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INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES · 2021 ·Vol. 22 ·期 11 ·5680 · IF 5.924

Design, Synthesis, and Biological Evaluation of Novel 6H-Benzo[c]chromen-6-one Derivatives as Potential Phosphodiesterase II Inhibitors

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 · 有机化学 · 神经科学
✓ 已验证 DOI PubMed 高影响因子
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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY · 2023 · IF 4.4

Fluorescent composite based on peptide nanotubes activating coumarin 6 for sensitive detection of new coccine in food samples

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 · 食品科学 · 纳米技术 · 光谱学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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SENSORS AND ACTUATORS B-CHEMICAL · 2021 · IF 7.46

A novel insight into fluorescent sensor for patulin detection using thiol-terminated liposomes with encapsulated coumarin-6 as signal probe

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 · 纳米技术 · 食品安全 · 生物技术
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Nature Communications · 2022 ·Vol. 13 ·期 1 ·1-9 · IF 17.694

Coemissive luminescent nanoparticles combining aggregation-induced emission and quenching dyes prepared in continuous flow

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 · 纳米技术 · 化学 · 光学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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CARBOHYDRATE POLYMERS · 2022 · IF 10.723

N-acetylcysteine functionalized chitosan oligosaccharide-palmitic acid conjugate enhances ophthalmic delivery of flurbiprofen and its mechanisms

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 · 药物递送系统 · 眼科学 · 生物技术 · 药代动力学
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