JOURNAL OF ETHNOPHARMACOLOGY
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2015
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IF 2.998
Sheng Wang,Yang Zhao,Junqing Zhang,Xiaoxing Huang,Yifei Wang,Xiaotao Xu,Bin Zheng,Xue Zhou,Huajie Tian,Li Liu,Qibing Mei
Ethnopharmacological relevance The fructus Alpinia oxyphylla Miq. (AOM) has been used for treating diarrhea with spleen deficiency and gastralgia for thousands of years. A number of traditional Chinese medicine formulae provide AOM as an alternative herbal treatment for diarrhea, but the scientific basis for this usage has not been well defined. Aim of the study In this study, we tried to investigate the antidiarrheal activity and possible mechanisms of Fructus AOM, aiming to enrich our understanding to the scientific meanings and theoretical significance of Fructus AOM in clinical practice. Materials and methods The fructus of AOM collected from Hainan province in China were macerated in the 95% ethanol to obtain the crude 95% ethanol extract, followed by subjected to chromatographic separation over a Diaion HP20 column to obtain 90% and 50% ethanol eluted fractions. The activities of the crude extract and fractions on castor oil induced acute diarrhea , rhubarb induced chronic diarrhea , gastrointestinal transit (GIT) in mice, and contractions of isolated guinea-pig ileum were evaluated. Additionally, nitric oxide (NO), gastrointestinal peptides gastrin (GAS), motilin (MTL) and somatostatin (SS) levels that related to gastrointestinal motilities were detected to demonstrate the potential mechanisms. Ultimately, LC–MS/MS method was utilized to ensure the chemical consistency. Results The 95% ethanol extract and 90% ethanol eluted fraction significantly delayed the onset time and decreased the wet faeces proportion compared with control group in the castor oil induced acute diarrhea mice. In terms of further evaluation of antidiarrheal activity, the 95% ethanol extract and 90% ethanol elution displayed significant inhibition of the intestinal propulsion at the two highest oral doses of 20 g crude drug/kg and 1 g/kg. Moreover the 95% ethanol extract (10 and 20 g crude drug/kg) and 90% ethanol elution (0.5 and 1 g/kg) could significantly inhibit the GIT, which was partially attributed to the increase in NO and SS levels, and the decreased MTL. In vitro spontaneous contractions of the isolated guinea pig ileum induced by carbachol , neostigmine and histamine were attenuated by both the extract and elution. Phytochemical analysis of 95% ethanol extract and its fractions identified the presence of diphenylheptanes, sesquiterpenes , and flavones as the major components. Conclusions Our in vivo and in vitro data could partly support and justify the traditional usage of Fructus AOM on the treatment of diarrhea in traditional medicine.
研究领域:
药理学
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传统中药研究
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消化系统疾病
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DOI
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2021
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IF 4.36
Rifa Qiao,Lifen Zhou,Minyong Zhong,Min Zhang,Lin Yang,Yuanfeng Yang,Haifang Chen,Wuliang Yang,Jinbin Yuan
Ethnopharmacological relevance Nowadays, gastrointestinal motility disorders (GMD) have reduced the quality of people's daily life worldwide, but there is still a lack of effective western medicine treatment. Fructus aurantii (FA), a representative regulating-qi herbal medicine, has been widely used to treat GMD in China for thousands of years, but it is not clear that which specific components contribute to the efficacy. Aim of the study The efficacy differences of various fractions of FA on normal mice and GMD rats were compared, so as to find out the main effective fraction of FA, and to screen the main regulating-qi components based on spectrum-effect relationship and multivariate statistical analysis. Materials and methods The fingerprints of different fractions of FA were established and main compounds were identified with UHPLC-Q-TOF/MS technique. The promoting gastrointestinal motility activities of FA were evaluated by defecation test, gastric emptying and intestinal propulsion test in mice, and further investigated according to the biochemical analysis of 5-HT, SP , MLT, GAS and VIP in GMD rats’ plasma. One-way ANOVA was used to find out the difference of efficacy. The active components were screened through spectrum-effect relationship with PCA-X, Pearson bivariate correlation analysis and OPLS analysis. Conclusions Ethyl acetate fraction is the main active fraction, and nine compounds are the major regulating-qi components. The developed spectrum-effect analysis can be used for the screening of bioactive components in natural products with high accuracy and reliability.
