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1.
Nano Lett ; 24(17): 5197-5205, 2024 May 01.
Article En | MEDLINE | ID: mdl-38634879

Highly active nonprecious-metal single-atom catalysts (SACs) toward catalytic transfer hydrogenation (CTH) of α,ß-unsaturated aldehydes are of great significance but still are deficient. Herein, we report that Zn-N-C SACs containing Zn-N3 moieties can catalyze the conversion of cinnamaldehyde to cinnamyl alcohol with a conversion of 95.5% and selectivity of 95.4% under a mild temperature and atmospheric pressure, which is the first case of Zn-species-based heterogeneous catalysts for the CTH reaction. Isotopic labeling, in situ FT-IR spectroscopy, and DFT calculations indicate that reactants, coabsorbed at the Zn sites, proceed CTH via a "Meerwein-Ponndorf-Verley" mechanism. DFT calculations also reveal that the high activity over Zn-N3 moieties stems from the suitable adsorption energy and favorable reaction energy of the rate-determining step at the Zn active sites. Our findings demonstrate that Zn-N-C SACs hold extraordinary activity toward CTH reactions and thus provide a promising approach to explore the advanced SACs for high-value-added chemicals.

2.
Front Bioeng Biotechnol ; 11: 1150842, 2023.
Article En | MEDLINE | ID: mdl-36970633

Background: Plant cell culture technology is a potential way to produce polyphenols, however, this way is still trapped in the dilemma of low content and yield. Elicitation is regarded as one of the most effective ways to improve the output of the secondary metabolites, and therefore has attracted extensive attention. Methods: Five elicitors including 5-aminolevulinic acid (5-ALA), salicylic acid (SA), methyl jasmonate (MeJA), sodium nitroprusside (SNP) and Rhizopus Oryzae Elicitor (ROE) were used to improve the content and yield of polyphenols in the cultured Cyclocarya paliurus (C. paliurus) cells, and a co-induction technology of 5-ALA and SA was developed as a result. Meanwhile, the integrated analysis of transcriptome and metabolome was adopted to interpret the stimulation mechanism of co-induction with 5-ALA and SA. Results: Under the co-induction of 50 µM 5-ALA and SA, the content and yield of total polyphenols of the cultured cells reached 8.0 mg/g and 147.12 mg/L, respectively. The yields of cyanidin-3-O-galactoside, procyanidin B1 and catechin reached 28.83, 4.33 and 2.88 times that of the control group, respectively. It was found that expressions of TFs such as CpERF105, CpMYB10 and CpWRKY28 increased significantly, while CpMYB44 and CpTGA2 decreased. These great changes might further make the expression of CpF3'H (flavonoid 3'-monooxygenase), CpFLS (flavonol synthase), CpLAR (leucoanthocyanidin reductase), CpANS (anthocyanidin synthase) and Cp4CL (4-coumarate coenzyme A ligase) increase while CpANR (anthocyanidin reductase) and CpF3'5'H (flavonoid 3', 5'-hydroxylase) reduce, ultimately enhancing the polyphenols accumulation Conclusion: The co-induction of 5-ALA and SA can significantly promote polyphenol biosynthesis in the cultured C. paliurus cells by regulating the expression of key transcription factors and structural genes associated with polyphenol synthesis, and thus has a promising application.

