International Journal of Nanomedicine
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2026
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IF 8.7
Jieying Zhou,Wei Luo,Lingxin Zeng,Shihao Xu,Ruohan Wu,Jiaqi Lu,Ying Li,Wei Xiong
Purpose While bubble-carrier systems hold great promise for enhancing the oral bioavailability of poorly water-soluble drugs, a deeper understanding of their underlying absorption mechanisms is still required. This study aimed to address this gap by developing a bubble-driven delivery system (BDDS) using the poorly water-soluble andrographolide (AG) as a model drug, and systematically evaluating its solubilization capacity and intestinal permeability.Methods The BDDS was optimized through the screening of effervescent formulations (citric acid: Na2CO3 = 6:5) and bile salts (sodium deoxycholate, SDC). Its performance was comprehensively assessed via in vitro dissolution tests, an everted intestinal sac assay, Caco-2 cell monolayer experiments, pharmacokinetic studies, and yeast-induced fever rat models.Results The BDDS achieved 75.0%–88.7% dissolution in gastrointestinal pH media, which was markedly superior to that of commercial dripping pills (DP; 30.5–50.2%). Its apparent permeability coefficient was 7.7-fold and 3.6-fold higher than that of free AG and DP, respectively. Transport studies indicated that SDC enhanced AG permeability primarily via the apical sodium-dependent bile acid transporter (ASBT)-mediated pathway, a mechanism further confirmed by inhibition with linerixibat. The relative oral bioavailability of BDDS versus DP reached 257.1%. BDDS demonstrated enhanced efficacy by significantly inhibiting key pro-inflammatory cytokines and thermoregulatory mediators in yeast-induced fever rats.Discussion The BDDS effectively overcomes AG’s low solubility (by SDC solubilization and CO2 bubbles) and permeability (via ASBT transport), outperforming conventional formulations in terms of preparation simplicity and storage stability.Conclusion BDDS is a promising strategy to improve oral absorption and therapeutic efficacy of BCS Class IV drugs like AG, with ASBT-mediated transport as a key mechanism.
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JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
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2022
·Vol. 103
·期 3
·1283-1293
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IF 4.125
Wei Xu,Yingying Kong,Tuo Zhang,Zhihua Gong,Wenjun Xiao
BACKGROUND l -Theanine (LTA) is a biologically active ingredient in tea that shows great potential for regulating lipid metabolism. Bile acids (BA), an important end-product of cholesterol catabolism, participate in the regulation of lipid metabolism and gut microbiota. Here, we investigated the effect of LTA on lipid metabolism and the mechanism by which it regulates BA metabolism and gut microbiota. Male BALB/c mice were treated with LTA for 28 days. RESULTS Daily LTA doses of 100 and 300 mg kg −1 d −1 altered the gut microbiota in mice, predominantly by decreasing Lactobacillus , Streptococcus, Bacteroides , Clostridium and Enterorhabdus microbes associated with bile-salt hydrolase (BSH) activity, thereby decreasing the activity of BSH and increasing the levels of ileum conjugated BA (such as glycocholic acid (GCA) and lithocholic acid), thereby inhibiting the intestinal farnesoid X receptor (FXR)-fibroblast growth factor 15 (FGF15) signaling pathway. Inhibition of FXR-FGF15 signaling was accompanied by upregulation of cholesterol 7α-hydroxylase (CYP7A1) mRNA and protein expression and increased hepatic production of cholic acid, deoxycholic acid, GCA, glycine cholic acid and glycine ursodeoxycholic acid. Meanwhile, increasing hepatic unconjugated BA upregulated the mRNA and protein expression of liver 3-hydroxy-3-methylglutaryl-CoA reductase and downregulated the mRNA and protein expression of stearoyl-CoA desaturase-1, liver low-density lipoprotein receptor and type B scavenger receptor. Therefore, the serum levels of cholesterol and triglycerides decreased. CONCLUSION Our findings indicate that LTA regulates lipid metabolism by modulating the gut microbiota and BA metabolism via the FXR-FGF15-CYP7A1 pathway. © 2022 Society of Chemical Industry.
