BIOCHEMICAL PHARMACOLOGY
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2026
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IF 6.5
Yu-Jing Wang,Shuai-Bing Ying,Lin Liu,Qiu-Dan Zhang,Yong Pan,Yu-Qi Hong,Hao-Yang Hu,Yi Liu,Jia-Ni Wei,Zhi-Juan Zhang,Yun-Qing Qiu,Yan Lou
Combretastatin A4 (CA4) is a potent microtubule inhibitor, but its phenolic hydroxyl group is prone to oxidation into toxic quinone products, leading to poor metabolic stability and dose-limiting toxicity that restricts its clinical application. To overcome this limitation, we propose a novel dimer prodrug strategy that covalently links two CA4 molecules via an enzyme-cleavable linker, achieving temporary masking of the phenolic hydroxyl group. The resulting CA4-dimer1 and CA4-dimer2 exhibited potent in vitro antiproliferative activity. Of the two dimers evaluated, CA4-dimer1 demonstrated superior in vitro potency. Crucially, CA4-dimer1 achieved significant tumor suppression rates in patient-derived xenograft (PDX) liver cancer models without notable toxicity. CA4-dimer2 releases active CA4 through gradual hydrolysis but showed slightly lower in vivo release efficiency compared to CA4-dimer1. Flow cytometry and Western blot analysis revealed that this prodrug exerts antitumor activity through the same mechanism as the parent compound CA4. Collectively, the reported CA4-dimer prodrug strategy offers a highly promising approach for treating liver cancer and enhancing the therapeutic index of phenolic drugs, while also providing a potential strategy for structural optimization of drugs containing phenolic hydroxyl groups
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JOURNAL OF NANOBIOTECHNOLOGY
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2026
·
IF 15
Tang Honglin,Wu Chongzhi,Wang Wei,Cheng Xi,Dong Yong,Gao Zhiyuan,Chen Pengfei,Xie Xin,Huang Yong,Sun Lihe,Li Bowen,Li Da
Ferroptosis, an iron-dependent form of regulated cell death driven by lipid peroxidation (LPO), has emerged as a promising strategy for cancer therapy but remains limited by insufficient hydrogen peroxide (H₂O₂), restricted catalytic iron availability, and the extremely short lifetime of hydroxyl radicals (·OH) in the tumor microenvironment. Here, we report a self-assembled nano-prodrug designed to amplify oxidative stress through coordinated reactive oxygen species (ROS)-reactive nitrogen species (RNS) cascades. Transcriptomic analyses of melanoma cohorts revealed that the redox enzyme NAD(P)H: quinone oxidoreductase-1 (NQO1) is frequently upregulated and associated with oxidative stress and ferroptosis-related transcriptional programs, suggesting a potential redox vulnerability that can be therapeutically exploited. Guided by this observation, a glutathione-responsive nanoplatform (HFSAL) was constructed from a disulfide-bridged ferrocene–arginine scaffold (Fc-SS-Arg) with β-lapachone (β-lapa) co-loaded and hyaluronic acid coating for tumor-targeted delivery. Upon intracellular activation, β-lapa undergoes NQO1-mediated redox cycling to generate H₂O₂, which is further converted into ·OH through ferrocene-catalyzed Fenton reactions. Meanwhile, arginine-derived nitric oxide (NO) reacts with ROS intermediates to form highly reactive peroxynitrite (ONOO⁻), thereby amplifying oxidative damage and extending the effective range of redox stress. In addition, NO-mediated vascular remodeling alleviates tumor hypoxia and enhances intratumoral drug accumulation. Consequently, the HFSAL nano-prodrug effectively induces synergistic ferroptosis and apoptosis, leading to significant tumor growth inhibition and metastasis suppression in vivo with favorable biosafety. This work presents a redox-amplifying nano-prodrug strategy that exploits NQO1-associated metabolic vulnerability to enhance ferroptosis-based cancer therapy. Graphical
