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  • MDPI AG  (2,980)
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  • 1
    Online Resource
    Online Resource
    Structurally Simple Phenanthridine Analogues Based on Nitidine and Their Antitumor Activities
    MDPI AG ; 2019
    In:  Molecules Vol. 24, No. 3 ( 2019-01-26), p. 437-
    Details
    In: Molecules, MDPI AG, Vol. 24, No. 3 ( 2019-01-26), p. 437-
    Abstract: A series of novel structurally simple analogues based on nitidine was designed and synthesized in search of potent anticancer agents. The antitumor activity against human cancer cell lines (HepG2, A549, NCI-H460, and CNE1) was performed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay in vitro. The results showed that some of them had good anticancer activities, especially derivatives with a [(dimethylamino)ethyl]amino side chain in the C-6 position. Planar conjugated compounds 15a, 15b, and 15c, with IC50 values of 1.20 μM, 1.87 μM, and 1.19 μM against CNE1 cells, respectively, were more active than nitidine chloride. Compound 15b and compound 15c with IC50 values of 1.19 μM and 1.37 μM against HepG2 cells and A549 cells demonstrated superior activities to nitidine. Besides, compound 5e which had a phenanthridinone core displayed extraordinary cytotoxicity against all test cells, particularly against CNE1 cells with the IC50 value of 1.13 μM.
    Type of Medium: Online Resource
    ISSN: 1420-3049
    URL: Article
    DOI: 10.3390/molecules24030437
    Language: English
    Publisher: MDPI AG
    Publication Date: 2019
    detail.hit.zdb_id: 2008644-1
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  • 2
    Online Resource
    Online Resource
    White Peony (Fermented Camellia sinensis) Polyphenols Help Prevent Alcoholic Liver Injury via Antioxidation
    MDPI AG ; 2019
    In:  Antioxidants Vol. 8, No. 11 ( 2019-10-31), p. 524-
    Details
    In: Antioxidants, MDPI AG, Vol. 8, No. 11 ( 2019-10-31), p. 524-
    Abstract: White peony is a type of white tea (Camellia sinensis) rich in polyphenols. In this study, polyphenols were extracted from white peony. In vitro experiments showed that white peony polyphenols (WPPs) possess strong free radical scavenging capabilities toward 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS). Long-term alcohol gavage was used to induce alcoholic liver injury in mice, and relevant indices of liver injury were examined. WPPs effectively reduced the liver indices of mice with liver injury. The serum levels of aspartate aminotransferase (ATS), alanine aminotransferase (ALT), alkaline phosphatase (ALP), triglycerides (TG), total cholesterol (TC), blood urea nitrogen (BUN), nitric oxide (NO), and malondialdehyde (MDA) were downregulated, while those of albumin (ALB), superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH-Px) were upregulated. WPPs also reduced the serum levels of interluekin-6 (IL-6), interluekin-12 (IL-12), tumor necrosis factor-alpha (TNF-α), and interferon-gamma (IFN-γ) in mice with liver injury. Pathology results showed that WPPs reduced alcohol-induced liver cell damage. Quantitative polymerase chain reaction (qPCR) and western blot results revealed that WPPs upregulated the mRNA and protein expressions of neuronal nitric oxide synthase (nNOS), endothelial nitric oxide synthase (eNOS), manganese superoxide dismutase (Mn-SOD), cupro–zinc superoxide dismutase (Cu/Zn-SOD), and CAT and downregulated iNOS expression in the liver of mice with liver injury. WPPs protected against alcoholic liver injury, and this effect was equivalent to that of silymarin. High-performance liquid chromatography revealed that WPPs mainly contained the polyphenols gallic acid, catechinic acid, and hyperoside, which are critical for exerting preventive effects against alcoholic liver injury. Thus, WPPs are high-quality natural products with liver protective effects.
