INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2025
·Vol. 26
·期 6
·2727
·
IF 4.9
Kang Li,Xiaomei Ge,Wei Liu,Lei Huang,Xinye Lv,Yuhui Tang,Zhehao He,Yingxue Yang,Miaofen Chen,Jianguo Zeng,Pi Cheng
B-cell lymphoma-2 (Bcl-2) family proteins are fundamental regulators of intrinsic cell apoptosis, and overexpression of apoptotic proteins (Bcl-2 and Mcl-1) is a characteristic of many haematological malignancies. Thus, it is necessary to discover novel inhibitors to treat leukemia. In the current study, we synthesized a series of quercetagetin derivatives (compounds2a–2t,3a–3jand4a–4g) and evaluated their anticancer activities on four leukemia cells (U937, K562, K562R and KG-1). Among those synthesized derivatives, compounds2aexhibited the best antiproliferative activity (IC50= 0.276, 0.159, 0.312 and 0.271 µM to U937, K562, K562R and KG-1, respectively). In addition,2ainduced apoptosis in K562 and markedly arrested the cell cycle G2/M phase of K562. The Western blot assay showed that2ais a potential inhibitor that can effectively suppress the expression of Bcl-2 and Mcl-1. The molecular docking study predicted that2ahad firm interactions with the active pockets of Bcl-2 and Mcl-1. Finally, in silico pharmacokinetic evaluation of2aindicated its potential as an anti-leukemia drug lead in the future.
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Materials Today Bio
·
2025
·
IF 10.2
Qiang Zhang,Tuo Wang,Junyu Ren,Yanru Guo,Ziyi Yin,Chenrui Zhang,Honglin Fan,Yinting Ren,Junlong Da,Narisu Hu
Oral ulcers, a prevalent mucosal disorder with high recurrence rates, remain challenging to treat due to the oral cavity’s dynamic environment and the multifactorial nature of ulcer progression. Here, we report a multifunctional microneedle (MN) patch loaded with astragalus polysaccharide (APS-MN) that integrates rapid mucosal penetration, reactive oxygen species (ROS) scavenging, and ferroptosis inhibition to accelerate ulcer healing. Unlike conventional MN systems reliant on synthetic drugs or prolonged dissolution, APS-MN leverages the natural antioxidant and immunomodulatory properties of APS-a traditional Chinese medicine-derived polysaccharide-enabling complete drug release within 2 minutes and targeted delivery to ulcer bases. In vitro and in vivo studies demonstrate that APS-MN promotes M2 macrophage polarization, suppresses pro-inflammatory cytokines (TNF-α, IL-1β), and inhibits ferroptosis via the Nrf2/HO-1/SLC7A11 axis, achieving 88.2% wound closure in rats within 6 days. Notably, this work combined herbal polysaccharides with MN technology for oral ulcer therapy, offering a biocompatible, non-invasive alternative to corticosteroids and antibiotics. The rapid dissolution, dual antioxidant/anti-ferroptotic action, and scalability of APS-MN position it as a transformative platform for managing recurrent oral ulcers and other redox-imbalanced mucosal diseases.
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高影响因子
MOLECULES
·
2025
·Vol. 30
·期 16
·3400
·
IF 4.6
Lina Hu,Mengjiao Li,Zheng Liu,Hui Yan,Xuekun Wang,Shiben Wang
To discover novel, potent anticonvulsant compounds, a series of compounds containing triazole structural fragments were synthesized and evaluated for their anticonvulsant activity. Compounds6f(maximal electroshock (MES), 50% effective dose (ED50) = 13.1 mg/kg; subcutaneous pentylenetetrazole (scPTZ), ED50= 19.7 mg/kg) and6l(MES, ED50= 9.1 mg/kg;scPTZ, ED50= 19.0 mg/kg) showed the best activity in MES andscPTZ tests. The results of an affinity test showed that the potent compounds had better binding to the GABAAreceptors. The results of an inhibitory neurotransmitter GABA content test in brain tissue indicated that compounds6fand6lexerted anticonvulsant activity which may be associated with the increase of GABA content in the rat brain. Elevated plus maze (EPM) assay results showed that compounds6fand6lpossessed anxiolytic effects, and their effects correlated with the binding sites of benzodiazepines (BZs) in the GABAAreceptors. Molecular docking was performed to investigate the interactions of the studied compound6lwith the GABAAreceptors on the molecular level.