研究领域:
药理学
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民族药理学
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分析化学
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中药学
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产品关联
DOI
PubMed
高影响因子
BIOMATERIALS
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2024
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IF 12.8
Jinbin Pan,Jiaojiao Wang,Yujie Zhao,Bing Han,Gang Shu,Min Ma,Xu Wang,Xi Wei,Wenjing Hou,Shao-Kai Sun
Anastomotic leaks are among the most dreaded complications following gastrointestinal (GI) surgery, and contrast-enhanced X-ray gastroenterography is considered the preferred initial diagnostic method for GI leaks. However, from fundamental research to clinical practice, the only oral iodinated contrast agents currently available for GI leaks detection are facing several challenges, including low sensitivity, iodine allergy, and contraindications in patients with thyroid diseases. Herein, we propose a cinematic contrast-enhanced X-ray gastroenterography for the real-time detection of GI leaks with an iodine-free bismuth chelate (Bi-DTPA) for the first time. The Bi-DTPA, synthesized through a straightforward one-pot method, offers distinct advantages such as no need for purification, a nearly 100 % yield, large-scale production capability, and good biocompatibility. The remarkable X-ray attenuation properties of Bi-DTPA enable real-time dynamic visualization of whole GI tract under both X-ray gastroenterography and computed tomography (CT) imaging. More importantly, the leaky site and severity can be both clearly displayed during Bi-DTPA-enhanced gastroenterography in a rat model with esophageal leakage. The proposed movie-like Bi-DTPA-enhanced X-ray imaging approach presents a promising alternative to traditional GI radiography based on iodinated molecules. It demonstrates significant potential in addressing concerns related to iodine-associated adverse effects and offers an alternative method for visually detecting gastrointestinal leaks.
研究领域:
医学影像学
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胃肠病学
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
International Journal of Nanomedicine
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2018
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IF 4.37
Jiao Liu,Jie Cao,Jianhua Cao,Shangcong Han,Yan Liang,Mingfeng Bai,Yong Sun
Introduction Nanoparticles are increasingly used as drug carriers for oral administration. The delivery of drug molecules is largely dependent on the interaction of nanocarriers and gastrointestinal (GI) mucus, a critical barrier that regulates drug absorption. It is therefore important to understand the effects of physical and chemical properties of nanocarriers on the interaction with GI mucus. Unfortunately, most of the nanoparticles are unable to be prepared with satisfactory structural monodispersity to comprehensively investigate the interaction. With controlled size, shape, and surface chemistry, copolymers are ideal candidates for such purpose. Materials and methods We synthesized a series of diblock copolymers via the atom transfer radical polymerization method and investigated the GI mucus permeability in vitro and in vivo. Results Our results indicated that uncharged and hydrophobic copolymers exhibited enhanced GI absorption. Conclusion These results provide insights into developing optimal nanocarriers for oral administration.
研究领域:
药学
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材料科学
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
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2024
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IF 3.3
Buqing Wang,Yasen Wang,Xiaoman Zhou,Xiao-Dong Gao,Morihisa Fujita,Zijie Li
BACKGROUND Acidic lipases with high catalytic activities under acidic conditions have important application values in the food, feed and pharmaceutical industries. However, the availability of acidic lipases is still the main obstacle to their industrial applications. Although a novel acidic lipase Rasamsonia emersonii (LIPR) was heterologously expressed in Escherichia coli , the expression level was unsatisfactory. RESULTS To achieve the high-efficiency expression and secretion of LIPR in Pichia pastoris GS115, the combinatorial optimization strategy was adopted including gene codon preference, signal peptide, molecular chaperone co-expression and disruption of vacuolar sorting receptor VPS10 . The activity of the combinatorial optimization engineered strain in a shake flask reached 1480 U mL −1 , which was 8.13 times greater than the P. pastoris GS115 parental strain. After high-density fermentation in a 5-L bioreactor, the highest enzyme activity reached as high as 11 820 U mL −1 . LIPR showed the highest activity at 40 °C and pH 4.0 in the presence of Ca 2+ ion. LIPR exhibited strong tolerance to methanol, indicating its potential application in biodiesel biosynthesis. Moreover, the gastrointestinal digestion simulation results demonstrated that LIPR was tolerant to pepsin and trypsin, but its activity was inhibited by sodium taurodeoxycholate. CONCLUSION This study provided an effective approach for the high expression of acidic lipase LIPR. LIPR was more appropriate for lipid digestion in the stomach than in intestine according to the gastrointestinal digestion simulation results. © 2024 Society of Chemical Industry.
