Latest ArticlesPresent research on the antimalarial mechanisms of artemisinin (ART) is mainly focused on covalent drug binding targets alkylated by free radicals, while non-covalent binding targets have rarely been reported. Here, we developed a novel photoaffinity probe of ART to globally capture and identify the antimalarial target proteins of ART through chemical proteomics. The results demonstrated that ART can bind to parasite proteins by both covalent and non-covalent modification, and these may jointly contribute to the antimalarial effects. Our work enriches the research on the antimalarial targets of ART, and provides a new perspective for further exploring the antimalarial mechanism of ART.
Following our previous work on human immunodeficiency virus-1 (HIV-1) non-nucleoside reverse transcriptase inhibitors (NNRTIs), a series of novel biphenyl-pyridone derivatives were synthesized and evaluated for their anti-HIV-1 activity to expand their structure–activity relationship. Some of them exhibited low nanomolar activity toward wild-type HIV-1 and clinically relevant single/double mutant strains. The most active compound B1 was 231-fold more potent (EC50 = 17 nmol/L) than the lead compound 2 (EC50 = 3.93 µmol/L) against wild-type (WT) HIV-1. This compound was approximately 3.5-fold less cytotoxic (CC50 = 100.58 µmol/L) than compound 2 (CC50 = 28.24 µmol/L), presenting a higher selectivity index (SI) value of 5923. Compared with 2, the antiviral potency of B1 was significantly increased against five single mutant strains (L100I, K103N, E138K, Y181C and Y188L) and two double mutant strains (F227L+V106A and K103N+Y181C). Especially, K103N, Y181C and K103N+Y181C were more sensitive to B1 than both 2 and doravirine. Besides, the enzymatic inhibitory activity of B1 against wild-type HIV-1 reverse transcriptase was approximately 32-fold higher (IC50 = 100 nmol/L) than 2 (IC50 = 3.21 µmol/L). Molecular docking studies and dynamic simulations were conducted to explain their potent activity. Taken together, this research represents an important step toward the discovery of novel biphenyl-pyridone drug candidates for HIV therapy.
Carbon is a promising capacitive electrode material for Zn-ion hybrid supercapacitors (ZHSCs), as it is low-cost, environmentally friendly, controllable and adjustable. By now, achieving both high energy and high power with carbon electrodes is still challenging, limited by their intrinsic properties. In this work, we have designed and presented an amorphous hollow carbon bowl material with surface chemical modifications of oxygen groups to figure out these concerns. The preparation of bowl-like structures and the storage behavior between Zn2+ and oxygen functional groups have also been discussed. With the contributions from its unique hollow structure and surface functional groups, it can significantly enhance the electrode pseudocapacitance and the entire electrochemical performance.
There are some critical issues hindering the practical applications of aqueous zinc-ion batteries (ZIBs), although they possess high safety and low cost as one of promising energy storge devices, such as the Zn dendrite growth and the by-product of Zn4SO4(OH)6·xH2O (ZHS) resulted from some side reactions in a mild electrolyte. Herein, a compact and self-repairing solid electrolyte interface (SEI) film, as labeled the PVDF-Zn(TFSI)2-ZHS coating [The PVDF and Zn(TFSI)2 are polyvinylidene fluoride and zinc bis(trifluoromethanesulfonyl)imide, respectively], which turns the in-situ generated ZHS into a beneficial ingredient onto the pre-coated PVDF-based composite coating layer containing Zn(TFSI)2, was designed and fabricated by a simple doctor blade method. It is shown that the SEI layer can effectively isolate Zn from the electrolyte and homogenize the Zn2+ flux, and thus effectively suppress side reactions and dendrites growth. Benefiting from the hybrid SEI layer, a symmetric cell exhibits a high cycling stability over 750 h at 2.0 mA/cm2 and 2.0 mAh/cm2, and meanwhile, a full-cell, coupled with K+ pre-intercalation α-MnO2 (KMO) cathode, displays excellent rate performance, stable coulombic efficiency and an acceptable cycle life. This work provides a feasible approach for simple and scalable modification of Zn anodes to achieve high performance.
Aging-related diseases are gradually becoming a major problem with the rapid development of aged population in human society. Although many fluorescent probes have been employed to diagnosis senescence via imaging senescence-associated β-galactosidase (SA-β-Gal), which is proved to be closely associated with senescent cells, the similar catalytic effectiveness of enzymatic reaction of ovarian cancer-associated β-Gal (OA-β-Gal) will interfere with imaging accuracy. Herein, a near-infrared (NIR) hemicyanine based fluorescent probe HCyXA-βGal was designed for light-up imaging of live cells containing β-Gal. With the organelle-targeting morpholinyl and positive charge moieties, HCyXA-βGal was successfully applicated to image the difference of enzymatic location in senescent cells and ovarian cancer cells. Furthermore, inspired by the fast response performance, fast and precise imaging of the two cell lines was realized via covering another dimension of fluorescence signal: time-dependent intensity.
