Three oxovanadium complexes, namely [VO(NOSAA)(bpy)] (1) (NOSAA = 2-hydroxy-5-nitrosalicylidene anthranilic acid, bpy = 2,2′-bipyridyl), [VO(NOSAA)(4,4′-dimebpy)] (2) (4,4′-dimebpy = 4,4′-dimethyl-2,2′- bipyridyl), and [VO(NOSAA)(phen)] (3) (phen = 1,10-phenanthroline), have been prepared and characterized. The binding modes and strengths of these complexes with calf thymus DNA (CT-DNA) were studied using various techniques. The chemical nuclease activities and photocleavage reactions of the complexes were also tested. All three complexes interact with CT-DNA through intercalative modes, and complex 3 possesses the largest binding affinity. All three complexes can efficiently cleave pBR322 DNA upon irradiation or under physiological conditions in the presence of H2O2, and complex 3 has the best cleaving ability. In vitro experimental results showed that the three complexes are cytotoxic against myeloma (Ag8.653) and gliomas (U251) cell lines and complex 3 again showed the highest efficacy. 相似文献
New Delhi metallo-β-lactamase-1 (NDM-1) has emerged as a major global threat to human health for its rapid rate of dissemination and ability to make pathogenic microbes resistant to almost all known β-lactam antibiotics. In addition, effective NDM-1 inhibitors have not been identified to date. In spite of the plethora of structural and kinetic data available, the accurate molecular characteristics of and details on the enzymatic reaction of NDM-1 hydrolyzing β-lactam antibiotics remain incompletely understood. In this study, a combined computational approach including molecular docking, molecular dynamics simulations and quantum mechanics/molecular mechanics calculations was performed to characterize the catalytic mechanism of meropenem catalyzed by NDM-1. The quantum mechanics/molecular mechanics results indicate that the ionized D124 is beneficial to the cleavage of the C–N bond within the β-lactam ring. Meanwhile, it is energetically favorable to form an intermediate if no water molecule coordinates to Zn2. Moreover, according to the molecular dynamics results, the conserved residue K211 plays a pivotal role in substrate binding and catalysis, which is quite consistent with previous mutagenesis data. Our study provides detailed insights into the catalytic mechanism of NDM-1 hydrolyzing meropenem β-lactam antibiotics and offers clues for the discovery of new antibiotics against NDM-1 positive strains in clinical studies. 相似文献
Four novel terminal modified antisense oligonucleotides (ODNs) were designed, synthesized and tested for their anti-influenza virus activity. Initial biological studies indicated that lipophilic and rimantadin emodificated Flutide exhibited more potent anti-H1N1 activity than Flutide. Among them, lipophilic modificated ODN (Flutide-I) showed the most antiviral activity. The EC50 value of Flutide-I for inhibiting H1N1 induced cytopathic effect (CPE) and H1N1 RNA were respectively (0.26 ± 0.16) μM and (0.11 ± 0.03) μM. The cytotoxicity of these compounds has also been assessed. No significant cytotoxicities were found for any of these compounds with the concentrations up to 20 μM. 相似文献
As a prominent member of the 5′-kinase family, T4 polynucleotide kinase (PNK) plays an important role in gene function regulations, and the study of PNK activity and its potential inhibitors is significant for research related to the DNA phosphorylation process. Here, we proposed a novel strategy for the detection of PNK activity and its inhibition, which combines exonuclease enzyme reaction and nicking enzyme-assisted fluorescence signal amplification. Through recycling cleavage of DNA fluorescence probe for signal amplification, a highly sensitive PNK sensing platform is developed, and a very low detection limit of 0.05 mU/mL is achieved, which is better than or comparable to that of the previously reported PNK assays. The present approach adopts a simple separation-free procedure in which the enzyme assay is conducted in homogeneous solutions. Additionally, the inhibitory effects of several known kinase inhibitors on PNK have been successfully detected. Since the proposed assay exhibits the advantages of high sensitivity and simplicity, it holds great potential in providing a promising platform for convenient and highly sensitive detection of PNK activity and its inhibitors.
Figure
Schematic illustration of the strategy for sensitive PNK activity detection based on coupled lambda exonuclease reaction and nicking enzyme-assisted fluorescence signal amplification 相似文献
We demonstrate here a novel method for the design of liquid crystals (LCs) via the cyclization of mesogens by flexible chains. For two azobenzene-4,4′-dicarboxylate derivatives, the cyclic dimer, cyclic bis(tetraethylene glycol azobenzene-4,4′-dicarboxylate) (CBTAD), shows LC properties with smectic A phase, while its linear counterpart, bis(2-(2′-hydroxyethyloxy)ethyl azobenzene-4,4′-dicarboxylate (BHAD), has no LC phase. The difference is ascribed to the shackling effect from the cyclic topology, which leads to the much smaller entropy change during phase transitions and increases the isotropic temperature greatly for cyclics. In addition, the trans-to-cis isomerization of azobenzene groups under UV-light is also limited in CBTAD. With the reversible isomerization of azobenzene groups, CBTAD showed interesting isothermal phase transition behaviors, where the LC phase disappeared upon photoirradiation of 365 nm UV-light, and recovered when the UV-light was off. Combined with the smectic LC nature, a novel UV-light tuned visible light regulator was designed, by simply placing CBTAD in two glass plates. The scattered phase of smectic LC was utilized as the “OFF” state for light passage, while the UV-light induced isotropic phase was utilized as the “ON” state. The shackling effect outlined here should be applicable for the design of cyclic LC oligomers/polymers with special properties.
We report a higher precision measurement of the refractive index of carbon dioxide using a frequency comb as the light source in a Mach-Zehnder interferometer setup. The experimental sensitivity can reach the level of 8.8x10(-9). Taking into account the measurement accuracy of temperature and pressure, the experimental accuracy has a value of 1.2x10(-8). The measurement result has a deviation from the commonly quoted result [Old , J. Opt. Soc. Am.61, 89 (1971)] by 6.4x10(-7) at 800 nm. 相似文献
Chemistry of Natural Compounds - Benzomalvins B, C, and E (1, 2, and 3) were simultaneously obtained from the marine fungus Aspergillus sp. isolated from the soft coral Sinularia sp., collected... 相似文献
Journal of Sol-Gel Science and Technology - Zeolitic Imidazolate Framework (ZIF-8) micropolyhedra were employed as a raw material for the synthesis of fine cadmium sulfide/zinc sulfide (CdS/ZnS)... 相似文献