FITOTERAPIA
·
2025
·
IF 2.6
Jinyuan Yang,Zhaojing Chen,Yikun Ren,Chunlei Yuan,Senhua Hu,Yiyang Liu,Dahong Li,Huiming Hua
Phytochemical investigation of Thalictrum baicalense Turcz. roots, traditionally used for inflammatory conditions, led to the isolation of three novel isoflavones, thalibaicalins A-C ( 1 – 3 ), and a new lignan, (7 R , 8 S , 7′ R , 8′ S )-9 E -feruloylneoolivill ( 6 ), alongside six known compounds ( 4 – 5 , 7 – 10 ). Structural characterization was accomplished by HRESIMS, comprehensive NMR analysis, and quantum chemical calculations. Anti-inflammatory evaluation in lipopolysaccharide-stimulated RAW 264.7 macrophages identified potent NO inhibitors, with lignan 6 exhibiting the highest activity (IC 50 = 9.56 ± 2.03 μM). This study expands the phytochemical diversity of T. baicalense Turcz. and highlights its potential as a source of anti-inflammatory lead compounds, particularly the highly active lignan derivative.
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Talanta Open
·
2025
·
IF 3.7
Qiao Chen,Xiaoran Zhang,Xinyue Zhou,Peng Huang,Daming Feng,Xu Xu,Chunhua Ge
We report a metal-free perylene-based polyimide framework (PDI-PB) as an efficient electrocatalyst for oxygen reduction reaction (ORR)-enhanced cathodic electrochemiluminescence (ECL). PDI-PB enhances reactive oxygen species (ROS) generation via oxygen reduction that significantly amplify the luminol–dissolved oxygen ECL signal. The resulting biosensor enables ultrasensitive detection of dopamine (DA) over a wide linear range (5 × 10 -5 to 100 μM) with a record-low detection limit of 9.76 pM (S/N = 3). The sensor exhibits excellent selectivity, stability, and reproducibility, and was successfully applied to detect DA in human sweat, serum, and urine, yielding recoveries of 97.0–101.1%. Density functional theory (DFT) calculations reveal that PDI-PB’s superior electronic structure facilitates efficient charge transfer and oxygen activation. This work presents a new strategy for metal-free organic electrocatalyst design, combining mechanistic insight with high-performance ECL biosensing for non-invasive health monitoring and clinical diagnostics.
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MOLECULES
·
2025
·Vol. 31
·期 1
·122
·
IF 4.6
Xinyue Ma,Qinqing Zhang,Ying Yang,Yuqi Zhan,Xiangyu Zhang,Yanli Zhao,Jinlian Li,Dongmei Wu
Fatty acid vesicles (FAVs) are promising nanocarriers, but their application is limited by a narrow, alkaline pH formation window that mismatches the weak acidity of physiological environments, such as skin. To overcome this, we developed composite vesicles using oleic acid (OA) and the non-ionic surfactant Tween 40 (TW40). pH titration confirmed that the OA/TW40 system successfully broadened the vesicle formation window from 8.2–10.08 to 3.1–7.2, aligning it with the physiological pH range. The bioactive flavonoid luteolin (LUT) was efficiently encapsulated into these OA/TW40-FAVs, achieving a high encapsulation efficiency (EE) of 87.13% and a drug loading capacity (DLC) of 9.58. The formulation demonstrated superior topical delivery performance: the cumulative transdermal flux (933.08 µg·cm−2) and skin retention (68.18 µg·cm−2) were both approximately double that of the free LUT solution. Furthermore, the OA/TW40/LUT-FAVs provided sustained drug release and exhibited synergistically enhanced antioxidant and antimicrobial activities compared to free LUT or blank vesicles. Collectively, these findings establish OA/TW40 composite vesicles as a robust and efficient nanoplatform for the topical delivery of bioactive compounds.
