Latest ArticlesMultifunctional molecules with both optical signal and pharmacological activity play an important role in drug development, disease diagnosis, and basic theoretical research. Aminopeptidase N (APN), as a representative tumor biomarker with anti-tumor potential, still lacks a high-precision theranostic probe specifically targeting it. In this study, a novel quaternity design strategy for APN theranostic probe was developed. This proposed strategy utilizes advanced machine learning and molecular dynamics simulations, and cleverly employs the strategy of conformation-induced fluorescence recovery to achieve multi-objective optimization and integration of functional fragments. Through this strategy, a unique "Off–On" theranostic probe, ABTP-DPTB, was ingeniously constructed to light up APN through fluorescence restoration, relying on conformation-induced effects and solvent restriction. Differ from the common diagnostic probes, the intelligent design with non-substrated linkage makes ABTP-DPTB for long-term in-situ imaging. The fabricated probe was used for detecting and inhibiting APN in various environments, with a better in vitro inhibitory than golden-standard drug bestatin.
Bridged polycyclic lactams are important structural units in organic functional materials, natural products, and pharmaceuticals. A flexible and efficient anion cascade reaction was developed for the preparation of bridged polycyclic lactams from readily available malonamides and 1, 4-dien-3-ones. Various highly substituted bridged polycyclic lactams were synthesized in good to excellent yields by tandem nucleophilic sequences in the presence of BuOK in commercially available EtOH solvent at 60 ℃. Notably, the simple reactions can be run on a gram scale. Mechanistically, bis-Michael addition reaction and hemiaminalization reactions are involved in the tandem transformation.
An additive-free and environmentally friendly strategy has been realized for the construction of S-substituted isothioureas through visible-light-induced multicomponent reaction starting from α-diazoesters, aryl isothiocyanates, amines and cyclic ethers. This methodology features simple operation, mild reaction conditions, favorable functional group tolerance, easily available starting materials and high efficiency.
Nasopharyngeal carcinoma (NPC), a malignant tumor originating from the nasopharynx, is one of the common malignant tumors of the head and neck. There are significant geographical differences in the incidence of nasopharyngeal carcinoma, with a high incidence in China and Southeast Asian countries. Herein, we designed and synthesized a novel near-infrared fluorescent (NIRF) probe to detect glutathione (GSH) in cellular and tumor environments using semi-naphthofluorescein (SNAFL) as the fluorescent molecular backbone and 2-fluoro-4-nitrobenzenesulfonate as the recognition moiety. Upon reaction with GSH, SNAFL-GSH emitted a fluorescence signal, and its emission wavelength at 650 nm was remarkably enhanced. The results of selectivity experiments indicated that SNAFL-GSH was able to discriminate GSH from Cys, Hcy, and H2S. Moreover, SNAFL-GSH could image both endogenous and exogenous GSH and distinguish normal and cancer cells by fluorescence signal difference. At the cellular level, cisplatin (DDP)-induced ferroptosis and inhibition of proliferation of various NPC cell lines (CNE2, CNE1, 5–8F cells) by erastin combined with DDP were visualized with the help of SNAFL-GSH. In a mouse tumor xenograft model, we successfully employed SNAFL-GSH for the evaluation of the efficacy of erastin combined with DDP in the treatment of NPC. More importantly, the probe could image cancerous tissue sections from NPC patients with an imaging depth of approximately 80 µm. It was foreseen that SNAFL-GSH offered great potential for application in the diagnosis and evaluation of the therapeutic efficacy of NPC, and these results would also provide new ideas for the clinical treatment of NPC.
Nanoemulsions are widely used as advanced pharmaceutical delivery systems in biomedical field, due to their high encapsulation efficiency and good therapy efficacy. Nanoemulsification techniques that produce nanoemulsions with controllable sizes and compositions are promising for creating advanced nanoemulsion systems for pharmaceutical delivery. This review summarizes recent advances on low-energy emulsification techniques for producing nanoemulsions, and the use of these nanoemulsions as advanced pharmaceutical delivery systems and as templates to create drug-loaded functional particles for biomedical application. First, nanoemulsification techniques that utilize elaborate interfacial physics/chemistry and micro-/nano-fluidics, featured with relatively-low energy input, to produce nanoemulsions with controllable sizes and compositions, are introduced. Uses of these nanoemulsions to create nanoemulsion-incorporated milli-particles, drug-loaded nanoparticles and nanoparticle-incorporated microparticles with sizes ranging from several millimeters to sub-10 nm are emphasized. Flexible and efficient use of the nanoemulsions, functional nanoparticles and milli-/micro-particles integrated with nanoemulsions or nanoparticles for advanced pharmaceutical delivery in biomedical field are highlighted, with focus on how the interplay between their sizes and compositions achieve desired pharmaceutical-delivery performances. Finally, perspectives on further advances on the controllable production of nanoemulsions are provided.
