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排序方式: 共有479条查询结果,搜索用时 515 毫秒
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Dr. Ivan A. Yaremenko Dr. Paolo Coghi Parichat Prommana Congling Qiu Peter S. Radulov Yuanqing Qu Yulia Yu. Belyakova Dr. Enrico Zanforlin Dr. Vladimir A. Kokorekin Yuki Yu Jun Wu Prof. Fabrice Fleury Dr. Chairat Uthaipibull Dr. Vincent Kam Wai Wong Prof. Alexander O. Terent'ev 《ChemMedChem》2020,15(13):1118-1127
This article discloses a new horizon for the application of peroxides in medical chemistry. Stable cyclic peroxides are demonstrated to have cytotoxic activity against cancer cells; in addition a mechanism of cytotoxic action is proposed. Synthetic bridged 1,2,4,5-tetraoxanes and ozonides were effective against HepG2 cancer cells and some ozonides selectively targeted liver cancer cells (the selectivity indexes for compounds 11 b and 12 a are 8 and 5, respectively). In some cases, tetraoxanes and ozonides were more selective than paclitaxel, artemisinin, and artesunic acid. Annexin V flow-cytometry analysis revealed that the active ozonides 22 a and 23 a induced cell death of HepG2 by apoptosis. Further study showed that compounds 22 a and 23 a exhibited a strong inhibitory effect on P-glycoprotein (P-gp/ABCB5)-overexpressing HepG2 cancer cells. ABCB5 is a key player in the multidrug-resistant phenotype of liver cancer. Peroxides failed to demonstrate a direct correlation between oxidative potential and their biological activity. To our knowledge this is the first time that peroxide diastereoisomers have been found to show stereospecific antimalarial action against the chloroquine-sensitive 3D7 strain of Plasmodium falciparum. Stereoisomeric ozonide 12 b is 11 times more active than stereoisomeric ozonide 12 a (IC50=5.81 vs 65.18 μm ). Current findings mean that ozonides merit further investigation as potential therapeutic agents for drug-resistant hepatocellular carcinoma. 相似文献
3.
EL Nazarenko RP Gorshkova VA Zubkov AS Shashkov EP Ivanova IuS Ovodov 《Canadian Metallurgical Quarterly》1993,19(7):733-739
An acidic polysaccharide from Alteromonas sp. 4MC17 is built up of trisaccharide repeating units containing D-glucose, D-mannose and D-galacturonic acid residues. On the basis of methylation studies, 1H and 13C NMR-spectroscopy data, including two-dimensional homonuclear correlation spectroscopy and nuclear Overhauser effects, the following structure was suggested for the polysaccharide repeating unit: -->4)-beta-D-Glcp-(1-->4)-beta-D-GalpA-(1-->4)-beta-D-Manp-( 1-->. 相似文献
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SA Nazarenko NV Ostroverkhova VP Puzyrev LP Nazarenko MN Filimonova OIu Koriagina 《Canadian Metallurgical Quarterly》1998,34(1):114-121
BACKGROUND: Many species of bats have two sets of submandibular glands, principal and accessory. The accessory gland may resemble the principal one but more often shows wide morphological divergence. The free-tailed bat, Tadarida thersites, is very unusual in that it has two sets of parotid glands rather than binary submandibular glands. We studied the ultrastructure of the principal parotid gland to establish a baseline for comparison with the accessory parotid. METHODS: Two specimens of adult free-tailed bats, one male and one female, were live-trapped in western Kenya. Parotid glands were fixed for electron microscopy using a protocol expressly designed for field fixation and then embedded by conventional means. RESULTS: Histologically, the principal parotid is a typical serous gland. The secretory granules of the endpiece cells have an unusual substructure in that they contain variable numbers of lucent halos and one or several spherules. Intercalated duct cells contain a significant number of dense, serous-like granules. Striated ducts have the usual basal configuration of mitochondria and folded plasma membranes, but the supranuclear cytoplasm contains many small, dense granules, so that these ducts resemble the granular convoluted tubules found in the submandibular glands of many families of rodents. The apices of the duct cells have a peculiar contour--the luminal surfaces obliquely invaginate into the apical cytoplasm, so that in thin section the luminal membranes appear to be underlaid by a layer of vacuoles. CONCLUSION: Although the principal parotid gland of the free-tailed bat shows some distinctive, species-specific ultrastructural features, it basically is similar to the parotid gland in two other molossid bats, Tadarida brasiliensis and Molossus molossus. The distinctive features in the principal parotid gland of T. thersites might relate to its feeding on hard-bodied insects and perhaps to the production of lysozyme. 相似文献
6.
Galina M. Viryasova Ekaterina A. Golenkina Tibor Hianik Nataliya V. Soshnikova Nina G. Dolinnaya Tatjana V. Gaponova Yulia M. Romanova Galina F. Sudina 《International journal of molecular sciences》2021,22(5)
Neutrophil-mediated innate host defense mechanisms include pathogen elimination through bacterial phagocytosis, which activates the 5-lipoxygenase (5-LOX) product synthesis. Here, we studied the effect of synthetic oligodeoxyribonucleotides (ODNs), which mimic the receptor-recognized sites of bacterial (CpG-ODNs) and genomic (G-rich ODNs) DNAs released from the inflammatory area, on the neutrophil functions after cell stimulation with Salmonella typhimurium. A possible mechanism for ODN recognition by Toll-like receptor 9 (TLR9) and RAGE receptor has been proposed. We found for the first time that the combination of the magic peptide LRR11 from the leucine-rich repeat (LRR) of TLR9 with the CpG-ODNs modulates the uptake and signaling from ODNs, in particular, dramatically stimulates 5-LOX pathway. Using thickness shear mode acoustic method, we confirmed the specific binding of CpG-ODNs, but not G-rich ODN, to LRR11. The RAGE receptor has been shown to play an important role in promoting ODN uptake. Thus, FPS-ZM1, a high-affinity RAGE inhibitor, suppresses the synthesis of 5-LOX products and reduces the uptake of ODNs by neutrophils; the inhibitor effect being abolished by the addition of LRR11. The results obtained revealed that the studied peptide-ODN complexes possess high biological activity and can be promising for the development of effective vaccine adjuvants and antimicrobial therapeutics. 相似文献
7.
