JOURNAL OF BIOACTIVE AND COMPATIBLE POLYMERS
·
2013
·
IF 2.207
Feng Xu,Ting-Ting Yan,Yan-Ling Luo
Novel amphiphilic block copolymers consisting of hydrophobic poly(D,L-lactide) segments and hydrophilic poly(N-isopropylacrylamide-co-N, N-dimethylacrylamide) blocks were designed and synthesized through a simple free radical copolymerization route based on a bifunctional initiator, followed by the ring-opening polymerization of D,L-lactide. The copolymers self-assembled into thermosensitive spherical-nanosized core–shell micelles in aqueous solution in the presence or the absence of the model drug prednisone. The chemical and physical characterizations of drug-loaded and unloaded micelles revealed a lower critical solution temperature of 40°C–47°C, and a critical micelle concentration less than 7.20 mg L−1, a transmission electron microscope mean particle size from 50 to 75 nm, and a narrow dynamic light scattering diameter below 180 nm. The prepared blank and drug-loaded micellar nanoparticles were thermodynamically stabile and employed in targeted drug delivery by responding to the higher temperature of the local microenvironment. Based on prednisone release kinetic studies, structural changes of the self-assembled micelles as well as temperature- or environment-induced diffusion controlled drug release and improved bioavailability. The copolymer micelles exhibited good biocompatibility as established by the MTT cytotoxicity assay. Therefore, an effective target therapy against lesion tissues is feasible using these polymeric micelles.
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LWT-FOOD SCIENCE AND TECHNOLOGY
·
2022
·
IF 6.056
Renjie Zhou,Cheng Yang,Ting Xie,Jian Zhang,Chenqiang Wang,Ziqiang Ma,Lianfu Zhang
Amadori compounds (ACs) are the first stable product formed in the initial stage of the Maillard reaction and are widely present in processed foods. In addition to being widely known as the flavor precursors, ACs have attracted attention in recent years because many functions have been revealed, including ACE inhibition. In this work, we synthesized four ACs ( N -(1-Deoxy-D-fructos-1-yl)-glycine (Fru-Gly), N -(1-Deoxy-D-fructos-1-yl)-proline (Fru-Pro), N -(1-Deoxy-D-fructos-1-yl)-serine (Fru-Ser) and N -(1-Deoxy-D-fructos-1-yl)-threonine (Fru-Thr)) and characterized them using UPLC-Q-TOF-MS spectra. The four ACs’ angiotensin-converting enzyme (ACE) inhibitory activities were verified for the first time, the IC 50 value range was 1.447–4.204 mmol/L, the Fru-Gly has the best effect. And all the four ACs showed good digestion stability, the content remained above 70% after 5 h of continuous digestion simulation. In order to reveal the mechanism of ACs inhibiting ACE, we selected Fru-Gly, beacuse of the best inhibitory effect, to carried out enzyme kinetics, circular dichroism spectroscopy, fluorescence spectroscopy, thermodynamics and molecular docking analysis. The results showed that Fru-Gly was a noncompetitive inhibitor, it spontaneously binds to the inactive site of ACE by hydrogen bond and causes the conformation change of ACE to inactivate it. The reaction is easier to proceed at low temperatures.
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JOURNAL OF MEDICINAL CHEMISTRY
·
2024
·
IF 6.8
Ruoqing Zeng,Meimiao Fang,Ancheng Shen,Xiaolei Chai,Yumiao Zhao,Mingyao Liu,Lingfeng Zhu,Weiwei Rui,Bo Feng,Liang Hong,Chunyong Ding,Zilan Song,Weiqiang Lu,Ao Zhang
Accumulating evidence has demonstrated a critical pathological role of oxysterol receptor GPR183 in various inflammatory and autoimmune diseases, including inflammatory bowel disease (IBD). However, the currently reported GPR183 antagonists are very limited and not qualified for in vivo studies due to their inferior druglike properties. Herein, we conducted a structural elaboration focusing on improving its PK and safety profile based on a reference antagonist NIBR189. Of note, compound 33, bearing an aminobenzothiazole motif, exhibited reduced hERG inhibition, improved PK properties, and robust antagonistic activity (IC50 = 0.82 nM) with high selectivity against GPR183. Moreover, compound 33 displayed strong in vitro antimigration and anti-inflammatory activity in monocytes. Oral administration of compound 33 effectively improved the pathological symptoms of DSS-induced experimental colitis. All of these findings demonstrate that compound 33 is a novel and promising GPR183 antagonist suitable for further investigation to treat IBD.