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CHEMICAL ENGINEERING JOURNAL
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2026
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IF 12.5
Yuyuan Zhuang,Xuenong Gao,Ziye Ling,Xiaoyu Song
Phase change materials (PCMs) can store thermal energy in the form of latent heat. However, traditional PCMs suffer from spontaneous solidification and uncontrolled heat release in the absence of effective insulation or continuous energy input, severely limiting their practical application. To address this, optically-controlled PCMs have emerged as a novel solution, developed by integrating molecular photoswitches into traditional PCM matrices. Solar energy can be converted and stored in the form of photochemical enthalpy and phase change enthalpy, and the thermophysical properties of the materials can be changed through photoisomerization. In this paper, 4-octanoyloxyazobenzene (4-OcOAzo), an azophenyl photo controlled PCM, was prepared experimentally. The phase transition temperatures for the cis and trans isomers were determined to be 294.37 K and 335.76 K, respectively. The material exhibits an energy storage density of 139.356 kJ/kg, and the thermal conductivity was 0.292 W/(m·K) at room temperature. Subsequently, a microscopic model of 4-OcOAzo was established, and its thermophysical properties were analyzed based on molecular dynamics. The calculated results show that the phase transition temperature of the trans sample is 333 K, the phase transition temperature of the cis sample is 296.41 K, and the thermal conductivity at room temperature is 0.282 ± 0.017 W/(m·K), which is highly consistent with the experimental results. In addition, through the analysis of microstructure parameters, the mechanism of optically controlled phase transition can also be clarified.
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2026
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IF 5.4
Qing Jia,Wengang Liu,Wenbao Liu,Yonglun Wang,Zongxu Li
The flotation performance of traditional fatty acid collectors for apatite is significantly reduced under low-temperature conditions, limiting their industrial application. To overcome this limitation, a novel collector, N-fatty acyl sarcosine (N-FAS), was synthesized from vegetable fatty acid and evaluated for low-temperature flotation separation of fluorapatite from quartz and K-feldspar. Micro-flotation tests demonstrated that N-FAS exhibited superior selectivity, enhanced collecting power, and improved low-temperature tolerance compared to conventional sodium fatty acid (SFA). The adsorption mechanism was investigated using Fourier transform infrared spectroscopy (FTIR) and X-ray photoelectron spectroscopy (XPS), revealing that N-FAS adsorbs onto the fluorapatite surface through synergistic coordination of both acyl and carboxyl groups with surface Ca²⁺ sites. In contrast, SFA adsorbs via a single carboxyl group interaction with Ca²⁺ sites. Total organic carbon (TOC) measurements confirmed that N-FAS adsorption on fluorapatite was approximately 40 % higher than SFA at low temperature. Molecular dynamics simulations (MDS) further demonstrated that at 10 ℃, N-acyl sarcosine exhibits lower interaction energy with water molecules and adopts a more compact spatial configuration in proximity to the fluorapatite surface compared to sodium fatty acid. These results indicate that N-FAS is a highly efficient low-temperature collector for apatite. In conclusion, this research provides a novel multidimensional interpretation of the N-FAS mechanism by bridging molecular-level MDS with macroscopic dynamic foam analysis, offering a scientific framework for the rational development of low-temperature collectors.
