccharides from Luobuma (Apocynum L.) tea

Aminu Shehu Abubakar,Bilal Ahmad,Nabi Ahmad,Liangliang Liu,Bin Liu,Yatong Qu,Jikang Chen,Ping Chen,Haohan Zhao,Jia Chen,Kunmei Chen,Gang Gao,Aiguo Zhu

Luobuma tea is made from the leaves of Apocynum hendersonii (Bt) and A. venetum (Ht) and has been used for a very long time in China and Japan as herbal tea. This study isolated water-soluble polysaccharides from the two species` teas. Physicochemical properties, structural properties, in vitro and in vivo antioxidant and immunomodulatory activities were determined for the first time. The results showed that the Bt and Ht polysaccharides with molecular weights of 31.21 and 49.11 kDa, respectively, composed of arabinose, galactose, rhamnose, glucose, xylose, fucose, and mannose. A dose-dependent nitric oxide production and interleukin-6 inhibitory effects were obtained. Also, they suppressed the expression of cyclooxygenase-2, tumor necrosis factor-α and interleukin-6 mRNA in LPS-induced RAW 264.7 macrophages. Likewise, Bt and Ht have significantly reduced edema in the paws of mice after carrageenan injection. These results suggested that the Luobuma teas polysaccharides can be explored as potential antioxidants and anti-inflammatory agents.

CAS / MDL: 74-88-4
研究领域: 药理学 · 生物化学 · 免疫学 · 植物科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of Materials Chemistry B · 2022 ·Vol. 10 ·期 18 ·3491-3500 · IF 7.571

Self-assembled D-arginine derivatives based on click chemical reactions for intracellular codelivery of antigens and adjuvants for potential immunotherapy

Xiao He,Yannv Qu,Xiaohong Lin,Jiapan Sun,Zhiru Jiang,Chaodong Wang,Yuanfei Deng,Fei Yan,Yansun Sun

Self-assembled amino acid derivatives could form well-defined nanostructures which have great application value for drug delivery systems. In particular, D-amino acid derivatives possess tremendous advantages including anti-degradation and good lysosome escape compared with L-amino acid derivatives. In this work, 9-fluorenylmethyloxycarbonyl (Fmoc) neighboring D-arginine derivatives were replaced by dibenzocyclooctyne (DBCO) to extend the class of functional D-arginine derivatives, which were further reacted with various cross-linkers including azide to construct a library of self-assembled supramolecular nanovehicles and strengthen the stability of nanostructures for disease immunotherapy. Moreover, in vitro studies demonstrated that the combination of DBCO modified D-arginine derivative DR3 and cross-linker C1 not only reinforced the cellular uptake efficiency of ovalbumin (OVA) which was chosen as the model antigen, but also promoted the cytokine TNF-α release of RAW 264.7 cells after the introduction of adjuvant unmethylated cytosine-phosphate-guanine dinucleotides (CpG). Furthermore, the nanovaccine based on DR3C1 could enhance the antigen OVA and adjuvant cytosolic delivery of marrow derived dendritic cells (BMDCs), which improved the antigen-presentation cross efficiency and induced the maturation of BMDCs. Taken together, we believe that D-arginine derivatives functionalized by DBCO provide an effective strategy for disease immunotherapy and act as a great potential delivery tool.

CAS / MDL: 157-06-2
研究领域: 纳米技术 · 免疫学 · 药物递送系统 · 生物材料 · 药学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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International Journal of Nanomedicine · 2024 · IF 6.6

Fe-Capsaicin Nanozymes Attenuate Sepsis-Induced Acute Lung Injury via NF-κB Signaling

Ruijie Wang,Quan Li,Pengxin Wu,Ke Ren,Yan Li,Yang Wang,Huadong Zhu,Chuanzhu Lv

Background In sepsis, the lungs are one of the most severely affected organs, usually resulting in acute lung injury (ALI). Capsaicin (CAP) is a natural compound found in chili peppers that has pain-relieving and anti-inflammatory properties. Here, we report that nanoparticles containing capsaicin and iron (Fe-CAP NPs) exhibited anti-inflammatory effects in the treatment of ALI. Methods The morphological characteristics of nanozymes were detected. RAW 264.7 cells were divided into four groups: control, lipopolysaccharide (LPS), CAP+LPS and Fe-CAP+LPS groups. The expression of inducible nitric oxide synthase (iNOS), transforming growth factor-β (TGF-β), and tumor necrosis factor-α (TNF-α) was assessed by immunofluorescence, Western blot, and enzyme-linked immunosorbent assay (ELISA). Nuclear factor kappa-B (NF-κB) expression was determined by Western blot. C57 mice were divided into control, LPS, CAP+LPS and Fe-CAP+LPS groups. Interleukin-6 (IL-6) and iNOS expression in the lung was detected by Western Blot. IL-6 and TNF-α expression in serum was detected by ELISA. Extravasated Evans blue, histopathological evaluation and wet-to-dry (W/D) weight ratio were used to assess pulmonary capillary permeability. The blood and major organs (heart, liver, spleen, lung and kidney) of mice were tested for the toxicity of Fe-CAP NPs. Results In the LPS group, TNF-α, iNOS, p-NF-κB and p-IKBα expression increased. However, their expression was significantly decreased in the Fe-CAP+LPS group. TGF-β expression showed the opposite trend. In vivo, IL-6 and iNOS expression was notably increased in the lungs of LPS group of mice but decreased with Fe-CAP pretreatment. Fe-CAP significantly ameliorated lung EB leakage, improved the histopathology of lung tissue and reduced the W/D weight ratio. The nanoparticles showed non-cytotoxicity, when studying these biological activities. Conclusion Fe-CAP NPs could alleviated inflammation by inhibiting the expression of pro-inflammatory factors in macrophages, increasing the expression of anti-inflammatory factors, and alleviating lung tissue damage.

CAS / MDL: 10025-77-1 9003-39-8
研究领域: 药理学 · 免疫学 · 纳米技术 · 分子生物学 · 病理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ENVIRONMENTAL TOXICOLOGY · 2019 ·Vol. 35 ·期 2 ·159-166 · IF 2.649

Tetrabromoethylcyclohexane (TBECH) exhibits immunotoxicity in murine macrophages

Xia Wang,Lai Wei,Jianbo Zhu,Bingnan He,Baida Kong,Yuanxiang Jin,Zhengwei Fu

Tetrabromoethylcyclohexane (TBECH) has been linked to endocrine disruption, hepatotoxicity, and reproductive toxicity. However, its immunotoxicity remains largely unknown. In the present study, RAW 264.7 cells, mouse macrophage cell line, were exposed to TBECH. MTT assays showed that TBECH significantly enhanced lactate dehydrogenase (LDH) release in RAW 264.7 cells. The mRNA expression of some proapoptotic genes was upregulated by TBECH. Accordingly, TBECH elevated caspase-3 activity. In addition, TBECH upregualted the mRNA levels of some pro-inflammatory cytokines, whereas it downregulated LPS-stimulated mRNA expression of these cytokines. Moreover, TBECH downregulated the mRNA expression of selected antigen presenting-related genes. Furthermore, TBECH increased reactive oxygen species level, reduced glutathione content and the activities of superoxide dismutase and catalase, and upregulated the mRNA expression of selected oxidative stress-related genes. The obtained data demonstrated that TBECH exhibits immunotoxicity in macrophages, and will help to evaluate its health risks.

CAS / MDL: 3322-93-8
研究领域: 毒理学 · 免疫学 · 细胞生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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