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FUEL
·
2022
·
IF 8.035
Yongtao Zhang,Fulin Chen,Yan He,Fei Wang
CO 2 sequestration based on hydrate technology is considered to be the most promising long-term CO 2 sequestration technology. In this study, a method of using initial stirring to activate CO 2 hydrate formation process was proposed in the aim of saving energy and avoiding the problem of stirring shaft stuck, where the stirring only played a role in activating hydrate formation process. Two amino acids, l -Methionine and d -leucine, were chosen as promoters for improving the formation kinetics of CO 2 hydrates, and l -Methionine presents better than d -leucine. When the concentration of l -methionine solution is equal to or greater than 4 mmol/L, even with the initial stirring of 10 rpm within 8 min, T 90 can be shortened to close to or less than 40 min with a high gas consumption of more than 7.3 mmol gas/mL water, where the promoting effect is similar to the condition of continuous stirring of about 100 min, indicating that about 90 % of the energy consumed for mechanical stirring can be saved. Moreover, an interesting phenomenon was observed that CO 2 hydrates firstly nucleated inside the l -methionine solution, and a large number of small hydrate floccules rapidly formed and filled the entire solution under the action of magnetic stirring, which proved the instantaneous excitation effect of stirring on hydrate formation. This work contributes to rethinking the promoting roles of stirring and promoters in CO 2 hydrate formation.
研究领域:
环境科学
·
能源化学
·
物理化学
·
气体水合物
·
碳捕集与封存
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JOURNAL OF COLLOID AND INTERFACE SCIENCE
·
2026
·
IF 9.6
Boheng Chen,Hongpo Liu,Huiyin Zheng,Che Liu,Zhuosen Wang,Yapeng Tian,Xinwei Cui
Lithium oxalate (Li 2 C 2 O 4 ) is regarded as a promising prelithiation agent due to its high specific capacity and cost-effectiveness. However, its intrinsically poor electronic conductivity and sluggish reaction kinetics result in a high lithium liberation potential (typically above 4.5 V), which challenges the stability of electrolytes and electrode materials, and deteriorates overall battery performance. In this work, the intermetallic NiBi 3 catalyst with metallic conductivity and strong interfacial interaction is introduced to promote the low-potential decomposition of Li 2 C 2 O 4 . Benefiting from the synergistic electronic effect between Ni and Bi, the incorporation of Bi effectively modulates the electronic structure of Ni sites via d – p orbital hybridization, thereby enhancing the adsorption and activation of Li 2 C 2 O 4 , weakening the Li 2 C 2 O 4 framework and facilitating its decomposition. When coupled with ultrahigh-Ni NCM96 cathodes, the NiBi 3 -Li 2 C 2 O 4 prelithiation system provides higher charge capacity (273.3 mAh g −1 ) and improved reaction kinetics compared to the pristine counterpart. Furthermore, full-cell configurations based on SiO x anodes exhibit enhanced lithium compensation capability, maintaining a capacity retention of 52.9% after 150 cycles at 0.5C. These results demonstrate that intermetallic NiBi 3 is an efficient catalyst for activating Li 2 C 2 O 4 and provides a viable strategy for developing high-performance cathode prelithiation systems. Download: Download high-res image (119KB) Download: Download full-size image
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POULTRY SCIENCE
·
2026
·Vol. 105
·期 5
·106672
·
IF 4.5
Guangxiao Zhang,Yawen Sun,Ling He,Bowen Zhao,Hongchao Jiao,Jingpeng Zhao,Xiaojuan Wang,Min Liu,Kelin Li,Hai Lin,Haifang Li
Vitamin D 3 (VD 3 ) is an essential fat-soluble micronutrient that regulates diverse biological processes. However, its long-term impact on avian intestinal development remains largely unknown. In this study, we detected that the VD 3 content was significantly lower in late-cycle production eggs (68 weeks old, termed “LP eggs”) compared to the peak-cycle production eggs (44 weeks old, named “PP eggs”) ( P < 0.05). Notably, the intestine index was reduced ( P < 0.05), and the intestinal expression of tight junction (TJ) proteins (Occludin and ZO-1) was decreased for chicks hatched from LP eggs versus those from PP eggs ( P < 0.05). Thus serial dosages of VD 3 (2.5, 5.0, or 7.5 μg VD 3 /egg) were injected into the amniotic cavity of embryos hatched from LP eggs on embryonic day 17 (E17). This intervention effectively improved hatchability, promoted intestinal development that persisted through 14-days post-hatch, and showed immuno-modulatory effects manifesting as Interleukin-6 ( IL-6 ) downregulation and Interleukin-10 ( IL-10 ) upregulation. Further in vivo and in vitro analysis revealed that VD 3 improved intestinal development by activating TJ-related genes ( P < 0.05), with vitamin D receptor (VDR) mediating these effects. Chromatin immunoprecipitation (ChIP) assays confirmed that 1,25-(OH) 2 D 3 strengthened VDR binding to promoter regions of Occludin and ZO-1 but decreased the interaction degree of VDR with the IL-6 promoter ( P < 0.05). These findings establish that in ovo injection of VD 3 is an efficacious perinatal intervention strategy, which significantly mitigates developmental constraints in late-phase poultry production through VDR-dependent intestinal barrier potentiation and immuno-homeostasis modulation.
