MEDICINAL CHEMISTRY RESEARCH
·
2022
·Vol. 32
·期 2
·288-313
·
IF 2.351
Zhang Yuanwen,Zheng Yueming,Wu Qingqing,Tian Fuyun,Ma Chuanjun,Xu Haiyan,Zhan Li,Gao Zhaobing,Zhao Guilong,Ti Huihui
A clinical therapy for chronic neuropathic pain is urgently needed, and the voltage-gated calcium channel (VGCC) α2δ subunit is among the most promising therapeutic targets. To intensively explore the structure-activity relationship (SAR) of the lipophilic moiety in VGCC α2δ subunit ligands (gabapentinoids), we designed and synthesized 11 bicyclic and monocyclic derivatives based on mirogabalin, a third-generation VGCC α2δ subunit ligand. The competitive binding of the synthesized compounds to the human VGCC α2δ-1 subunit was measured in vitro, and the results demonstrated that the lipophilic moiety size was strictly limited in gabapentinoids, in which conformationally rigid bicylo[3.2.0]heptane/heptene with a cis -fusion was the most preferred structure. In contrast, monocyclic cyclobutane was associated with a markedly decreased binding affinity except in 4 (IC 50 = 15.2 nM), in which the substituents could mimic the rigid conformation of bicylo[3.2.0]heptane/heptene; heteroatoms in the lipophilic moiety were detrimental to the binding affinity ( 2 , IC 50 > 729 nM). The SAR findings obtained in the present study will be valuable for designing novel gabapentinoid drugs to treat chronic neuropathic pain in the future. Graphical abstract
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Science China-Life Sciences
·
2022
·Vol. 66
·期 7
·1569-1588
·
IF 10.372
Ma Ning,Guo Pingting,Chen Jingyu,Qi Zengkai,Liu Chunchen,Shen Jiakun,Sun Yiwei,Chen Xiyue,Chen Guo-Qiang,Ma Xi
Maintainance of sulfomucin is a key end point in the treatment of diarrhea and inflammatory bowel disease (IBD). However, the mechanisms underlying the microbial sense to sulfomucin are poorly understood, and to date, there are no therapies targeting the secretion and maturation of sulfomucin in IBD. Herein, we biosynthesized poly-β-hydroxybutyrate (PHB) and found that PHB could alleviate inflammation caused by diarrhea and colitis by enhancing the differentiation of sulfomucin. Microbiota transplantation and clearance together demonstrate that PHB promoting sulfomucin is mediated by Lactobacillus johnsonii ( L. johnsonii ). Further studies revealed that PHB provides a favorable niche for L. johnsonii biofilm formation to resist disturbance and support its growth. L. johnsonii -biofilm alleviates colitis by regulating fucose residues to promote goblet cell differentiation and subsequent sulfomucin maturation. Importantly, PHB alleviates colitis by enhancing sulfomucin secretion and maturation in a L. johnsonii -dependent manner. PHB represents a class of guardians, acting as a safe probiotic-biofilm delivery system that significantly promotes probiotic proliferation. Altogether, this study adds weight to the possible role of probiotics and functional materials in the treatment of intestinal inflammation. The application of PHB and biofilm self-coating L. johnsonii carries high translational potential and may be of clinical relevance.