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Nature Protocols
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2026
·
IF 18.4
Wu Yinglong,Zhang Chaobang,Chen Junjie,Zeng Fang,Wu Shuizhu,Zhao Yanli
Light-excited dual-mode imaging that integrates multispectral optoacoustic tomography (MSOT) and near-infrared region II fluorescence (NIR-II FL) imaging allows complementary deep-tissue visualization with high anatomical resolution and molecular sensitivity, thereby enhancing the accuracy of biomedical diagnostics. Activatable probes further advance this approach by producing signals upon recognition of disease-related biomarkers, which reduces background interference and improves imaging specificity. BTPE-NO 2 @F127, a benzothiadiazole-based nanoprobe, exhibits selective activation of both optoacoustic and NIR-II FL signals in response to hydrogen peroxide (H 2 O 2 ), a crucial early stage biomarker of liver injury, thus permitting cross-validated detection of hepatic damage in vivo with excellent signal-to-background ratio contrast. Here we present detailed procedures for preparation of the BTPE-NO 2 @F127 nanoprobe and its applications in MSOT/NIR-II FL dual-mode imaging of trazodone- or ischemia–reperfusion-induced liver injury in mice. Compared to conventional liver injury diagnostic methods, such as invasive tissue biopsy, ex vivo blood analysis and previously reported fluorescent/optoacoustic probes, BTPE-NO 2 @F127 offers real-time, in situ monitoring with high sensitivity and signal-to-background ratio, as well as mutually corroborating signals for increased reliability. The fabrication of BTPE-NO 2 @F127, including the chemical synthesis and characterization, requires ~17 d, while the in vitro validation of its H 2 O 2 responsiveness takes ~5 d. Notably, the complete workflow of data acquisition and analysis for MSOT/NIR-II FL dual-mode imaging of liver injury in mice using BTPE-NO 2 @F127 can be accomplished within 10 h. The protocol is easy to follow and suitable for clinicians and researchers with a basic understanding of chemistry and bioimaging techniques.
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ACS Nano
·
2023
·
IF 17.1
Qingyan Zhang,Pengkai Wu,Jicheng Wu,Hao Shou,Xinliang Ming,Shuqi Wang,Ben Wang
Classical chemotherapeutic drugs may cause immunogenic cell death (ICD), followed by activating CD8+ T cells to promote cell-mediated antitumor immune responses. However, CD8+ T cells become exhausted due to tumor antigens’ continuous stimulation, creating a major obstacle to effectively suppressing tumor growth and metastasis. Here, we develop an approach of chemo-gene combinational nanomedicine to bridge and reprogram chemotherapy and immunotherapy. The dually loaded nanomedicine induces ICD in tumor cells through doxorubicin and reverses the antitumor effects of exhausted CD8+ T cells through the small interfering RNA. The synergistic chemo-gene and fluorine assembly nanomedicine enriched in reactive oxygen species and acid-sensitive bonds results in enhanced cancer immunotherapy to inhibit tumor growth and the lung metastasis of breast cancer in a mouse model of breast cancer and melanoma. This study provides an efficient strategy and insights into chemoimmunological cascade therapy for combating malignant metastatic tumors.
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INDUSTRIAL CROPS AND PRODUCTS
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2023
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IF 5.9
Lirong Liao,Zhijun Ke,Xiang Wang,Shuchun Li,Sijie Wang,Xiaoping Rao
Antibacterial food packaging can effectively extend the shelf life of food . The bactericidal activity of rosin quaternary ammonium salt has been demonstrated in highly efficient. In this study, a new type of rosin quaternary ammonium salt antibacterial agent was grafted onto ethyl cellulose (EC-B), and the EC/EC-B recyclable composite films (0.5/1/3 wt% EC-B) for packaging material were then prepared by solution casting. These films have high transparency (> 93 % of 400 nm ultraviolet transmittance) and decent tensile strength (∼25 MPa). Because of the grafting of rosin based quaternary ammonium salt, the 1 wt% EC-B/EC film has a satisfactory bactericidal rate (> 97 %) toward both gram-positive and negative bacteria, suggesting its potential broad-spectrum antibacterial effect. In the experiment of food preservation, the apple slices packed with the film doped with 1 wt% EC-B maintained high freshness after three days storage. After two recycling loops, the tensile strength and the bactericidal rate for S. aureus and E. coli of the film were retained at 80 %, 93 %, and 80 % of the initial, respectively. This work explored the feasibility of using recyclable antibacterial cellulose composite in food packaging applications.