研究领域:
生物技术
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酶工程
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食品科学
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DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
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2024
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IF 5.3
Yong Cao,Qianfeng Chen,Qing He,Gaojin Zhou,Ali Ahmad,Shun Yao
Considering the controversial safety and risk solutions of ionic liquids (ILs), more essential basic researches are required as their applied fields become broader and applied scale grows larger. Under this background, the permeation behaviors of six common imidazole ILs on porcine gastric and enteric membranes together with the feasibility of their removal by adsorption with montmorillonite were investigated in vitro. Through the single-factor investigation of different cations, anions and ionic liquid concentrations, the current results show that the IL of 1-ethyl-3-methylimidazolium bromide ([Emim]Br) has the strongest permeation capacity on the gastric membrane during the tests. The cumulative permeation amount of Q n can reach 0.72 mg/cm 2 , and the cumulative permeation percentage alsoreaches 95.77 %; the whole permeation process conforms to the Hixcon-Crowell model. As comparison, the maximum cumulative penetration percentage of [Emim]Br on enteric member was determined as 89.11 %, and related models was also compared. In order to remove the potential IL in digestive tract, montmorillonite was screened out from those popularily used antidotes in clinic and the adsorption of [Emim]Br in gastric fluid by montmorillonite has been proved more consistent with the second-order kinetics and Langmuir model. The results of molecular simulation, infrared spectrum (IR), X-ray diffraction (XRD) and thermogravimetric (TG) characterization exhibit that [Emim]Br has been successfully adsorbed into the interlayer of montmorillonite. As a whole, the study provided a scientific and effective way to diminish the hidden danger of ionic liquid entering the blood through the digestive system.
研究领域:
药理学
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毒理学
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产品关联
DOI
高影响因子
Food Bioscience
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2024
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IF 4.8
Shanting Lin,Xiao Hu,Shengjun Chen,Hui Huang,Xiaoshan Long,Zhenxing Li
The aims of this study were to investigate the effect of precise phosphorylation of Ser in GL-Hyp-GPSGEEGKR on its Fe 2+ chelating capacity, and the effects and mechanisms of folic acid coupling to GL-Hyp-GPS (PO4) GEEGKR on its resistance against degradation by gastrointestinal enzymes. The results demonstrated that GL-Hyp-GPS (PO4) GEEGKR exhibited significantly enhanced Fe 2+ chelating capability compared to GL-Hyp-GPSGEEGKR. This was attributed to the phosphorylation of Ser introducing more Fe 2+ chelating sites. Furthermore, the results of UV–Vis, FTIR, and 1 H NMR showed that folic acid has successfully coupled with GL-Hyp-GPS (PO4) GEEGKR to generate folic acid-GL-Hyp-GPS (PO4) GEEGKR. Folic acid-GL-Hyp-GPS (PO4) GEEGKR demonstrated superior resistance against degradation by gastrointestinal enzymes. This may be attributed to the coupling of folic acid altering the original zeta potential of the peptide and the steric hindrance effect of folic acid hindering the interaction between enzymes and peptide. These findings can provide valuable insights for the production of high Fe 2+ chelating peptides that resist gastrointestinal enzyme degradation.