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PubMed
高影响因子
NEUROCHEMICAL RESEARCH
·
2022
·Vol. 48
·期 2
·625-640
·
IF 4.414
Hui Yuzuo,Zhao Han,Shi Lei,Zhang Haitao
8-Methoxypsoralen (8-MOP) has anti-inflammatory, antioxidant and tissue-repairing abilities. Here, we probed the function and mechanism of 8-MOP in traumatic brain injury (TBI). The in - vivo TBI model was constructed in Sprague-Dawley (SD) rats using controlled cortical impact (CCI) surgery. In parallel, BV2 microglia and HT22 neurons were activated by lipopolysaccharide (LPS) to establish an in-vitro model. The modified neurological score (mNSS) and the Morris water maze experiment were employed to evaluate the rats’ neurological functions. The rats’ brain edema was assessed by the dry and wet method, and neuronal apoptosis in damaged brain tissues was monitored by terminal deoxynucleotidyl transferase-mediated dUTP-biotin nick end labeling (TUNEL) and Nissl’s staining. Immunohistochemistry (IHC) was applied to verify Iba1-microglial activation in brain lesions of rats. The expression of inflammatory cytokines in BV2 microglia and HT22 neurons in the injured lesion of TBI rats was examined by the enzyme-linked immunosorbent assay (ELISA). The levels of iNOS, COX2, TLR4, PPARγ, STAT3, and NF-κB in brain lesions, BV2 microglia and HT22 neurons were compared by Western blot. As a result, 8-MOP administration reduced inflammation and LPS-induced neuronal damage in BV2 microglia. In vivo, 8-MOP treatment relieved neurological deficits in TBI rats, improved cognitive, learning and motor functions and mitigated brain edema and neuroinflammation induced by TBI. Furthermore, LPS or TBI activated the NF-κB and STAT3 pathways and repressed the PPARγ expression. However, 8-MOP treatment attenuated NF-κB and STAT3 phosphorylation and elevated PPARγ levels. Hence, 8-MOP exerts neuroprotective and anti-inflammatory effects in TBI rats by modulating the PPARγ/NF-κB pathway.
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高影响因子
Journal of Analysis and Testing
·
2018
·Vol. 2
·期 4
·332-341
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IF 0
Wei Yin Hui,Li Xin Yu,Gao Jie,Liu Jia Jun,Yuan Dan,Yin Bin Cheng,Wang Jian
As an antibiotic, tetracycline has been widely used against bacterial infection or as feed additives for growth promotion, which may lead to the enrichment of antibiotic residues in animals or their products. Therefore, the detection of tetracycline is closely related to human health. The morphological transformation of CoOOH nanoflakes induced by tetracycline was monitored by scanning electron microscope images, dark-field light scattering images and optical spectra, which found that tetracycline could decompose CoOOH nanoflakes into small nanoparticles with low light scattering signal. As a result, the reduced light scattering of CoOOH nanoflakes was proportional to the increased concentration of tetracycline in the range of 1.0–250 μmol/L, and the limit of determination (LOD) was 0.23 μmol/L (3σ/k). Most foreign substances did not interfere in the analysis of tetracycline. Furthermore, the concentration of tetracycline in different milk samples detected with the standard addition method was so low that it accorded with the safety regulation, which was similar to the detection result with high-performance liquid chromatography (HPLC).
研究领域:
分析化学
·
纳米技术
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食品安全
·
药物分析
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JOURNAL OF MATERIALS SCIENCE
·
2019
·Vol. 54
·期 7
·5961-5970
·
IF 3.442
Luo Shuai,Qiao Xuan,Wang Qiu-Yu,Zhang Yun-Fei,Fu Ping,Lin Zhi-Dong,Du Fei-Peng,Cheng Chun
To develop low-cost and high-performance self-healing antifogging coatings, polyvinyl alcohol/hydrolyzed poly(styrene-co-maleic anhydride) (PVA/H-PSMA) coatings were prepared from a mixed solution of polyvinyl alcohol (PVA) and hydrolyzed poly(styrene-co-maleic anhydride) (H-PSMA) via spin coating and annealing. The microstructure, antifogging behavior, and self-healing ability were investigated. High transparency and low surface roughness were observed when the PVA/H-PSMA film was coated on glass slides. The PVA/H-PSMA coatings showed excellent antifogging performance in a warm, humid environment. The coatings also performed well when transferred from a refrigerator to room temperature. The antifogging coatings showed desirable water resistance due to strong chemical bonding between PVA and H-PSMA, as well as excellent self-healing ability due to hydrogen bonding self-assembly in the PVA/H-PSMA structure. The coatings still exhibited excellent antifogging effects after 20 scratching-repairing cycles, illustrating their potential use in practical applications.
