Latest ArticlesNonfullerene acceptors (NFAs), which usually possess symmetric skeletons, have drawn great attention in recent years due to their pronounced advantages over the fullerene counterparts. Moreover, breaking the symmetry of NFAs could fine tune the molecular dipole, solubility, energy level, intermolecular interaction, molecular packing, crystallinity, etc., and give rise to improved photovoltaic performance. Currently, there are three main strategies for the design of asymmetric NFAs. This review highlights the recent advances of high-performance asymmetric NFAs and briefly outlooks the materials exploration for the future.
Neglected tropical diseases (NTDs) refer to infectious diseases caused by multiple pathogens that are prevalent in hot, humid climates in tropical areas. With the global economic growth and the improvement of public health status, eliminating neglected tropical diseases will be of great significance to the healthy development of human beings. However, the number of drugs and vaccines for NTDs treatment is extremely limited, so it is urgent to develop new drugs. Since most NTDs are caused by parasites, this paper selected parasitic diseases with high morbidity and mortality, and focused on new effective therapeutic targets and excellent lead compounds for these diseases. Schistosomiasis, human African trypanosomiasis (HAT), Chagas disease, leishmaniasis, filariasis and toxoplasmosis correspond to a series targets such as smHDAC8, thioredoxin glutathione reductase (TGR), T. cruzi glucokinase (TcGlcK), phosphofructokinase (PFK), type IB topoisomerase, cell division cycle-2-related Kinase, sterolmethyl transferase, calumenin, dihydrofolate reductase (DHFR) and Toxoplasma gondii farnesyl-diphosphate synthase (TgFPPs). In this paper, the pharmacological effects of typical lead compounds corresponding to each disease, the structural characteristics of the mother nucleus and the pharmacological activities of the substituent. In addition, the binding patterns of some involved targets (such as smHDAC8) with corresponding lead compounds (such as compound 13) and the signaling pathways associated with gluconeogenesis, glycolysis, and pentose phosphate pathways are analyzed in detail. In this paper, the interaction mechanism between the lead compounds and the target were thoroughly discussed, in order to provide the research ideas of potential anti-parasite compounds, and further improve the understanding and prevention ability of such diseases of NTDs.
Catalyzed by cerium ammonium nitrate (CAN), the oxidative cracking reaction of alkenes occurred to produce carbonyls in good yields under mild conditions. The reaction employed molecular oxygen (O2) as the safe and clean oxidant. The catalyst dosage was reduced to as low as 0.5 mol%, while no additive was required. Thus, it may afford a generally green synthetic approach for introducing oxygen into organic molecules as well as the biomass degradation and the resource recycling from the C=C bond-containing waste polymers. X-ray photoelectron spectroscopy (XPS) analysis and control experiments demonstrated that the process proceeded via a single electron transfer (SET) reaction-initiated free radical reaction mechanism. In the process, both Ce and NO3− acted as the oxygen carrier to promote the oxidation reaction. The application of the abundantly existed nitrate in CAN was found to be the key for reducing the catalyst loading.
Parkinson's disease (PD) is a complex neurological disorder that typically worsens with age. A wide range of pathologies makes PD a very heterogeneous condition, and there are currently no reliable diagnostic tests for this disease. The application of metabolomics to the study of PD has the potential to identify disease biomarkers through the systematic evaluation of metabolites. In this study, urine metabolic profiles of 215 urine samples from 104 PD patients and 111 healthy individuals were assessed based on liquid chromatography-mass spectrometry. The urine metabolic profile was first evaluated with partial least-squares discriminant analysis, and then we integrated the metabolomic data with ensemble machine learning techniques using the voting strategy to achieve better predictive performance. A combination of 8-metabolite predictive panel performed well with an accuracy of over 90.7%. Compared to control subjects, PD patients had higher levels of 3-methoxytyramine, N-acetyl-l-tyrosine, orotic acid, uric acid, vanillic acid, and xanthine, and lower levels of 3, 3-dimethylglutaric acid and imidazolelactic acid in their urine. The multi-metabolite prediction model developed in this study can serve as an initial point for future clinical studies.
Uncontrolled microglial activation is decisively involved in the neuroinflammatory pathogenesis of brain diseases. Consequently, suppression of microglial overactivation appears to be a strategy for the prevention of nerve injury. In this paper, a novel vanadium complex, vanadyl N-(p-N,N-dimethylaminophenylcarbamoylmethyl)iminodiacetate (VO(p-dmada)), was synthesized from vanadyl sulfate and N,N-dimethyl-p-phenylenediamine, which was structurally characterized by Fourier transform infrared spectrum and ESI-MS analysis. The effect of VO(p-dmada) on neuroinflammation was investigated by using the models of lipopolysaccharide (LPS)-induced BV2 microglial cells and BALB/c mice. Our data demonstrated that VO(p-dmada) significantly suppressed microglial activation by downregulating inflammatory mediators and associated proteins, and inactivating nuclear factor-κB (NF-κB) signaling pathway. VO(p-dmada) also upregulated peroxisome proliferator activated receptor gamma (PPARγ) by reducing transglutaminase 2 and heat shock protein 60 expression. Co-treatment with PPARγ antagonist GW9662 significantly impeded the inhibitory effect of VO(p-dmada) on LPS-induced neuroinflammation. These cumulative findings demonstrated that VO(p-dmada) is a potential new drug for the treatment of neuroinflammation-related neurodegenerative diseases.
