INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
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2022
·Vol. 24
·期 1
·64
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IF 6.208
Lini Huo,Xiaochen Liu,Yogini Jaiswal,Hao Xu,Rui Chen,Rumei Lu,Yaqin Nong,Leonard Williams,Yan Liang,Zhiruo Jia
We report herein the design and synthesis of a series of novel acridine-triazole and acridine-thiadiazole derivatives. The newly synthesized compounds and the key intermediates were all evaluated for their antitumor activities against human foreskin fibroblasts (HFF), human gastric cancer cells-803 (MGC-803), hepatocellular carcinoma bel-7404 (BEL-7404), large cell lung cancer cells (NCI-H460), and bladder cancer cells (T24). Most of the compounds exhibited high levels of antitumor activity against MGC-803 and T24 but low toxicity against human normal liver cells (LO2), and their effect was even better than the commercial anticancer drugs, 5-fluorouracil (5-FU) and cis-platinum. Further, pharmacological mechanisms such as topo I, cell cycle, cell apoptosis, and neovascularization were all evaluated. Only a few compounds exhibited potent topo I inhibitory activity at 100 μM. In addition, the most active compounds with an IC50value of 5.52–8.93 μM were chosen, and they could induce cell apoptosis in the G2 stage of MGC-803 or mainly arrest T24 cells in the S stage. To our delight, most of the compounds exhibited lower zebrafish cytotoxicity but could strongly inhibit the formation of zebrafish sub-intestinal veins, indicating a potential for clinical application.Keywords:acridine-triazole;acridine-thiadiazole;topoisomerase I;anti-angiogenesis;zebrafish
研究领域:
肿瘤学
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药理学
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分子生物学
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化学
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EXPERIMENTAL NEUROLOGY
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2020
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IF 4.691
Shuai Zhang,Mei-Ling Yan,Lin Yang,Xiao-Bin An,Hong-Mei Zhao,Sheng-Nan Xia,Zhuo Jin,Si-Yu Huang,Yang Qu,Jing Ai
Chronic cerebral hypoperfusion (CCH) promotes the development of Alzheimer's pathology. However, whether and how CCH impairs the synaptic vesicle trafficking is still unclear. In the present study, we found that the hippocampal glutamatergic vesicle trafficking was impaired as indicated by a significant shortened delayed response enhancement (DRE) phase in CA3-CA1 circuit and decreased synapsin I in CCH rats suffering from bilateral common carotid artery occlusion (2VO). Further study showed an upregulated miR-153 in the hippocampus of 2VO rats. In vitro, overexpression of miR-153 downregulated synapsin I by binding the 3′UTRs of SYN1 mRNAs, which was prevented by its antisense AMO-153 and miRNA-masking antisense oligodeoxynucleotides ( SYN1-ODN ). In vivo , the upregulation of miR-153 elicited similar reduced DRE phase and synapsin I deficiency as CCH. Furthermore, miR-153 knockdown rescued the downregulated synapsin I and shortened DRE phase in 2VO rats. Our results demonstrate that CCH impairs hippocampal glutamatergic vesicle trafficking by upregulating miR-153 , which suppresses the expression of synapsin I at the post-transcriptional level. These results will provide important references for drug research and treatment of vascular dementia .
研究领域:
神经科学
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分子生物学
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神经退行性疾病
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BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
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2021
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IF 3.575
Dequan Kong,Baoying Xie,Yuhang Li,Yaping Xu
Palmitoylethanolamide (PEA) offers a strong protection against BBB disruption and neurological deficits after cerebral ischaemic/reperfusion (I/R) injury. To date, these BBB protective effects of PEA are mainly attributed to PPARα-mediated actions. However, whether PEA protects against BBB disruption through direct regulation of cytoskeletal microfilaments remains unknown. Here, we identified PEA as a Rho-associated protein kinase (ROCK2) inhibitor (IC 50 = 38.4 ± 4.8 μM). In vitro data suggested that PEA reduced the activation of ROCK/MLC signaling and stress fiber formation within microvascular endothelial cells (ECs) after oxygen-glucose deprivation (OGD), and consequently attenuated early (0–4 h) EC barrier disruption. These actions of PEA could not be blocked by the PPARα antagonist GW6471. In summary, the present study described a previously unexplored role of PEA as a ROCK2 inhibitor, and propose a PPARα-independent mechanism for pharmacological effects of PEA.
