INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2021
·Vol. 22
·期 11
·5680
·
IF 5.924
Long Tang,Jianchun Jiang,Guoqiang Song,Yajing Wang,Ziheng Zhuang,Ying Tan,Yan Xia,Xianfeng Huang,Xiaoqing Feng
Urolithins (hydroxylated 6H-benzo[c]chromen-6-ones) are the main bioavailable metabolites of ellagic acid (EA), which was shown to be a cognitive enhancer in the treatment of neurodegenerative diseases. As part of this research, a series of alkoxylated 6H-benzo[c]chromen-6-one derivatives were designed and synthesized. Furthermore, their biological activities were evaluated as potential PDE2 inhibitors, and the alkoxylated 6H-benzo[c]chromen-6-one derivative1fwas found to have the optimal inhibitory potential (IC50: 3.67 ± 0.47 μM). It also exhibited comparable activity in comparison to that of BAY 60-7550 in vitro cell level studies.Keywords:alkoxylated 6H-benzo[c]chromen-6-one;phosphodiesterase II;inhibitors;biological activities
研究领域:
药理学
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有机化学
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神经科学
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DOI
PubMed
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
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2023
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IF 4.4
Fang Li,Rong Tang,Yujie Kang,Xiaoyan Cui,Ya Wang,Xiupei Yang
New coccine (NC), as a kind of common colorant, has been frequently used in our daily life. Herein, the fluorescent composite (PNTs@C6) prepared by the hydrophobic non-covalent interaction between peptide nanotubes and coumarin 6 (C6) was designed for the determination of NC. Due to the activation of C6 by peptide nanotubes, the composite exhibits strong green fluorescence emission, which can be selectively quenched by NC through the inner filter effect. Therefore, a new fluorescent method based on the PNTs@C6 composite for NC detection was constructed. Under optimal conditions, the fluorescence quenching of the sensor exhibits a good linear relationship with the concentration of NC in the range of 0.01–10 μM and the limit of detection is 3.6 nM. Furthermore, the strategy shows simplicity, rapid response and high selectivity and has been successfully applied to the detection of NC in food samples.
研究领域:
分析化学
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食品科学
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纳米技术
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光谱学
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PubMed
高影响因子
SENSORS AND ACTUATORS B-CHEMICAL
·
2021
·
IF 7.46
Dongxia Nie,Dakai Guo,Qingwen Huang,Wenbo Guo,Jianhua Wang,Zhihui Zhao,Zheng Han
Nanocomposites of thiol-terminated liposomes encapsulating with coumarin-6 ( [email protected] ) were successfully prepared via a simple thin-film dispersion method to construct a novel fluorescent sensor for selectively detecting trace amounts of patulin. Thiol group ( SH) was designed not only as a specific recognition element to capture patulin, but also as a convenient linker for the further separation of patulin-derivatized and un-derivatized [email protected] by combination with magnetic NH 2 [email protected] 3 O 4 nanoparticles. Liposomes primarily provided an effective platform with a large surface area for facilitated accommodation of large amounts of recognition element ( SH group) and fluorophore (coumarin-6). In such an assay protocol, a reliable link was established between the changes in fluorescent intensity (ΔF) from the nanocomposites of [email protected] /NH 2 [email protected] 3 O 4 and the concentrations of patulin in the range of 0.05–20 ng mL −1 , with the correlation coefficient of 0.996. This approach also effectively eliminated the background interference from other mycotoxins and metal ions. Under the optimal conditions, the designed sensor displayed excellent performance for patulin analysis, with an extremely low detection limit (0.033 ng mL −1 ), high recovery (96.2–107.6 %) and excellent selectivity. Furthermore, the feasibility of its applications has also been demonstrated in the analysis of real juice samples, providing a novel tactics for rational design of a fluorescence assay, for point-of-care diagnostics of patulin, with great potential to be extended to other hazardous compounds by substitution of the recognition elements.
