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1.
J Mech Behav Biomed Mater ; 145: 105942, 2023 09.
Article in English | MEDLINE | ID: mdl-37423009

ABSTRACT

The development of multifunctional and low-cost hydrogel dressings with good mechanical properties, antibacterial activity, and nontoxicity is of great relevance in healthcare. This study aimed to prepare a series of hydrogels consisting of maltodextrin (MD), polyvinyl alcohol (PVA), and tannic acid (TA) through a freeze-thaw cycling technique. Micro-acid hydrogels with different mass ratios (0, 0.25, 0.5, and 1 wt%) were obtained by adjusting the TA content. Among all hydrogels, TA-MP2 hydrogels (with a TA content of 0.5 wt%) showed good physicochemical and mechanical properties. In addition, the biocompatibility of TA-MP2 hydrogels was confirmed by the high cell survival rate of NIH3T3 cells, which was over 90% after 24 h and 48 h of incubation. Additionally, TA-MP2 hydrogels showed multifunctional properties, including antibacterial and antioxidative effects. In vivo experiments showed that TA-MP2 hydrogel dressings significantly accelerated wound healing in a full-layer skin wound model. These findings indicated the potential of TA-MP2 hydrogel dressings in promoting wound healing.


Subject(s)
Polyvinyl Alcohol , Tannins , Animals , Mice , Polyvinyl Alcohol/chemistry , Tannins/pharmacology , NIH 3T3 Cells , Hydrogen Bonding , Wound Healing , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Hydrogels/chemistry
2.
Chem Asian J ; 18(13): e202300263, 2023 Jul 03.
Article in English | MEDLINE | ID: mdl-37211540

ABSTRACT

Exploring efficient cocatalysts capable of accelerating surface catalytic reaction is of great significance for the development of solar-driven hydrogen production. Herein, on the basis of NiFe hydroxide, we developed a series of Pt doped NiFe-based cocatalysts to promote the photocatalytic hydrogen production of graphitic carbon nitride (g-C3 N4 ). We find that the Pt doping can trigger phase reconstruction of NiFe hydroxide and lead to the formation of NiFe bicarbonate, which displays higher catalytic activity toward hydrogen evolution reaction (HER). The Pt doped NiFe bicarbonate modified g-C3 N4 shows excellent photocatalytic activity with H2 evolution rate up to 100 µmol/h, which is more than 300 times that of pristine g-C3 N4 . The experimental and calculation results demonstrate that the greatly improved photocatalytic HER activity of g-C3 N4 is not only due to the efficient carrier separation, but also attributed to the accelerated HER kinetics. Our work may provide guidance for designing novel and superior photocatalysts.

3.
Bioorg Med Chem ; 81: 117202, 2023 03 01.
Article in English | MEDLINE | ID: mdl-36804726

ABSTRACT

In previous decades, patients with the most active EGFR mutations in non-small cell lung cancer (NSCLC) have significantly benefited from EGFR tyrosine kinase inhibitors (TKIs). However, a minority with EGFR and HER2 exon 20 mutations are inherently resistant to treatment. Several molecular TKIs (such as TAK788 and Poziotinib) were recently discovered and demonstrated as effective inhibitors against the most prevalent HER2 or EGFR exon 20 mutations. However, low clinical efficiency and uncertain adverse reaction indicated that the development of effective therapies is still demanded. In the present work, we designed several hybrid compounds learning from 3D modeling of kinase structure. One lead compound (compound 56) was found to be the most potent compound with IC50 value of 0.027 nM against EGFR D770-N771 ins NPG and reduced binding affinity with hERG protein. In vitro and in vivo biological results suggested that compound 56 demonstrated good oral bioavailability, and it was significantly capable of inhibiting the growth of tumor cells with a variety of HER2 exon 20 mutations and EGFR mutants with negligible toxic effects. It was identified that compound 56 might be considered a potential drug candidate for NSCLC target therapy.