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AAPS PHARMSCITECH
·
2019
·Vol. 20
·期 2
·1-15
·
IF 2.608
Zhang Shudong,Wan Qiang,Xing Yidan,Ding Jiafeng,Yang Shizhuang,Sun Weiwei,Lu Mengmeng,Pan Baoliang
Drugs with pH-dependent solubility that have poor water solubility can be identified in the drug discovery pipeline. Some of them have poor oral absorption, which can result in insufficient efficacy. Micro-environmental pH-modifying solid dispersion (micro pHm SD) is a promising approach to overcome the poor oral absorption of these drugs. In the present study, toltrazuril (TOL), a weakly acidic drug with poor aqueous and pH-dependent solubility, was used as a model drug. Using micro pHm SD, a novel oral oil-based suspension of TOL SD (TSDS) was developed, and the stability of this formulation was evaluated based on particle size, settling volume ratio, redispersibility, thermal stability, and drug content. The optimized soybean oil-based TSDS (S-TSDS) had high physicochemical stability and good histocompatibility with common inflammatory reactions. The results of the in vitro dissolution analysis showed that S-TSDS rapidly and markedly released the drug and provided higher efficacy and longer persistence against coccidiosis (above 90.9%) in rabbits. This technique could increase the oral absorption and bioavailability of new drug candidates.
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Algal Research-Biomass Biofuels and Bioproducts
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2025
·
IF 4.5
Yongqi Tian,Ding Deng,Haitao Luo,Mingfeng He,Shaoyun Wang
Phlorotannins, recognized for their efficacy and safety as natural tyrosinase in hibitors, have posed challenges due to their limited extraction efficiency and the elusive nature of their mechanism of action. Here, we developed an ultrasonic-assisted enzymatic extraction (UAEE) protocol that significantly enhanced phlorotannin recovery from Sargassum horneri, achieving a total phenolic content (TPC) of 21.51 mg PGE/g DW. Subsequent purification using solvent extraction and Sephadex LH-20 yielded high-purity alginate phlorotannins (SHP), exhibiting potent DPPH radical scavenging and tyrosinase inhibitory activities, with IC 50 values of 22.71 and 26.90 μg/mL, respectively. Structural elucidation based on NMR and MS data suggested that SHP predominantly comprises fucophloroethols, with a degree of polymerization ranging from 3 to 8. Reciprocal plot analysis indicated that SHP inhibits tyrosinase activity through a competitive inhibition mechanism, while fluorescence spectroscopy revealed a dynamic quenching effect of SHP on tyrosinase. Molecular docking studies further elucidated t hat van der Waals forces and hydrophobic interactions are the primary forces governing the interaction between SHP and tyrosinase. Cellular experiments demonstrated the significant inhibitory effects of SHP on both melanin production and tyrosinase activity in B16-F10 cells. This research presents promising lead compounds for the development of novel tyrosinase inhibitors, while also providing theoretical and methodological foundations for the comprehensive utilization of Sargassum horneri.
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BIOMACROMOLECULES
·
2015
·
IF 5.75
Menglin Wang,Jin Sun,Yinglei Zhai,He Lian,Cong Luo,Lin Li,Yuqian Du,Dong Zhang,Wenya Ding,Shuhong Qiu,Yuhai Liu,Longfa Kou,Xiangfei Han,Rongwu Xiang,Yongjun Wang,Zhonggui He
To improve the bioavailability of orally administered drugs, we synthesized a pH-sensitive polymer (poly(ethylene glycol)–poly(2-methyl-2-carboxyl-propylene carbonate)–vitamin E, mPEG–PCC–VE) attempting to integrate the advantages of enteric coating and P-glycoprotein (P-gp) inhibition. The aliphatic polycarbonate chain was functionalized with carboxyl groups and vitamin E via postpolymerization modification. Optimized by comparison and central composite design, mPEG113–PCC32–VE4 exhibited low critical micelle concentration of 1.7 × 10–6 mg/mL and high drug loading ability for tacrolimus (21.2% ± 2.7%, w/w). The pH-responsive profile was demonstrated by pH-dependent swelling and in vitro drug release. Less than 4.0% tacrolimus was released under simulated gastric fluid after 2.5 h, whereas an immediate release was observed under simulated intestinal fluid. The mPEG113–PCC32–VE4 micelles significantly increased the absorption of P-gp substrate tacrolimus in the whole intestine. The oral bioavailability of tacrolimus micelles was 6-fold higher than that of tacrolimus solution in rats. This enteric polymer therefore has the potential to become a useful nanoscale carrier for oral delivery of drugs.
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Analytical Methods
·
2025
·
IF 2.6
Wei-Chuang Kong,Chen-Chen Li,Jun-Tao Niu,Xu-Ying Liu,Dong Wei,Yan-Fei Kang
Enrofloxacin (ENR), a third-generation fluoroquinolone antibiotic, poses significant health risks due to potential drug residues in the food chain, necessitating effective monitoring methods. Here, we synthesized a G-quadruplex-targeted fluorescent probe PBTZM containing styrylbenzothiazole. Using this probe, we successfully developed an aptasensor for the detection of ENR by combining it with an ENR aptamer. Under optimal conditions, the aptasensor provided a linear range of 0.001–5 μM and a detection limit of 24.74 nM. In addition, this method showed good performance for ENR detection in river water, milk, serum and urine samples and was further validated by standard HPLC techniques without a significant difference (p > 0.05). It will have great potential in advancing research of quinolone antibiotics and the development of aptamer-based biosensing technologies.
