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排序方式: 共有120条查询结果,搜索用时 765 毫秒
111.
《Saudi Journal of Biological Sciences》2023,30(8):103731
Guar Gum has been evaluated for its importance in food and pharmaceutical industry. A blended biopolymeric hydrogel was prepared by solution casting technique using guar gum (GG), chitosan (CS), polyvinyl alcohol (PVA), chemically crosslinked with tetra orthosilicate (TEOS) and impregnated with methotrexate (MTX) to assess its drug carrying capacity against colon cancer (HCT-116). The surface morphology, chemical bonding, hydrophilicity and water absorbing capacity were analyzed by atomic force microscopy (AFM), Fourier transform infrared spectroscopy (FTIR), contact angle measurements and swelling properties in variable conditions. Furthermore, degradation, drug release kinetics, hemocompatibility, and cytotoxicity of MTX-loaded hydrogel was tested. The release of MTX from GG/CS/PVA biopolymeric blend occurred in sustained manner. Results displayed that in 7 h 25 min duration 96% of the drug was released in phosphate buffer saline (PBS) at pH 7.4. These blends were non-hemolytic, and antiproliferative against HCT-116. Furthermore, the MTT assay has revealed that MTX-loaded hydrogel had prominently decreased the cell viability (with IC50 11.7 µg/ml) as compared to free MTX (with IC50 21.57 µg/ml). Hence, these results suggest that guar gum based hydrogels are potential biomaterials for colon cancer treatment. 相似文献
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Michael J Corley Wei Zhang Xin Zheng Annette Lum-Jones Alika K Maunakea 《Epigenetics》2015,10(2):153-166
Methylated DNA immunoprecipitation sequencing (MeDIP-Seq) is a widely used approach to study DNA methylation genome-wide. Here, we developed a MeDIP-Seq protocol compatible with the Ion Torrent semiconductor-based sequencing platform that is low cost, rapid, and scalable. We applied this protocol to demonstrate MeDIP-Seq on the Ion Torrent platform provides adequate coverage of CpG cytosines, the methylation states of which we validated at single-base resolution on the Infinium HumanMethylation450 BeadChip array, and accurately identifies sites of differential DNA methylation. Furthermore, we applied an integrative approach to further investigate and confirm the role of DNA methylation in alternative splicing and to profile 5mC and 5hmC variants of DNA methylation in normal human brain tissue that is localized over distinct genomic regions. These applications of MeDIP-Seq on the Ion Torrent platform have broad utility and add to the current methodologies for profiling genome-wide DNA methylation states in normal and disease conditions. 相似文献
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This study aims to investigate the mechanisms associated with the antiproliferation effect of guanosine on human colon carcinoma HCT 116 cells. In this study, guanosine induced more drastic cell cycle arrest effect than cell death effect on HCT 116 cells. The cell cycle arrest effect of guanosine on HCT 116 cells appeared to be associated with the increased activation of mitogen-activated protein kinases (MAPK) such as ERK1/2, p38 and JNK. The decrease of AMP-activated protein kinase (AMPK) activation and cyclin D1 expression was also involved. Thus, the antiproliferation of colon cancer cells of guanosine could be mediated by the disruption of MAPK and AMPK pathways. 相似文献
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Andrey G. Tereshchenkov Malgorzata Dobosz-Bartoszek Ilya A. Osterman James Marks Vasilina A. Sergeeva Pavel Kasatsky Ekaterina S. Komarova Andrey N. Stavrianidi Igor A. Rodin Andrey L. Konevega Petr V. Sergiev Natalia V. Sumbatyan Alexander S. Mankin Alexey A. Bogdanov Yury S. Polikanov 《Journal of molecular biology》2018,430(6):842-852
Antibiotic chloramphenicol (CHL) binds with a moderate affinity at the peptidyl transferase center of the bacterial ribosome and inhibits peptide bond formation. As an approach for modifying and potentially improving properties of this inhibitor, we explored ribosome binding and inhibitory activity of a number of amino acid analogs of CHL. The L-histidyl analog binds to the ribosome with the affinity exceeding that of CHL by 10 fold. Several of the newly synthesized analogs were able to inhibit protein synthesis and exhibited the mode of action that was distinct from the action of CHL. However, the inhibitory properties of the semi-synthetic CHL analogs did not correlate with their affinity and in general, the amino acid analogs of CHL were less active inhibitors of translation in comparison with the original antibiotic. The X-ray crystal structures of the Thermus thermophilus 70S ribosome in complex with three semi-synthetic analogs showed that CHL derivatives bind at the peptidyl transferase center, where the aminoacyl moiety of the tested compounds established idiosyncratic interactions with rRNA. Although still fairly inefficient inhibitors of translation, the synthesized compounds represent promising chemical scaffolds that target the peptidyl transferase center of the ribosome and potentially are suitable for further exploration. 相似文献
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《Bioorganic & medicinal chemistry letters》2020,30(2):126851
Quinoxaline derivatives are reported as antineoplastic agents against a variety of human cancer cell lines, with some compounds being submitted to clinical trials. In this work, we report the synthesis, characterization and cytotoxicity potential of a new series of quinoxalinyl-hydrazones. The most cytotoxic compound was (E)-2-[2-(2-pyridin-2-ylmethylene)hydrazinyl]quinoxaline (PJOV56) that presented a time-dependent effect against HCT-116 cells. After 48 h of incubation, PJOV56 was able to induce autophagy and apoptosis of HCT-116 cells, mediated by upregulation of Beclin 1, upregulation of LC3A/B II and activation of caspase 7. Apoptosis was induced along with G0/G1 cell cycle arrest at the highest concentration of PJOV56 (6.0 µM). Thus, PJOV56 showed a dose-dependent mode of action related to induction of autophagy and apoptosis in HCT-116 cells. 相似文献
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