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JOURNAL OF POLYMER RESEARCH
·
2026
·Vol. 33
·期 11
·435
·
IF 3.5
Chen Yuhuan,Zhang Yun,Chen Chunhong,Chen Jing
In the present work, a low viscosity polymer n EB-PEI 1800 ( n = 0.22, 0.29, 0.35) is synthesized for CO 2 capture. n EB-PEI 1800 is obtained by partially modifying poly(ethylene imine) (PEI 1800 ) with 1, 2-epoxybutane (EB) and is characterized by FT-IR, elemental analysis and liquid state 13 C NMR. The physical properties, density and viscosity, of aqueous n EB-PEI 1800 solutions with weight fraction w of 30% at the temperatures ranging from (293.15 to 313.15) K are reported. Additionally, CO 2 capture performance by aqueous n EB-PEI 1800 solution is examined. CO 2 absorption loading, average absorption rate, desorption loading, average desorption rate and desorption efficiency in a variety of aqueous n EB-PEI 1800 solution ( w = 5%, 10%, 15%, 20% and 30%) are investigated at different temperatures. The stability of PEI-based absorbent is also examined by four absorption–desorption cycles. The results reveal that modification can adjust the physical properties of n EB-PEI 1800 solutions. 0.29 EB-PEI system has the lowest viscosity and is favorable for CO 2 capture. 20% aqueous 0.29 EB-PEI solution provides excellent cycling stability and desorption performance, especially desorption efficiency, increasing by 55% compared to PEI system at 393.15 K.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2021
·
IF 6.953
Wenchao Zhang,Weiyi Wang,Xin Liu,Ying Chen,Kang Ouyang,Zuzhang Wei,Huan Liu,Weijian Huang
Porcine astrovirus (PAstV) is prevalent in pigs worldwide and could cause clinical symptoms such as diarrhea and encephalitis. The capsid protein (Cap) of PAstV plays a determinant role for virus immunological characteristics. In this study, the major antigenic regions of PAstV1 Cap were expressed through prokaryotic expression systems and immunized to BALB/c mice. Finally, two anti-Cap monoclonal antibodies (named mAb F4-4 and D3F10) were screened by indirect immune-fluorescence assay (IFA). A series of truncated GST-fused or artificially synthesized peptides were used to detect their reactivity with the mAbs and PAstV positive serum. Two novel B cell epitopes ( 120- GNNTFG -125 , 485- RISDPTWFSA -494 ) were identified by using these two mAbs. Moreover, sequence alignment result showed that epitope 120- GNNTFG -125 was highly conserved in type 1 PAstV capsid protein. Cross-reactivity analysis further confirmed the genotype-specificity of mAb F4-4. The results of this study demonstrated to be the first description of monoclonal antibody preparation and B-cell epitope mapping on PAstV capsid protein, which may provide new information on the biological significance of PAstV capsid protein and lay a foundation for the development of PAstV immunological tests and genotype diagnostic methods.
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RESPIRATORY PHYSIOLOGY & NEUROBIOLOGY
·
2022
·
IF 2.821
Jing Li,Meixue Chen,Lingling Lu,Jinfeng Wang,Liling Tan
Childhood asthma is a common chronic childhood disease. Branched-chain amino acid transaminase 1 (BCAT1) was reported to be upregulated in chronic airway diseases, while its role in childhood asthma is unclear. Asthma mouse models were established in neonatal mice by 10 µg ovalbumin (OVA) intraperitoneal injection and 3% OVA inhalational challenge. In OVA-challenged mice, BCAT1 levels were upregulated. BCAT1 inhibitor alleviated airway structure and inflammation by suppressing IgE, OVA-specific IgE and inflammatory cytokine release and inflammatory cell infiltration. BCAT1 inhibitor alleviated airway remodeling by inhibiting goblet cell hyperplasia, mucus secretion and the expression of α-SMA and collagen I/III. The BCAT1 inhibitor prevented OVA-enhanced autophagy by decreasing Beclin-1, Atg5 and LC3I/II and increasing p65 levels. In IL-13-stimulated BEAS-2B cells, rapamycin promoted inflammatory cytokine release and autophagy after BCAT1 inhibitor administration. Our research revealed that BCAT1 was upregulated in neonatal asthmatic mice and that a BCAT1 inhibitor might restrain airway inflammation and remodeling by decreasing autophagy, which offered a novel mechanistic understanding of childhood asthma.