Yulia Gryaditskya Tania Pouli Erik Reinhard Hans‐Peter Seidel 《Computer Graphics Forum》2014,33(7):61-69
Image calibration requires both linearization of pixel values and scaling so that values in the image correspond to real‐world luminances. In this paper we focus on the latter and rather than rely on camera characterization, we calibrate images by analysing their content and metadata, obviating the need for expensive measuring devices or modeling of lens and camera combinations. Our analysis correlates sky pixel values to luminances that would be expected based on geographical metadata. Combined with high dynamic range (HDR) imaging, which gives us linear pixel data, our algorithm allows us to find absolute luminance values for each pixel—effectively turning digital cameras into absolute light meters. To validate our algorithm we have collected and annotated a calibrated set of HDR images and compared our estimation with several other approaches, showing that our approach is able to more accurately recover absolute luminance. We discuss various applications and demonstrate the utility of our method in the context of calibrated color appearance reproduction and lighting design. 相似文献
8.
The objective of this research was to evaluate the effectiveness of several different methods for controlling the pore size and pore size distribution in activated carbon fibers. Variables studied included fiber shape, activation time, and the addition of small amounts of silver nitrate. Pure isotropic pitch and the same isotropic pitch containing 1 wt.% silver were melt spun to form fibers with round and trilobal cross sections. These fibers were then stabilized, carbonized, and activated in carbon dioxide. Field emission scanning electron microscopy (FE SEM), electron dispersive spectra (EDS), and wavelength dispersive spectra (WDS) were used to monitor the size and distribution of the silver particles in the fibers before and after activation. Each of these analyses showed that the distribution of silver particles was extremely uniform before and after activation. The fibers were also weighed before and after activation to determine the percent burn-off. The BET specific surface areas of the activated fibers were determined from N2 adsorption isotherms measured at −196 °C. The results showed that round and trilobal fibers with equivalent cross-sectional areas yielded similar burn-off values and specific surface areas after activation. Also, activation rates were found to be independent of CO2 flow rate. The porosity of the activated fibers depended on the total time of activation and the cross-sectional area of fibers. The N2 adsorption measurements showed that the activated fibers had extremely high specific surface areas (greater than 3000 m2/g) and high degrees of meso- and macro-porosity. FE SEM was also used to investigate surface texture and size of pore openings on the surfaces of the activated fibers. The photos showed that silver particles generated surface macro- and mesopores, in agreement with the inferences from N2 adsorption measurements. 相似文献
9.
Vladimir A. Tyurin Gianfranca Carta Yulia Y. Tyurina Sebastiano Banni Billy W. Day Francesco P. Corongiu Valerian E. Kagan 《Lipids》1997,32(2):131-142
Recent studies provide extensive evidence for the importance of carotenoids in protecting against oxidative stress associated
with a number of diseases. In particular, reactions of carotenoids with phenoxyl radicals generated by peroxidasecatalyzed
one-electron metabolism of phenolic compounds may represent an important antioxidant function of carotenoids. To further our
understanding of the antioxidant mechanisms of carotenoids, we used in the present work two different phenolic compounds,
phenol and a polar homologue of vitamin E (2,2,5,7,8-pentamethyl-6-hydroxychromane, PMC), as representatives of two different
types of phenols to study reactions of their respective phenoxyl radicals with carotenoids in cells and in model systems.
We found that phenoxyl radicals of PMC did not oxidize β-carotene in either HL-60 cells or in model systems with horseradish
peroxidase (HRP)/H2O2. In contrast, the phenoxyl radicals generated from phenol (by native myeloperoxidase in HL-60 cells or HRP/H2O2 in model systems) effectively oxidized β-carotene and other carotenoids (canthaxanthin, lutein, lycopene). One-electron reduction
of the phenoxyl radical by ascorbate (assayed by electron spin resonance-detectable formation of semidehydroascorbyl radicals)
prevented HRP/H2O2-induced oxidation of β-carotene. PMC, but not phenol, protected β-carotene against oxidation induced by a lipid-soluble azo-initiator
of peroxyl radicals. No adducts of peroxidase/phenol/H2O2-induced β-carotene oxidation intermediates with phenol were detected by high-performance liquid chromatography-mass spectrometry
analysis of the reaction mixture. Since carotenoids are essential constituents of the antioxidant defenses in cells and biological
fluids, their depletion through the reaction with phenoxyl radicals formed from endogenous, nutritional and environmental
phenolics, as well as phenolic drugs, may be an important factor in the development of oxidative stress. 相似文献
10.
V. R. Nazarenko L. I. Bondarenko V. F. Yankovskii M. A. Dolginskaya 《Metal Science and Heat Treatment》1989,31(9):712-716
The Russian term is "bulat" steel and to bulat is related the understanding of steel with high elastic and cutting properties, for which a unique microstructure, a patterned surface, is characteristic. To it was imparted special value and it was assumed to be a compulsory component of damask steel. The word "bulat" is of Iranian origin (pulad).In the modern understanding steel is a material with a certain chemical composition and damask steel does not fit under it. 相似文献