3.
J Sci Food Agric ; 103(7): 3437-3446, 2023 May.
Article En | MEDLINE | ID: mdl-36680508

BACKGROUND: Euryale ferox is an important cash crop and valuable tonic in traditional medicine. The seeds of E. ferox are rich in starch, which is hard to digest, and the digestion speed is significantly slower than that of rice starch. The goal of this study was to evaluate the effects of E. ferox seed-coat phenolics (EFCPs) on the digestion of E. ferox seed starch. RESULTS: EFCPs were extracted and identified by ultra-high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry. We optimized the extraction parameters, and the final extraction yield was about 1.49%. We identified seven phenolics from the E. ferox seed-coat extracts: gallic acid, digalloylhexoside, catechin, procyanidin B2, epicatechin, ellagic acid, and epicatechin gallate. Quantitative analysis results showed that the E. ferox seed phenolics mainly distributed in the seed coat and the gallic acid, digalloylhexoside, and epicatechin gallate were three main phenolic compounds. The phenolics displayed strong inhibitory activities on α-glucosidase and α-amylase with an IC50 of 3.25 µg mL-1 and 1.36 mg mL-1 respectively. Furthermore, these phenolics could interact with starch by hydrogen bonds, which might make its starch more difficult to digest. CONCLUSION: Our investigation suggests that the EFCPs can strongly inhibit the digestion of E. ferox seed starch by inhibiting the α-amylase and α-glucosidase activities and interacting with starch by hydrogen bonds; therefore, E. ferox seeds have a promising application prospect in foods for hypoglycemia. © 2023 Society of Chemical Industry.


Plant Extracts , Starch , Starch/analysis , Plant Extracts/chemistry , alpha-Glucosidases , Phenols/analysis , Seeds/chemistry , Gallic Acid/analysis , alpha-Amylases/analysis , Digestion
4.
Nucleic Acids Res ; 51(9): 4223-4236, 2023 05 22.
Article En | MEDLINE | ID: mdl-36484109

Rpc31 is a subunit in the TFIIE-related Rpc82/34/31 heterotrimeric subcomplex of Saccharomyces cerevisiae RNA polymerase III (pol III). Structural analyses of pol III have indicated that the N-terminal region of Rpc31 anchors on Rpc82 and further interacts with the polymerase core and stalk subcomplex. However, structural and functional information for the C-terminal region of Rpc31 is sparse. We conducted a mutational analysis on Rpc31, which uncovered a functional peptide adjacent to the highly conserved Asp-Glu-rich acidic C-terminus. This C-terminal peptide region, termed 'pre-acidic', is important for optimal cell growth, tRNA synthesis, and stable association of Rpc31 in the pre-initiation complex (PIC). Our site-directed photo-cross-linking to map protein interactions within the PIC reveal that this pre-acidic region specifically targets Rpc34 during transcription initiation, but also interacts with the DNA entry surface in free pol III. Thus, we have uncovered a switchable Rpc31 C-terminal region that functions in an initiation-specific protein interaction for pol III transcription.


RNA Polymerase III , Saccharomyces cerevisiae Proteins , Saccharomyces cerevisiae , Transcription Initiation, Genetic , Protein Binding , Protein Domains , RNA Polymerase III/chemistry , RNA Polymerase III/metabolism , RNA, Transfer/biosynthesis , Saccharomyces cerevisiae/genetics , Saccharomyces cerevisiae/metabolism , Saccharomyces cerevisiae Proteins/chemistry , Saccharomyces cerevisiae Proteins/genetics , Saccharomyces cerevisiae Proteins/metabolism
5.
Nat Prod Res ; 37(11): 1787-1796, 2023 Jun.
Article En | MEDLINE | ID: mdl-36095038

Four new norceanothane-type triterpenes, cyclopalin A-D (1-4), and sixteen known compounds (5-20) were obtained from the fruits of Cyclocarya paliurus. Their structures were determined by spectroscopic data, experimental electronic circular dichroism (ECD) and X-ray single crystal analyses. All isolated compounds were assayed for their anti-HIV-1IIIB activity. Compound 18 exhibited potent anti-HIV-1IIIB activity with an EC50 value of 1.32 µM (SI = 151.52).