研究领域:
生物化学
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药学
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营养科学
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
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2021
·Vol. 23
·期 1
·416
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IF 5.924
Jingjing Liu,Wenyang Zhao,Chun Li,Tongyu Wu,Liang Han,Zhuozhou Hu,Xiangxiang Li,Jing Zhou,Xinping Chen
Gastrointestinal disease is the most common health concern that occurs due to environmental, infectious, immunological, psychological, and genetic stress. Among them, the most frequent diseases are gastric ulcer (GU) and ulcerative colitis (UC). DSS-induced UC and ethanol-stimulated GU models resemble the pathophysiology of human gastrointestinal disease. The current study was designed to explore the anti-oxidation, anti-inflammation, anti-cell death properties of terazosin, an α-adrenergic receptor antagonist, in vivo and in vitro. Our results indicate that terazosin dramatically activates Pgk1, and upregulates glycose metabolism, evidenced by the enhanced ATP production and higher LDH enzymatic activity. Also, terazosin significantly enhances p-AKT expression and inhibits NF-κB p65 activation through abrogating the phosphorylation of IKBα, as well as lowers Caspase-1 and GSDMD expression. The findings in this study demonstrate that terazosin exhibits anti-inflammatory effects by downregulating NF-κB-GSDMD signal pathway, along with enhancing glycolysis for gastrointestinal disease treatment. Meanwhile, we also find terazosin ameliorates ethanol-induced gastric mucosal damage in mice. Collectively, as a clinical drug, terazosin should be translated into therapeutics for gastrointestinal disease soon.Keywords:terazosin;gastrointestinal disease;anti-inflammation;Pgk1;cell death
研究领域:
药理学
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胃肠病学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
FOOD HYDROCOLLOIDS
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2020
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IF 7.053
Luping Gu,David Julian McClements,Jiaying Li,Yujie Su,Yanjun Yang,Junhua Li
In this study, alginate/κ-carrageenan hydrogel beads were developed to encapsulate and release egg yolk immunoglobulin Y (IgY) under simulated gastrointestinal conditions. The effects of κ-carrageenan concentration on the encapsulation and loading efficiency of the hydrogel beads was assessed, as well as on their swelling and release behavior in a simulated human gut. An κ-carrageenan concentration of 0.30% gave the optimum encapsulation and loading efficiency. After incubation in simulated gastric fluids, there was no loss in IgY activity when it was encapsulated within alginate/carrageenan beads but around 35% loss when it was encapsulated in pure alginate beads. This effect was attributed to a stronger electrostatic attraction and a more closely packed biopolymer network formed within the composite beads, based on measurements of their electrical and microstructural properties. The composite beads were resistant to swelling in the stomach phase, but not in the intestine phase. The kinetics of swelling under simulated gastric conditions was found to follow Schott's second-order model. The gastrointestinal digestion of the IgY was slower in the composite beads than in the pure alginate beads. The release kinetics of IgY from the composite beads was fitted by an irregular release model. Our results suggest that alginate/κ-carrageenan composite beads are efficient carriers for the delivery systems of hydrophilic immunoglobins.
研究领域:
食品科学
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生物材料学
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DOI
高影响因子
CURRENT DRUG METABOLISM
·
2024
·Vol. 25
·期 3
·197-204
·
IF 2.1
Xin Lv,Zhen Wang,Zhe Wang,Hang Yin,Yangliu Xia,Lili Jiang,Yong Liu
Background: Avapritinib is the only drug for adult patients with PDGFRA exon 18 mutated unresectable or metastatic gastrointestinal stromal tumor (GIST). Although avapritinib has been approved by the FDA for four years, little is known about the risk of drug-drug interactions (DDIs) via UDP-glucuronyltransferases (UGTs) inhibition. Objective: The aim of the present study was to systematically evaluate the inhibitory effects of avapritinib against UGTs and to quantitatively estimate its potential DDIs risk in vivo. Methods: Recombinant human UGTs were employed to catalyze the glucuronidation of substrates in a range of concentrations of avapritinib. The kinetics analysis was performed to evaluate the inhibition types of avapritinib against UGTs. The quantitative prediction of DDIs was done using in vitro-in vivo extrapolation (IVIVE). Results: Avapritinib had a potent competitive inhibitory effect on UGT1A1. Quantitative prediction results showed that avapritinib administered at clinical doses might result in a 14.85% increase in area under the curve (AUC) of drugs primarily cleared by UGT1A1. Moreover, the Rgut value was calculated to be 18.44. Conclusion: Avapritinib has the potential to cause intestinal DDIs via the inhibition of UGT1A1. Additional attention should be paid when avapritinib is coadministered with UGT1A1 substrates.
