Latest ArticlesTumor penetration is important for effectively tumor targeting drug delivery. Recently, many researches are published to overcome the barriers that restrict tumor penetration and improve drug delivery efficiency. In the mini review, we first analyzed the barriers influence the tumor penetration, including tumor microenvironment barriers, nanoparticle properties, and interaction barriers between tumor and nanoparticles. To overcome the barrier, several strategies are developed, including modulating tumor microenvironment, changing particle size, transcytosis enabled tumor penetration, cell penetrating peptide modification and overcoming binding site barrier, which could effectively improve tumor penetration, and finally enhance tumor treatment outcome.
Chemodivergent reactions of 2, 2-dimethoxyacetaldehyde and anilines were described, which were established on the basis of either a CC bond cleavage or a rearrangement process of a reaction intermediate. These reactions proceeded in a condition-determined manner with good functional group tolerance. In the first model, 2, 2-dimethoxyacetaldehyde reacted with aniline to form a new CN bond, in the presence of O2, via a CC bond cleavage reaction. However, in the second model, by performing the reaction in the absence of O2, Heyns rearrangement occurred and generated a new CO bond to form methyl phenylglycinate. Such condition-determined reactions not only offered the new way for value-added conversion of biomass-derived platform molecule, 2, 2-dimethoxyacetaldehyde, but also provided efficient methods for the synthesis of N-arylformamides and methyl phenylglycinates.
The precise and real-time sensing of the temperature within the physiological range is of great significance in biology and medicine. Here, a Zn-based metal-organic framework (MOF) named Zn-TCOMA is synthesized with good SHG performance due to its unique structure of the ligand and 3D frameworks. By encapsulating the two-photon fluorescent dye DMASE into the pores of Zn-TCOMA, the composite Zn-TCOMA⊃DMASE is obtained and simultaneously exhibits SHG response and two-photon fluorescence. Utilizing the intensity ratio between two-photon fluorescence of DMASE and SHG signal of Zn-TCOMA, Zn-TCOMA⊃DMASE exhibits ratiometric temperature sensing property at physiological temperature region of 20~60 ℃ with high sensitivity. This MOF thermometer also shows excellent repeatability, good biocompatibility, and high temperature resolution of 0.018 ℃, opening a new avenue to develop diverse optical thermometric or thermographic applications in biotechnology or other areas.
Surface-enhanced Raman scattering (SERS) is a powerful spectroscopic tool in quantitative analysis of molecules, where the substrate plays a critical role in determining the detection performance. Herein, a silver nanocubes/polyelectrolyte/gold film sandwich structure was prepared as a reproducible, high-performance SERS substrate by the water/oil interfacial assembly method. In addition to the hot spots on the nanocubes surface, the edge-to-edge interspace of the Ag nanocubes led to marked enhancement of the SERS intensity, with a limit of detection of 10-11 mol/L and limit of quantitation of 10-10 mol/L for crystal violet. When rhodamine 6G and crystal violet were co-adsorbed on the Ag nanocube surfaces, the characteristic SERS peaks of the two molecules remained well resolved and separated, and the peak intensities varied with the respective concentration, which could be exploited for concurrent detection of dual molecules. Results from this work indicate that organized ensembles of Ag nanocubes can serve as effective SERS substrate can for sensitive analysis for complex molecular systems.
We describe an application of carrier protein-free strategy in constructing a fully synthetic methamphetamine (METH) vaccine that contains three components: Toll-like receptor 2 ligand, Th2 epitope, and METH hapten. The immunological evaluation in mice revealed high titers of METH-specific antibodies induced by the construct and the activation of humoral immunity that would be beneficial for neutralization and clearance of the METH molecule. Behavioral experiments indicated that the synthetic vaccine attenuated the acquisition of METH-induced conditioned place preference and inhibited the initiation and expression of METH-induced locomotor sensitization. These results demonstrate that the lipopeptide-based vaccine has invoked an immune response and showed the potential of preventing the rewarding and psychoactive effects of METH.