研究领域:
分析化学
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纳米技术
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食品安全
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生物技术
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DOI
高影响因子
Nature Communications
·
2022
·Vol. 13
·期 1
·1-9
·
IF 17.694
Li Chong,Liu Qi,Tao Shengyang
Achieving an ideal light-harvesting system at a low cost remains a challenge. Herein, we report the synthesis of a hybrid dye system based on tetraphenylene (TPE) encapsulated organic dyes in a continuous flow microreactor. The composite dye nanoparticles (NPs) are synthesized based on supramolecular self-assembly to achieve the co-emission of aggregation-induced emission dyes and aggregation-caused quenching dyes (CEAA). Numerical simulations and molecular spectroscopy were used to investigate the synthesis mechanism of the CEAA dyes. Nanoparticles of CEAA dyes provide a platform for efficient cascade Förster resonance energy transfer (FRET). Composite dye nanoparticles of TPE and Nile red (NiR) are synthesized for an ideal light-harvesting system using coumarin 6 (C-6) as an energy intermediate. The light-harvesting system has a considerable red-shift distance (~126 nm), high energy-transfer efficiency (Φ ET ) of 99.37%, and an antenna effect of 26.23. Finally, the versatility of the preparation method and the diversity of CEAA dyes are demonstrated.
研究领域:
材料科学
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纳米技术
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化学
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光学
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DOI
PubMed
高影响因子
CARBOHYDRATE POLYMERS
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2022
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IF 10.723
Yuhui Sheng,Xingchen Sun,Jingtian Han,Wei Hong,Jie Feng,Shuyang Xie,Youjie Li,Fangwei Yan,Keke Li,Baocheng Tian
An N -acetylcysteine functionalized chitosan oligosaccharide-palmitic acid conjugate (NAC-COS-PA) with bioadhesive and permeation promoting properties was synthesized to enhance transocular drug delivery. Flurbiprofen (FB) loaded self-assembled NAC-COS-PA nanomicelles (NAC-COS-PA-FB) were prepared and the drug loading was 7.35 ± 0.32%. Human immortalized corneal epithelial (HCE-T) cell cytotoxicity and hen's egg test-chorioallantoic membrane assays confirmed that the conjugate had good biocompatibility. The transportation efficiency of coumarin-6 (C6) loaded nanomicelles in the HCE-T cell monolayer was approximately 1.97 times higher than that of free C6. Decreased intracellular Ca 2+ concentration and cell membrane potential , increased cell membrane fluidity , and reversible changes in the F-actin cytoskeleton are presumed to be responsible for the enhanced drug permeation. NAC-COS-PA exhibited strong binding capacity with mucin and rabbit eyeball. In vivo pharmacokinetics indicated that the area under the curve (AUC 0 – 6 h ) and the maximum concentration (C max ) of NAC-COS-PA-FB were approximately 1.92 and 2.44 times that of the FB solution, respectively. NAC-COS-PA-FB demonstrated the best in vivo anti-inflammatory efficacy compared to unfunctionalized nanomicelles (COS-PA-FB) and FB solution. Consequently, NAC-COS-PA appears to be a promising bioadhesive carrier for ophthalmic delivery.