研究领域:
神经科学
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药理学
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细胞生物学
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Journal of Functional Foods
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2020
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IF 3.701
Zhenbang Xiao,Shengtao Yang,Jiali Chen,Chengyong Li,Chunxia Zhou,Pengzhi Hong,Shengli Sun,Zhong-Ji Qian
Ultraviolet radiation B cause photoaging of the skin by enhancing the high expression of matrix metalloproteinases (MMPs) to degrade collagen and inhibit the synthesis of procollagen. Trehalose (TRE), a widely occurring natural disaccharide, has been shown to play a cytoprotective role in many pathological processes. However, few studies have evaluated whether it has anti-photoaging potential. In this study, we investigated the anti-photoaging and mechanism of action of TRE using Human immortalized keratinocytes (HaCaT) cells. The results indicated that TRE pretreatment effectively scavenges reactive oxygen species (ROS) accumulation induced by UVB and increases the content of certain endogenous antioxidant factors in HaCaT cells. TRE suppressed UVB-induced MMP expression by blocking mitogen-activated protein kinases (MAPKs), activator protein 1 (AP-1) and NF-κB signaling. TRE treatment increased procollagen I synthesis via activating transforming growth factor-β (TGF-β)/Smad pathway and demonstrated that TRE may be a potential natural disaccharide for photoaging therapy in the future.
研究领域:
皮肤科
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细胞生物学
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药理学
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DENTAL MATERIALS
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2026
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IF 6.3
Zhiwen Liu,Danni Wang,Leiqing Zhang,Yuan Xie,Taoyu Chen,He Wen,Wenjia Chen,Baiping Fu,Ruikang Tang,Hongqiang Cheng,Zhe Wang
Mineralization of reconstituted type I collagen and demineralized dentin exhibited a biphasic concentration-dependent response to Sr²⁺. • Higher intrafibrillar mineralization was observed at 0.1–0.5 mM Sr²⁺, whereas lower levels were observed at 0.75–1 mM Sr²⁺. • Dentin mineralization showed a similar trend consistent with the collagen observations. • A Sr²⁺ concentration-dependent hypothesis is proposed for ion-regulated biomineralization. Objectives To investigate the concentration-dependent effects of strontium on the mineralization of reconstituted type I collagen and demineralized dentin remineralization. Methods Sr²⁺ at varying concentrations (0, 0.1, 0.25, 0.5, 0.75, 1 mM) was incorporated into polyacrylic acid-stabilized amorphous calcium phosphate (PAA-ACP) mineralization solutions. The mineralization solutions with 1 mM Sr²⁺ were characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier-transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD). Cytocompatibility was assessed using the CCK-8 assay. Reconstituted type I collagen and demineralized dentin models were employed to explore mineralization differences; high-resolution TEM (HRTEM) and selected area electron diffraction (SAED) were applied to investigate the underlying biphasic mineralization mechanism of Sr²⁺. Results In the reconstituted type I collagen model, early crystalline mineralization was detected at 12 h in the 0.25 mM group, while 0.5 mM Sr²⁺ induced more ordered apatite crystal alignment along the collagen long axis. The observed lattice expansion ( d -spacings of 0.35–0.37 nm and 0.29 nm) was consistent with the formation of Sr-containing apatite-like mineral. At ≥ 0.75 mM Sr²⁺, the minerals deposited preferentially on the fibril surface replaced intrafibrillar mineralization. In the demineralized dentin model, a consistent biphasic concentration-dependent pattern was observed: 0.1–0.5 mM Sr²⁺ was associated