To search naturally occurring interleukin-1β (IL-1β) inhibitors, biscaesalmins A (1) and B (2), two highly oxidized dimeric cassane diterpenoids with a newly formed alicyclic skeleton, have been isolated from the traditional Chinese medicine Kushilian (Caesalpinia minax). Their full structures were determined by comprehensive spectroscopic analysis and quantum chemical TD-DFT (time-dependent density functional theory) calculation. Biosynthetically, 1 and 2 were formed via an intermolecular [4+2] Diels-Alder cycloaddition of two monomers, affording an additional six-membered carbon ring linkage. Compounds 1 and 2 inhibited nitric oxide production on lipopolysaccharide-stimulated THP-1 macrophages, with IC50 values being at 1.20±0.23 and 2.30±0.15 μmol/L, respectively. Furthermore, compound 1 inhibited NLRP3 (NOD-, LRR- and pyrin domain-containing protein 3) inflammasome-mediated IL-1β production and blocked the migration of macrophages towards adipocyte conditioned medium. Biscaesalmins A and B might be candidates for treating inflammation-related metabolic diseases.
Mercury ions are highly toxic and can accumulate along food chains in water, soil, crops and animals. Effective detection of mercury ions in various media is of great significance for maintaining the ecological environment and protecting people's health. In this work, a mercury ions specific fluorescent probe was developed by a simple one-step reaction of commercial substrates of 4-chloro-7-nitro-2, 1, 3-benzoxadiazole and 1-(2-aminoethyl)-4-methylpiperazine. Investigation on sensing behavior showed that this probe had high sensitivity and selectivity towards mercury ions. Furthermore, this probe could be used as a tool to track the level of mercury ions in living system. In living cells, the probe with green emission emitted a bright red fluorescence when it was bound to mercury ions. In Arabidopsis thaliana, similar red emission could be detected from the root tip and stalk when A. thaliana was grown in culture medium containing mercury ions. The imaging in zebrafish showed that mercury ions were mainly concentrated in the stomach and head of zebrafish. Especially, this probe could be applied in quantitative analysis of mercury ions in tap water, green tea, sea shrimp and soil. This work provided a practical tool for the detection of mercury ions in living systems and quantitative analysis in real samples.
TiO2 photocatalysts have been widely studied and applied for removing bacteria, but its antibacterial efficiency is limited to the ultraviolet (UV) range of the solar spectrum. In this work, we use the gold (Au) nanorods to enhance the visible and near-infrared (NIR) light absorption of TiO2 NBs, a typical UV light photocatalyst, thus the enhancement of its full solar spectrum (UV, visible and NIR) photocatalytic antibacterial properties is achieved. Preliminary surface plasmon resonance (SPR) enhancement photocatalytic antibacterial mechanism is suggested. On one hand, transverse and longitudinal SPR of Au NRs is beneficial for visible and NIR light utilization. On the other hand, Au NRs combined with TiO2 NBs to form the heterostructure, which can improve the photogenerated carrier separation and direct electron transfer increases the hot electron concentration while Au NRs as the electron channel can well restrain charge recombination, finally produces the high yield of radical oxygen species and exhibits a superior antibacterial efficiency. Furthermore, we design a sterilization file cabinet with Au NR/TiO2 NB heterostructures as the photocatalytic coating plates. Our study reveals that Au NR/TiO2 NB heterostructure is a potential candidate for sterilization of bacteria and archives protection.
An interlocked M4L8 coordination cage was synthesized by coordination-driven self-assembly of palladium(Ⅱ) ions with aromatic amide bidentate ligands. The reaction of the ligand and the metal at 2:1 ratio led to the monomeric M2L4 cage as the kinetic product, while the thermodynamic product M4L8 cage was obtained by prolongating the reaction. This conversion and the interlocked structure was clearly revealed by using 1H NMR, mass spectrometry and X-ray crystallography. The driving force of interlocking was mainly attributed to the interactions (hydrogen bonding, aromatic stacking and electrostatic interaction) arising from the aptitude of flexibility of the amide ligand.
A purely organic D-π-A-π-D type emitter showing thermally activated delayed fluorescence (TADF) and room temperature phosphorescence (RTP) was designed and synthesized by utilizing the benzophenone as an acceptor and the N-phenyl-2-napthylamine as a donor moiety. It exhibits considerable TADF character in doped PMMA film and room temperature phosphorescence with a long lifetime of 74 ms at 466 nm in solid state. The devices with the configuration of ITO/Mo2O3 (4 nm)/mCP (30 nm)/mCP: x wt% NP2BP/TmTyPB (60 nm)/LiF (1.5 nm)/Al (100 nm) were prepared by vacuum evaporation to explore their electroluminescent performance. Interestingly, the non-doped device has obtained near-white emission with a fluorescence emission peak at 475 nm and a phosphorescence emission peak at 563 nm having the CIE coordinate of (0.23, 0.32) and the maximum external quantum efficiency of 1.09%.
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