Frontiers in Pharmacology
·
2025
·
IF 4.8
Yuhang Xu,Jing Li,Mengyao Cui,Xiaoliang Li,Hongyan Zhai,Deling Wu,Xiaoqin Chu
Introduction: Cinnamomi Ramulus (CR) is the dried bark of Cinnamomum cassia Presl, Lauraceae. Puerariae Lobatae Radix (PLR) is the dried root of the Pueraria lobata (Wild.) Ohwi, Leguminosae. This Chinese herb couple come from the classic formula “Gui Zhi Ge Gen Tang,” which is included in the TCM classic “Treatise on Febrile Diseases.” Our previous studies have found that CR related herbal compound and PLR related herbal compound are useful in improving type 2 diabetes mellitus (T2DM), which is expected to be an antidiabetic candidate with fewer side effects. However the mechanism of action of CR-PLR on T2DM has not yet been fully elucidated.Methods: The decoction of CR-PLR was prepared by aqueous extraction method and the composition of it was analyzed using UPLC-Q-TOF-MS and HPLC. The T2DM model was established by intraperitoneal injection of streptozotocin, and the groups of drug administration were metformin, CR, PLR and CR-PLR groups, with continuous gastric gavage for 6 weeks, and the serological indexes were detected by ELISA. The abundance of rats’ gut flora was detected by 16s rDNA sequencing, and changes in the content of short-chain fatty acids (SCFAs) in feces of rats were detected by GC-MS; and the expression of G protein-coupled receptor43 (GPR43) and glucagon-like peptide-1 (GLP-1) proteins in colonic tissues of rats were detected by Western Blot. The pharmacokinetic behavior of CR-PLR was investigated in both normal and T2DM model rats. Caco-2/HT29 co-culture cell model was established in vitro, transepithelial electrical resistance (TEER) and ALP activity of epithelial cells were measured to evaluate cell model integrity and cell polarization, Alcian blue staining was used to verify the presence of mucus production, and CCK-8 was used to screen drug safe concentration. The bidirectional transport of puerarin was studied to investigate the transport mechanism of puerarin and the effect of leuric acid on puerarin transport.Results and discussion: The results indicated that CR-PLR can stimulate intestinal flora, increase the content of SCFAs, activate intestinal GPR43 protein, and promote the secretion of GLP-1 in intestinal L cells, which plays a therapeutic role in the treatment of T2DM. Additionally, cytology and pharmacokinetics experiments have proved that cinnamic acid (CA) can enhance the absorption and transport of puerarin (PUR) by inhibiting the efflux effects mediated by P-gp and MRP efflux transporters. The present study exhibites the scientific and reasonable menaning of this novel Chinese herb couple treating T2DM from the perspecives of pharmacodynamics and pharmacokinetics.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
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.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
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.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2025
·
IF 5.2
Qiantong Liu,Dongming Liu,Ji Wen,Li Yang
To address the limitations of single therapy and ensure the safe and efficient delivery of nanomedicine, we developed carbon/manganese nanoparticles (NPs). These NPs were engineered by depositing manganese dioxide on the surface of mesoporous carbon (MMCN), thus enabling Peroxidase (POD)-Catalase (CAT)-Glutathione peroxidase (GPX)-like function. Following the modification with AS1411 aptamer (AMMCN), doxorubicin hydrochloride (DOX) was incorporated to produce AMMCN@DOX. This compound demonstrated satisfactory biocompatibility, efficient tumor tissue accumulation, and the capability to release DOX in response to the tumor microenvironment (TME). It was confirmed that AMMCN@DOX is effectively endocytosed by cells, releases DOX, decomposes H 2 O 2 to generate O 2 to alleviate tumor hypoxia, and mediates a Fenton-like reaction. Additionally, AMMCN@DOX showed excellent photothermal conversion efficiency, producing localized heating in tumors and yielding superior synergistic anti-tumor activity in mice with solid tumors. Thus, this study proposes a safe, targeted delivery strategy for carbon/manganese NPs, facilitating chemical, chemokinetic, and photothermal synergistic therapy.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Algal Research-Biomass Biofuels and Bioproducts
·
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.