with increased density of the remineralized layer and enhanced dentinal tubule occlusion, the enlarged lattice spacing ( d -spacings of 0.35 nm) was consistent with that observed in the reconstituted type I collagen model. In contrast, 0.75–1 mM Sr²⁺ was associated with reduced remineralization and intratubular mineral filling. Both the collagen and dentin models suggested the biphasic effect of strontium on biomimetic mineralization. Significance Sr²⁺ shows a biphasic concentration-dependent response on collagen mineralization and dentin remineralization. These findings provide preliminary concentration-response information for the rational design of Sr-containing biomimetic materials. Download: Download high-res image (196KB) Download: Download full-size image
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Results in Chemistry
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2026
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IF 5.8
Xianping Luo,Sihao Yu,Hepeng Zhou,Yongbing Zhang,Jin-Ru Feng
Porous biochar derived from discarded corn stalks was developed as a regenerable adsorbent for treating Tl-containing wastewater. The Tl adsorption capacity of Fe–Mn–Y doped biochar (FMYBC) was significantly enhanced compared to unmodified biochar. The IPD model accurately described Tl(I) adsorption on FMYBC, indicating that intraparticle diffusion is a key controlling step. Removal efficiency remained largely stable over a broad initial pH range of 3–13. Doping with rare earth elements markedly improved the adsorption performance of Fe Mn modified biochar under acidic conditions. However, the presence of coexisting ions (Na + , Mg 2+ , Ca 2+ ) reduced FMYBC's Tl + adsorption capacity. After two adsorption–desorption cycles, MFYBC retained 86.4% of its initial Tl removal capacity, demonstrating good stability and regeneration potential. Based on XPS and FTIR analyses, the primary Tl(I) removal mechanisms include ion exchange, surface complexation, and oxidation.
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ADVANCED MATERIALS
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2026
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IF 29.1
Haoyang Guan,Luxuan Men,Zhuoer Cai,Yiping Du,Qingsong Hu,Taifeng Lin,Feng Luo,Zhengguang Yan,Jiawen Xiao
Copper(I)-based halides are promising for X-ray detection due to their excellent scintillation efficiency and solution processability. However, the structure–property relationship remains elusive, and their practical viability for X-ray imaging is largely unverified. In this work, we employ a bond‑mode control strategy to synthesize two compounds from the same amine precursor: ionic (4‑ATHP) 2 CuI 3 and coordinative (4‑ATHP) 4 Cu 4 I 4 (4-ATHP = 4-Aminotetrahydropyran), providing a model system to study their photophysics and underlying mechanism. (4‑ATHP) 2 CuI 3 adopts a unique 1D crystal structure with alternating arrangement of Cu 2 I 6 dimers, which shows excitation‑dependent dual emissions. Experimental and calculation results indicate that the dual emissions originate from the Cu 2 I 6 dimer with a different Cu─Cu bond length. In contrast, the (4‑ATHP) 4 Cu 4 I 4 shows single emission centered at 635 nm, in which the organic component contributes to the excited state. The ionic (4‑ATHP) 2 CuI 3 achieves a much higher light yield (55 923 photons/MeV) than that of the coordinative counterpart (31 866 photons/MeV). Furthermore, a large‑area flexible film (15 × 20 cm 2 ) based on (4‑ATHP) 2 CuI 3 delivers a spatial resolution of 20 lp/mm. Critically, integrating this film into a CMOS imager demonstrates superior dynamic imaging without afterglow, outperforming the commercialized CsI: Tl screen. This study not only deciphers the bond‑mode‑dependent photophysics but also validates a commercial‑grade scintillator, paving the way for high‑performance X‑ray imaging materials.