    Type of Medium: Online Resource
    ISSN: 2076-3921
    URL: Article
    DOI: 10.3390/antiox8110524
    Language: English
    Publisher: MDPI AG
    Publication Date: 2019
    detail.hit.zdb_id: 2704216-9
    SSG: 15,3
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  • 3
    Online Resource
    Online Resource
    Oxidative Stress and Genotoxicity of Long-Term Occupational Exposure to Low Levels of BTEX in Gas Station Workers
    MDPI AG ; 2016
    In:  International Journal of Environmental Research and Public Health Vol. 13, No. 12 ( 2016-12-06), p. 1212-
    Details
    In: International Journal of Environmental Research and Public Health, MDPI AG, Vol. 13, No. 12 ( 2016-12-06), p. 1212-
    Type of Medium: Online Resource
    ISSN: 1660-4601
    URL: Article
    DOI: 10.3390/ijerph13121212
    Language: English
    Publisher: MDPI AG
    Publication Date: 2016
    detail.hit.zdb_id: 2175195-X
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  • 4
    Online Resource
    Online Resource
    Theoretical Study of Hydrogen Production from Ammonia Borane Catalyzed by Metal and Non-Metal Diatom-Doped Cobalt Phosphide
    MDPI AG ; 2022
    In:  Molecules Vol. 27, No. 23 ( 2022-11-24), p. 8206-
    Details
    In: Molecules, MDPI AG, Vol. 27, No. 23 ( 2022-11-24), p. 8206-
    Abstract: The decomposition of ammonia borane (NH3BH3) to produce hydrogen has developed a promising technology to alleviate the energy crisis. In this paper, metal and non-metal diatom-doped CoP as catalyst was applied to study hydrogen evolution from NH3BH3 by density functional theory (DFT) calculations. Herein, five catalysts were investigated in detail: pristine CoP, Ni- and N-doped CoP (CoPNi-N), Ga- and N-doped CoP (CoPGa-N), Ni- and S-doped CoP (CoPNi-S), and Zn- and S-doped CoP (CoPZn-S). Firstly, the stable adsorption structure and adsorption energy of NH3BH3 on each catalytic slab were obtained. Additionally, the charge density differences (CDD) between NH3BH3 and the five different catalysts were calculated, which revealed the interaction between the NH3BH3 and the catalytic slab. Then, four different reaction pathways were designed for the five catalysts to discuss the catalytic mechanism of hydrogen evolution. By calculating the activation energies of the control steps of the four reaction pathways, the optimal reaction pathways of each catalyst were found. For the five catalysts, the optimal reaction pathways and activation energies are different from each other. Compared with undoped CoP, it can be seen that CoPGa-N, CoPNi-S, and CoPZn-S can better contribute hydrogen evolution from NH3BH3. Finally, the band structures and density of states of the five catalysts were obtained, which manifests that CoPGa-N, CoPNi-S, and CoPZn-S have high-achieving catalytic activity and further verifies our conclusions. These results can provide theoretical references for the future study of highly active CoP catalytic materials.
    Type of Medium: Online Resource
    ISSN: 1420-3049
    URL: Article
    DOI: 10.3390/molecules27238206
    Language: English
    Publisher: MDPI AG
    Publication Date: 2022
    detail.hit.zdb_id: 2008644-1
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  • 5
    Online Resource
    Online Resource
    Hot Deformation Behavior and Microstructure Evolution of Ti–6Cr–5Mo–5V–4Al–1Nb Alloy
    MDPI AG ; 2023
    In:  Crystals Vol. 13, No. 2 ( 2023-01-20), p. 182-
    Details
    In: Crystals, MDPI AG, Vol. 13, No. 2 ( 2023-01-20), p. 182-
    Abstract: This study looked into the thermo-mechanical properties and the recrystallization mechanisms of the Ti–5.5Cr–5Mo–5V-4Al–1Nb alloy (wt.%, Ti−65541). Hot compression experiments were conducted at two phase regions (740~950 °C) and strain rates from 0.001 to 1 s−1. The compressive strain–stress curves were corrected by the adiabatic heating effect. The Arrhenius model was established and provided a reliable prediction of the value of stress with a 0.992 correlation coefficient. The constructed processing map demonstrated that when the temperature rose and the strain rate fell, the power dissipation efficiency (η) showed a rising trend. By utilizing electron backscattered diffraction (EBSD), the microstructural evolution and deformation process were analyzed. It was possible to witness both continuous dynamic recrystallization (cDRX) and discontinuous dynamic recrystallization (dDRX). The dynamic recovery (DRV) and dDRX eventually replaced dDRX while η decreased. Moreover, the deformation band (DB) impeded re-crystallization in the low η area. This study can supply a relatively reliable processing interval for the new Ti−65541 alloy.
