Latest ArticlesInhibition of foam cell formation is considered a promising treatment method for atherosclerosis, the leading cause of cardiovascular diseases worldwide. However, currently available therapeutic strategies have shown unsatisfactory clinical outcomes. Thus, herein, we design aloperine (ALO)-loaded and hyaluronic acid (HA)-modified palladium (Pd) octahedral nanozymes (Pd@HA/ALO) that can synergistically scavenge reactive oxygen species (ROS) and downregulate cyclooxygenase-2 (COX-2) expression to induce macrophage polarization, thus inhibiting foam cell formation to attenuate atherosclerosis. Due to the targeted effect of HA on stabilin-2 and CD44, which are overexpressed in atherosclerotic plaques, Pd@HA/ALO can actively accumulate in atherosclerotic plaques. Subsequently, the antioxidative effects of Pd octahedral nanozymes are mediated by their intrinsic superoxide dismutase- and catalase-like activities capable of effective scavenging of ROS. In addition, anti-inflammatory effects are mediated by controlled, on-demand near-infrared-triggered ALO release leading to inhibition of COX-2 expression. Importantly, the combined therapy can promote the polarization of macrophages to the M2 subtype by upregulating Arg-1 and CD206 expression and downregulating expression of TNF-α, IL-1β and IL-6, thereby inhibiting atherosclerosis-related foam cell formation. In conclusion, the presented in vitro and in vivo data demonstrate that Pd@HA/ALO enhanced macrophage polarization to reduce plaque formation, identifying an attractive treatment strategy for cardiovascular disease.
An N-heterocyclic carbene (NHC)-catalyzed carbonyl nucleophilic substitution reaction between 1-cyclopropylcarbaldehydes and N-sulfonyl imines is developed for access to linear β-aminoenone products. The β-aminoenones containing cyclopropyl fragments can be afforded in moderate to excellent yields under mild conditions. The reaction features excellent trans-diastereoselectivities and the desired aminoenone products are all afforded as Z-isomers.
In this paper, supra-amphiphilic compounds containing disaccharides and azobenzene ends have been constructed via dynamic covalent bond. It was found that the slight structural difference of the disaccharides made significant difference in the self-assembled morphologies. Namely, three kinds of azo-disaccharide supra-amphiphiles were found to assemble into different morphologies, with the only difference in chemical structure from the disaccharides. More importantly, the structural difference between the disaccharides, including lactoside, maltoside and cellobioside was trivial. Molecular simulation revealed the packing of molecules was due to the different contribution from hydrogen bonds. The above results clearly indicated the contribution of saccharide packing, especially the related hydrogen bonding, to the final morphology of the assembled structures.
The magnetism of nanographene is dominated by the structure of its carbon skeleton. However, the magnetism engineering of nanographene is hindered due to finite precursors. Here, we demonstrate an ingenious synthetic strategy to engineer the magnetism of nanographene through hetero-coupling two precursors on Au(111) surface. Bond-resolved scanning tunneling microscopy and spectroscopy results show that two homo-coupled products host a closed-shell structure, while the products with five membered ring defects perform as an open-shell one with the total spin number of 1/2, confirmed by spin-polarized density functional theory calculations. While two hetero precursors on Au(111) substrate, the hetero-coupled products both perform as the magnetic structure with total spin quantum numbers of 1/2 and 1, resulting from carbon skeleton transformations. Our work provides an effective way to engineer the magnetism of nanographene by enriching the magnetic products simultaneous, which could be extended into other controllable magnetic nanographene instruction.
Stability of liposomes plays a crucial role in drug delivery, especially in oral aspect. The structural modification of liposomes has been the orientation of efforts to improve their stability and enable the controllability of payload release. This study reported a selenylation strategy to optimize the liposomal structure in an attempt to enhance the nanocarrier's stability, hence the bioavailability of emodin (EM), an active compound with poor water-solubility. EM-loaded selenized liposomes (EM-Se@LPs) were prepared by thin film dispersion followed by in situ reduction technique. The results showed that EM-Se@LPs were provided with enhancive gastrointestinal stability and exhibited sustained release of drug compared with EM-loaded liposomes (EM-LPs). However, the modified liposomes with Se depositing onto the interior and exterior bilayers did not substantially facilitate absorption of EM. The reinforced structure of liposomes irrelevant to absorption was affirmed to be due to good stability and absorbability of EM itself. Nevertheless, the present work provides an alternative option for stabilization of liposomes instead of conventional methods, which may be promising for oral delivery of physiologically unstable and/or poorly absorbed drugs and systemic drug delivery.