The efficiency of photocatalytic CO2 reduction reaction (PCRR) is restricted by the low solubility and mobility of CO2 in water, poor CO2 adsorption capacity of catalyst, and competition with hydrogen evolution reaction (HER). Recently, hydrophobic modification of the catalyst surface has been proposed as a potential solution to induce the formation of triple-phase contact points (TPCPs) of CO2 (gas phase), H2O (liquid phase), and catalysts (solid phase) near the surface of the catalyst, enabling direct delivery of highly concentrated CO2 molecules to the active reaction sites, resulting in higher CO2 and lower H+ surface concentrations. The TPCPs thus act as the ideal reaction points with enhanced PCRR and suppressed HER. However, the initial synthesis of triple-phase photocatalysts tends to possess a lower bulk density of TPCPs due to the simple structure leading to limited active points and CO2 adsorption sites. Here, based on constructing a hydrophobic hierarchical porous TiO2 (o-HPT) with interconnected macropores and mesopores structure, we have significantly increased the density of TPCPs in a unit volume of the photocatalyst. Compared with hydrophobic macroporous TiO2 (o-MacPT) or mesoporous TiO2 (o-MesPT), the o-HPT with increased TPCP density leads to enhanced photoactivity, enabling a high methanol production rate with 1111.5 µmol g−1 h−1 from PCRR. These results emphasize the significance of high-density TPCPs design and propose a potential path for developing efficient PCRR systems.
In recent years, with the emergence of non-fullerene fused-ring acceptors, power conversion efficiencies (PCEs) of organic solar cells (OSCs) have exceeded 19%. However, compared to inorganic or perovskite photovoltaic cells, a higher voltage loss has become one of the key factors limiting further improvement in the PCEs of OSCs. The ternary/quaternary strategy has been identified as a feasible and effective way to obtain high-efficiency OSCs. In this review, a brief outline is given of the key roles that guest materials played in reducing voltage losses in solar cell devices and a brief look at the future material design and the design of ternary/quaternary systems.
Due to their excellent fluorescence properties and biological function, cyanine dyes have been widely applied in biological imaging. Heptamethine cyanine (Cy7) dyes, as a type of classic near-infrared (NIR) fluorescent dyes, are considered as one of the effective fluorescent tools in the living organisms due to their good biocompatibility and very low background interference. Bioorthogonal reactions performed in living cells and tissues have developed by leaps and bounds in recent years. The NIR fluorescent labeling technique involving cyanine has attracted widespread attention. This review summarizes their recent application in the field of bioorthogonal imaging, mainly concluding Cy7-type dyes, labeling strategy, bioimaging application, etc. We expect this work can provide some helps for the studies of NIR bioorthogonal reaction in vivo.
Organofluorine compounds are widely used in the realm of drug discovery and material science. Herein, we developed palladium catalyzed intermolecular aminofluorination and oxy-aminofluorination of gem-difluoroalkenes with N-fluorobenzenesulfonimide (NFSI), in which NFSI was used as the nitrogen source and oxidant. The reaction provides an efficient and straightforward synthesis route of a series of α-trifluoromethyl benzylic amines. Notably, three/four components oxy-aminofluorination processes were realized to give α-trifluoromethyl benzylic ether with a terminal amino group, which proceed through C(sp3)–O bond cleavage of easily available ether and simultaneous introduced a fluorine, an amino and an oxy substituent in one pot with excellent regioselectivity. The divergent reactivity not only included the incorporation of one ether molecular, but also much more challenged two ether insertion with excellent selectivity through succession C(sp3)–O bonds cleavage. This protocol allows for concise synthesis of high value amines with fluoroalkyl-substituents and selectively transformation of easily available ethers by high-valent palladium catalysis.
The cubic S/N co-doped TiO2 (TNSx, x is the calcination temperature) photocatalysts with rich oxygen vacancies were obtained by high temperature calcination of sulfur powder and titanium-based MOFs NH2-MIL-125 for the photocatalytic removal of gaseous formaldehyde (a volatile organic compound). Among the obtained catalysts, the presence of oxygen vacancies restricted photogenerated electron and holes recombination. 98.00% removal of gaseous formaldehyde in 150 min could be achieved over TNS600 by xenon lamp. The removal efficiency for formaldehyde was well retained for five cycle experiment. The results from PL, TRPL and EIS revealed that TNS600 had the best separation efficiency of photogenerated electrons and holes, and the enhanced charge separation led to a significant increase in photocatalytic activity. The photocatalytic oxidation mechanism indicated that the •OH and •O2− radicals were mainly involved in the efficient elimination of gaseous formaldehyde and were able to mineralize formaldehyde to H2O and CO2.
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