Juglandaceae , Triterpenes , Triterpenes/chemistry , Fruit , Spectrum Analysis , Juglandaceae/chemistry , Plant Leaves/chemistry
6.
Molecules ; 27(21)2022 Nov 04.
Article En | MEDLINE | ID: mdl-36364410

Chalcone-1-deoxynojirimycin heterozygote (DC-5), a novel compound which was designed and synthesized in our laboratory for diabetes treatment, showed an extremely strong in vitro inhibitory activity on α-glucosidase in our previous studies. In the current research, its potential in vivo anti-diabetic effects were further investigated by integration detection and the analysis of blood glucose concentration, blood biochemical parameters, tissue section and gut microbiota of the diabetic rats. The results indicated that oral administration of DC-5 significantly reduced the fasting blood glucose and postprandial blood glucose, both in diabetic and normal rats; meanwhile, it alleviated the adverse symptoms of elevated blood lipid level and lipid metabolism disorder in diabetic rats. Furthermore, DC-5 effectively decreased the organ coefficient and alleviated the pathological changes of the liver, kidney and small intestine of the diabetic rats at the same time. Moreover, the results of 16S rDNA gene sequencing analysis suggested that DC-5 significantly increased the ratio of Firmicutes to Bacteroidetes and improved the disorder of gut microbiota in diabetic rats. In conclusion, DC-5 displayed a good therapeutic effect on the diabetic rats, and therefore had a good application prospect in hypoglycemic drugs and foods.


Chalcone , Chalcones , Diabetes Mellitus, Experimental , Diabetes Mellitus, Type 2 , Gastrointestinal Microbiome , Rats , Animals , Blood Glucose , Diabetes Mellitus, Experimental/pathology , 1-Deoxynojirimycin/pharmacology , 1-Deoxynojirimycin/therapeutic use , Chalcones/pharmacology , Chalcones/therapeutic use , Chalcone/pharmacology , Heterozygote , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/therapeutic use , Diabetes Mellitus, Type 2/drug therapy
7.
Sensors (Basel) ; 22(18)2022 Sep 19.
Article En | MEDLINE | ID: mdl-36146421

Vehicle fault detection and diagnosis (VFDD) along with predictive maintenance (PdM) are indispensable for early diagnosis in order to prevent severe accidents due to mechanical malfunction in urban environments. This paper proposes an early voiceprint driving fault identification system using machine learning algorithms for classification. Previous studies have examined driving fault identification, but less attention has focused on using voiceprint features to locate corresponding faults. This research uses 43 different common vehicle mechanical malfunction condition voiceprint signals to construct the dataset. These datasets were filtered by linear predictive coefficient (LPC) and wavelet transform(WT). After the original voiceprint fault sounds were filtered and obtained the main fault characteristics, the deep neural network (DNN), convolutional neural network (CNN), and long short-term memory (LSTM) architectures are used for identification. The experimental results show that the accuracy of the CNN algorithm is the best for the LPC dataset. In addition, for the wavelet dataset, DNN has the best performance in terms of identification performance and training time. After cross-comparison of experimental results, the wavelet algorithm combined with DNN can improve the identification accuracy by up to 16.57% compared with other deep learning algorithms and reduce the model training time by up to 21.5% compared with other algorithms. Realizing the cross-comparison of recognition results through various machine learning methods, it is possible for the vehicle to proactively remind the driver of the real-time potential hazard of vehicle machinery failure.


Automobile Driving , Deep Learning , Algorithms , Neural Networks, Computer , Wavelet Analysis
8.
Biomed Pharmacother ; 150: 112959, 2022 Jun.
Article En | MEDLINE | ID: mdl-35430392

The metabolism, tissue distribution and excretion of taxifolin in rat after oral administration of taxifolin encapsulated zein-caseinate Nanoparticles (TZP) were studied. The isomerization of taxifolin in rat small intestine and colon was found. Besides isomers, 16 metabolites of taxifolin were identified in rat feces, plasma and urine by UPLC-QTOF-MS. In colon, taxifolin underwent the metabolism of hydration, dehydration and ring-fission through the gut microflora. The main metabolites of taxifolin found in plasma and urine were its sulfated, glucuronidated, and/or methylated products. The dynamic variation of taxifolin and its metabolites in tissues and urine were quantified by UPLC-QqQ-MS/MS. Taxifolin and its metabolites could be quickly absorbed and distributed in the tissues, and relatively low concentrations were found in the heart and brain. The feces excretion of taxifolin was determined by HPLC. The total excretion during 24 h was 2.83 ± 0.80% to its given does, and the maximum excretion was found during 8-10 h post administration. Compared with feces, the excretion of taxifolin and its metabolites in urine was much faster, and the total excretion was 1.96 ± 0.23% during 12 h.