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JOURNAL OF CONTROLLED RELEASE
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2022
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IF 11.467
Jianing Zhao,Longbing Ling,Wei Zhu,Tianhao Ying,Tao Yu,Mengmeng Sun,Xuan Zhu,Yuan Du,Leiming Zhang
Atherosclerosis (AS), a leading cause of death worldwide, involves chronic macrophage inflammation from its initiation to the emergence of complications. Targeting plaque inflammation by re-polarizing pro-inflammatory M1 to anti-inflammatory M2 could therefore provide a promising strategy to treat AS, but currently available anti-inflammatory drugs limit clinical outcomes. In this study, we found that kaempferol (KPF) is capable of potential anti-inflammation as a novel drug candidate, which has been scarcely reported. Building upon these findings, we fabricated a macrophage-biomimetic KPF delivery platform, abbreviated as [email protected] to potentiate therapeutic payloads, wherein the designed ROS-responsive Dextran- g -PBMEO NPs with π-π stacking were coated with macrophage membrane (MM) for effective target and accumulation in atherosclerotic lesions. Therapy of [email protected] afforded significant decrease in proliferating macrophage inflammation while went with the reduction of key pro-inflammatory cytokines and re-polarization M1 to M2 phenotype, inducing excellent anti-AS responses in ApoE −/− mice after i.p. delivery. The mechanism of [email protected] was further investigated and found it related to block the ROS/NF-κB signaling pathways. Together with as well demonstrated biosafety profiles, this proof-of-concept opens an instructive door for the study of KPF-mediated nanodrugs in treatment of AS based on biomimetic NPs.
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2022
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IF 5.062
Qida Zong,Shiya Zhou,Jing Ye,Xinxuan Peng,Huiying Wu,Mohan Li,Xuanjiayi Ye,Naixin Tian,Wei Sun,Yinglei Zhai
In addition to various functions, hydrogels used to promote wound healing should also have good biocompatibility , stability and mild degradability. Therefore, we designed and synthesized aldehyde modified aliphatic cyclic carbonate monomer (MTC-Ba). Then the hydrogel matrix (MTC-Ba n -b-PEG 6k -b-MTC-Ba n , MBP) was prepared by ring opening polymerization using polyethylene glycol (PEG) as the initiator and hydrophilicity enhancer. The matrix was covalently linked with the crosslinker adipic acid dihydrazide (ADH) through dynamic hydrazide bond to form a self-healing hydrogel (SH-Gel). At the same time, curcumin was loaded into the hydrogel as a functional model drug. The resulting hydrogel has porosity, injectability, appropriate swelling rate, friendly cell compatibility and safe degradability. In addition, in vivo wound healing evaluation, histological evaluation and immunofluorescence staining showed that this gel could the wound closure, re-epithelium and collagen regeneration. In conclusion, this study provides a new choice for the application of synthetic biodegradable polymer materials in promoting skin wound healing.
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Acta Biomaterialia
·
2023
·
IF 9.7
Yuan Chen,Zhuo Yao,Peilian Liu,Qida Hu,Yong Huang,Li Ping,Fu Zhang,Honglin Tang,Tao Wan,Yuan Ping,Bowen Li
Chemotherapeutics have been recommended as the standard protocol for inoperable patients with triple-negative breast cancer (TNBC) at advanced stage, yet limited success has been achieved in prolonging survival rates by this monotherapy. A major reason for this failure is the chemo-resistance from traditional apoptotic pathways resulting in poor therapeutic effect. Ferroptosis has become a powerful modality of no-apoptotic cell death, which can effectively evade chemo-resistance in apoptotic pathways. Herein, we propose an active-targeting small-molecular self-assembly nano-prodrug for co-delivery of chemotherapeutics (CPT), Ferrocene (Fc) and GPX4 inhibitor (RSL3) to overcome the chemo-resistance from traditional apoptotic pathways. In this nano-prodrug, the disulfide linkage not only serves as a GSH-responsive trigger, but also exhibits a stable self-assembly behavior that forms nanoparticle . Interestingly, the RSL3 can be loaded during this self-assembly process that forms a three-components nano-prodrug. In tumor environment, the high GSH level can disassemble the nano-prodrug to trigger the release of the parent drug, which can improve the therapeutic effect by synergistic effects of ferroptosis and apoptosis. In different TNBC mice models, the nano-prodrug is encapsulated into RGD-modified phospholipid micelles (DSPE-PEG2000-RGD) and exhibits high anti-tumor and anti-metastasis efficacy, especially in orthotopic models. The application of ferroptosis to assist the enhancement of chemotherapeutics may serve as a promising strategy for TNBC treatment. Statement of significance Chemotherapeutics have been recommended as the standard of care for palliative and adjuvant treatment in patients with triple-negative breast cancer (TNBC), yet limited success has been achieved in prolonging the overall survival of patients by this monotherapy. A major reason for this failure is the chemo-resistance from traditional apoptotic pathways resulting in poor therapeutic effect. Thus, the co-delivery of the apoptosis and ferroptosis drug may overcome or evade the resistance in chemotherapy-induced apoptotic pathways and provide a promising strategy to combat TNBC. In this work, we developed a small-molecular self-assembly nano-prodrug for co-delivery of chemotherapeutics (CPT), Ferrocene (Fc) and ferroptosis resistance inhibitor (RSL3), which could overcome the chemo-resistance and improve the therapeutic effect by synergistic effects of ferroptosis and apoptosis.