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CELLULAR SIGNALLING
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2022
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IF 4.85
Zihang Yuan,Jie Wang,Haoran Zhang,Yuanyuan Chai,Yunxia Xu,Yingying Miao,Ziqiao Yuan,Luyong Zhang,Zhenzhou Jiang,Qinwei Yu
Aims The precise role of bile acid in the progression of liver fibrosis has yet to be elucidated. In this study, common bile duct ligation was used as an in vivo mouse model for the evaluation of bile acids that promote liver connective tissue growth factor expression. Main methods Primary rat and mice hepatocytes, as well as primary rat hepatic stellate and HepaRG cells were evaluated as in vitro models for promoting the expression of connective tissue growth factor by bile acids. Key findings Compared with taurochenodeoxycholic acid , glycochenodeoxycholic acid, and taurocholic acid , glycocholic acid (GCA) most strongly promoted the secretion of connective tissue growth factor in mouse primary hepatocytes, rat primary hepatocytes and HepaRGs. GCA did not directly promote the activation of hepatic stellate cells . The administration of GCA in mice with ligated bile ducts promotes the progression of liver fibrosis, which may promote the yes-associated protein of hepatocytes into the nucleus, resulting in the hepatocytes secreting more connective tissue growth factor for hepatic stellate cell activation. In conclusion, our data showed that GCA can induce the expression of connective tissue growth factor in hepatocytes by promoting the nuclear translocation of yes-associated protein, thereby activating hepatic stellate cells. Significance Our findings help to elucidate the contribution of GCA to the progression of hepatic fibrosis in cholestatic disease and aid the clinical monitoring of cholestatic liver fibrosis development.
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CARBOHYDRATE POLYMERS
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2022
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IF 10.723
Tao Wang,Junjie Han,Huanqin Dai,Jingzu Sun,Jinwei Ren,Wenzhao Wang,Shanshan Qiao,Chang Liu,Li Sun,Shuangjiang Liu,Dianpeng Li,Shenglong Wei,Hongwei Liu
Polysaccharides are known to confer protection against obesity via modulation of gut microbiota . To expand our knowledge of mushroom-derived prebiotics , we investigated the structural characteristics and anti-obesity effects of Lyophyllum decastes polysaccharides. Two heteroglycans were purified and characterized. The isolated polysaccharides effectively reduced obesity and the related disorders in the diet-induced obese (DIO) mice. An altered gut microbiota with enrichments of Bacteroides intestinalis and Lactobacillus johnsonii and an increase of secondary bile acids were detected in the polysaccharide-treated mice. Supplementation of B. intestinalis and L. johnsonii prevented the obesity and hyperlipidemia in DIO mice, demonstrating their causal linkage to the efficacy of polysaccharides. An enhancement of energy expenditure in the brown adipose tissues due to up-regulation of the secondary bile acids-activated TGR5 pathway was deduced to be one of the mechanisms underlying the effect of polysaccharides. These results confirmed Lyophyllum decastes -derived polysaccharides as new prebiotics for preventing and treating obesity.
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MICROCHIMICA ACTA
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2022
·Vol. 189
·期 7
·1-8
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IF 6.408
Ma Wen,Yang Bingxin,Li Jun,Liu Mingxia,Li Xianjiang,Liu Huwei
A series of functional metal–organic frameworks (MOFs) were facilely prepared through an one-pot procedure or post-synthetic modification strategy and used as matrices in laser desorption ionization mass spectrometry (LDI-MS). Compared with traditional organic matrices and other MOFs, maltose-functional MOF MIL-101-maltose demonstrated ultrahigh ionization efficiency, free matrix background, uniform crystallization, and good dispersibility. A simple, general, and efficient LDI-MS platform was developed for rapid detection of various small biomolecules using MIL-101-maltose as matrix, providing several advantages including low sample consumption of 500 nL, short analysis time of few seconds, strong salt tolerance (500 mM NaCl), and satisfactory reproducibility. The MIL-101-maltose matrix was used for serum glucose determination and successfully distinguished the diabetic patients from the healthy controls. This work provides a generic LDI-MS platform for fast determination of small biomolecules with high potential in clinical diagnosis and disease monitoring. Graphical abstract
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JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
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2022
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IF 3.318
Xiaoxu Cheng,Zifeng Pi,Zhong Zheng,Shu Liu,Fengrui Song,Zhiqiang Liu
Wu-tou decoction (WTD) is a traditional Chinese medicine (TCM) formula which has been used for treating rheumatoid arthritis (RA) for a thousand years. However, the underlying mechanism of WTD in treating RA is still unclear. In recent years, more and more attention has been paid to the role of gut microbiota and microbiota-derived metabolites in the treatment of RA. Hence, this study aims to investigate the roles of microbiota and microbial metabolites in the treatment of RA with WTD. Firstly, the therapeutic effects of WTD on adjuvant-induced arthritis (AIA) rats were evaluated. Then, the 16S rRNA sequencing analysis was used to clarify the changes of the intestinal microbiota and obtain the key microbiota affected by WTD. The important microbial metabolites were quantitated to explore the metabolic characteristics of WTD against RA by targeted metabolomics method. Finally, correlation analysis was performed to investigate the functional correlation among the gut microbiota, metabolites and RA-related serum indexes. The results indicated that WTD could relieve arthritis and reverse gut microbiota dysbiosis. The variation of short-chain fatty acids, bile acids, tryptophan metabolites and amino acids, which are important microbial metabolites, were reversed by WTD intervention. The correlation studies proved that WTD could regulate inflammation and intestinal barrier function partially by modulating Bacteroides, Prevotella, Akkermansia and their associated acetic acid, butyric acid, cholic acid and indole propionic acid. The anti-RA effects of WTD were partially mediated by gut microbiota and microbial metabolites. This study provides a new insight for treating RA and highlights the importance of gut microbiota in the treatment of diseases.