Quercetin , Tandem Mass Spectrometry , Administration, Oral , Animals , Chromatography, High Pressure Liquid , Quercetin/analogs & derivatives , Rats , Tissue Distribution
9.
Article En | MEDLINE | ID: mdl-35245842

A new method involving gut microbiota biotransformation, spectrum-effect relationship analysis and metabolomics analysis was developed to study the antitussive and expectorant microbial metabolites of platycosides fraction (MPFs) of Platycodonis Radix. Furthermore, their possible metabolic mechanisms were studied for the first time. The findings showed that the antitussive and expectorant effects of the platycosides fraction (PF) were significantly enhanced by the gut microbiota biotransformation. 11 active antitussive microbial metabolites and 12 active expectorant microbial metabolites, which shared 8 components, were successfully screened out via spectrum-effect relationship analysis. The prototypes of the active microbial metabolites could be reversely traced according to the gut microbiota biotransformation pathways. It was found out that one platycoside could produce several active microbial metabolites and several different platycosides could produce the same active microbial metabolite. In addition, the metabolomics analysis showed that both the PF and its active microbial metabolites could regulate the same metabolomic pathways of Linoleic acid metabolism, Arachidonic acid metabolism and Glycerophospholipid metabolism to exert antitussive activity, and regulate the same metabolomic pathway of Arachidonic acid metabolism to exert expectorant activity. These findings suggested the microbial metabolites may be the active forms of the platycosides. Overall, the proposed approach was useful in screening the active microbial metabolites; this work explained the in vivo antitussive and expectorant metabolic mechanisms of multi-constituents, multi-targets and synergistic effects of PF of Platycodonis Radix.


Antitussive Agents , Expectorants , Metabolome/drug effects , Plant Extracts , Platycodon , Animals , Antitussive Agents/chemistry , Antitussive Agents/pharmacology , Chromatography, Liquid , Expectorants/chemistry , Expectorants/pharmacology , Gastrointestinal Microbiome , Metabolomics , Mice , Oleanolic Acid/analogs & derivatives , Plant Extracts/chemistry , Plant Extracts/pharmacology , Platycodon/chemistry , Saponins
10.
Medicine (Baltimore) ; 101(1): e28421, 2022 Jan 07.
Article En | MEDLINE | ID: mdl-35029887

BACKGROUND: : Colorectal cancer patients with permanent colostomy may suffer stigma, negative coping style, and low quality of life at varying degrees, which may be improved by the mindfulness-based stress reduction (MBSR). In recent years, MBSR has been used in the comprehensive treatment of colorectal cancer with permanent colostomy, hoping to bring a positive outcome. However, the practical application effect of MBSR has not been elucidated so far. Therefore, this study conducted a meta-analysis to evaluate the effects of MBSR on stigma, coping style, and quality of life in colorectal cancer patients with permanent colostomy, providing reliable evidence for clinical application. METHODS: : Randomized controlled trials (RCTs) reporting MBSR on stigma, coping style, and quality of life in patients with permanent stoma of colorectal cancer published before December 2021 will be searched in online databases such as the PubMed, Web of Science, The Cochrane Library, Embase, China National Knowledge Infrastructure, Wanfang Database, China Biomedical Literature Database, and Chinese Scientific Journal Database. The quality of the literature will be evaluated using the risk of bias assessment tool in Revman 5.4. Meta-analysis will be performed using Revman 5.4 software. RESULTS: : The Social Impact Scale (SIS), Simplified Coping Style Questionnaire (SCSQ), and quality of life scale will be used to evaluate the effects of MBSR on stigma, coping style, and quality of life in colorectal cancer patients with permanent colostomy. CONCLUSION: : This study will provide a reliable evidence-based basis for MBSR to reduce stigma, improve coping style, and improve quality of life for colorectal cancer patients with permanent colostomy. OSF REGISTRATION NUMBER: DOI 10.17605/OSF.IO/CD4PV.


