Journal of Pharmaceutical Analysis
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2025
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IF 8.9
Lingyun Fu,Shidie Tai,Jiajia Liao,Youqi Du,Guangqiong Zhang,Die Guo,Xingmei Chen,Tian Zheng,Xiaoxia Hu,Wenbing Yao,Ling Tao,Xueting Wang,Yini Xu,Xiangchun Shen
Vascular endothelial senescence is an important pathophysiological factor in the development and exacerbation of cardiovascular health problems linked to diabetes mellitusn (DM). Accumulating evidence confirms that 1,8-cineole has multiple pharmacological properties, including anti-inflammatory, anti-microbial, and antioxidant activities. We investigated whether 1,8-cineole could ameliorate cardiovascular diseases and endothelial dysfunction, as the pharmacological properties and mechanism of diabetic vascular ageing remain unknown. Our results revealed notable senescence biomarkers in both in vivo and in vitro models. Treatment with 1,8-cineole alleviated lipid profiles and vascular senescence in mice with DM. Additionally, bioinformatics analysis suggested that peroxisome proliferator-activated receptor-γ (PPAR-γ) plays a crucial role in DM and ageing. We confirmed the binding capacity PPAR-γ with 1,8-cineole. Accordingly, experiments with the PPAR-γ agonist rosiglitazone, the PPAR-γ inhibitor GW9662, and PPAR-γ siRNA were performed to validate the pharmacological characteristics of 1,8-cineole. Finally, we clarified that 1,8-cineole can directly target PPAR-γ protein, as verified by cellular thermal shift assay, drug affinity responsive target stability, and surface plasmon resonance analyses. Taken together, these results provide the first evidence that 1,8-cineole ameliorates DM-induced vascular endothelial ageing via stabilising PPAR-γ protein by promoting deubiquitination at the Lys-466 site.
研究领域:
药理学
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心血管疾病
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分子生物学
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PubMed
高影响因子
Drug Design Development and Therapy
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2019
·
IF 3.208
Mahmoud M Omar,Nermin E Eleraky,Amani M El Sisi,Omiya Ali Hasan
Background Sumatriptan succinate (SUT) is a potent drug used for relieving or ending migraine and cluster headaches. SUT bioavailability is low (15%) when it is taken orally owing to its gastric breakdown and bloodstream before reaching the target arteries. Aim The aim of the study was to enhance SUT bioavailability through developing an intranasal transferosomal mucoadhesive gel. Methods SUT-loaded nanotransferosomes were prepared by thin film hydration method and characterized for various parameters such as vesicle diameter, percent entrapment efficiency (%EE), in vitro release and ex vivo permeation studies. The in-situ gels were prepared using various ratios of poloxamer 407, poloxamer 188, and carrageenan and characterized for gelation temperature, mucoadhesive strength, and rheological properties. Results The prepared transferosomes exhibited percent entrapment efficiencies (%EE) of 40.41±3.02 to 77.47±2.85%, mean diameters of 97.25 to 245.01 nm, sustained drug release over 6 hours, and acceptable ex vivo permeation findings. The optimum formulae were incorporated into poloxamer 407 and poloxamer 188-based thermosensitive in-situ gel using carrageenan as a mucoadhesive polymer. Pharmacokinetic evaluation showed that the prepared in-situ gel of SUT-loaded nano-transferosomes gave enhanced bioavailability, 4.09-fold, as compared to oral drug solution. Conclusion Based on enhancing the bioavailability and sustaining the drug release, it can be concluded that the in-situ gel of SUT-loaded nano-transferosomes were developed as a promising non-invasive drug delivery system for treating migraine.