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2023
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IF 6.1
Wei Jia,Jiying Zhu
ε-Polylysine is a novel food preservative approved by the U.S. Food and Drug Administration (FDA), yet the mechanism of its effect on animal-derived foods remains unclear. Assessment of the effect of preservatives on goat meat products is necessary. Herein, metabolite accumulation and protein expression of ε-polylysine (0.025%, w/w) spiked with goat meat were investigated by nontarget metabolomics and proteomics combined with ultrahigh performance liquid chromatography quadrupole-Orbitrap high-resolution-mass spectrometry (UHPLC-Q-Orbitrap HRMS) in a simulated in vitro digestion model. The amino side chain of ε-polylysine increased the activity of glycine aminotransferase due to its nucleophilic nature, inducing a significant upregulation of l-arginine (0.43–0.72 mg kg–1) and creatine (3.98–6.89 mg kg–1), with an improvement in muscle quality of goat meat. Downregulation of enzyme phenylalanine hydroxylase expression led to upregulation of l-phenylalanine (2.26–3.25 mg kg–1) and l-tyrosine (0.98–1.29 mg kg–1). Collectively, this study first revealed the biochemical mechanism of ε-polylysine in goat meat products, which makes available new prospects for more accurate use of ε-polylysine in animal-derived foods.
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BMC Chemistry
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2021
·Vol. 15
·期 1
·1-9
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IF 2.61
Chen Lirong,Guo Yuqiu,Li Xiaoyue,Gong Kuijie,Liu Kaichang
The polyphenol distribution in fresh waxy corns of different color varieties and their functional activities, which may be useful for treating various chronic diseases, were investigated. The in vitro antioxidant activity, and hypoglycemic and hypocholesterolemic effects of the free and bound corn phenolics were determined to evaluate the edible value of fresh waxy corn. The colored varieties contained more phenols than the common varieties (white and/or yellow). The total free phenolic acid content of the six varieties was 6637.73 µg/g DW (dry weight), which was slightly higher (P > 0.05) than that of the total bound form (6276.65 µg/g DW). The total free flavonoid content was 5850.09 µg/g DW, which was higher (P < 0.05) than that of the total bound form (4874.51µg/g DW). No bound anthocyanin was detected in the methanol extracts of the tested varieties. For all the varieties, free polyphenols contributed 86−100 % and 70−78 % of the 2, 2-diphenyl-1-picrylhydrazyl (DPPH) and hydroxyl radical scavenging abilities, respectively, and 100 % of the ferric reducing capacity. The free phenolics in fresh waxy corn showed better (P < 0.05) hypoglycemic effect than the bound form in terms of inhibition of α-amylase activity, whereas the bound phenolics of most varieties showed higher α-glucosidase inhibitory activity than the free forms. The free phenolics showed better (P < 0.05) glycocholesterol binding than the bound form for all varieties. The bound polyphenols showed better sodium cholate and taurocholate binding than the free form for most varieties. In conclusion, the difference between free and bound polyphenol content and functional activities indicates that fresh waxy corn can be potentially used for the development of functional food.
