Reported herein is the rhodium(III)‐catalyzed C−H activation of anilines bearing an N‐isoquinolyl directing group for oxidative 3+2 annulation with four classes of internal alkynes, leading to ...atroposelective indole synthesis via dynamic kinetic annulation with C‐N reductive elimination constituting the stereo‐determining step. This reaction proceeds under mild conditions with high regio‐ and enantioselectivity and functional group compatibility.
C−H activation of N‐isoquinolylanilines catalyzed by chiral rhodium(III) cyclopentadienyls has been realized in 3+2 annulation with four classes of internal alkynes under mild oxidative condition and allowed the atroposelective synthesis of biaryl indoles in high regio‐ and enantioselectivity (>50 examples, 71–96 % ee).
Neural stem cells (NSCs), capable of ischemia‐homing, regeneration, and differentiation, exert strong therapeutic potentials in treating ischemic stroke, but the curative effect is limited in the ...harsh microenvironment of ischemic regions rich in reactive oxygen species (ROS). Gene transfection to make NSCs overexpress brain‐derived neurotrophic factor (BDNF) can enhance their therapeutic efficacy; however, viral vectors must be used because current nonviral vectors are unable to efficiently transfect NSCs. The first polymeric vector, ROS‐responsive charge‐reversal poly(2‐acryloyl)ethyl(p‐boronic acid benzyl)diethylammonium bromide (B‐PDEA), is shown here, that mediates efficient gene transfection of NSCs and greatly enhances their therapeutics in ischemic stroke treatment. The cationic B‐PDEA/DNA polyplexes can effectively transfect NSCs; in the cytosol, the B‐PDEA is oxidized by intracellular ROS into negatively charged polyacrylic acid, quickly releasing the BDNF plasmids for efficient transcription and secreting a high level of BDNF. After i.v. injection in ischemic stroke mice, the transfected NSCs (BDNF‐NSCs) can home to ischemic regions as efficiently as the pristine NSCs but more efficiently produce BDNF, leading to significantly augmented BDNF levels, which in turn enhances the mouse survival rate to 60%, from 0% (nontreated mice) or ≈20% (NSC‐treated mice), and enables more rapid and superior functional reconstruction.
The first nonviral gene carrier, reactive‐oxygen‐species‐responsive charge‐reversal poly(2‐acryloyl)‐ethyl(p‐boronic acid benzyl)diethylammonium bromide (B‐PDEA), is shown to mediate efficient gene transfection to neural stem cells (NSCs). When BDNF gene plasmids are used, the transfected NSCs homing to the ischemic regions increase animal survival and reconstruct functions.
Wireless charging technology has become an important development trend in future electric vehicle (EV) power supply technology due to its safety, flexibility, and convenience. With its industrialized ...development, interoperability has become an essential technical link. The interoperability of wireless charging systems refers to the ability of output performance to meet specified indicators when different transmitter and receiver devices are matched. This study reviews the research status of the interoperability of EV wireless charging technology. First, the definition and composition of the interoperability of wireless charging systems are briefly given. Then, the article provides a review of standards about interoperability so far. The interoperability of various magnetic couplers and compensation topologies is also analyzed and summarized. After that, the paper reviews the existing interoperability evaluation methods. Finally, this work highlights the existing problems and challenges in current research of interoperability. We hope that this work will contribute to the further development of EV wireless charging technology.
Spectroscopic techniques, electrochemical methods, nanozymes, computer vision, and modified chromatographic techniques are the emerging techniques for determining the quality and safety parameters ...(e.g., physical, chemical, microbiological, and classified parameters, as well as inorganic and organic contaminants) of tea products (such as fresh tea leaves, commercial tea, tea beverage, tea powder, and tea bakery products) effectively. By simplifying the sample preparation, speeding up the detection process, reducing the interference of other substances contained in the sample, and improving the sensitivity and accuracy of the current standard techniques, the abovementioned emerging techniques achieve rapid, cost‐effective, and nondestructive or slightly destructive determination of tea products, with some of them providing real‐time detection results. Applying these emerging techniques in the whole industry of tea product processing, right from the picking of fresh tea leaves, fermentation of tea leaves, to the sensory evaluation of commercial tea, as well as developing portable devices for real‐time and on‐site determination of classified and safety parameters (e.g., the geographical origin, grade, and content of contaminants) will not only eliminate the strong dependence on professionals but also help mechanize the production of tea products, which deserves further research. Conducting a review on the application of spectroscopic techniques, electrochemical methods, nanozymes, computer vision, and modifications of chromatographic techniques for quality and safety determination of tea products may serve as guide for other types of foods and beverages, offering potential techniques for their detection and evaluation, which would promote the development of the food industry.
Carboxylation of easily available alkenes with CO2 is highly important to afford value‐added carboxylic acids. Although dicarboxylation of activated alkenes, especially 1,3‐dienes, has been widely ...investigated, the challenging dicarboxylation of unactivated 1,n‐dienes (n>3) with CO2 remains unexplored. Herein, we report the first dicarboxylation of unactivated skipped dienes with CO2 via electrochemistry, affording valuable dicarboxylic acids. Control experiments and DFT calculations support the single electron transfer (SET) reduction of CO2 to its radical anion, which is followed by sluggish radical addition to unactivated alkenes, SET reduction of unstabilized alkyl radicals to carbanions and nucleophilic attack on CO2 to give desired products. This reaction features mild reaction conditions, broad substrate scope, facile derivations of products and promising application in polymer chemistry.