研究领域:
药学
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药物递送系统
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眼科学
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生物技术
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药代动力学
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产品关联
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING JOURNAL
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2025
·
IF 13.2
Hongyan Lu,Ying Cheng,Xiangling Pu,Xingtao Zhao,Ruolan Li,Ruiqi Sun,Xiaoman Xie,Mingyue Wu,Shuo Zhang,Qiong Pan,Jin Chai
Simultaneously alleviating oxidative stress and remodeling inflammatory microenvironment holds great promise for treating inflammatory bowel disease (IBD). Nevertheless, the efficacy of conventional therapies remains limited by poor targeting, insufficient modulation of the inflammatory microenvironment and serious adverse effects. Here, inspired by the intrinsic biological properties of metal-curcumin (Cur) complexes, a nanozyme-mediated ion-exchange strategy was proposed to enhance the targeted therapeutic effect of Cur for IBD. Specifically, copper-doped mesoporous polydopamine nanoparticles (Cu-mPDA) with dual enzyme-like activities were served as drug carriers to encapsulate water-soluble zinc-curcumin (Zn-Cur) and further modified with hyaluronic acid (HA), yielding Zn-Cur/Cu-mPDA@HA. Encouragingly, Zn-Cur/Cu-mPDA@HA could degrade in inflammatory microenvironment, releasing Zn-Cur and Cu 2+ , which subsequently in situ generate Cu-Cur with high antioxidant activity by ion-exchange reaction. Notably, Zn-Cur/Cu-mPDA@HA not only exhibited favorable targeting specificity toward M1 macrophages in inflamed colon tissues, but also displayed enhanced abilities to scavenge ROS, inhibit pro-inflammatory factors secretion and promote macrophages repolarization from the pro-inflammatory M1 state to the anti-inflammatory M2 subtype. Mechanistically, Zn-Cur/Cu-mPDA@HA suppressed the TLR4/MyD88/NF-κB pathway, breaking the inflammation-free radical vicious cycle, thereby attenuating chronic inflammation and fostering a favorable microenvironment for intestinal barrier restoration. Such a nanozyme-mediated ion-exchange and in situ drug generation strategy offers a new insight for designing nanomedicines for the treatment of IBD and other inflammatory diseases.
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高影响因子
JOURNAL OF CONTROLLED RELEASE
·
2025
·
IF 11.5
Zhiwei Chen,Xinyu Di,Heyan Chen,Shengnan Song,Siyi Zhu,Leer Cai,Yuqi Han,Yongshuai Kang,Dingchao Shen,Huirong Huang,Aimin Cai,Hailun Zheng,Qing Yao,Maoping Chu,Ruijie Chen,Longfa Kou
Coronary artery lesions are a major complication of Kawasaki disease (KD), where the local microenvironment is marked by excessive oxidative stress and persistent inflammation, presenting significant challenges for effective treatment. M1-polarized macrophages dominate these lesions, releasing pro-inflammatory mediators that aggravate vascular injury. Regulating macrophage polarization from the M1 to M2 phenotype thus offers a promising therapeutic strategy. Here, we developed a reactive oxygen species (ROS)-responsive nanoplatform, HA-Sim@BRPL, to deliver simvastatin (Sim) specifically to inflamed coronary tissues. The nanocarrier is constructed from poly- l -lysine conjugated with bilirubin (BR), which self-assembles and enables ROS-triggered Sim release through BR's oxidative conversion to hydrophilic biliverdin. Surface decoration with hyaluronic acid (HA) facilitates selective uptake by CD44-expressing macrophages rather than cardiomyocytes. HA-Sim@BRPL effectively reduces intracellular ROS, promotes M2 macrophage polarization, and enhances endothelial cell survival via intercellular signaling. In a KD mouse model, HA-Sim@BRPL significantly attenuated coronary artery lesions and improved cardiac function. These results highlight a rationally designed nanomedicine that integrates oxidative stress responsiveness and inflammatory cell targeting, providing a promising therapeutic approach for coronary complications in KD.
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF CONTROLLED RELEASE
·
2025
·
IF 11.5
Kaiming Li,Ziming Lin,Ting Wu,Jintong Zhou,Jie Wu,Yupeng Zhou,Huimin Gao,Ya Lin,Xufeng Chen,Huae Xu,Xiaolin Li
Small cell lung cancer (SCLC) is a highly lethal malignancy with a < 7 % 5-year survival rate. Platinum-based chemotherapy remains the standard treatment; however, its clinical efficacy is limited. There is an urgent need for new therapeutic strategies. In this study, we developed a RGD labeled liposome (CS/RGD-Lipo) encapsulating both cisplatin and surufatinib as a target delivery system against SCLC, aimed at enhancing ferroptosis to improve cisplatin efficacy, inhibiting angiogenesis, and reversing TAM phenotypes to overcome immunosuppression. Additionally, we combined CS/RGD-Lipo with αCD47 to further enhance antitumor activity. In tumor-bearing mice, CS/RGD-Lipo effectively targeted tumor tissues for the delivery of cisplatin and surufatinib. The combination of CS/RGD-Lipo with αCD47 significantly promoted ferroptosis in SCLC, improved anti-angiogenesis, induced the conversion of M2 macrophages to M1 macrophages, and enhanced the M1 macrophages-mediated antitumor immune response, resulting in a marked inhibition of tumor growth in SCLC mouse models. Taken together, this work demonstrates a feasible therapeutic approach to inhibit SCLC by combining cisplatin, surufatinib, and αCD47 to leverage tumor ferroptosis, angiogenesis inhibition and tumor-associated macrophage polarization.