研究领域:
药物学
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药物递送系统
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纳米技术
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药代动力学
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PubMed
高影响因子
DRUG METABOLISM AND DISPOSITION
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2025
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IF 4
Hong Zhang,Gengyao Qin,Liqi Shi,Ruixing Li,Liang Shen,Weiqun Cao,Yi Tao
GalNAc-conjugated small interfering RNAs (siRNAs) have emerged as a promising new class of therapeutics, demonstrating potential across various disease areas. Metabolic stability is a critical factor in the development of siRNA therapies, necessitating the selection of suitable in vitro metabolism models for comprehensive studies. However, many existing in vitro models often fail to accurately predict in vivo metabolism. Therefore, our objective was to systematically identify the optimal models and conditions that can simulate in vivo metabolism. Inclisiran, a representative GalNAc-conjugated siRNA, was chosen as the model compound for this investigation. A thorough comparison of in vitro metabolism was conducted to identify optimal models and corresponding conditions that could predict Inclisiran's metabolic profiles in rat plasma and liver in vivo. The models tested included serum, plasma, plated hepatocytes, liver homogenate, S9 fractions, tritosomes, lysosomes, and cytosol, reflecting Inclisiran's trajectory from injection to RNA-induced silencing complex (RISC) in hepatocytes. The results indicated that both rat serum and heparin-anticoagulant plasma are suitable models to mimic the nucleolytic metabolism of Inclisiran in in vivo blood. For hepatic metabolism, liver homogenate in phosphate buffer (pH 6.0), liver tritosomes in acetate buffer (pH 5.0), and plated hepatocytes were suitable models. Liver homogenate and cytosol in Tris-HCl buffer (pH 7.4) were effective for studying nuclease-mediated metabolism of Inclisiran's antisense strand under neutral conditions, though they did not fully simulate in vivo metabolism of the sense strand. These findings underscore the importance of selecting appropriate in vitro models and conditions to accurately simulate in vivo metabolism of Inclisiran.
研究领域:
药理学
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分子生物学
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PubMed
高影响因子
CHEMICAL ENGINEERING JOURNAL
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2025
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IF 13.2
Cao Yang,Shanshan Shang,Yixuan Wang,Pei Wang,Lianpeng Sun,Xiao-yan Li
Single-atom catalysts (SACs) have garnered significant attention owing to their high reactivity; however, precise control of their electronic structure for Fenton-like process remains a challenge. In this study, we develop a novel technique for regulating the electronic environment of Cu-SACs to activate peroxymonosulfate (PMS) for highly effective degradation of emerging organic pollutants in water. By in-situ axial modification of Cu-SACs with Cu 2 O nanoclusters within a porphyrin metal–organic framework (Cu 2 O clu -Cu SA /PMOF), we finely tuned the electronic structure of Cu-SACs, leading to the selective generation of singlet oxygen ( 1 O 2 ) as the predominant reactive species in a nonradical Fenton-like process. The rate constant of the Cu 2 O clu -Cu SA /PMOF catalyst for PMS oxidation of sulfamethoxazole (SMX) surpassed that of Cu 2 O and Cu SA /PMOF by 12.9 and 3.7 times, respectively, outperforming most state-of-the-art heterogeneous catalysts for PMS activation. Density functional theory calculations elucidated that the modulation of electronic structure of the Cu sites in Cu 2 O clu -Cu SA /PMOF led to the preferred adsorption of PMS in the terminal-O mode and altered the electron transfer from PMS to the Cu sites for 1 O 2 generation through the self-reaction of SO 5 •− intermediates. This work presents a new material strategy by modulating the functionality of single-atoms via axial incorporation of nanoclusters in MOFs, realizing a highly efficient and selective Fenton-like oxidation process for sustainable water purification.
研究领域:
环境科学
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材料科学
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化学工程
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高影响因子
Food Bioscience
·
2025
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IF 5.9
Di Zhang,Ruren Li,Ying Xu,Futong Song,Nan Zhang,Ting Sun,Liangyan Rong
This study aimed to investigate the impact of intraspecific heterogeneity of Staphylococcus equorum on the physicochemical and aroma characteristics of Chinese fermented sausage. S. equorum strains E-1, NY-3, EH-4, and EH-6 were selected for their environmental resilience, flavor-enhancing potential, and safety, and each was co-inoculated with Pediococcus pentosaceus TP-1 and Staphylococcus xylosus TS-1 to prepare Chinese fermented sausage. The results demonstrated that, compared with the uninoculated fermented sausages, inoculation with starter cultures significantly decreased the pH, moisture content, and water activity ( a w ) of the sausages ( P < 0.05). In particular, the pH declined by approximately 0.14–0.23 units on average, the moisture content decreased by about 0.09–2.5%, and the a w was reduced by 0.004–0.035. Sausage inoculated with S. equorum NY-3, P. pentosaceus TP-1, and S. xylosus TS-1 (TNY-3) exhibited the highest fruity, cheesy, and sweet scores, attributed to elevated levels of ethyl esters and aldehydes. TE-1, inoculated with S. equorum E-1, P. pentosaceus TP-1, and S. xylosus TS-1, showed an increased concentration of ethyl ester compounds. Meanwhile, TEH-4 and TEH-6 exhibited higher levels of methyl esters, which have relatively high odor detection thresholds.