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Science Advances
·
2025
·Vol. 11
·期 20
·
IF 12.5
Hanxi Zhang,Jiazhen Lv,Hao Wu,Yuhan He,Mengyue Li,Chunhui Wu,Dong Lv,Yiyao Liu,Hong Yang
Apoptosis resistance and immune evasion of tumor cells substantially increase the risk of cancer treatment failure. Here, a multifunctional nanozyme MET-CMS@FeTA (MCMSFT) formulated to induce nonapoptotic ferroptosis and boost immune recognition/attack, where compensatory mechanisms collectively overcome intrinsic tumor therapeutic limitations and improve medical intervention outcomes. Leveraging the multienzyme-like activity of MCMSFT to achieve oxygen generation, hydroxyl radical production, and glutathione depletion promotes hypoxia relief and triggers apoptosis/ferroptosis. Notably, MCMSFT-mediated photothermal therapy (PTT) facilitates direct tumor thermal ablation and offers exogenous heat to accelerate nanocatalytic reactions. Furthermore, PTT/ferroptosis-caused immunogenic cell death favors antitumor immunity initiation. Simultaneously, metformin administration and hypoxia amelioration down-regulate programmed death ligand 1 alleviating immune evasion. Interferon-γ secretion poses positive feedback to ferroptosis, thereby establishing a ferroptosis-immune mutual amplification loop. Antitumor performances illustrate that MCMSFT eliminates primary tumors and suppresses metastasis/rechallenge tumors. Collectively, MCMSFT surmounts the predicament of apoptosis resistance and immune evasion in cancer treatment to acquire more effective and comprehensive therapy efficacy.
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Journal of Inflammation Research
·
2025
·
IF 4.1
Siyue Bo,Xiaotong Wang,Jiani Qian,Guoqiang Ma,Zheng Ying,Duanmin Hu,Chunyan Hou,Junfeng Ma,Longjiang Xu,Shuang Yang
Background Ulcerative colitis (UC) disrupts the colon’s protective mucus layer, exposing the epithelium to bacteria and triggering inflammation. This barrier, crucial for intestinal health, depends on complex glycosylation, notably sialic acid modifications. However, the precise role of sialic acid acetylation and the enzyme SIAE (sialic acid acetylesterase) in UC pathogenesis remains unclear. This study investigates the role of glycosylation changes, specifically sialic acid de-acetylation, in UC progression.Methods Tissue samples were obtained from patients with ulcerative colitis (UC) and colorectal cancer at the Second Affiliated Hospital of Soochow University. HT-29 cells were utilized to investigate the molecular mechanisms of SIAE in UC pathogenesis. Mass spectrometry was performed to analyze differences in protein and glycoprotein expression. Western blot (WB) and immunohistochemistry (IHC) were used to examine SIAE protein expression changes during inflammation. Furthermore, polymerase chain reaction (PCR) and immunofluorescence were employed to determine the effects of SIAE on sialic acid levels and mucosal immunity.Results In this study, we characterized proteins and glycoproteins from patient tissues with UC, finding that sialic acid acetylesterase (SIAE) is upregulated in UC. HT-29 cells exposed to TNF-α induced an inflammatory response with a 5-fold increased expression of SIAE and NEU1 when TNF-α was at a concentration of 100 ng/mL. Mass spectrometry analysis revealed a reduction in acetylation on glycans and glycoproteins, while confocal microscopy confirmed a decrease in sialic acid on the cell surface. Gene expression analysis showed that CDH1, CTNND1, and ITGA8 were significantly downregulated in HT-29 cells stimulated by TNF-α, suggesting a reduction in cell-cell adhesion. SNA lectin-confocal microscopy revealed a reduction of sialic acid on HT-29 cells in TNF-α-induced UC cell models.Conclusion This study demonstrates that SIAE is significantly upregulated in ulcerative colitis (UC) tissues and TNF-α-stimulated HT-29 cells, leading to a marked reduction in sialic acid acetylation and cell surface sialic acid levels. These changes correlate with decreased expression of cell adhesion molecules, suggesting a disruption of the mucosal barrier integrity. Consequently, SIAE-mediated sialic acid de-acetylation emerges as a critical factor in UC pathogenesis, potentially serving as both a valuable biomarker and a promising therapeutic target.