Adaptation, Psychological , Colorectal Neoplasms , Mindfulness , Social Stigma , Stress, Psychological/prevention & control , Colorectal Neoplasms/therapy , Humans , Meta-Analysis as Topic , Quality of Life , Research Design , Systematic Reviews as Topic
11.
Scand J Gastroenterol ; 56(12): 1473-1479, 2021 Dec.
Article En | MEDLINE | ID: mdl-34428128

PURPOSE: To evaluate the relative clinical efficacy associated with the unilateral and bilateral insertion of a stent with a radioactive strand (RS) for the treatment of inoperable hilar cholangiocarcinoma (HCCA) patients. METHODS: From January 2017 to June 2020, consecutive patients diagnosed with inoperable HCCA underwent either unilateral or bilateral stent with RS insertion in our hospital. Outcomes compared between these groups included rates of technical success, clinical success, stent-related complications, stent patency and overall survival (OS). RESULTS: Unilateral and bilateral stent with RS insertion procedures were performed in 36 and 30 patients over the study period, respectively, with 100% technical and clinical success rates in both groups. No instances of procedure-related complications were reported. Cholangitis was observed in 7 (19.4%) and 6 (20%) patients in unilateral and bilateral groups (p= .955), respectively, while these groups exhibited respective cholecystitis in 2 (5.5%) and 1 (3.3%) cases, respectively (p=.662), and stent restenosis in 9 (25%) and 7 (23.3%) cases, respectively (p=.661). The median duration of stent patency in the unilateral and bilateral groups was comparable at 208 and 222 d, respectively (p=.889). All patients died over the course of follow-up, with similar median OS rates in the unilateral and bilateral groups of 250 and 246 d, respectively (p=.483). CONCLUSIONS: These data indicated that similar inoperable HCCA patient clinical outcomes are achieved following stent with RS insertion regardless of whether it is conducted via a unilateral or bilateral approach.


Bile Duct Neoplasms , Cholangiocarcinoma , Cholestasis , Klatskin Tumor , Cholangiocarcinoma/complications , Cholangiocarcinoma/radiotherapy , Cholangiocarcinoma/surgery , Cholestasis/etiology , Humans , Klatskin Tumor/complications , Klatskin Tumor/surgery , Palliative Care/methods , Retrospective Studies , Stents/adverse effects , Treatment Outcome
12.
Article En | MEDLINE | ID: mdl-33872929

The antitussive effect of Platycodonis Radix is closely related to the components in saponins fraction of Platycodonis Radix extract (SFPRE); however, these active components and their holistic mechanism remain unknown. Hence, a new method by integrating spectrum-effect relationship analysis with metabolomics analysis was applied to study the active components and their holistic mechanism simultaneously. For spectrum-effect relationship analysis, chemical fingerprints of ten batches of SFPRE were developed using UHPLC-LTQ-Orbitrap MSn; antitussive effect were evaluated using a classic mice-cough model induced by ammonia liquor. Spectrum-effect relationship was analyzed by partial least squares regression (PLSR) analysis. For metabolomics analysis, the altered metabolites related to cough in serum were identified by UHPLC-Q-TOF/MS and orthogonal partial least squares-discriminant analysis (OPLS-DA); metabolic pathway analysis was depended on MetaboAnalyst 4.0, KEGG database, METLIN database and HMDB database. Our findings showed that 10 identified components of Polygalacin D (peak 26), Deapio-platycodin D (peak 21), Platycodin D (peak 23), ß-Gentiotriosyl platycodigenin (peak 37), Platycoside G3 (peak 17), Platycoside C (peak 25), Platycodin D3 (peak 16), 3-O-ß-D-glucopyranosyl platycodigenin (peak 33), Platycoside F (peak 19) and 3″-O-acetyl platycodin D3 (peak 15), and 2 unidentified components (peak 45 and 44) possessed antitussive effects. The metabolomics analysis result showed that 19 metabolites were potential biomarkers related to the cough, 16 of which could be restored to normal levels by SFPRE. These biomarkers were involved in arachidonic acid metabolism, linoleic acid metabolism and glycerophospholipid metabolism. The current study may facilitate the development of antitussive medicines with fewer side-effects based on Platycodonis Radix.