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Journal for ImmunoTherapy of Cancer
·
2026
·Vol. 14
·期 5
·e014533
·
IF 11.7
Qindan Du,Zhen Han,Yumeng Zhang,Ying Li,Ao Sun,Bin Wang,Yongquan Chen,Xiaoying Wang
Background The N-terminal domain of gasdermin D (GSDMD) is a known suppressor of prostate cancer (PCa), primarily recognized for its tumoricidal pyroptotic function. However, research on the full-length GSDMD protein and its relationship with PCa remains unexplored. Therefore, the aim of this study was to investigate the potential non-pyroptotic mechanism of action of GSDMD in preventing PCa immune evasion. Methods The study used GSDMD deletion models to assess its impact on tumor progression and immune cell profiles. Molecular techniques, including protein interaction analysis, were employed to identify the binding partner of GSDMD and the subsequent signaling pathways. Correlative analysis was performed between GSDMD expression and immune markers in human PCa samples. Results GSDMD deletion increased tumor progression and reduced survival, cytotoxic T lymphocyte (CTL) activation/infiltration and tumor cell susceptibility to T-cell death, promoting an immunosuppressive tumor microenvironment (TME). GSDMD-bound laminin subunit gamma-2 (LAMC2), thus inducing its ubiquitin-mediated degradation. Consequently, GSDMD deficiency stabilized LAMC2, driving M2 macrophage polarization and CXC motif chemokine ligand 5 (CXCL5) secretion. CXCL5 interacted with CXCR2 to activate the AKT/NF-κB axis, increasing vascular endothelial growth factor (VEGF)/vascular endothelial growth factor receptor 2 (VEGFR2) and suppressing CTL activity. GSDMD expression in human PCa positively correlated with CD8 + T-cell infiltration and negatively with M2-phenotype tumor-associated macrophages. Conclusion This study reveals a novel non-pyroptotic pathway through which GSDMD inhibits PCa immune evasion by targeting LAMC2 for degradation, thereby preventing the establishment of an immunosuppressive TME. The findings suggest that activating GSDMD represents a promising therapeutic strategy to reprogram the TME from immunosuppressive (“cold”) to immunoreactive (“hot”), potentially enhancing the efficacy of immunotherapy in advanced PCa.
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Antioxidants
·
2026
·Vol. 15
·期 5
·652
·
IF 8.2
Haoyang Dai,Qinqin Zhang,Pei Chen,Suiqing Chen
The pathogenesis of acute liver injury (ALI) involves the loss of hepatic detoxification function, massive death of liver parenchymal cells within a short period, and excessive inflammatory responses. Studies have shown that Esculetin (Esc) possesses potent anti-inflammatory, antioxidant, and anti-tumor properties. In this study, we investigate whether Esc has a protective effect against ALI in mice and its potential mechanism. Esculetin markedly decreased ROS, MitoSOX, and apoptosis levels in AML12 cells and restored MMP. H&E staining demonstrated that Esc alleviated hepatic histopathological injury, and its intervention reduced serum ALT and AST levels. Moreover, Esc diminished ROS and apoptosis levels in the liver. Hepatic proteomic profiling identified the AMPK signaling pathway. Esc reduced the protein levels of p-AMPK/AMPK, PGC-1α, p-SIRT1/SIRT1, and BAX and upregulated the levels of Bcl-2 in liver tissue. Concomitantly, we added inhibitor Compound C (CC) to the AML12 cells to assess whether Esc acted through the AMPK pathway. The results showed that CC exacerbated the degree of liver injury, whereas Esc was able to reverse these phenomena, thus exerting an anti-liver injury effect. These findings provide mechanistic insights into the protective effects of Esc against ALI and support its potential as a therapeutic candidate for ALI.
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2026
·Vol. 74
·期 33
·26532-26543
·
IF 6.7
Chen Yuehua,Liu Peng,Sheng Binbin,Xing Jiaxin,Ouyang Jia,Zheng Zhaojuan
Lignocellulosic
biomass is an abundant renewable resource that
is rich in aldohexoses and aldopentoses. Efficient biocatalysts for
aldopentose oxidation remain limited, and few enzymes exhibit high
catalytic efficiency toward both aldohexoses and aldopentoses. Here,
a naturally promiscuous pyrroloquinoline quinone-dependent glucose
dehydrogenase (PQQ-GDH) from Pseudomonas fragi NL20W was selected as an engineering template and tailored by semirational
design to expand aldopentose oxidation while preserving native d -glucose activity. The V706P/L723 M mutant exhibited markedly
enhanced catalytic efficiency toward d -xylose and l -arabinose, reaching 8.0- and 2.4-fold those of the wild-type, respectively,
while its efficiency toward d -glucose was 1.3-fold that of
the wild-type. Molecular simulations suggested that the improved catalysis
was associated with an optimized substrate positioning and enhanced
conformational flexibility of the active-site region. This study highlights
the significance of natural enzyme scaffold selection in substrate
scope engineering and expands the application potential of PQQ-GDH
in the sustainable valorization of lignocellulosic sugars.