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Advanced Healthcare Materials
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2026
·
IF 11
Jinling Zheng,Yingying Ke,Dandan Meng,Marie Helene Delville,Shiwen Yu,Yiteng Huang,Xiaoyu Xu,Xu Zhang,Shayibai Shabiti,Na Liang,Yujue Wang,Fangjie Li,Hongfei Chen,Wenjun Li
Sono-photodynamic therapy (SPDT) offers a non-invasive, spatiotemporally precise approach to cancer treatment, but its effectiveness is still limited by poor tumor specificity and penetration. To address this, we developed a cascade-targeted type I/II sensitizer, Ce6-TPP-Phe-Tyr (CTPT), which integrates chlorin e6 (Ce6), triphenylphosphonium (TPP), and a phospho-peptide motif for precise tumor targeting and potent SPDT. Upon dephosphorylation by tumor-overexpressed alkaline phosphatase (ALP), CTPT undergoes enzyme-instructed self-assembly (EISA) into nanoparticles (CTPT NPs), promoting their accumulation and retention in tumors. The TPP cations then guide these nanoparticles to mitochondria, concentrating the therapeutic payload at this critical organelle for cellular energy metabolism. Subsequent ultrasound/laser irradiation further enhances tissue permeability and triggers the generation of both type I and type II reactive oxygen species (ROS), leading to potent oxidative damage. This integrated strategy of EISA and mitochondria-targeted SPDT achieved approximately 86% tumor regression in ALP-overexpressing xenografts. This strategy minimizes systemic toxicity and achieves potent tumor regression by cascade delivery of the therapeutic agent, thereby significantly enhancing the precision and efficacy of SPDT.
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BIOELECTROCHEMISTRY
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2026
·
IF 4.9
Huang Wei,Xu Yiwei,Guo Yaojie,Chen Dingyao,Ren Wenjie,Suo Zhiguang,He Baoshan
In this work, a novel electrochemical aptasensor was constructed for the sensitive detection of DON by integrating the synergistic effect between the catalytic signal enhancement of Cu-Pt NPs and Exo I-assisted cyclic amplification, with an MWCNTs-AuNPs modified electrode serving as the sensing platform. Cu-Pt NPs with outstanding peroxidase-like catalytic activity were synthesized and used as signal probes to catalyze the substrate, generating significantly enhanced electrochemical signals. Meanwhile, Exo I enabled target recycling via specific strand cleavage. The two amplification mechanisms synergistically amplify the detection signal by enhancing catalytic efficiency and increasing cycle numbers. MWCNTs-AuNPs possess both a high specific surface area and superior conductivity, facilitating efficient electron transfer and biomolecule immobilization. In the presence of DON, the Exo I mediated recycling reaction is triggered, which leads to a reduction in the amount of the immobilized Cu-Pt NPs signal probes on the aptasensor surface. Under optimal conditions, the proposed aptasensor demonstrated a detection range from 0.1 to 500 ng/mL, and a low detection limit of 0.06 ng/mL, along with high selectivity, reproducibility, and stability for DON detection. Furthermore, the proposed aptasensor achieved satisfactory recovery rates in real sample analysis, indicating its promising potential for practical applications.