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DRUG DELIVERY
·
2023
·
IF 6
Ru Wang,Nuannuan Li,Tianyu Zhang,Yiying Sun,Xiaoyan He,Xiaoyan Lu,Liuxiang Chu,Kaoxiang Sun
Mitoxantrone (MX) can induce the immunogenic-cell death (ICD) of tumor cells and activate anti-tumor immune responses. However, it can also cause high expression of indole amine 2, 3-dioxygenase (IDO) during ICD, leading to T-cell apoptosis and a weakened immune response. An IDO inhibitor, 1-methyl tryptophan (1-MT), can inhibit the activity of IDO caused by MX, resulting in enhanced chemo-immunotherapy. Here, MX-1-MT was connected by ester bond which could be broken in an acidic tumor microenvironment. MX-1-MT was combined with polyethylene glycol (PEG) via a disulfide bond which could be reduced by glutathione overexpressed in tumors, thereby accelerating drug release at target sites. Folic acid-modified distearoyl phosphoethanolamine-polyethylene glycol (DSPE-PEG-FA) was introduced to form targeting micelles. The micelles were of uniform particle size, high stability, and high responsiveness. They could be taken-up by drug-resistant MCF-7/ADR cells, displayed high targeting ability, and induced enhanced cytotoxicity and ICD. Due to 1-MT addition, micelles could inhibit IDO. In vivo studies demonstrated that micelles could accumulate in the tumor tissues of nude mice, resulting in an enhanced antitumor effect and few side-effects.
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Frontiers in Microbiology
·
2022
·
IF 6.064
Le Su,Feifan Ma,Zaiyong An,Xiuyu Ji,Ping Zhang,Qiulin Yue,Chen Zhao,Xin Sun,Kunlun Li,Baojun Li,Xinli Liu,Lin Zhao
Because of the increased incidence and prevalence, ulcerative colitis (UC) has become a global health issue in the world. Current therapies for UC are not totally effective which result in persistent and recurrent symptom of many patients. Lactobacillus with anti-inflammatory effects might be beneficial to the prevention or treatment for UC. Here, we examined the ameliorative effects of the metabolites of Lactobacillus fermentum F-B9-1 (MLF) in Caco-2 cells and dextran sodium sulfate (DSS)-induced UC model mice. MLF displayed intestinal barrier-protective activities in Caco-2 cells by increasing the expression of Occludin and ZO-1. They also showed anti-inflammatory potential in interleukin (IL)-1β and IL-6. In order to further examine the in vivo anti-inflammatory effect of MLF, the MLF was gavaged in the DSS-induced UC model mice. The intragastric administration of MLF effectively alleviated colitis symptoms of weight loss, diarrhea, colon shortening, and histopathological scores, protected intestinal barrier function by increasing Occludin and ZO-1, and attenuated colonic and systemic inflammation by suppressing production of IL-1β and IL-6. Finally, the use of MLF remodeled the diversity of the gut microbiota and increased the number of beneficial microorganisms. Overall, the results demonstrated that MLF relieved DSS-induced UC in mice. And MLF might be an effective therapy method to UC in the clinic in the future.
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ANALYST
·
2018
·Vol. 143
·期 11
·2501-2507
·
IF 3.864
Yong Liu,Xiaolin Xu,Haitang Yang,Ensheng Xu,Shuangshuang Wu,Wei Wei,Jin Chen
Poly(ADP-ribose) polymerase-1 (PARP-1) is a highly conserved nuclear enzyme, which binds tightly to damaged DNA and plays a key role in DNA repair, recombination, proliferation, and genomic stability. However, due to the poor electrochemical and optical activity of PARP-1 and its product PAR, only a few studies on its activity detection method have been reported. Herein, we report a simple and sensitive colorimetric strategy to monitor PARP-1 activity based on enzyme-initiated auto-PARylation-controlled aggregation of hemin-graphene nanocomposites (H-GNs). PARP, activated by dsDNA, catalyzed its substrate nicotinamide adenine dinucleotide (NAD+) to polymerize as a poly(ADP-ribose) polymer (PAR). PAR possesses several negative charges, and its charge density is twice that of a single-stranded DNA, which greatly impacts the dispersibility of H-GNs; due to their peroxidase-like catalytic activities, H-GNs can catalyze the chromogenic reaction of TMB and H2O2. As a result, in the presence of different PARP-1 activities, the supernatant of the corresponding solution contained different amounts of dispersed H-GNs and showed different colors after the chromogenic reaction that could be discerned easily by the absorbance or the color changes of the solution. The method was simple, sensitive, and reliable. The proposed method displays a linear range from 0.05 to 1 U with a detection limit of 0.03 U. In addition, this new method has been successfully applied to detect PARP-1 activity in human serum and different cancer cells and evaluate PARP-1 inhibitors.
