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排序方式: 共有10000条查询结果,搜索用时 171 毫秒
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Anna Stasiowicz Natalia Rosiak Ewa Tykarska Maciej Kozak Jacek Jenczyk Piotr Szulc Joanna Kobus-Cisowska Kornelia Lewandowska Anita Paziska Wojciech Paziski Judyta Cielecka-Piontek 《International journal of molecular sciences》2021,22(8)
Piperine is an alkaloid that has extensive pharmacological activity and impacts other active substances bioavailability due to inhibition of CYP450 enzymes, stimulation of amino acid transporters and P-glycoprotein inhibition. Low solubility and the associated low bioavailability of piperine limit its potential. The combination of piperine with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) causes a significant increase in its solubility and, consequently, an increase in permeability through gastrointestinal tract membranes and the blood–brain barrier. X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR), nuclear magnetic resonance (NMR) were used to characterize interactions between piperine and HP-β-CD. The observed physicochemical changes should be combined with the process of piperine and CD system formation. Importantly, with an increase in solubility and permeability of piperine as a result of interaction with CD, it was proven to maintain its biological activity concerning the antioxidant potential (2,2-diphenyl-1-picryl-hydrazyl-hydrate assay), inhibition of enzymes essential for the inflammatory process and for neurodegenerative changes (hyaluronidase, acetylcholinesterase, butyrylcholinesterase). 相似文献
23.
《Ceramics International》2021,47(23):32521-32533
In the current report, pure V2O5, a series of Gd doped V2O5 (1 wt%, 3 wt%, 5 wt% and 10 wt%) and graphene integrated Gd–V2O5 photocatalysts have been prepared using a facile wet chemical approach. The effect of Gd+3 ions substitution and RGO support on V2O5 was studied by the different analytical techniques. X-ray diffraction (XRD) results showed the orthorhombic crystal structure of synthesized samples with crystallize size in range of 22–35 nm. Morphological analysis showed nanorods and nanorod arrays like appearance of V2O5, Gd–V2O5 and GdV-2O5/RGO, respectively. Gd–V2O5 and Gd–V2O5/RGO exhibited enhanced optical response in the visible region along with decrease in the band gap values for Gd doped V2O5 samples. BET surface area of Gd–V2O5 and Gd- V2O5/RGO was calculated as 12.39 g/m2 and 15.35 g/m2 that was found to be higher than pristine V2O5. To study the photocatalytic activity of synthesized photocatalysts, methylene blue (MB) was chosen as model pollutant. Among the Gd doped V2O5 samples, highest photocatalytic activity (45.62%) was achieved by optimal concentration of 5 wt% Gd–V2O5 that is accredited to effective separation of electron-hole pairs. While Gd–V2O5/RGO showed 2.1 times higher dye removal (97.12%) than unsupported Gd–V2O5, under the visible light irradiation. The significantly high photocatalytic activity of Gd–V2O5/RGO is due to the synergistic effect aroused by combined action of Gd+3 ions doping and advantageous properties of highly conductive and large surfaced graphene. Recycling experiments for V2O5 derivatives showed good stability and recyclability of photocatalysts. Additionally, Gd–V2O5/RGO was found to be more potential anti-bacterial agent than V2O5 and Gd–V2O5. 相似文献
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Lucas Portela Oliveira Camila Cristina de Foggi Bruna Natália Alves da Silva Pimentel Marcelo Assis Juan Andrés Elson Longo Carlos Eduardo Vergani 《Ceramics International》2021,47(16):22604-22614