研究领域:
材料科学
·
表面化学
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高影响因子
FIBERS AND POLYMERS
·
2022
·Vol. 23
·期 4
·1040-1049
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IF 2.347
Jin Liang,Qian Tao,Zhu Tao,Wang Ren-Liang,Chen Wei-Guo,Jiang Hua,Cui Zhi-Hua
Carboxylic acid ester disperse dyes containing an azo pyridone structure have a high molar extinction coefficient, excellent washing color fastness, and simple synthetic methods. Dyes were readily synthesized through a conventional diazo coupling reaction between the reactant ethyl p -aminobenzoate and a coupling component containing an azo pyridone structure. Subsequently, the molecular structures of the target products were characterized by FTIR, mass spectrometry, 1 H NMR, 13 C NMR, UV-vis absorption spectroscopy, and elemental analysis. The synthesized dyes were used to dye poly(ethylene terephthalate) fabric, and their washing and rubbing color fastness properties were tested and compared under different post-treatment methods. Moreover, under the condition of alkali clearing, the relationships among different alkali concentrations and clearing effects were studied to determine the optimal alkali clearing process conditions for dyed fabrics, and the minimum alkali consumption required to obtain the best results was determined. It was found that carboxylic ester disperse dyes containing an azo pyridone structure showed good dyeing performance and alkali-clearable properties on polyester fibers. In addition, in hydrolyzate recovery, BaCl 2 (salting out) can be used instead of acidification to recover the dye hydrolyzate, which has good environmental benefits.
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JOURNAL OF NANOBIOTECHNOLOGY
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2026
·
IF 15
Pang Wenyang,Cao Yin,Du Shuang,Liang Zuowen,Wang Hongliang,Liu Lingyun
Background Tire wear particles (TWPs) are a major source of micro- and nanoplastics. However, reports on nanoscale tire wear particles, especially regarding their potential hazards to the male reproductive system, remain scarce. Results Here, we examined whether nanoscale tire wear particles impair spermatogenesis and blood-testis barrier integrity through ROS-linked ferroptotic injury. Using a 70-day oral exposure model in pubertal male mice and complementary GC-2 and TM4 cell models, we found that high-dose particle exposure reduced epididymal sperm density, increased sperm abnormalities, disrupted seminiferous epithelial organization, and increased BTB permeability. TWPs shifted metabolomic profiles toward lipid and iron dysregulation, suppressed SLC7A11/GPX4, increased ACSL4 and labile Fe²⁺, and depleted junctional proteins. Ferrostatin-1 reduced lipid peroxidation, iron accumulation, cell death, and junctional protein loss, indicating a functional contribution of ferroptosis. Mechanistically, TWPs first induced total and mitochondrial reactive oxygen species and mitochondrial depolarization, which were restrained by N-acetylcysteine. Downstream, autophagic ferritin degradation amplified ferroptotic injury, as chloroquine or NCOA4 knockdown preserved ferritin, reduced malondialdehyde accumulation, restored GPX4/SLC7A11, and improved viability. NCOA4 depletion did not substantially blunt ROS induction, placing ferritinophagy after redox imbalance. Conclusions Together, these data define a ROS-initiated, NCOA4-dependent ferritinophagy-ferroptosis axis that connects nanoscale TWPs to BTB failure and impaired spermatogenic homeostasis. This work provides a mechanistic basis for future assessment of reproductive health risks associated with TWPs exposure. Graphical abstract
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高影响因子
Phytopathology Research
·
2026
·Vol. 8
·期 1
·65
·
IF 4.3
Tang Jiejing,Zhou Hang,Jiao Chen,Li Hongye
Alternaria alternata tangerine pathotype causes Alternaria brown spot, a major fungal disease threatening citrus production in susceptible cultivars. This pathogen produces the host-specific toxin Alternaria citri toxin (ACT), which serves as the primary virulence factor. However, the regulatory mechanisms controlling ACT biosynthesis remain largely unclear. Here, we characterized the biological functions of the transcription factor AaSom1 and explored its target genes involved in ACT synthesis. Deletion of AaSom1 significantly reduced mycelial growth rate, abolished sporulation, suppressed ACT production, and eliminated pathogenicity. Both the LisH and Med15 domains of AaSom1 are essential for its complete biological function. RNA-seq, ChIP-seq, and DAP-seq analyses revealed that AaSom1 directly binds to the promoter of AapksA, which encodes a polyketide synthase involved in DHN-melanin biosynthesis, and subsequently activates AapksA transcription. AapksA deletion did not affect mycelial growth but significantly reduced conidiation, ACT production, lesion expansion rate, and pathogenicity. Collectively, AaSom1 functions as a multifunctional transcription factor that regulates development and pathogenicity, with AapksA as a key downstream target in A. alternata . These findings reveal a novel regulatory pathway that controls fungal pathogenesis through AaSom1-mediated transcriptional regulation.