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高影响因子
CARBOHYDRATE POLYMERS
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2025
·
IF 12.5
Chen-Chen Wang,Ran Feng,Fan Wang,Yan Liu,Bao Zhang
Resveratrol (RES) is a promising anti-inflammatory polyphenol for treating ulcerative colitis (UC), but its efficacy is constrained by poor solubility and colon-targeting efficiency. Biotin, as an active ligand, has been widely used to functionalize nanocarriers to enhance intestinal cell permeability, thereby increasing the absorption of bioactive components. Biotin modification enlarged the helical cavity of starch into a V7-type structure, creating a more favorable hydrophobic microenvironment for the encapsulation of guest molecules. The mass ratio of resveratrol to starch was 1:10 to 1:2, resveratrol acted as a nucleator, forming ordered B+V crystals with minimal size (312.4 nm), uniform distribution, and high encapsulation (20.02 %). Excess resveratrol distorted helices, causing aggregation and reduced efficiency. Biotin modification facilitating nanoparticles uptake by Caco-2 via receptor-mediated endocytosis. Furthermore, the colon length of colitis mice treated with resveratrol-loaded BSNP increased by 25 % ( P < 0.001) compared to that of untreated colitis mice. RES@BSNP can increase the relative abundance of beneficial gut microbiota such as Christensenellales and Lactobacillus and suppressing pro-inflammatory factor secretion, ultimately alleviating UC. This work elucidates the role of guest-molecule concentration and biotin functionalization in starch-based nanoparticle design, offering a promising strategy for targeted polyphenol delivery in colitis treatment.
研究领域:
纳米医学
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药物递送
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炎症性肠病
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多酚治疗
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功能纳米材料
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产品关联
DOI
PubMed
高影响因子
International Journal of Pharmaceutics-X
·
2025
·
IF 6.4
Haiming Huang,Jiyong Peng,Zhiting Gao,Yongtong Huang,Wenyang Song,Wenhao Wu,Song Gao,Songsen Chen,Qingchun Xie,Shu Zhang,Jiu Wang
Glioblastoma treatment is hindered by the blood-brain barrier (BBB), which limits the penetration and accumulation of chemotherapeutic agents. Paclitaxel (PTX), an effective chemotherapeutic drug, faces clinical challenges due toits poor solubility and restricted ability to traverse the BBB. Consequently, there is an urgent need for advanced drug delivery systems to facilitate the efficient and safe translocation of PTX across the BBB. In this study, PTX was encapsulated within nanoemulsions (NEs) conjugated to lactoferrin (Lf) via electrostatic interactions, followed by the optimization of its formulation. To investigate cellular uptake and BBB penetration, fluorescent dye coumarin 6 (C6) was incorporated into NEs. Uptake was evaluated in GL261 cells and BBB penetration in hCMEC/D3 cells. Further studies were conducted on the biodistribution in mice and the therapeutic efficacy in murine intracranial glioblastoma model. Characterization of PTX@Lf-NE demonstrated stability, biological safety, and favorable release properties. Notably, the fluorescence intensity of C6@Lf-NE was twice of C6@NE in one hour post-administration, and the drug uptake rate decreased with the addition of free Lf, suggesting that Lf promotes the ability of NEs to traverse the BBB. In vivo distribution further revealed that Lf-NE increased brain distribution while reduced accumulation in other organs. In the glioblastoma model, it was found that the bioluminescent intensity of PTX@Lf-NE was significantly decrease than that of PTX@NE on the 15th day of administration, indicating that the modification with Lf facilitated the targeted delivery of PTX and enhanced its therapeutic efficacy. This study successfully designed and developed an effective drug delivery system for glioblastoma treatment, which improves the translocation of drugs across the BBB.