13.
Ecotoxicol Environ Saf ; 214: 112084, 2021 May.
Article En | MEDLINE | ID: mdl-33640726

Direct Black G (DBG) is a highly toxic synthetic azo dye which is difficult to degrade. Biological treatment seems to be a promising option for the treatment of azo dye containing effluent. A thermophilic bacterial strain (Anoxybacillus sp. PDR2) previously isolated from the soil can effectively remove DBG. However, the molecular underpinnings of DBG degradation and the microbial detoxification ability remains unknown. In the present study, the genetic background of PDR2 for the efficient degradation of DBG and its adaptation to azo dye-contaminated environments was revealed by bioinformatics. Moreover, the possible biodegradation pathways were speculated based on the UV-vis spectral analysis, FTIR, and intermediates identified by LC-MS. Additionally, phytotoxicity and the comet experiment studies clearly indicated that PDR2 converts toxic azo dye (DBG) into low toxicity metabolites. The combination of biodegradation pathways and detoxification analysis were utilized to explore the molecular degradation mechanism and bioremediation of azo dye for future applications. These findings will provide a valuable theoretical basis for the practical treatment of azo dye wastewater.


Anoxybacillus/metabolism , Azo Compounds/metabolism , Biodegradation, Environmental , Anoxybacillus/genetics , Bacteria/metabolism , Color , Coloring Agents/metabolism , Humans , Soil , Wastewater
14.
Org Biomol Chem ; 19(7): 1616-1619, 2021 02 25.
Article En | MEDLINE | ID: mdl-33533370

A novel and straightforward intramolecular cyclization of glycine derivatives to 2-substituted benzoxazoles through copper-catalyzed oxidative C-H/O-H cross-coupling was described. A variety of glycine derivatives involving short peptides underwent cross-dehydrogenative-coupling readily to afford diverse 2-substituted benzoxazoles. The synthetic method has the advantages of simple operation, broad substrate scope and mild reaction conditions, thus providing an alternative effective approach for benzoxazole construction.

15.
Hum Immunol ; 82(1): 54-59, 2021 Jan.
Article En | MEDLINE | ID: mdl-33288226

BACKGROUND: As the survival rate of premature infants increases, the incidence of bronchopulmonary dysplasia (BPD), a chronic complication of premature infants, is also higher than before. The pathogenesis of BPD is complicated, and immune imbalance and inflammatory response may play important roles in it. OBJECTIVE: To investigate the correlation between lymphocyte subsets in peripheral blood, especially γδ-T cells, and BPD of preterm infants. MATERIALS AND METHOD: The study was carried out with the peripheral blood of premature infants (GA < 32 weeks, BW < 1500 g), which were collected at 24 h or 3-4 weeks after birth. The infants were divided into non-BPD groups and BPD groups that were classified as mild or moderate and severe in preterm infants based on the magnitude of respiratory support at 28 days age and 36 weeks postmenstrual age. The γδ-T, CD3+, CD4+, CD8+ and total lymphocyte subsets in peripheral blood were detected by flow cytometry. RESULTS: The percentages of T lymphocyte subsets in peripheral blood were not different between BPD and non-BPD within 24 h after birth. And no significant difference was found in T lymphocyte subsets among neonates with BPD of different severities. However, the infants who developed BPD had a significant increase in γδ-T cells compared to non-BPD ones within 3-4 weeks after birth. CONCLUSIONS: It seems that γδ-T cells in peripheral blood are correlated with BPD. However, the causality of BPD and various lymphocytes remains unclear, which need to be further studied.