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RSC Advances
·
2025
·Vol. 15
·期 22
·17781-17794
·
IF 4.6
Jiayu Song,Huanhuan Zhang,Xiaohui Zhang,Meiying Liu,Dan Peng,Yuan Ren,Yan Sun,Yunlan Li
The safe and efficient delivery of chemicals and biologics remains crucial for liver disease therapy. In this study, we developed a targeted drug delivery system utilizing a galactose-modified erythrocyte membrane coating technique and drug liposome nanoparticles, which were further optimized using orthogonal experiments and response surface analysis. The specificity, precision, accuracy, and stability exhibited satisfactory performance in bioanalytical analysis. Specifically, targeting ligands (Gal-DSPE-PEG3400) were efficiently inserted into red blood cell (RBC) membranes using a facile insertion method. When Gal-DSPE-PEG3400-RBC was fused with fenofibrate liposome nanoparticles (FNB-Lip) by co-extrusion, the resulting galactose-modified erythrocyte membrane fusion liposome nanoparticles (Gal-RBC-FNB-Lip) showed long-term stability, excellent biocompatibility, prolonged retention time, and superior liver accumulation and therapeutic efficacy. These qualities make it suitable for effective drug delivery. The findings of this study will provide a fundamental basis for research and development of liver-targeted drugs and offer novel insights into the treatment of clinical liver diseases.
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MICROCHEMICAL JOURNAL
·
2025
·
IF 5.1
Yapeng Li,Qinghong Pan,Huiting Shi,Youyou Du,Ailing Yang,Da-Peng Yang
The quantitative determination of cholesterol in foods, drugs, and biological fluids holds significant importance due to its potential health risks. Herein, a self-powered photoelectrochemical (PEC) sensor was developed for cholesterol detection. The photoelectrochemical system was constructed by modifying fluorine-doped tin oxide (FTO) electrodes with ZnO/C (serving as the photoanode) and iron-modified CuBi 2 O 4 (denoted as CBFO, functioning as the photocathode) through a controlled deposition process. To enhance detection selectivity, molecularly imprinted polymers (MIPs) were electrodeposited on the photocathode surface. The optimized sensor exhibited a linear detection range of 1–1000 nmol L −1 and a detection limit of 0.26 nmol L −1 (S/N = 3). Practical application of the sensor for cholesterol detection in milk samples demonstrated satisfactory recovery rates (98.6 %–107 %) with relative standard deviations (RSD) ranging from 2.38 % to 4.25 %. These results underscore the potential of this self-powered PEC sensor as a robust platform for rapid and accurate cholesterol determination in food products, pharmaceuticals, and environmental samples.
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Materials Today Bio
·
2025
·
IF 10.2
Ming Zhang,Yamei Wang,Yao Dai,Yan Hu,Wanting Fu,Yuhao Zhao,Hanyu Ma,Di Zhang,Ying Chen,Yixuan Zhou,Lei Du,Jing Chang,Fang Liu,Shuyan Chen,Fei Wang,Dongdong Xiao,Zhen Li
Chronic wounds, especially diabetic foot ulcers, pose a major clinical challenge due to persistent inflammation, impaired angiogenesis, and cellular senescence. Senolytic therapies, which selectively eliminate senescent cells, have shown promise in promoting healing, but systemic toxicity limits their application. To address this, we developed an asymmetric fabric-based composite platform for localized senolytic delivery. Using single-cell RNA sequencing, we characterized senescence-associated alterations in human diabetic foot ulcer tissues and screened several senolytic candidates in skin fibroblasts and endothelial cells. Among these, navitoclax (ABT-263) emerged as the most effective senolytic. Incorporating ABT-263 into the fabric-based platform to prepare ABT-263-CGH, we confirmed its ability to reduce senescent cell burden while maintaining biocompatibility. In a diabetic mouse model, the ABT-263-CGH significantly enhanced wound healing, reduced senescence markers, and exhibited no detectable systemic toxicity. These findings highlight the potential of localized senolytic therapy using an asymmetric fabric-based wound dressing as a novel strategy for enhancing chronic wound healing, offering a promising therapeutic avenue for diabetic wound management, and paving the way for future clinical applications.
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