Repeated waves of influenza virus H7N9 epidemics after 2013 have caused severe influenza in humans, with mortality reaching approximately 40%–50%. To prevent possible pandemics, the development of highly effective vaccines against influenza virus H7N9 is highly desired. In the present study, by taking advantage of the d-tetra-peptide adjuvant (GDFDFDY), we reported a simple method to prepare H7N9 vaccines. Naproxen (Npx), with good anti inflammatory and broad anti-viral effects, was employed as an N-terminal capping group to construct a hydrogel precursor, Npx-GDFDFDY. The hydrogel adjuvant was prepared using a routine heating cooling protocol and the final vaccine was ready after mixing with the split A/Zhejiang/DTID-ZJU01/2013 (H7N9) antigen by vortexing. Compared with the traditional Al(OH)3 adjuvant vaccine and the split vaccine, our hydrogel adjuvant vaccine showed the best preventive effects against H7N9 infection. A mechanistic study illustrated that higher antibody responses and variations in cytokine expression might account for its increased protective effects. Our strategy demonstrated the advantages of a peptide hydrogel adjuvant in the application of vaccines against H7N9 and demonstrated its potential application in vaccines against emerging threats from other viruses.
Nine new fluorine-containing drugs have been approved by the US Food and Drug Administration (FDA) in 2021, which are presented in this review article. These small molecular drugs feature aromatic fluorine, trifluoromethyl and chlorodifluoro groups. The therapeutic areas of these fluorine-containing drugs include multiple myeloma, lymphoma, HIV, chronic heart failure, chronic myeloid leukemia, (ANCA)-associated vasculitis, migraines, von Hippel-Lindau disease, and non-small cell lung cancer. The brief biological activities and the synthetic methods have been discussed in this review for each of these nine drugs.
Three-residue cyclophane-forming enzymes (3-CyFEs) are a group of radical S-adenosylmethionine (SAM) enzymes involved in the biosynthesis of ribosomally synthesized and posttranslationally modified peptides (RiPPs). 3-CyFE catalyzes the crosslinking between an aromatic residue (Ω1) and a non-aromatic residue (X3) in a Ω1-X2-X3 motif to produce a cyclophane ring, a key step in the biosynthesis of the RiPP natural product triceptide. In this study, we perform a genome-wide search for the Xye-type triceptides, showing these RiPPs are likely class-specific and only present in gamma-proteobacteria. The 3-CyFE PauB from Photorhabdus australis exhibits a relaxed substrate specificity on the X3 position, but glycine in this position is not suitable for cyclophane formation. We also reconstituted the activity of PauB in vitro, showing it produces the N-terminal cyclophane firstly, and then the C-terminal ring, whereas the middle cyclophane is produced in the last step.
O-Acyl ketoximes has been proven to be versatile building blocks for practical construction of N-heterocycles. In the last few years, diverse catalytic systems have been discovered to enable efficient transformations of O-acyl ketoximes to a range of nitrogen-heterocycles. Herein, we summarized our recent examples of novel nitrogen-heterocycle formation with new function findings of O-acyl ketoximes through facile aerobic copper catalysis, metal-free NO bond activation, multi-component assembly, and bis-annulations. From the green chemistry perspective, these works represent efficient methods with high atom economy, high selectivity, and minimized chemical waste. These findings also complement well to the previous mainly copper-based catalytic systems and more importantly enrich the oxime chemistry in organic synthesis.
Plaque plays a central role in atherosclerosis (AS) progression, whereas inflammation and destruction of the plaque microenvironment contribute to plaque advancement. As a result, a therapy regime, which combines anti-inflammation and inhibition-degradation of plaque matrix, appears to be a promising strategy to combat AS. Herein, we report a pH-sensitive liposome co-loading with the anti-inflammatory agent (oridonin, ORD) and plaque-collagen protector (marimastat) for anti-AS therapy. ORD was first conjugated with hyaluronic acid (HA) to target the inflammation contributor, pro-inflammatory macrophages. Then, the conjugate assembled onto the MATT-loaded liposomes. The co-loaded system (~150 nm) significantly improved pharmacokinetics over the liposomes without anchoring the conjugate and accumulated effectively in the plaque. The preparation administration allowed efficient anti-AS activities in high-fat diet (HFD)-Apoe-/- mice by decreasing the pro-inflammatory cytokine expression in the serum, lessening the lesion area, alleviating the plaque collagen degradation, promoting macrophage polarization from phenotypic M1 to M2, reducing T helper (Th) 17 cells (Th17)/T regulatory cells (Tregs) and Th1/Th2 ratio, etc. Furthermore, the serum determination in AS patients demonstrated high expression of the inflammatory cytokines, indicating our finding may offer a potential guideline for clinical practice.
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