✓ 已验证
产品关联
DOI
高影响因子
Advanced Healthcare Materials
·
2025
·
IF 9.6
Liuxian Chen,Qin Huang,Yongjie Liu,Ke Chen,Qing Yang,Hua Tang,Dan Wang,Zhenrong Tang
Complete hepatitis B virus (HBV) cure is hindered primarily by the stable persistence of covalently closed circular DNA (cccDNA). Gene editing approaches to eradicate HBV by targeting cccDNA face challenges and limitations due to suboptimal editing efficiency and substantial off-target effects. Herein, a combinatorial therapeutic strategy is developed that integrates CRISPR/Cas9-mediated cccDNA disruption with an antisense oligonucleotide (ASO)-targeted degradation of pregenomic RNA (pgRNA). To overcome delivery challenges, a hepatocyte-targeting nanocarrier (UACPG) is engineered, featuring low immunogenicity, high payload capacity, and dual-stimuli responsiveness. The UACPG platform enabled liver-specific delivery through surface-conjugated targeting ligands, followed by on-demand release of Cas9 ribonucleoprotein complexes and ASO via RNase H-dependent degradation and near-infrared (NIR) light activation. The results demonstrated that UACPG can effectively reduce HBV replication and viral antigen levels, while significantly lowering cccDNA in hydrodynamic HBV-infected mouse models, with no significant off-target effects observed. This nanocarrier achieved the spatiotemporally controlled release of gene-editing systems in vitro and in vivo, significantly inhibiting the replication of HBV, thereby establishing an innovative technological platform for developing curative HBV therapies.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
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.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
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.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
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.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
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.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Diabetes & Metabolism Journal
·
2025
·
IF 8.5
Lei Zhou,Yuwen Jiao,Jiaming Xue,Xiaoqiang Zhan,Dongmei Wang,Liming Tang
Background: To investigate the biological functions of the transcription factor LRR binding FLII interacting protein 1 (LRRFIP1) in white adipocyte differentiation (WAD) and elucidate the underlying molecular regulatory mechanisms involved. Methods: Consensus clustering, differential gene expression screening, and intersection analysis were used to identify transcription factors involved in WAD. Adipogenic differentiation experiments were conducted using C3H10T1/2 cells, and a diet-induced obesity model in C57BL/6J mice was established to investigate the function of LRRFIP1 in WAD in vitro and in vivo. Molecular mechanisms were examined through quantitative real-time polymerase chain reaction, Western blotting, luciferase assays, and chromatin immunoprecipitation. Results: Bioinformatics analyses identified LRRFIP1 as a transcription factor associated with WAD. LRRFIP1 expression was downregulated in white adipose tissues from obese patients and in mature white adipocytes. Silencing LRRFIP1 significantly inhibited WAD in C3H10T1/2 cells and reduced differentiation biomarker expression; in contrast, overexpressing LRRFIP1 had the opposite effects. Mechanistically, LRRFIP1 bound to the E2F transcription factor 6 (E2F6) promoter to suppress E2F6 transcription, thereby downregulating a key differentiation regulator, CCAAT enhancer binding protein alpha (C/EBPα). Furthermore, in a diet-induced obesity model, LRRFIP1 could regulate the differentiation and maturation of inguinal white adipose tissue. Conclusion: Our findings reveal that LRRFIP1 plays a crucial inhibitory role in WAD by negatively regulating the E2F6/C/EBPα axis. This discovery not only enriches our understanding of the molecular networks governing WAD but also holds great promise for creating targeted therapies for obesity and associated metabolic conditions.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Materials Today Communications
·
2025
·
IF 4.5
Renzhang Liang,Cuilian Yu,Dong Ma,Xiaohan Cao,Liying Bai,Yulan Li,Jingxian Zhang,Jiayue Liu,Xia Qiao,Bingren Tian
Curcumin, a polyphenolic compound, demonstrates neuroprotective potential through its antioxidant, anti-inflammatory, and anti-amyloid activities. To enhance its delivery, we fabricated poly(lactic-co-glycolic acid) (PLGA) nanoparticles encapsulating curcumin and stabilized them with chitosan. Successful formulation was confirmed by FTIR, XRD, and SEM analyses. Zeta potential measurement confirmed a surface charge reversal from -28.1 mV (uncoated PLGA) to + 14.7 mV after chitosan coating. The nanoparticles exhibited favorable drug loading (4.09 ± 0.02 % to 5.67 ± 0.01 %) and encapsulation efficiency (14.33 ± 0.08 % to 19.85 ± 0.04 %), and provided a sustained release profile (>24 h) enhanced by chitosan. The curcumin encapsulated PLGA-chitosan nanocarriers demonstrated potent antioxidant activity (>80 % DPPH scavenging at 0.75 mg/mL) and no significant cytotoxicity against PC12 cells at concentrations up to 80 μg/mL. In HCT116 cells, the chitosan coating enhanced cellular uptake and cytoplasmic distribution. Crucially, the nanocarriers promoted PC12 cells differentiation, resulting in a high proportion of neurite-bearing cells. These findings indicate that the designed chitosan-coated PLGA nanoparticles are a promising delivery system for promoting neuronal differentiation.
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）