A powerful electrochemical protocol that enables the first dicarboxylation of unactivated skipped dienes with CO2 is reported. Various valuable tethered adipic acids are formed in moderate‐to‐good yields under mild conditions, showing great potential in synthetic, medicinal and polymer chemistry.
The coronavirus disease (COVID-19) caused by the novel severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has now spread to >200 countries posing a global public health concern. Patients ...with comorbidity, such as hypertension suffer more severe infection with elevated mortality. The development of effective antiviral drugs is in urgent need to treat COVID-19 patients. Here, we report that calcium channel blockers (CCBs), a type of antihypertensive drug that is widely used in clinics, inhibited the post-entry replication events of SARS-CoV-2 in vitro, while no in vitro anti-SARS-CoV-2 effect was observed for the two other major types of antihypertensive drugs, namely, angiotensin-converting enzyme inhibitors and angiotensin II receptor blockers. CCB combined with chloroquine showed a significantly enhanced anti-SARS-CoV-2 efficacy. A retrospective clinical investigation on hospitalized COVID-19 patients with hypertension as the only comorbidity revealed that the CCB amlodipine besylate therapy was associated with a decreased case fatality rate. The results from this study suggest that CCB administration to COVID-19 patients with hypertension as the comorbidity might improve the disease outcome.
Parkinson's disease (PD) is a common neurodegenerative disorder associated with striatal dopaminergic neuronal loss in the Substantia nigra. Oxidative stress plays a significant role in several ...neurodegenerative diseases. Paraquat (PQ) is considered a potential neurotoxin that affects the brain leading to the death of dopaminergic neurons mimicking the PD phenotype. Various scientific reports have proven that cryptotanshinone possesses antioxidant and anti‐inflammatory properties. We hypothesized that cryptotanshinone could extend its neuroprotective activity by exerting antioxidant effects. This study was designed to evaluate the effects of cryptotanshinone in both cellular and animal models of PQ‐induced PD. Annexin V‐PI double staining and immunoblotting were used to detect apoptosis and oxidative stress proteins, respectively. Reactive oxygen species kits were used to evaluate oxidative stress in cells. For in vivo studies, 18 B6 mice were divided into three groups. The rotarod data revealed the motor function and immunostaining showed the survival of TH+ neurons in SNpc region. Our study showed that cryptotanshinone attenuated paraquat‐induced oxidative stress by upregulating anti‐oxidant markers in vitro, and restored behavioral deficits and survival of dopaminergic neurons in vivo, demonstrating its therapeutic potential.
Selenium is an essential micronutrient element. For the extremely biotoxic of selenite, Selenium nanoparticles (SeNPs) is gaining increasing interest. In this work, a selenium-enriched strain with ...highly selenite-resistant (up to 173 mmol/L) was isolated from the local specialty food of longevity area and identified as Paenibacillus motobuensis (P. motobuensis) LY5201. Most of the SeNPs were accumulated extracellular. SeNPs were around spherical with a diameter of approximately 100 nm. The X-ray photoelectron spectroscopy and Fourier transform infrared spectroscopy showed that the purified SeNPs consisted of selenium and proteins. Our results suggested that P. motobuensis LY5201could be a suitable and robust biocatalyst for SeNPs synthesis. In addition, the cytotoxicity effect and the anti-invasive activity of SeNPs on the HepG2 showed an inhibitory effect on HepG2, indicating that SeNPs could be used as a potential anticancer drug.
Contrast-induced acute kidney injury (CIAKI) is a leading cause of acute kidney injury following radiographic procedures. Intrarenal oxidative stress plays a critical role in CIAKI. Nicotinamide ...adenine dinucleotide 3-phosphate (NADPH) oxidases (Noxs) are important sources of reactive oxygen species (ROS). Among the various types of Noxs, Nox4 is expressed predominantly in the kidney in rodents. Here, we evaluated the role of Nox4 and benefit of Nox4 inhibition on CIAKI using in vivo and in vitro models. HK-2 cells were treated with iohexol, with or without Nox4 knockdown, or the most specific Nox1/4 inhibitor (GKT137831). Effects of Nox4 inhibition on CIAKI mice were examined. Expression of Nox4 in HK-2 cells was significantly increased following iohexol exposure. Silencing of Nox4 rescued the production of ROS, downregulated pro-inflammatory markers (particularly phospho-p38) implicated in CIAKI, and reduced Bax and caspase 3/7 activity, which resulted in increased cellular survival in iohexol-treated HK-2 cells. Pretreatment with GKT137831 replicated these effects by decreasing levels of phospho-p38. In a CIAKI mouse model, even though the improvement of plasma blood urea nitrogen was unclear, pretreatment with GKT137831 resulted in preserved structure, reduced expression of 8-hydroxy-2'-deoxyguanosine (8OHdG) and kidney injury molecule-1 (KIM-1), and reduced number of TUNEL (terminal deoxynucleotidyl transferase dUTP nick end labeling)-positive cells. These results suggest Nox4 as a key source of reactive oxygen species responsible for CIAKI and provide a novel potential option for prevention of CIAKI.
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