    Type of Medium: Online Resource
    ISSN: 2073-4352
    URL: Article
    DOI: 10.3390/cryst13020182
    Language: English
    Publisher: MDPI AG
    Publication Date: 2023
    detail.hit.zdb_id: 2661516-2
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  • 6
    Online Resource
    Online Resource
    Hypermethylation of UCHL1 Promotes Metastasis of Nasopharyngeal Carcinoma by Suppressing Degradation of Cortactin (CTTN)
    MDPI AG ; 2020
    In:  Cells Vol. 9, No. 3 ( 2020-02-27), p. 559-
    Details
    In: Cells, MDPI AG, Vol. 9, No. 3 ( 2020-02-27), p. 559-
    Abstract: Epigenetic regulation plays an important role in the development and progression of nasopharyngeal carcinoma (NPC), but the epigenetic mechanisms underlying NPC metastasis remain poorly understood. Here, we demonstrate that hypermethylation of the UCHL1 promoter leads to its downregulation in NPC. Restoration of UCHL1 inhibited the migration and invasion of NPC cells in vitro and in vivo, and knockdown of UCHL1 promoted NPC cell migration and invasion in vitro and in vivo. Importantly, we found that UCHL1 interacts with CTTN, and may function as a ligase promoting CTTN degradation by increasing K48-linked ubiquitination of CTTN. Additionally, restoration of CTTN in NPC cells that overexpressed UCHL1 rescued UCHL1 suppressive effects on NPC cell migration and invasion, which indicated that CTTN is a functional target of UCHL1 in NPC. Our findings revealed that UCHL1 acts as a tumor suppressor gene in NPC and thus provided a novel therapeutic target for NPC treatment.
    Type of Medium: Online Resource
    ISSN: 2073-4409
    URL: Article
    DOI: 10.3390/cells9030559
    Language: English
    Publisher: MDPI AG
    Publication Date: 2020
    detail.hit.zdb_id: 2661518-6
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  • 7
    Online Resource
    Online Resource
    Glass-Forming Ability and Early Crystallization Kinetics of Novel Cu-Zr-Al-Co Bulk Metallic Glasses
    MDPI AG ; 2016
    In:  Metals Vol. 6, No. 9 ( 2016-09-15), p. 225-
    Details
    In: Metals, MDPI AG, Vol. 6, No. 9 ( 2016-09-15), p. 225-
    Type of Medium: Online Resource
    ISSN: 2075-4701
    URL: Article
    DOI: 10.3390/met6090225
    Language: English
    Publisher: MDPI AG
    Publication Date: 2016
    detail.hit.zdb_id: 2662252-X
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  • 8
    Online Resource
    Online Resource
    Set-Based Discriminative Measure for Electrocardiogram Beat Classification
    MDPI AG ; 2017
    In:  Sensors Vol. 17, No. 2 ( 2017-01-25), p. 234-
    Details
    In: Sensors, MDPI AG, Vol. 17, No. 2 ( 2017-01-25), p. 234-
    Type of Medium: Online Resource
    ISSN: 1424-8220
    URL: Article
    DOI: 10.3390/s17020234
    Language: English
    Publisher: MDPI AG
    Publication Date: 2017
    detail.hit.zdb_id: 2052857-7
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  • 9
    Online Resource
    Online Resource
    Metabolomics Tools Assisting Classic Screening Methods in Discovering New Antibiotics from Mangrove Actinomycetia in Leizhou Peninsula
    MDPI AG ; 2021
    In:  Marine Drugs Vol. 19, No. 12 ( 2021-12-01), p. 688-
    Details
    In: Marine Drugs, MDPI AG, Vol. 19, No. 12 ( 2021-12-01), p. 688-