Bronchopulmonary Dysplasia/immunology , Intraepithelial Lymphocytes/immunology , Bronchopulmonary Dysplasia/blood , Female , Gestational Age , Humans , Infant, Newborn , Infant, Premature/blood , Infant, Premature/immunology , Infant, Very Low Birth Weight/blood , Infant, Very Low Birth Weight/immunology , Male
16.
Front Microbiol ; 11: 584331, 2020.
Article En | MEDLINE | ID: mdl-33240238

Penicillium digitatum is a widespread pathogen among Rutaceae species that causes severe fruit decay symptoms on infected citrus fruit (known as citrus green mold). The employment of fungicides can effectively control the citrus green mold, significantly reducing agricultural economic loss. In this study, we found that the X33 antifungal extract produced by Streptomyces lavendulae strain X33 inhibited the hyphae polarization of P. digitatum. Additionally, physiological and proteomic analysis strategies were applied to explore the inhibitory mechanism of the X33 antifungal extract of the S. lavendulae strain X33 on the mycelial growth of P. digitatum. A total of 277 differentially expressed proteins, consisting of 207 upregulated and 70 downregulated, were identified from the comparative proteomics analysis. The results indicated that the X33 antifungal extract induced mitochondrial membrane dysfunction and cellular integrity impairment, which can affect energy metabolism, oxidative stress, and transmembrane transport. The improved alkaline phosphatase activity and extracellular conductivity, increased H2O2 and malondialdehyde contents, and inhibition of energy, amino acid, and sugar metabolism indicated that the oxidative stress of P. digitatum is induced by the X33 antifungal extract. These findings provided insight into the antifungal mechanism of the X33 antifungal extract against P. digitatum by suggesting that it may be an effective fungicide for controlling citrus postharvest green mold.

17.
J Enzyme Inhib Med Chem ; 35(1): 1879-1890, 2020 Dec.
Article En | MEDLINE | ID: mdl-33003963

A series of novel N-alkyl-1-deoxynojirimycin derivatives 25 ∼ 44 were synthesised and evaluated for their in vitro α-glucosidase inhibitory activity to develop α-glucosidase inhibitors with high activity. All twenty compounds exhibited α-glucosidase inhibitory activity with IC50 values ranging from 30.0 ± 0.6 µM to 2000 µM as compared to standard acarbose (IC50 = 822.0 ± 1.5 µM). The most active compound 43 was ∼27-fold more active than acarbose. Kinetic study revealed that compounds 43, 40, and 34 were all competitive inhibitors on α-glucosidase with Ki of 10 µM, 52 µM, and 150 µM, respectively. Molecular docking demonstrated that the high active inhibitors interacted with α-glucosidase by four types of interactions, including hydrogen bonds, π-π stacking interactions, hydrophobic interactions, and electrostatic interaction. Among all the interactions, the π-π stacking interaction and hydrogen bond played a significant role in a various range of activities of the compounds.


Glucosamine/analogs & derivatives , Glycoside Hydrolase Inhibitors/chemical synthesis , alpha-Glucosidases/metabolism , 1-Deoxynojirimycin/chemical synthesis , 1-Deoxynojirimycin/pharmacokinetics , Acarbose/pharmacology , Acarbose/standards , Benzylidene Compounds/chemistry , Glucosamine/chemical synthesis , Glucosamine/pharmacokinetics , Glycoside Hydrolase Inhibitors/pharmacokinetics , Humans , Hydrogen Bonding , Hydrophobic and Hydrophilic Interactions , Kinetics , Molecular Docking Simulation , Structure-Activity Relationship
18.
Food Chem ; 330: 127245, 2020 Nov 15.
Article En | MEDLINE | ID: mdl-32521399

Dihydromyricetin (DMY) encapsulated zein-caseinate nanoparticles (DZP) were fabricated by antisolvent method. The encapsulation and loading efficiency of DMY in DZP were 90.2% and 22.6% as determined by HPLC. DZP is spherical with particle size and ζ potential of 206.4 nm and -29.6 mV, respectively. Physicochemical characterization showed that DMY existed in amorphous form in DZP and its interaction with proteins was found. The fabrication of DZP significantly improved the stability of DMY. Besides, the diffusion rate of DMY in DZP was faster than its suspensions in both simulated gastric and intestinal fluid. The adhesion of DMY in mice gastrointestinal tract was also improved. Besides DMY itself, its methylated metabolites with further sulfation and glucuronide were identified in rat plasma by UPLC-QTOF-MS. UPLC-QqQ-MS/MS quantitative analysis showed that the oral bioavailability of DMY was 1.95 times enhanced. Besides, the concentration of DMY metabolites in plasma were all increased.