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Small
·
2023
·
IF 13.3
Chongzhi Wu,Fu Zhang,Bowen Li,Zhiyao Li,Xin Xie,Yong Huang,Zhuo Yao,Yuan Chen,Yuan Ping,Weidong Pan
Triple-negative breast cancer (TNBC) displays a highly aggressive nature that originates from a small subpopulation of TNBC stem cells (TNBCSCs), and these TNBCSCs give rise to chemoresistance, tumor metastasis, and recurrence. Unfortunately, traditional chemotherapy eradicates normal TNBC cells but fails to kill quiescent TNBCSCs. To explore a new strategy for eradicating TNBCSCs, a disulfide-mediated self-assembly nano-prodrug that can achieve the co-delivery of ferroptosis drug, differentiation-inducing agent, and chemotherapeutics for simultaneous TNBCSCs and TNBC treatment, is reported. In this nano-prodrug, the disulfide bond not only induces self-assembly behavior of different small molecular drug but also serves as a glutathione (GSH)-responsive trigger in controlled drug release. More importantly, the differentiation-inducing agent can transform TNBCSCs into normal TNBC cells, and this differentiation with chemotherapeutics provides an effective approach to indirectly eradicate TNBCSCs. In addition, ferroptosis therapy is essentially different from the apoptosis-induced cell death of differentiation or chemotherapeutic, which causes cell death to both TNBCSCs and normal TNBC cells. In different TNBC mouse models, this nano-prodrug significantly improves anti-tumor efficacy and effectively inhibits the tumor metastasis. This all-in-one strategy enables controlled drug release and reduces stemness-related drug resistance, enhancing the chemotherapeutic sensitivity in TNBC treatment.
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APPLIED ORGANOMETALLIC CHEMISTRY
·
2023
·Vol. 37
·期 10
·e7230
·
IF 3.9
Dingning Chen,Haojie Yu,Li Wang,Sergey Z. Vatsadze,Jinyi Liu,Yu Wang
Ferrocene-based compounds are promising burning rate catalysts due to their attractive catalytic activity, flammability, and non-toxic performance. Unfortunately, the high-migration issue of the ferrocene-based catalysts makes it challenging to store composite solid propellants for a long time. Therefore, a dendrimer containing ferrocene units with anti-migration ability was designed herein. The introduction of polar groups provides a large number of interaction sites for anti-migration, and no migration of the dendrimer in the propellant was observed after 4 weeks of the aging test. For catalytic performance, the results showed that the thermal decomposition temperature of ammonium perchlorate could be reduced from 404°C to 369°C by adding 3 wt% ferrocene-based dendrimer. Moreover, compared with the propellant mixed with Catocene, the propellant containing ferrocene-based dendrimer showed a lower pressure exponent (0.47) and a higher burning rate (2.03 mm·s −1 , at 0.1 MPa).
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