    Abstract: Mangrove actinomycetia are considered one of the promising sources for discovering novel biologically active compounds. Traditional bioactivity- and/or taxonomy-based methods are inefficient and usually result in the re-discovery of known metabolites. Thus, improving selection efficiency among strain candidates is of interest especially in the early stage of the antibiotic discovery program. In this study, an integrated strategy of combining phylogenetic data and bioactivity tests with a metabolomics-based dereplication approach was applied to fast track the selection process. A total of 521 actinomycetial strains affiliated to 40 genera in 23 families were isolated from 13 different mangrove soil samples by the culture-dependent method. A total of 179 strains affiliated to 40 different genera with a unique colony morphology were selected to evaluate antibacterial activity against 12 indicator bacteria. Of the 179 tested isolates, 47 showed activities against at least one of the tested pathogens. Analysis of 23 out of 47 active isolates using UPLC-HRMS-PCA revealed six outliers. Further analysis using the OPLS-DA model identified five compounds from two outliers contributing to the bioactivity against drug-sensitive A. baumannii. Molecular networking was used to determine the relationship of significant metabolites in six outliers and to find their potentially new congeners. Finally, two Streptomyces strains (M22, H37) producing potentially new compounds were rapidly prioritized on the basis of their distinct chemistry profiles, dereplication results, and antibacterial activities, as well as taxonomical information. Two new trioxacarcins with keto-reduced trioxacarcinose B, gutingimycin B (16) and trioxacarcin G (20), together with known gutingimycin (12), were isolated from the scale-up fermentation broth of Streptomyces sp. M22. Our study demonstrated that metabolomics tools could greatly assist classic antibiotic discovery methods in strain prioritization to improve efficiency in discovering novel antibiotics from those highly productive and rich diversity ecosystems.
    Type of Medium: Online Resource
    ISSN: 1660-3397
    URL: Article
    DOI: 10.3390/md19120688
    Language: English
    Publisher: MDPI AG
    Publication Date: 2021
    detail.hit.zdb_id: 2175190-0
    SSG: 15,3
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  • 10
    Online Resource
    Online Resource
    Akkermansia muciniphila Cell-Free Supernatant Improves Glucose and Lipid Metabolisms in Caenorhabditis elegans
    MDPI AG ; 2023
    In:  Nutrients Vol. 15, No. 7 ( 2023-03-31), p. 1725-
    Details
    In: Nutrients, MDPI AG, Vol. 15, No. 7 ( 2023-03-31), p. 1725-
    Abstract: To explore the mechanism by which Akkermansia muciniphila cell-free supernatant improves glucose and lipid metabolisms in Caenorhabditis elegans, the present study used different dilution concentrations of Akkermansia muciniphila cell-free supernatant as an intervention for with Caenorhabditis elegans under a high-glucose diet. The changes in lifespan, exercise ability, level of free radicals, and characteristic indexes of glucose and lipid metabolisms were studied. Furthermore, the expression of key genes of glucose and lipid metabolisms was detected by qRT-PCR. The results showed that A. muciniphila cell-free supernatant significantly improved the movement ability, prolonged the lifespan, reduced the level of ROS, and alleviated oxidative damage in Caenorhabditis elegans. A. muciniphila cell-free supernatant supported resistance to increases in glucose and triglyceride induced by a high-glucose diet and downregulated the expression of key genes of glucose metabolism, such as gsy-1, pygl-1, pfk-1.1, and pyk-1, while upregulating the expression of key genes of lipid metabolism, such as acs-2, cpt-4, sbp-1, and tph-1, as well as down-regulating the expression of the fat-7 gene to inhibit fatty acid biosynthesis. These findings indicated that A. muciniphila cell-free supernatant, as a postbiotic, has the potential to prevent obesity and improve glucose metabolism disorders and other diseases.
    Type of Medium: Online Resource
    ISSN: 2072-6643
    URL: Article
    DOI: 10.3390/nu15071725
    Language: English
    Publisher: MDPI AG
    Publication Date: 2023
    detail.hit.zdb_id: 2518386-2
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