Caseins/chemistry , Flavonols/chemistry , Nanoparticles/chemistry , Zein/chemistry , Animals , Biological Availability , Caseins/metabolism , Chromatography, High Pressure Liquid , Female , Flavonols/metabolism , Mice , Particle Size , Rats , Tandem Mass Spectrometry , Zein/metabolism
19.
ACS Appl Mater Interfaces ; 12(22): 24786-24795, 2020 Jun 03.
Article En | MEDLINE | ID: mdl-32372639

As an important organic intermediate, benzonitrile (BN) is widely involved in organic synthetic chemistry and pharmaceutical and dyestuff industries. However, the exploration of a more efficient and controllable synthesis technique and the corresponding greener catalysts for the synthesis of BN still poses a great challenge. Herein, with multimetallic two-dimensional conductive metal-organic frameworks (2D cMOF) as anodic electrocatalysts, we develop a green, convenient, and highly efficient electrochemical synthesis strategy for BN. Thanks to the intrinsic 2D electrically conductive structure and the optimized the multimetallic coupling catalytic effect, the resulting multimetallic 2D cMOFs exhibit excellent benzylamine (BA) electrooxidation performance. Especially, the trimetallic 2D cMOF (NiCoFe-CAT) requires an ultralow potential of 1.29 V vs reversible hydrogen electrode (RHE) to achieve a 10 mA·cm-2 current density, which indicates the fastest reaction and the most favorable thermodynamic condition. A very high yield (0.058 mmol·mg-1·h-1) and faradic efficiency (∼87%) of benzonitrile are both achieved during the BA electrooxidation reaction at 1.45 V. The reaction mechanism investigations indicated that the various redox mediators of MII/MIII (Ni, Co, Fe) may be regarded as multimetal active species to promote BA conversion. Also, the excellent cycling durability of multimetallic 2D cMOFs further promotes their potential practical applications. These electrocatalytic performances are considered excellent and nearly surpass all other reported Ni-based inorganics or MOF-based electrocatalysts for the electrocatalytic oxidation of benzylamine.

20.
Anal Chem ; 91(11): 7360-7365, 2019 06 04.
Article En | MEDLINE | ID: mdl-31062588

Hydrazine induced toxicity causes serious harm to the health of humans. The detection of N2H4 in vitro and in vivo has attracted a great deal of attention, especially in the context of fluorescent probes. Although some fluorescent N2H4 probes have been reported, only a few operate in purely aqueous media and, as a result, require the use of organic cosolvents which hinders their use in analysis of real samples. In addition, most of the current N2H4 probes are either "off-on" or "on-off" types, in which it is difficult to eliminate interference from background fluorescence commonly occurring in in vitro and in vivo systems. Furthermore, some probes are unable to differentiate hydrazine from other organic amines. To address the above problems, we developed a novel oligo(ethylene glycol)-functionalized fluorescent probe for the detection of N2H4. The probe, which has a donor-π-acceptor (D-π-A)-type structure, is water-soluble, and it can be utilized to selectively detect N2H4 in both colorimetric and ratiometric mode. Furthermore, the probe is able to differentiate hydrazine from other organic amines and can be used to detect hydrazine vapor and for imaging A549 cells and zebrafish.


Ethylene Glycol/chemistry , Fluorescent Dyes/chemistry , Hydrazines/analysis , A549 Cells , Animals , Colorimetry , Ethylene Glycol/chemical synthesis , Fluorescent Dyes/chemical synthesis , Humans , Molecular Structure , Optical Imaging , Quantum Theory , Tumor Cells, Cultured , Zebrafish
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