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PHYTOTHERAPY RESEARCH
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2021
·Vol. 35
·期 5
·2678-2690
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IF 5.882
Yufei Sun,Zhiqiang Liu,Zifeng Pi,Fengrui Song,Jianlin Wu,Shu Liu
Alzheimer's disease (AD) is the most common neurodegenerative disorder. Amyloid beta-protein (Aβ) plaques, which are the hallmark of AD, are formed from the imbalance of Aβ production and clearance accompanied by neuroinflammation, gut dysbiosis, and metabolite dysfunction. All of these processes give rise to neurochemical deficiencies and synaptic dysfunction, which ultimately contribute to recognition dysfunction. Poria cocos (PC), which contains multiple active ingredients, plays a significant role in the treatment of multiple-pathogenesis senile diseases such as AD. Nevertheless, there are only very few investigations on the intricate action mechanism of PC for the treatment of AD. In this study, we evaluate the multi-target cure effect of PC on APP/PS1 mice by behavioral, immunohistochemical (IHC), targeted metabolomics, and 16S rRNA sequencing experiments. Mice treated with PC showed significant improvements in cognitive function as evaluated by the behavioral experiment. IHC revealed that PC treatment relieved Aβ deposition by reducing the formation of Aβ and increasing its clearance. Moreover, PC treatment improved gut dysbiosis, which reversed the metabolite dysfunction of bile acid. These findings reveal that PC is a promising therapeutic agent, which might ameliorate the cognitive function of AD by restoring the imbalance of Aβ production and clearance and gut microbiota dysbiosis.
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
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2020
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IF 3.209
Qiyi He,Huiyi Yang,Yingshan Chen,Ding Shen,Xiping Cui,Chunguo Zhang,Huanxin Xiao,Sergei A. Eremin,Yanxiong Fang,Suqing Zhao
Prussian Blue nanoparticles (PBNPs) were utilized in a lateral flow immunoassay (LFA) and in an indirect competitive nanozyme-linked immunosorbent assay (icELISA), respectively, for their intense blue color and peroxidase (POx) -like activity. The PBNPs with good POx-like activity was linked to the antibody. Under the optimal parameters, both the PBNP-icELISA and PBNP-LFA perform very well. The icELISA has an IC50 value of 190 ng/mL, the working range extends from 29 to 1200 ng/mL, and the limit of detection is 22 ng/mL. The visual cut-off limit is 10 ng/mL. The dual immunoassay was used to quantify glycocholic acid in spiked human urine. Excellent recoveries and correlation between the two methods were observed.
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Journal of Functional Foods
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2015
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IF 3.574
Guan-Lin Chen,Song-Gen Chen,Fu Chen,Ying-Qing Xie,Men-Di Han,Chun-Xia Luo,Ying-Ying Zhao,Yong-Qing Gao
In order to find new sources of natural antioxidants, total phenolic contents and antioxidant capacities of 11 fruit seeds before and after in vitro digestion were evaluated by Folin–Ciocalteu method, 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity assay (DPPH), ferric reducing antioxidant power assay (FRAP), and ABTS •+ scavenging activity (ABTS) assay, respectively. The correlations between DPPH, FRAP, ABTS values and total phenolic contents were also evaluated. The results showed that 11 fruit seeds had diverse antioxidant capacities and the variation was very large. Furthermore, the main compounds of 11 fruit seeds were identified and quantified. Four fruit seeds, Dimocarpus longgana Lour, Vitis vinifera Linn (red), Vitis vinifera Linn (black), and Litchi chinensis Sonn showed the strongest antioxidant activities whether before or after digestion, which implied that these fruit seeds are important natural sources for preventing oxidative stress diseases.
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Journal of Functional Foods
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2015
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IF 3.574
Guan-Lin Chen,Song-Gen Chen,Ying-Qing Xie,Fu Chen,Ying-Ying Zhao,Chun-Xia Luo,Yong-Qing Gao
In order to provide new information on the antioxidant activities before and after in vitro digestion of the selected flowers for consumers, nutritionists, and food policy makers, total phenolic and flavonoid contents and antioxidant capacities of 23 edible flowers were evaluated. In addition, some bioactive components in the flowers were also identified and quantified by ultra performance liquid chromatography (UPLC). The correlations between 2, 2-diphenyl-1-picrylhydrazylradical scavenging activity assay (DPPH), Ferric reducing antioxidant power assay (FRAP), and ABTS •+ radical cation scavenging activity assay (ABTS) values and total flavonoid contents and total phenolic contents were also evaluated. Three flowers, Osmanthus fragrans (Thunb.) Lour, Paeonia lactiflora Pall, and Rosa rugosa Thunb (purple) showed the strongest antioxidant activities before or after the digestion, which implied that these flowers are important natural sources for the prevention of oxidative stress diseases.
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