Three isomorphic polytungstates, Cs9K18H10{[Sm2(H2O)4W4O10(AsW9O33)3]2(N(CH2PO3)2)}·46.5H2O (1), Cs10K9H18{[Eu2(H2O)4W4O10(AsW9O33)3]2(N(CH2PO3)2)}·41.5H2O (2), Cs10K9H18{[Gd2(H2O)4W4O10 (AsW9O33)3]2(N(CH2PO3)2)}·46H2O (3), have been successfully synthesized and characterized by routine methods, and demonstrated excellent catalytic activities in Knoevenagel condensation reaction as heterogeneous catalysts. Notably, catalyst 1 achieved higher reaction activity than catalysts 2 and 3, where a satisfactory reaction yield (95%) and high TON value (6380) could be obtained at moderate reaction condition. In addition, in the scale-up experiment, with the help of catalyst 1, 7.8 g benzaldehyde and 5.7 g ethyl cyanoacetate could transform into corresponding condensation product with a satisfactory yield (83%) and impressive TON value (13,883).
Researchers engrossed in enantioseparation keep seeking for versatile chiral separation selectors. This work proposes a concept of quasi-dual-chiral-channel (QDCC) enantioseparation platform, where the surface sequentially grafted quinine (QN) and functional cyclodextrin (CD) can imitate two independent chiral channels without mutual interference to achieve wide spectrum chiral resolution. Chiral separation results combined with molecular docking simulation indicates that the different interaction mode of QN and functional CD layer renders QDCC the wide separation capability. This work provides a valuable insight into the rational design of versatile enantioseparation materials.
Bacterial infection of wounds is an escalating medical problem, issuing threats to both global public health and personal health. Photothermal antibacterial technology as a novel sterilization strategy has outstanding sterilization efficiency, high safety and low risk of emergence of drug-resistant bacteria. By combining inherent antibacterial activity and light-assisted antibacterial treatment, developing novel multifunctional dressings with synergistic high-efficiency antibacterial effects and also promoting wound healing possesses attractive advantages in the field of treating bacterial wound infections in clinical care. Herein, a multifunctional hydrogel formed by in situ photo-cross linking was designed and prepared by first grafting methacrylic anhydride as a photosensitizer onto chitosan, and then introducing oxidatively synthesized polydopamine (PDA). The physicochemical characterizations of the synthesized hydrogels demonstrated their tunability certainly associated with PDA concentration, including pore size, water swelling, rheological properties and in vitro degradability. In addition, the composite hydrogels exhibited good adhesion, anti-oxidation and photothermal properties due to the existence of PDA. Within 10 min upon exposure to 808 nm near-infrared (NIR) light irradiation, this hydrogel system displayed outstanding antibacterial activity against Staphylococcus aureus with almost 100% killing efficiency, of which rapid efficient sterilization plays a significant role in wound healing. Moreover, the hydrogel is capable of cytocompatibility and has low toxicity to murine fibroblasts (L929 and NIH/3T3). In the full-thickness wound defect infection model in mice, the wound closure ratio, inflammatory response, fibroblasts, neovascularization and epithelialization were measured. Animal experiments also reveal that the hydrogel assisted with NIR laser irradiation can inhibit effectively infection at an early stage and accelerate the wound healing process. In summary, this novel multifunctional injectable hydrogel exhibits excellent swelling capacity, bio-adhesion, antioxidant property, photothermal activity, efficient antibacterial property and facilitates skin healing, which has great promising application as a medical dressing biomaterial in infected wound care fields.
The trade-off between mass-loading and cycling stability is always a big challenge for iron oxide-based electrodes. Herein, α-Fe2O3 nanoparticles uniformly anchored on nitrogen-doped wood carbons with high mass-loading have been synthesized via a facile electrodeposition method accompanied by post-heating treatment. The resultant composite delivers a high specific capacitance of 603 F/g at 0.1 A/g and superior capacitance retention of 85.5% after 10,000 cycles at 10 A/g, indicating excellent long-term cycling stability. Such excellent electrochemical performance can be attributed to the synergistic effects of α-Fe2O3 nanoparticles and the conductive matrix as well as the formation of interfacial Fe-O-C bonding, which enables the composite electrode to provide plenty of accessible redox active sites, sufficient electron transport and electrolyte ions diffusion, and robust interfacial interaction. Consequently, the asymmetrical supercapacitor exhibits a high energy density of 30.3 Wh/kg at 125 W/kg, suggesting its great potential for practical applications.
The deterioration of water caused by industrial production is a thorny problem. Solving the problem cogently through innovative coagulationstrategies has been recognized of important practical significance. In this work, a simple enhanced coagulation by using ferric chloride (FC) and poly-ferric chloride (PFC) coupled with polyamidine (PA) were tried to remove the toxic organics. The results shown that PA addition could obviously enhance coagulation performances of the iron-based coagulants. The synergic coagulation process and mechanism were studied and discussed in detail based on the coagulation behaviors, flocs properties, removal efficiency and zeta potentials. FC and PFC remove organics mainly through charge neutralization and adsorption-bridging, resulting in a good purification performance. While PA with a higher charge density showed better purification performance due to enhanced charge neutralization. It is worth mentioning that the addition of PA could make the coagulants adapt to a wider pH range, and remove the toxic organics more effectively. That is to say, the practical adaptability of the coagulant was enhanced. This work thus provides a simple strategy to effectively purify wastewater and further improve the water safety.
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