研究领域:
药理学
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临床医学
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生物化学
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DOI
PubMed
高影响因子
FOOD CHEMISTRY
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2021
·
IF 7.514
Jia-Yi Yin,Ya-Ning Han,Meng-Qi Liu,Zan-Hao Piao,Xu Zhang,Yu-Ting Xue,Ying-Hua Zhang
Human health can be damaged by free radicals, and antioxidant peptides are excellent radical scavengers. Antioxidant tripeptides data set based on 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulofnic acid) (ABTS) assay was created, 9 types of descriptors were integrated and 4 quantitative structure–activity relationship (QSAR) models were constructed in this study. Several structural factors influencing the activity of antioxidant tripeptides and the dominant amino acids at each position of tripeptides were revealed by the optimal model. Ten food-derived tripeptides with higher activity were selected for synthesis and activity determination. Molecular docking results demonstrated that these tripeptides were stably bound to the Keap1 receptor, further elucidating the antioxidant mechanism. It was known from the simulation of gastrointestinal digestion experiments that the model results possessed a guiding effect on the selection of proteins with high antioxidant activity . The performance of the model was proved to be robust after validation.
研究领域:
生物信息学
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营养学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
FOOD RESEARCH INTERNATIONAL
·
2025
·
IF 8
Bingxin Zhang,Yuxin Sun,Wenyu Han,Wenwen Ge,Zhenbo Xu,Shuo Wang,Zhenquan Yang,Lei Yuan
Probiotics are live microorganisms offering various health benefits to hosts, but exposure to adverse conditions can compromise their viability during gastrointestinal transit. Probiotics in the biofilm state have been proven as an alternative way to the probiotic survival challenge; however, knowledge of mixed-species biofilms by probiotics is limited. This study aimed to examine the ecological interactions between Lactiplantibacillus plantarum LP-52 and Limosilactobacillus fermentum LF-56 from a phenotypic and metabolomics perspective during their mixed-species biofilm development. In specific, we investigated how their interaction changes bacterial growth, biofilm-forming capacity, biofilm structure, biofilm metabolic activity, EPS production, and biofilm tolerance under gastrointestinal conditions. Moreover, a comprehensive metabolomics analysis was conducted to identify different metabolic profiles and elucidate the underlying mechanisms during the development of mixed-species biofilm. Results showed that their cooperative interaction significantly promoted the planktonic cell growth of L. fermentum LF-56 and L. plantarum LP-52 during their co-cultivation. The synergistic effect also markedly improved the biofilm formation, with increased cell counts in biofilms and higher metabolic activity when compared to each single-species biofilm. Confocal laser scanning microscopy imaging showed denser and more diverse structures of mixed-species biofilm with higher coverage and thickness. In addition, dual-species biofilms were best tolerated under simulated gastric and intestinal conditions. Untargeted metabolomics assay identified 852 differential metabolites, primarily associated with seven pathways: two pathways of nucleotide metabolism (purine metabolism, pyrimidine metabolism), two pathways of carbohydrate metabolism (TCA cycle, glycolysis), alanine, aspartate, and glutamate metabolism, riboflavin metabolism, and ABC transporters, which an enhanced energy metabolism, stress adaptation, and potential biofunctional benefits. With this respect, this investigation underscores the benefits of mixed probiotics biofilms and contributes to further application of probiotics in the food and biotechnology industry.
研究领域:
微生物学
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食品科学
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生物技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）