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高影响因子
Nature Chemical Biology
·
2022
·Vol. 18
·期 11
·1196-1203
·
IF 16.174
Lin Hui,Xiao Peng,Bu Rui-Qian,Guo Shengchao,Yang Zhao,Yuan Daopeng,Zhu Zhong-Liang,Zhang Chuan-Xin,He Qing-Tao,Zhang Chao,Ping Yu-Qi,Zhao Ru-Jia,Ma Chuan-Shun,Liu Chang-Hao,Zhang Xiao-Ning,Jiang Dan,Huang Shaohui,Xi Yue-Tong,Zhang Dao-Lai,Xue Chen-Yang,Yang Bai-Sheng,Li Jian-Yuan,Lin Hao-Cheng,Zeng Xu-Hui,Zhao Han,Xu Wen-Ming,Yi Fan,Liu Zhongmin,Sun Jin-Peng,Yu Xiao
Adhesion G protein-coupled receptors are elusive in terms of their structural information and ligands. Here, we solved the cryogenic-electron microscopy (cryo-EM) structure of apo-ADGRG2, an essential membrane receptor for maintaining male fertility, in complex with a G s trimer. Whereas the formations of two kinks were determinants of the active state, identification of a potential ligand-binding pocket in ADGRG2 facilitated the screening and identification of dehydroepiandrosterone (DHEA), dehydroepiandrosterone sulfate and deoxycorticosterone as potential ligands of ADGRG2. The cryo-EM structures of DHEA–ADGRG2–G s provided interaction details for DHEA within the seven transmembrane domains of ADGRG2. Collectively, our data provide a structural basis for the activation and signaling of ADGRG2, as well as characterization of steroid hormones as ADGRG2 ligands, which might be used as useful tools for further functional studies of the orphan ADGRG2.
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高影响因子
Journal of Central South University
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2026
·
IF 4.7
Ma Zhi-yuan,Wang Jing,Feng Jia-ming,Chen Chang-hao,Jiang Xin-yu,Wang Hai-bo,Zhou Liu-jiang,Guo Bing-shu,Chen Jun-chen,Yu Bo,Zhang Jin,Zhang Jing
Transition metal oxides are promising cathode catalysts for lithium – oxygen batteries owing to their low cost and high catalytic activity. However, conventional synthesis methods often lead to particle agglomeration, limited active-site exposure, and poor structural control. In this work, 1,3,5-benzenetricarboxylic acid (H 3 BTC) was used to coordinate Co, Cu, Mn, and Ni ions to form metal – organic framework (MOF) precursors, followed by calcination at 400 °C to obtain MOF-derived metal oxide catalysts. This MOF-derived strategy effectively alleviates particle agglomeration, preserves advantageous structural features, and enables a systematic comparison of the influence of different metal centers on catalyst structure and electrochemical behavior. Among the as-prepared catalysts, Co-BTC-400 exhibits a hierarchical hollow microsphere structure and delivers a high specific capacity of 30980 mAh g −1 at 200 mA g −1 , with stable cycling over 1000 cycles at 500 mA g −1 . Density functional theory calculations reveal moderate Li 2 O 2 adsorption and a reduced OER energy barrier on Co active sites. This work provides valuable insight into the design of MOF-derived transition metal oxide cathode catalysts for lithium – oxygen batteries.