Subject(s)
Carcinoma, Non-Small-Cell Lung , Lung Neoplasms , Humans , Carcinoma, Non-Small-Cell Lung/drug therapy , Lung Neoplasms/drug therapy , Lung Neoplasms/genetics , Lung Neoplasms/pathology , Mutagenesis, Insertional , ErbB Receptors , Protein Kinase Inhibitors/chemistry , Mutation , Exons
4.
Chem Commun (Camb) ; 58(92): 12859-12862, 2022 Nov 17.
Article in English | MEDLINE | ID: mdl-36317636

ABSTRACT

Herein, V-doped cobalt hydroxides grown on carbon cloth (V-Co(OH)2/CC) were prepared via hydrothermal method. The incorporation of V can trigger phase transition and tune the local electronic structure of Co(OH)2, thereby improving the intrinsic alkaline HER activity. We find that the V-Co(OH)2 dominated by ß-Co(OH)2 exhibits excellent HER activity with only 83 mV overpotential at a current density of 10 mA cm-2, which outperforms most reported hydroxide-based catalysts and even surpasses the commercial Pt/C at large current density (>160 mA cm-2).

5.
Microbes Infect ; 17(9): 665-70, 2015 Sep.
Article in English | MEDLINE | ID: mdl-26003522

ABSTRACT

We previously identified an HIV-1 fusion inhibitor P20A targeting HIV-1 gp41 6-HB fusion core. Using alanine scanning mutagenesis, we investigated the effect of 6-HB surface residue mutations on the binding affinity between P20A and 6-HB. Substitution of positively or negatively charged residues in the distal region of 6-HB with alanines resulted in significant decrease or increase of its binding affinity to P20A, respectively. The 6-HB with E630K, D632K, or E634K mutation exhibited enhanced binding affinity with P20A, suggesting that P20A blocks HIV-1 fusion through electrostatic interaction with the positively charged residues in the distal region of the gp41 fusion core.


Subject(s)
HIV Envelope Protein gp41/chemistry , HIV Envelope Protein gp41/metabolism , HIV Fusion Inhibitors/chemistry , HIV Fusion Inhibitors/metabolism , Amino Acid Sequence , Binding Sites , HIV Envelope Protein gp41/genetics , HIV-1/genetics , Molecular Sequence Data , Mutagenesis, Site-Directed , Protein Binding/drug effects , Protein Binding/genetics , Sequence Alignment , Static Electricity , Virus Internalization
6.
Nucleic Acids Res ; 43(9): e58, 2015 May 19.
Article in English | MEDLINE | ID: mdl-25722369

ABSTRACT

In this study, a universal protein expression enhancement RNA tool, termed RNAe, was developed by modifying a recently discovered natural long non-coding RNA. At the moment, RNAe is the only technology for gene expression enhancement, as opposed to silencing, at the post-transcriptional level. With this technology, an expression enhancement of 50-1000% is achievable, with more than 200% enhancement achieved in most cases. This work identified the sufficient and necessary element for RNAe function, which was found to be merely 300 nucleotides long and was named minRNAe. It contains a 72-nt 5' pairing sequence which determines the specificity, a 167-nt short non-pairing interspersed nuclear element (SINE) B2 sequence which enhances ribosome recruitment to the target mRNA, and a poly(A) tail, provided together on a plasmid bearing the appropriate sequences. Cellular delivery of RNAe was achieved using routine transfection. The RNAe platform was validated in several widely-used mammalian cell lines. It was proven to be efficient and flexible in specifically enhancing the expression of various endogenous and exogenous proteins of diverse functions in a dose-dependent manner. Compared to the expression-inhibitory tool RNAi, the RNAe tool has a comparable effect size, with an enhancing as opposed to inhibitory effect. One may predict that this brand new technology for enhancing the production of proteins will find wide applications in both research and biopharmaceutical production.


Subject(s)
Gene Expression Regulation , Protein Biosynthesis , Protein Engineering/methods , RNA, Long Noncoding/chemistry , Antibody Formation , Cell Line , Genetic Vectors , Green Fluorescent Proteins/analysis , Green Fluorescent Proteins/genetics , HEK293 Cells , Humans , Proteomics , RNA, Antisense/chemistry , Repetitive Sequences, Nucleic Acid , Ribosomes/metabolism
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