研究领域:
食品微生物学
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应用微生物学
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食品化学
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发酵工程
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风味科学
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高影响因子
ANALYTICA CHIMICA ACTA
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2018
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IF 5.123
Feng Tan,Xiao Jiang,Xianliang Qiao,Daming Sun,Jinsuo Gao,Xie Quan,Jingwen Chen,Suyu Ren,Yi Wang
A diffusive gradients in thin films (DGT) method using a new high-capacity cerium oxide (CeO 2 ) binding gel, for the first time, was developed for measuring dissolved inorganic arsenic in freshwater and seawater . The capacities of the new CeO 2 binding gel were 682 μg and 375 μg for As III and As V , respectively. The masses of As III and As V accumulated by CeO 2 -DGT device increased linearly with time and agreed well with the theoretical value calculated by DGT equation. The arsenic accumulation by CeO 2 -DGT was independent of pH (4.05–9.04) and ionic strength (0.1–750 mM), and common anions including CO 3 2− , SO 4 2− , Cl − and PO 4 3− had no obvious interference. CeO 2 -DGT showed excellent long-term deployment performance in freshwater and synthetic seawater . Field trials with CeO 2 -DGT achieved successfully the time-weighted-average concentrations of total inorganic arsenic in reservoir water (1.38 ± 0.09 μg/L) and coastal seawater (0.45 ± 0.06 μg/L). The results were comparable to those measured by grab sampling. The proposed method was reliable and robust for in-situ measurements of dissolved inorganic arsenic in environmental waters.
研究领域:
环境化学
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分析化学
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水环境监测
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环境地球化学
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污染生态学
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DOI
高影响因子
DYES AND PIGMENTS
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2026
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IF 3.9
Shengjie Feng,Min Wu,Xiaoqian Yi,Xianggao Li,Hongli Liu,Shirong Wang,Dewang Li
Designed a bipolar monomer V–O-8FTPB with D-A structure and styrene groups. • In-situ crosslinked with TEMPIC during annealing to form a polymer network enabling ambipolar transport. • PCE improved from 20.76% to 23.04%, with only 11% degradation after 3000 h at 60–70% relative humidity (RH). Perovskite solar cells (PSCs) have been developed intensively with the rocketing power conversion efficiency (PCE). However, the moisture and thermal instability primarily hinders their practical application, calling for essential crystal bulk and interface protections. Herein a novel cross linkable bipolar semiconductor material, N,N′-diphenyl-N,N′-bis(4-(4-vinylbenzyloxy)phenyl)-2,2′,3,3′,5,5′,6,6′-octafluoro-1,1′-biphenyl-4,4′-diamine (V–O-8FTPB), was designed for perovskite additive engineering. Specifically, this monomer incorporates styrene terminals for crosslinking, as well as the core of fluorinated biphenyl and triphenylamine as respective n-type and p-type moieties. The crosslinking happened during precursor annealing for perovskite crystallization with the aid of another crosslinking agent tri[2-(3-mercaptopropionyl) ethyl]isocyanurate (TEMPIC). A polymer network wrapping perovskite grains was thus constructed. Such modification on grain boundaries and surfaces endowed defect suppression and reinforced resistance against moisture and further harsh liquid-heat damage. Notably, the bipolar V–O-8FTPB better matched the bipolar transporting of perovskites, neither impeding hole nor electron transport. The optimized photovoltaic device with an active area of 0.09 cm 2 delivered a champion PCE of 23.04%. Furthermore, the encapsulated devices retained 90% of initial efficiency after immersion in water for 72 h, or only 17% decay after 48 h in the 85 °C hot water. This work highlights a novel criteria of bipolar monomer design for in-situ cross-linkable additives to enable the framework charge transport and great hydrophobicity. Download: Download high-res image (335KB) Download: Download full-size image
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高影响因子
Plants-Basel
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2025
·Vol. 14
·期 22
·3535
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IF 4.1
Xiuxiu Shen,Shengwen Chen,Mengting Zeng,Benyin Zhang