研究领域:
肿瘤学
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纳米医学
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药物递送系统
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制药纳米技术
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神经肿瘤学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF CONTROLLED RELEASE
·
2025
·
IF 11.5
Zhong Shao,Ke Li,Hao Guo,Yangyang Cheng,Shiyong Zhang
Hypertensive chronic kidney disease (CKD) remains incurable, mainly because the current therapies are difficult to concurrently target elevated blood pressure and multifaceted renal abnormalities. Herein, we present an oral H 2 S nanomedicine, poly(lipoic acid trisulfide) (pLATS), with synergistic antihypertensive and renoprotective activities for treating hypertensive CKD. pLATS not only enables efficient oral delivery across multiple biological barriers via trisulfide exchange with thiols at mucosal, epithelial, and renal cellular interfaces, but also undergoes thiol-triggered intracellular depolymerization to achieve sustained release H 2 S and lipoic acid (LA)/LATS over 60 h, with H 2 S exerting multifactorial regulatory effects underlying hypertensive CKD. Meanwhile, LA/LATS upregulate H 2 S-producing enzymes, promoting sustained endogenous H 2 S biogenesis. In vivo, pLATS demonstrates markedly improved pharmacokinetics over its monomeric precursor, effectively lowering blood pressure, urine albumin-to-creatinine ratio, and plasma urea and creatinine by modulating genes in the renin-angiotensin system and endothelial function, surpassing the clinical antihypertensive losartan. In essence, this study pioneers a paradigm for comprehensive treatment of hypertensive CKD, with potential applications extending to broader chronic diseases.
研究领域:
纳米医学
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心肾综合征
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药理学
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药物递送
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慢性肾病
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产品关联
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2025
·
IF 13.2
Jingzhe Sheng,Tengda Du,Jingyi Zhang,Yuetong Huang,Shuo Wang,Mengyu Liu,Tao Zhang,YingJie Zhao,Hao Zhang,Qian Lv,Can Zhao,Xiaoxue He,Xinyu Cui,Mengze Gao,Qi Lu,Zhonggui He,Bingjun Sun,Tian Liu,Jin Sun
Hybrid chalcogen bonds bridged homodimer prodrug nanoassemblies demonstrated excellent self-assembly stability, sensitive redox responsiveness, and high drug delivery efficiency. However, nonadjustable high sensitivity of hybrid chalcogen bonds was usually accompanied by oxidative instability in the oxygen-rich systemic circulation, which limited their efficacy. To address this dilemma, we developed Mn 2+ -coordinated homodimer prodrug nanoassemblies. The coordination between Mn 2+ and chalcogen (Te, Se, S) mediated electron cloud redistribution through d-orbital hybridization, facilitating electron sharing. This electronic delocalization reduced the electron density surrounding chalcogen centers, improving their chemical stability and the pharmacokinetic properties of prodrugs. This coordination complex acted as a programmable dual-lock activation nanoregulator: (1) pH-sensitive cleavage of Mn 2+ coordination bonds within the tumor microenvironment mediated nanostructural disassembly, followed by (2) GSH/ROS-responsive prodrug release. Critically, the sequential activation mechanism maintained systemic inertness in normal tissues while exhibiting superior activation efficiency within tumors. Meanwhile, Mn 2+ activated the cyclic GMP-AMP synthase-stimulator of interferon genes pathway, enhancing antigen presentation and immune responses for a combined chemoimmunotherapeutic effect. This work proposed the reasonable design and construction of the metal-coordinated homodimer prodrug nanoassemblies based on the interactions between chalcogen of linkers and metal atoms, opening up new opportunities for developing more effective cancer therapeutics.
研究领域:
纳米医学
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癌症治疗
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药物递送
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肿瘤免疫学
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配位化学
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材料科学
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产品关联
DOI
高影响因子