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CHEMICAL ENGINEERING SCIENCE
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2026
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IF 5.1
Huiyun Xia,Zeliang Wu,Kaixuan Fan,Lifang Song,Sen Huang,Meiqi Yang
In response to the problem of nitrogen oxide pollution in tunnel environments, this study successfully prepared I - doped Bi 2 O 2 CO 3 photocatalyst I-BOC through solid-phase grinding method. The introduction of I - leads to a notable reduction in the bandgap of BOC, while also enhancing the specific surface area and pore volume, thereby facilitating the effective separation of photogenerated carriers. When exposed to visible light, I-BOC demonstrates a peak degradation efficiency of 58% for NO, and experiments involving free radical capture indicate that ·O 2 – is the primary active species, and explore the impact of the tunnel environment on the degradation efficiency of the catalyst. Additionally, epoxy resin served as the substrate for film formation, and 1H, 1H, 2H, 2H-perfluorodecyltrimethoxysilane (PFDTES) was incorporated as a low surface energy additive. A superhydrophobic photocatalytic self-cleaning coating (FBIE) characterized by a micro-nano rough structure was created using a one-step spraying technique. This coating showcases outstanding superhydrophobic properties and water contact angle exceeding 150°, along with excellent mechanical durability and chemical stability, achieving a visible light degradation efficiency of up to 65% for NO, and outstanding physical and chemical self-cleaning ability. By exploring the catalytic effects of I-BOC and FBIE coatings under different humidity conditions, the synergistic mechanism of coating photocatalysis and self-cleaning is revealed, providing broad application prospects for coatings in tunnel air purification.
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Inorganic Chemistry Frontiers
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2026
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IF 6.2
Jia-Wei Liu,Dan Li,Peng-Xu Lu,Tao-Xiao Wen,Yan-Ru Chen,Jian-Hua Jia,Ming-Liang Tong
Luminescent metal nanoclusters featuring near-infrared (NIR) emission hold promise for diverse applications. Although ligand engineering can modulate their NIR optical properties, separating the effects of single-ligand in dual-ligand systems remains challenging. In this study, we employed a controlled variable approach to prepare three structurally comparable silver-rich clusters-Ag11Cu3, Cu@Ag14-xCux, and Ag18. By maintaining a constant thiolate ligand and solely varying the phosphines, we elucidated the synergistic regulatory impacts of the ligands on the core configuration and excited-state dynamics. Structural and optical analyses reveal that the monodentate phosphine (TPP) stabilizes an Ag6@Ag5Cu3 core of the cluster Ag11Cu3, leading to NIR-I emission (720 nm) originating from mixed triplet state metal-centered and charge transfer transitions. In contrast, the bidentate phosphine (trans-dppe) facilitates the formation of a nested Ag6@Ag8@Ag4 core of the cluster Ag18, triggering NIR-II emission (1424 nm) associated with highly delocalized core-based excited states. Moreover, the spatial influence of the chiral bidentate phosphine ((S,S)-BDPP) can induce core-structural distortion, which promotes nonradiative decay and results in luminescence quenching of the cluster Cu@Ag14-xCux. This work clarifies the relation between the structure and luminescence properties of ligand-mediated metal clusters, offering valuable insights for the design of tailored NIR optical materials.
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Collagen and Leather
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2026
·Vol. 8
·期 1
·23
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IF 10.1
Wei Nannan,Zhang Yuchen,Huang Wenjie,Tian Xinyu,Yao Linyan,Xiao Jianxi
Ultraviolet (UV) irradiation is a major cause of photoaging, driving oxidative stress, inflammation, and extracellular matrix (ECM) degradation. Collagen is central to dermal integrity, yet animal-derived sources pose immunogenic and pathogen risks, while recombinant collagens reported to date often lack the stable triple-helical architecture required for bioactivity. Here, we present a triple-helical recombinant humanized type I collagen (THRCI) that combines native-like conformation with excellent biosafety and regenerative efficacy. THRCI supported fibroblast adhesion, proliferation, migration, and collagen synthesis, while suppressing intracellular reactive oxygen species and pro-inflammatory cytokines. In zebrafish, THRCI reduced oxidative stress and alleviated UV-induced caudal fin atrophy. In a murine model of acute UV photodamage, topical THRCI accelerated epidermal recovery, restored hydration and barrier function, increased dermal density, and promoted collagen fiber remodeling, while downregulating IL-6 , IL-1β , MMP-1 , and MMP-9 . Collectively, these findings indicate that THRCI exhibits effective photodamage-repair properties in our established models and represents a promising animal-free collagen biomaterial for skin regeneration. Graphical The alternative text for this image may have been generated using AI.
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