Mitochondria are essential for eukaryotic life as powerhouses for energy metabolism. Excessive mitochondrial hyperthermia and reactive oxygen species (ROS) production have been associated with aging, cancer, neurodegenerative diseases, and other disorders. Uncoupling protein 2 (UCP2) is the effector responsible for regulating cellular thermogenesis and ROS production via dissipating protons in an electrochemical gradient. A UCP2 inhibitor named genipin (GNP) is being researched for its effect on mitochondrial temperature, but little is known about its mechanisms. This study developed several molecular probes to explore the interactions between GNP and UCP2. The result indicated that the hemiacetal structure in GNP could selectively react with the ɛ-amine of lysine on the UCP2 proton leakage channel through ring-opening condensation at the mitochondrial, cellular, and animal levels. A notable feature of the reaction is its temperature sensitivity and ability to conjugate with UCP2 at high fever as lysine-specific covalent inhibitors that prevent mitochondrial thermogenesis. The result not only clarifies the existence of an antipyretic properties of GNP via its irreversible coupling to UCP2, but also reveals a bioorthogonal reaction of hemiacetal iridoid aglycone for selectively binding with the ɛ-amine of lysine on proteins.
Fe-NX/C electrocatalysts have aroused extensive interest in accelerating sluggish oxygen reduction reaction (ORR) kinetics as potential alternatives to platinum catalysts in rechargeable Zn-air batteries (ZABs). However, the low density and poor accessibility of Fe-NX sites have severely restricted the electrocatalytic performance of Fe-NX/C. Herein, Fe, N co-doped ordered mesoporous carbon fiber bundles are prepared through a ligand-assisted strategy with nitrogen-rich 1,10-phenanthroline as space isolation agent. 1,10-Phenanthroline reveals a six-membered heterocyclic structure containing abundant nitrogen species to tightly coordinate with Fe ions, which is conducive to achieving high-density Fe-NX sites. Meanwhile, the adoption of SBA-15 as hard-templates enables the catalysts with highly ordered channels and large specific surface areas, improving the accessibility of Fe-NX sites. The optimal catalyst (PDA-Fe-900) demonstrates a positive half-wave potential of 0.84 V (vs. RHE) in alkaline solution, outperforming the commercial Pt/C (0.83 V). In addition, PDA-Fe-900 delivers comparable ORR performance to commercial Pt/C in acidic electrolyte. Impressively, when PDA-Fe-900 is employed as an air cathode, it achieves large power densities of 163.0 mW/cm2 in liquid-state ZAB and 116.6 mW/cm2 in the flexible solid-state ZAB. This work provides an efficient ligand-assisted pathway for fabricating catalysts with dense and accessible Fe-NX sites as high-performance ORR electrocatalysts for ZABs.
The effective removal and selective detection of explosive and toxic pollutant trinitrophenol (TNP) is an attractive but challenging field. Herein, a double-cavity nor-seco-cucurbit[10]uril (ns-Q[10])-based supramolecular assembly 8-HQ@ns-Q[10] was fabricated and its structure was characterized by X-ray single crystal diffraction. In this assembly, the stoichiometric ratio of ns-Q[10] and 8-hydroxyquinoline (8-HQ) is 1:2, which is also attributed to the special double-cavity structure of ns-Q[10]. The luminescence sensing experiments showed that 8-HQ@ns-Q[10] can be used as a good fluorescence-enhanced sensing material (enhanced 27-fold) for the rapid detection of explosives and the aqueous contaminant TNP, with a limit of detection (LOD) of 2.07 × 10−5 mol/L, without interference from other phenolic compounds. Furthermore, TNP can be efficiently removed in the presence of assembly 8-HQ@ns-Q[10], and the removal efficiency is more than 89%. Therefore, the supramolecular assembly 8-HQ@ns-Q[10], as a fluorescence-enhanced luminescence sensor and adsorption material, has rich research value and potential application prospect when applied to the detection and removal of TNP in aqueous environment.
Glutathione depletion provides a promising strategy for the design of non-platinum anticancer drugs. Here we report a series of electrophilic (salen)osmium(Ⅵ) nitrides that react with glutathione to generate (salen)osmium(Ⅲ) ammine compounds. In vitro studies indicate that these osmium(Ⅵ) nitrides show comparable cytotoxicity to cisplatin against various carcinoma. Mechanistic studies with the representative compound [OsⅥ(N)(LH)(OH2)](PF6) (1, LH = N,N′-bis(salicylidene)-o-cyclohexyldiamine dianion) suggest that 1 induces glutathione depletion, reactive oxygen species generation, endoplasmic reticulum stress, and in turn triggers death receptor-mediated apoptosis and autophagy in lung cancer cells. In vivo evaluations show that 1 can inhibit tumor xenograft growth effectively with no body weight drop.
Peptide-drug conjugates (PDCs) composed of peptide, spacer and drug have gained extensive attention in the field of drug delivery owing to its precise control over the drug payload and architecture. However, the achievement of controllable and rapid drug release at targeted site by PDCs is still a great challenge for pharmaceutist. Herein, we introduced the histidine residue into PDCs to generate a supramolecular hydrogel via a pH-trigger strategy, which exhibited an autocatalytic effect to precisely tune drug release from PDCs hydrogel. Using indomethacin (Idm) as model drug, various PDCs (Y(Idm)EEH, Y(Idm)EEK and Y(Idm)EER) were synthesized and their self-assembling properties were investigated in terms of critical aggregation concentration (CAC), transmission electron microscopy (TEM) and rheometer. Introduction of histidine residue into PDCs presented a robust catalytic activity on the ester hydrolysis of p-nitrophenyl acetate in aqueous solution, as well conferred the autocatalytic capacity to hydrolyze the PDCs into active parent drug (Idm). Overall, we reported an autocatalytic activity of histidine residue to precisely tune drug release from PDCs hydrogels.
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