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FOOD HYDROCOLLOIDS
·
2025
·
IF 12.4
Peiying He,Bin Zhang,Xiong Fu,Rungtiwa Wongsagonsup,Namfone Lumdubwong,Qing Gao,Qiang Huang
As a high-value spice and medicinal compound, the volatilization and degradation of D-borneol during processing pose significant challenges in the food and pharmaceutical industries. Considering the size matching, pre-formed V-type starch (V 6 and V 7 -type carrier) was used to improve the retention and stability of D-borneol in different encapsulation methods (Wet, Semi-dry, and Dry). The semi-dry method used with the V 7 -type carrier exhibited the highest loading capacity (90.79 mg/g), significantly higher than those obtained via Wet (55.55 mg/g) and Dry (22.52 mg/g) methods. The good complexation was under the balance of restricted dissolution at the ratio of 6:20 (V 7 -type starch: ethanol, w/v) and mechanical grinding at 25 °C via semi-dry method. The complexes prepared with the semi-dry method below 25 °C and 50 °C showed the lowest D-borneol release rate, primarily governed by concentration diffusion. At higher temperatures (75 °C), the slow release of D-borneol depended on its stable binding with starch helical interaction. These findings highlight the potential of semi-dry encapsulation method as an effective strategy for stabilizing D-borneol and enabling its controlled release in functional food applications.
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Advanced Science
·
2026
·
IF 14.1
Yinuo Zhao,Qingzhou Kong,Haifan Gong,Lixiang Li,Jialu Fu,Boyao Wan,Peizhu Wang,Xiaojuan Li,Yue Wang,Jinghui Zhang,Yanbo Yu,Xiaoyun Yang,Xiuli Zuo,Haina Wang,Yanqing Li
D-amino acid substitution provides an effective strategy for optimizing antimicrobial peptides (AMPs) by enhancing their stability. However, the absence of universal rules renders traditional screening methods time-consuming and labor-intensive, potentially leading to reduced or complete loss of activity. Here, we curated a D-amino acid-substituted AMP dataset from published literature and databases. We then developed ADAPT, an AI-based tool for predicting the functional impact of D-amino acid substitutions, and integrated it into a high-throughput screening pipeline for AMP optimization. Of the variants obtained through this pipeline, 80% exhibited enhanced antibacterial activity. Among these, dR2-1 showed exceptional broad-spectrum antimicrobial activity, reduced toxicity, and substantially improved stability. Mechanistic studies confirmed a membrane-targeting antibacterial mode of action. Furthermore, we engineered a hydrogel delivery system that effectively treated cutaneous infections in mice. Overall, our study established an AI-based framework for D-amino acid substitution in AMPs, enabling the efficient discovery of potent and stable candidates with enhanced clinical translation potential.
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
·
2015
·
IF 2.752
Junhao Huang,Jiacheng Li,Yuhong Feng,Ke Li,Huiqiong Yan,Pengbo Gao,Ting Xiao,Chunxiu Wang
In this study, the aggregation of N-octyl-β- d -glucopyranoside (OGP) and cholesteryl grafted sodium alginate derivative (CSAD) in solutions was investigated by surface tension method, fluorescence spectroscopy, dynamic light scattering, and transmission electron microscopy. Results showed that cholesteryl of CSAD and OGP were adsorbed competitively to the gas–solution interface. Four different conformations of complexes were found with the increasing of OGP concentration (C). When C < critical aggregation concentration (CAC), the OGP stimulates CSAD association. When CAC < C < critical micelle concentration (CMC), the OGP was stimulated by hydrophobic interaction, then it compounded CSAD to form polymer–surfactant complexes and some pearl-chain structure complexes. When CMC < C < adsorbed saturation concentration (C 2 ), the quantity of pearl-chain structure complexes increases, they interact to form core–shell structure complexes, and several core–shell structure complexes formed short string-structures by association of CSAD molecule. When C > C 2 , adsorption amount of OGP to CSAD reached saturation, OGP molecules formed small single OGP micelles , while the string-structures were dissolved because the cholesteryl among the micelles were replaced by the single OGP micelles.
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