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高影响因子
npj Science of Food
·
2026
·
IF 9.7
Jin Hongchen,Bai Huasong,Liu Tong,Wang Hengyan,Yin Yulong,Ruan Siyu,Li Yunliang,Wang Zhanzhong
Anti-aging bioproducts from natural active ingredients represent a core future direction in food research. Cardiovascular aging drives most age-related disorders. This study investigated the anti-aging effects of a postbiotic preparations derived from brown algae extract fermented by Bifidobacterium adolescentis Life Age 20 (LA20FM). Multi-model were used, including doxorubicin (DOX)-induced senescent canine (CVECs) and feline vascular endothelial cells (FVECs), senescence-accelerated mouse prone 8 (SAMP8) mice, Caenorhabditis elegans , and naturally aged dogs and cats. In vitro, LA20FM markedly attenuated DOX-induced endothelial senescence, reduced the secretion of senescence-associated secretory phenotype factors, and restored endothelial function-related markers. In aged SAMP8 mice, LA20FM alleviated vascular remodeling, reduced circulating senescence- and inflammation-related biomarkers, and improved physiological performance. In C. elegans , LA20FM extended lifespan by approximately 30%, enhanced reproductive capacity, and significantly reduced intracellular reactive oxygen species levels. Comparable improvements in physiological parameters were also observed in aged dogs and cats. Transcriptomic analyses of CVECs and SAMP8 vascular tissues revealed that LA20FM treatment was accompanied by downregulation of NF-κB-related inflammatory signaling. Phorbol 12-myristate 13-acetate rescue experiments and early time-point analyses further supported NF-κB signaling as an early and functionally important mediator of its protective effects. Metabolomic analysis further revealed metabolic remodeling characterized by reduced lipid-associated metabolic activity and enhanced amino acid biosynthesis and antioxidant-related metabolism. Collectively, these findings indicate that LA20FM alleviates canine and feline vascular endothelial senescence and improves aging-associated phenotypes across multiple experimental models, supporting its potential as a postbiotic preparation for canine and feline nutritional intervention against vascular functional decline and further aging.
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高影响因子
ANALYTICAL AND BIOANALYTICAL CHEMISTRY
·
2026
·
IF 4.1
Chu Shiqi,Yang Lian,Chi Zhongmei,Ma Jiahui,Wang Huanxiang,Yan Lihe,Li Zhaoye,Liu Guocheng
Dopamine (DA) in bovine serum served as a vital physiological biomarker for evaluating livestock health status and conducting translational biomedical research. Accurate and rapid detection of DA was therefore essential for agricultural breeding monitoring and clinical biological analysis. In this work, a novel Hemin@P 2 Mo 18 nanocomposite with peroxidase-mimicking activity was successfully prepared via a facile, green solvent-free grinding strategy. The introduction of water-soluble H 6 P 2 Mo 18 effectively suppressed the aggregation of free hemin molecules and yielded solid-phase Hemin@P 2 Mo 18 . Relative to natural peroxidases, the synthesized Hemin@P 2 Mo 18 featured convenient recovery and excellent reusability. Given the excellent peroxidase-mimicking activity of Hemin@P 2 Mo 18 , a sensitive and selective colorimetric platform was constructed for DA detection. Moreover, the proposed approach showed high selectivity against common interfering substances and excellent stability under different conditions. It was successfully applied to the quantitative determination of DA in bovine serum samples with satisfactory recovery rates ranging from 96.8% to 100.2%. This study provided a green and efficient solvent-free grinding synthesis strategy for high-performance POM-based nanozymes. It also offered a feasible and practical approach for rapid biomarker detection in complex biological matrices, which showed great application potential in veterinary monitoring and biosensing analysis. Graphical abstract
The schematic representation of the synthesis of Hemin@P 2 Mo 18 and the dual-mode detection of dopamine.
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