The present study reports for the first time the performance of silver phosphate (Ag3PO4) microcrystals as photocatalyst (degradation of Rodamine B-RhB) and antifungal agent (against Candida albicans–C. albicans) under visible-light irradiation (455 nm). Ag3PO4 microcrystals were synthesized by a simple co-precipitation (CP) method at room temperature. The structural and electronic properties of the as-synthetized Ag3PO4 have been investigated before and after 4 cycles of RhB degradation under visible light using X-ray diffraction (XRD), micro-Raman spectroscopy, UV–Vis spectrophotometer and field emission scanning electron microscopy (FE-SEM) images. The antifungal activity was analyzed in planktonic cells and 48h-biofilm of C. albicans by colony forming units (CFU) counting, confocal laser and FE-SE microscopies. Statistical analysis was carried out using SPSS software. Morphological and structural modifications of Ag3PO4 were observed upon recycling. After 4 recycles, the material maintained its photodegradation property; an eightfold increase in the efficiency of Ag3PO4 was observed in planktonic cells and a two fold increase in biofilm when irradiated under visible light. Thus, higher antifungal effectiveness against C. albicans was obtained when associated with visible-light irradiation. 相似文献
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Pawe Lenartowicz Mateusz Psurski Aleksandra Kotynia Aleksandra Pienina Monika Cuprych Klaudia Poniatowska Justyna Brasu Pawe Kafarski 《International journal of molecular sciences》2021,22(4)
Background: Dehydropeptides are analogs of peptides containing at least one conjugate double bond between α,β-carbon atoms. Its presence provides unique structural properties and reaction centre for chemical modification. In this study, the series of new class of dipeptides containing S-substituted dehydrocysteine with variety of heterocyclic moieties was prepared. The compounds were designed as the building blocks for the construction of artificial metalloenzymes (artzymes). Therefore, the complexing properties of representative compounds were also evaluated. Furthermore, the acknowledged biological activity of natural dehydropeptides was the reason to extend the study for antiproliferative action of against several cancer cell lines. Methods: The synthetic strategy involves glycyl and phenylalanyl-(Z)-β-bromodehydroalanine as a substrate in one pot addition/elimination reaction of thiols. After deprotection of N-terminal amino group the compounds with triazole ring were tested as complexones for copper(II) ions using potentiometric titration and spectroscopic techniques (UV-Vis, CD, EPR). Finally, the antiproliferative activity was evaluated by sulforhodamine B assay. Results and Conclusions: A simple and efficient procedure for preparation of dipeptides containing S-substituded dehydrocysteine was provided. The peptides containing triazole appeared to be strong complexones of copper(II) ions. Some of the peptides exhibited promising antiproliferative activities against number of cancer cell lines, including cell lines resistant to widely used anticancer agent. 相似文献
29.
Dr. Chungsik Kim Mintesinot Kassu Dr. Kenneth P. Smith Prof. James E. Kirby Prof. Roman Manetsch 《ChemMedChem》2021,16(18):2775-2780
Pyrazole-thiazole core-containing compound KP-40 and 20 novel derivatives were designed and synthesized through traditional SAR analysis. These molecules displayed adjunctive activity with meropenem against Gram-negative bacteria evidenced by a range of fractional inhibitory concentration (FIC=0.5–0.25) and minimum adjunctive concentration (MAC=128–32 μM) values. Of this series of molecules, four compounds displayed notable adjunctive potential, with FIC and MAC values of 0.25 and 32 μM, respectively. Moreover, the solubility of these compounds was improved to an acceptable range. Further analysis using our “in house” permeation and efflux multi parameter optimization (PEMPO) algorithm revealed key physicochemical properties that may be critical for the development of active Gram-negative antibacterials. Taking PEMPO scores into consideration prior to executing synthesis of analogs may be a simple, yet rapid and effective strategy that can be used in conjunction with traditional SAR approaches to aid in the design of potent Gram-negative antibacterials. 相似文献
30.
目的:研究贵长猕猴桃皮HPLC指纹图谱与抗氧化活性的关系。方法:采用高效液相色谱法建立10批不同来源地贵长猕猴桃皮的指纹图谱,采用SPSS 13.0进行样品聚类分析和主成分分析;并通过DPPH和ABTS法测定其抗氧化活性,以EC50与共有峰峰面积数据为基础,应用皮尔逊相关分析法和逐步回归分析法研究谱效关系。结果:建立了10批贵长猕猴桃皮HPLC指纹图谱,确定了14个共有峰,相似度均>0.90。采用对照品比对方法指认了其中6个峰:2号峰没食子酸,5号峰原儿茶酸,9号峰表儿茶素,10号峰二氢槲皮素,11号峰4-香豆酸,12号峰落新妇苷,样本可聚为3类。皮尔逊相关分析与逐步回归分析结果显示:5号峰(原儿茶酸)和9号峰(表儿茶素)峰面积变化与贵长猕猴桃皮抗氧化活性呈显著正相关,对其抗氧化活性贡献度较大。结论:贵长猕猴桃皮具有较高的体外抗氧化活性,抗氧化活性的物质基础初步确定为贵长猕猴桃皮开发利用、质量评价提供依据。 相似文献