Biebersteinia heterostemon is a traditional Tibetan medicine known for its antioxidant, hypoglycemic, and anti-atherosclerotic properties. However, its therapeutic effects and mechanisms in the treatment of hyperlipidemia remain unclear. In this study, the ethyl acetate extract of B. heterostemon (BHEE) was first identified as the most effective lipid-lowering fraction through its inhibitory activity on pancreatic lipase and cholesterol esterase. Chemical characterization of BHEE by UHPLC-MS/MS revealed 108 compounds. Network pharmacology and molecular docking analyses were then employed to predict key active components and signaling pathways involved in BHEE’s lipid-lowering effects. A total of 50 active components and 623 targets were selected from the PubChem, SwissADME, and Swiss Target Prediction databases. These targets were intersected with 1606 hyperlipidemia-related targets from GeneCards, OMIM, and DrugBank, resulting in 144 common targets. The “drug-active component-intersecting target-pathway-HLP” and protein–protein interaction (PPI) networks suggested key active components such as 6-methoxytricin, vulgarin, flazin, ganhuangenin, and eupatorin, and core targets including TNF, IL6, AKT1, PPARG, and EGFR. GO and KEGG pathway enrichment analysis highlighted potential signaling pathways, such as AGE-RAGE, PPAR, insulin resistance, TNF, and lipid and atherosclerosis pathways. Molecular docking further predicted the strong binding affinity between key active components and core targets. At the cellular level, BHEE dose-dependently reduced lipid accumulation in FFA-induced HepG2 cells and improved oxidative stress (CAT, GSH, SOD, MDA) and inflammation (TNF-α, IL-6) markers. In conclusion, BHEE may exert its anti-hyperlipidemic effects through modulation of key targets like TNF, IL6, AKT1, PPARG, and EGFR. These findings suggest a multi-target mechanism, though further experimental validation is necessary to confirm these effects. This study provides valuable insights into the potential application of B. heterostemon as a natural therapeutic agent for hyperlipidemia.
研究领域:
生药学
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民族药理学
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分子生物学
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网络药理学
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天然产物研究
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心血管医学
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代谢性疾病
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生物信息学
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DOI
PubMed
高影响因子
RARE METALS
·
2024
·Vol. 43
·期 6
·2682-2694
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IF 9.6
Hu Jie,Lao Hong-Xin,Xu Xiu-Wu,Wang Wei-Kang,Wang Le-Le,Liu Qin-Qin
Though there are numerous intrinsic merits of metal-organic frameworks (MOFs), low charge separation efficiency has imposed heavy restrictions on their photocatalytic application. Herein, in situ porphyrin ligand substitution, as a strategy for improving the charge separation efficiency and increasing the amounts of active sites, has been designed and realized in a Hf-biphenyl dicarboxylic acid (BPDC) MOF. Specifically, a size and geometry matched meso-tetra (4-carboxyphenyl) porphyrin (TCPP) ligand was selected and doped into Hf-BPDC MOF by forming coordinating bonds with Hf centers, forming dual-ligand Hf-BPDC-TCPP MOF. The resultant Hf-BPDC-TCPP MOF showed significantly improved activity and chemical stability in the photocatalytic H 2 generation (261 μmol·g −1 ·h −1 ) and tetracycline (TC) degradation reactions (95.8%), which was 48 and 1.47 folds higher than that of the Hf-BPDC MOF. Photophysical and electrochemical studies revealed that the introduction of porphyrin ligand could generate a stronger internal electric field for boosting the charge separation and transfer, increase the specific surface area for providing more active sites, and narrow the band gap to enhance the visible light absorption. This in situ ligand substitution method provides a promising approach to build a tunable platform for constructing high-performance MOF photocatalysts. Graphical Abstract
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JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
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2013
·Vol. 94
·期 7
·1403-1408
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IF 1.759
Shixiang Xu,Fujie Yan,Zhendan Ni,Qianru Chen,Hui Zhang,Xiaodong Zheng