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Frontiers in Physiology
·
2017
·
IF 4.134
Jiang Jianru,Xu Yili,Lin Xinda
Ovarian development plays an important role in the life history of insects and is crucial for control of the insect population. The metamorphosis of an insect is precisely regulated by the interaction of the juvenile hormone and ecdysone. To understand the role of NlBr and NlKr-h1 in ovary development, we used RNA interference (RNAi) to down-regulate the expression of Broad-Complex (Br) and Krüppel homolog 1 (Kr-h1), two important down-stream transcription factors of juvenile hormone and ecdysone signaling. We further investigated their effects on metamorphosis and ovary development. The results showed that both NlBr and NlKr-h1 are induced by ecdysone. The down-regulation of NlBr and NlKr-h1 alone or together by RNAi is more effective than the topical application of ecdysone on the number of ovarioles, suggesting the necessity of NlBr and NlKr-h1 in determining the number of ovarioles. The ovarian grade was significantly increased/decreased by the topical application of ecdysone and down-regulation of NlBr and NlKr-h1. The pre-oviposition period was also increased. When NlBr and NlKr-h1 were down-regulated together, the ovary grade was not significantly different compared to the control (dsGFP), indicating that the development of the ovary is under the control of both NlBr and NlKr-h1. The interaction between the NlBr and NlKr-h1 on the number of ovarioles and the development of the ovary indicates cross-talk between both juvenile hormone and ecdysone signaling at the transcription level in the brown planthopper. Both genes are nuclear transcription factors and may regulate signaling via down-stream genes. These results would help to both enhance the current understanding of the regulatory mechanism of the interaction between juvenile hormone and ecdysone signaling pathways during ovarian development and to design chemicals to control pests.
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JOURNAL OF CELLULAR PHYSIOLOGY
·
2018
·Vol. 234
·期 5
·6136-6146
·
IF 3.923
Yucang He,Xiaofang Yu,Zhuojie Chen,Liqun Li
Autologous fat transplantation is increasingly applied in plastic and reconstructive surgery. Stromal vascular fraction cells (SVFs) combined with angiogenic factors, such as VEGF (vascular endothelial growth factor A) and Ang-1 (angiogenin-1), can improve angiogenesis, which is a critical factor for graft survival. However, direct transplant with such a mixture is insufficient owing to the short half-life of angiogenic factors. In this study, we evaluated whether a double sustained release system of VEGF/ANG-1-PLGA (poly (lactic-co-glycolic acid)) microspheres plus SVFs can improve angiogenesis and graft survival after autologous fat transplantation. VEGF/ANG-1-PLGA-sustained release microspheres were fabricated by a modified double emulsion–solvent evaporation technique. Human aspirated fat was mixed with SVF suspension plus VEGF/ANG-1 sustained release microspheres (Group C), SVF suspension (Group B) alone, or Dulbecco’s modified Eagle’s medium as the control (Group A). Eighteen immunocompromised nude mice were injected with these three mixtures subcutaneously at random positions. After 8 weeks, the mean volume of grafts was greater in the SVFs plus VEGF/ANG-1-PLGA group than in the control and SVFs groups (1.08 ± 0.069 ml vs. 0.62 ± 0.036 ml, and 0.83 ± 0.059 ml, respectively). Histological assessments showed that lower fibrosis, but greater microvascular density in the SVFs plus VEGF/ANG-1-PLGA group than in the other groups, though the SVFs group also had an appropriate capillary density and reduced fibrosis. Our findings indicate that SVFs plus VEGF/ANG-1-PLGA-sustained release microspheres can improve angiogenesis and graft survival after autologous fat transplantation.
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ChemCatChem
·
2025
·
IF 3.9
Qian Li,Jie Zhang,Tong Yu,Jinwei Chen,Gang Wang,Zongbo Shi,Runsheng Zhuo,Ruilin Wang
Propane dehydrogenation (PDH) is a pivotal technology for propylene production. Supported Pt catalysts for PDH are often subjected to nanoparticle agglomeration and coke deposition, thus limiting their stability and efficiency. Herein, we constructed a high-performance Pt-Ce catalyst consisting of CeO x with redox properties and active Pt species with the regulated electronic properties. Through the controllable impregnation, the unique structure of adjacent Pt-CeO x sites were elaborately supported on the Mn-modified Silicalite-1 (Mn-S-1). Characterization results reveal that the generated Ce 3+ /V O species contribute to the formation of electron-deficient Pt 0 -V O -Ce 3+ active sites via hydrogen spillover and electron transfer. Benefiting from the high dispersion of active components, appropriate acidity, redox activity of V O , and electron-deficient Pt 0 sites, the optimal 0.5Pt0.2Ce/Mn-S-1 catalyst exhibits superior propane conversion of 38.23%, propylene selectivity of 88.45%, and excellent coke resistance. This study not only reveals the intrinsic correlation between active Pt and CeO x species but also provides valuable guidance for designing highly efficient catalysts. Graphical A high-performance Pt-Ce catalyst consisting of CeO x with redox properties and active Pt species with the regulated electronic properties was constructed through a controllable impregnation. Benefiting from the high dispersion of active components, appropriate acidity, redox activity of V O , and electron-deficient Pt 0 sites, the optimal 0.5Pt0.2Ce/Mn-S-1 catalyst exhibits superior propane dehydrogenation performance.
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