Selenocystine ([Sec]2) and aryl-substituted selenocysteine (Sec) derivatives are synthesized, starting from commercially available amino acid l-serine. These compounds are characterized by a number of analytical techniques such as NMR (1H, 13C and 77Se) and TOF mass spectroscopy. This study reveals that the introduction of amino/imino substituents capable of interacting with selenium may stabilize the Sec derivatives. This study further suggests that the oxidation-elimination reactions in Sec derivatives could be used for the generation of biologically active selenols having internally stabilizing substituents. 相似文献
The selenium analogues of anti-thyroid drugs exhibit their anti-thyroid action by a mechanism different from that of MMI. The selenium analogue of MMI and related selenium compounds exhibit high GPx activity, providing a novel method for the reversible inhibition of thyroid hormone biosynthesis. 相似文献
Large generation poly(propyl ether imine) (PETIM) dendrimers are synthesized in iterative synthetic cycles of two reductions and two Michael addition reactions. Dendrimers up to sixth generation, containing up to 128 peripheral functionalities, are synthesized. Growth of the PETIM dendrimers, possessing a tertiary amine as the branch juncture and an ether as the linker component, is assessed systematically by routine spectroscopic methods. The peripheries of these dendrimers possess either alcohols, amines, carboxylic acids, esters, or nitriles, thereby opening up possibilities for varied studies involving PETIM dendrimers. 相似文献
At the redox-active center of thioredoxin reductase (TrxR), a selenenyl sulfide (Se−S) bond is formed between Cys497 and Sec498, which is activated into the thiolselenolate state ([SH,Se−]) by reacting with a nearby dithiol motif ([SHCys59,SHCys64]) present in the other subunit. This process is achieved through two reversible steps: an attack of a cysteinyl thiol of Cys59 at the Se atom of the Se−S bond and a subsequent attack of a remaining thiol at the S atom of the generated mixed Se−S intermediate. However, it is not clear how the kinetically unfavorable second step progresses smoothly in the catalytic cycle. A model study that used synthetic selenenyl sulfides, which mimic the active site structure of human TrxR comprising Cys497, Sec498, and His472, suggested that His472 can play a key role by forming a hydrogen bond with the Se atom of the mixed Se−S intermediate to facilitate the second step. In addition, the selenenyl sulfides exhibited a defensive ability against H2O2-induced oxidative stress in cultured cells, which suggests the possibility for medicinal applications to control the redox balance in cells. 相似文献
The present study pertained to biosynthesis, characterization and biomedical application (larvicidal, histopathology, antibacterial, antioxidant and anticancer activity) of Zinc oxide nanoparticles (ZnONPs) from Pleurotus djamor. The synthesized NPs were characterized using spectral and microscopic analyses and further confirmed by UV–Visible spectrophotometer with apeak of 350 nm. The ZnONPs showed strong antioxidant property (DPPH, H2O2 and ABTS+ radical assay) and expressed good larval toxicity against Ae. aegypti and Cx. quinquefasciatus (IVth instar larvae) with the least LC50 and LC90 values (10.1, 25.6 and 14.4, 31.7 mg/l) after 24 h treatment, respectively. We noticed the morphological changes (damaged anal papillae area and the cuticle layers) in the treated larvae. For the antibacterial assay, the highest growth inhibition zone was recorded in C. diphteriae (28.6?±?0.3 mm), followed by P. fluorescens (27?±?0.5 mm) and S. aureus (26.6?±?1.5 mm). The in vitro cytotoxicity assay depicted a significant level of cytotoxic effects (LC50 values 42.26 μg/ml) of ZnONPs against the A549 lung cancer cells, even at low dose. The overall findings of the study suggest that P. djamor had the ability for the biosynthesis of ZnONPs and could act as an alternative biomedical agent for future therapeutic applications in medical avenues.
The kinetics of oxidation of aldonitrones by 4-(dimethylamino)pyridinium chlorochromate (DMAPCC) has been studied in aqueous
N,N-dimethylformamide in the presence of perchloric acid. The reaction follows first-order kinetics with respect to each of DMAPCC
and nitrone. The order with respect to [H+] was found to be close to zero. The rate of oxidation was unaltered by the variation of [NaClO4] but addition of MnSO4 decreased the rate. The reaction rate was found to decrease with a decrease in dielectric constant of the medium. Electron-releasing
and electron-withdrawing groups perturb the reaction rate with a good Hammett correlation. The oxidation products were found
to be benzaldehyde and nitrosobenzene. The reaction was carried out at four different temperatures and the activation parameters
have been calculated. On the basis of the experimental findings, a suitable mechanism has been proposed. 相似文献
Organophosphorus‐based nerve agents, such as paraoxon, parathion, and malathion, inhibit acetylcholinesterase, which results in paralysis, respiratory failure, and death. Bacteria are known to use the enzyme phosphotriesterase (PTE) to break down these compounds. In this work, we designed vacancy‐engineered nanoceria (VE CeO2 NPs) as PTE mimetic hotspots for the rapid degradation of nerve agents. We observed that the hydrolytic effect of the nanomaterial is due to the synergistic activity between both Ce3+ and Ce4+ ions located in the active site‐like hotspots. Furthermore, the catalysis by nanoceria overcomes the product inhibition generally observed for PTE and small molecule‐based PTE mimetics. 相似文献
Small‐molecule‐based fluorescent probes have become important tools in biology for sensing and imaging applications. However, the biological applications of many of the fluorescent molecules are hampered by low cellular uptake and high toxicity. In this paper, we show for the first time that the introduction of halogen atoms enhances the cellular uptake of fluorescent molecules and the nature of halogen atoms plays a crucial role in the plasma membrane transport in mammalian cells. The remarkably higher uptake of iodinated compounds compared to that of their chloro or bromo analogues suggests that the strong halogen bonding ability of iodine atoms may play an important role in the membrane transport. This study provides a novel strategy for the transport of fluorescent molecules across the plasma membrane in living cells. 相似文献