BACKGROUND Many essential oils were reported to be used as natural, environmental friendly antimicrobial agents. The antifungal activity in vitro and in vivo of an essential oil extracted from Chinese local Laurus nobilis leaves against Alternaria alternata has been studied . RESULT The main components of the essential oil were investigated by means of gas chromatography–mass spectrometry and 14 components were identified. The main ones were eugenol, caryophyllene and cinnamaldehyde. The antifungal test showed that at 800 µg mL −1 of L. nobilis oil completely inhibited the growth of A. alternata . In addition, the conidial germination of the pathogen was significantly inhibited at 200 µg mL −1 , and the weight of mycelia efficiently decreased at 500 µg mL −1 . The in vivo assay indicated that 500 µg mL −1 L. nobilis oil was effective in protecting cherry tomatoes ( Lycopersicon esculentum ) from infection of A. alternata , with an inhibition ratio of 33.9%. Scanning electron microscopy observations of the pathogen revealed significant morphological alterations in the hyphae . CONCLUSION This work suggested that L. nobilis oil could be used as a potential fungicide to control the post-harvest disease caused by A. alternata . © 2013 Society of Chemical Industry
研究领域:
植物学
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真菌学
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食品科学
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DOI
高影响因子
Journal of Environmental Sciences
·
2023
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IF 6.9
Sen Yan,Wei Sun,Sinuo Tian,Zhiyuan Meng,Jinling Diao,Zhiqiang Zhou,Li Li,Wentao Zhu
Several studies have confirmed that the health status of the paternal affects the health of the offspring , however, it remains unknown whether paternal exposure to pesticides affect the offspring health. Here, we used untargeted metabolomics and 16S rRNA sequencing technology, combined with tail suspension test and RT-qPCR to explore the effects of paternal exposure to nitenpyram on the neurotoxicity of offspring. Our results found that the paternal exposure to nitenpyram led to the offspring's depressive-like behaviors, accompanied by the reduction of tryptophan content and the disorder of microbial abundance in the gut of the offspring. Further, we determined the expression of tryptophan metabolism-related genes tryptophanase ( tnaA ) and tryptophan hydroxylase 1 ( TpH1 ) in gut bacteria and colonic tissues. We found that tryptophan is metabolized to indoles rather than being absorbed into colonocytes, which coursed the reduce of tryptophan availability after nitenpyram exposure. In conclusion, our study deepens our understanding of the intergenerational toxic effects of pesticides.
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PubMed
高影响因子
INFLAMMATION
·
2023
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IF 5.1
Feng Yong,Hu Jiapeng,Liu Fen,Shang Yunxiao
Asthma is a chronic inflammatory disease characterized by airway remodeling and lung inflammation. Collagen triple helix repeat containing 1 (CTHRC1), a glycoprotein, is involved in multiple pathological processes, including inflammation and fibrosis. However, the function of CTHRC1 in asthma remains unclear. In the present study, the mouse asthma model was successfully generated by sensitizing and challenging mice with ovalbumin (OVA). CTHRC1 expression at both RNA and protein levels was significantly upregulated in lung tissues of asthmatic mice. Asthmatic mice exhibited significant airway remodeling as evidenced by increased bronchial wall and smooth muscle cell layer thickness, goblet cell hyperplasia and collagen deposition, and epithelial-mesenchymal transition (EMT), but those characteristics were reversed by CTHRC1 silencing. The cell model with transforming growth factor-β1 (TGF-β1) induction in bronchial epithelial cells (BEAS-2B) was conducted to verify the effects of CTHRC1 on EMT, a classic mechanism that mediates airway remodeling. The results showed that TGF-β1 stimulation increased CTHRC1 expression, and CTHRC1 knockdown inhibited TGF-β1-induced EMT. OVA-treated mice also showed increased inflammatory cell infiltration and the production of OVA-specific immunoglobulin E (IgE), interleukin (IL)-4, IL-5, and IL-13, which were decreased by CTHRC1 downregulation. The effects of CTHRC1 on OVA-induced airway inflammation were further determined by treating BEAS-2B cells with IL-13, in which CTHRC1 knockdown reduced the IL-13-induced secretion of pro-inflammatory factors, including IL-4 and IL-5. In conclusion, these results indicate that CTHRC1 silencing attenuates asthmatic airway remodeling and inflammation in vivo and in vitro, suggesting that CTHRC1 may be a potential target for asthma treatment. Graphical Abstract
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高影响因子
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