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JOURNAL OF HETEROCYCLIC CHEMISTRY · 2015 ·Vol. 54 ·期 1 ·784-788 · IF 0.787

Synthesis of 10-substituted 3,6-Diphenyl-9-aryl-3,4,6,7,9,10-hexahydro-acridine-1,8(2H,5H)-dione Derivatives and Biological Activities

Fang-Ming Wang,Dan Bao,Bing-Xiang Hu,Ze-Yu Zhou,Deng-Deng Huang,Li-Zhuang Chen,Yuan-Yuan Dan

A series of novel 10-substituted 3,6-diphenyl-9-aryl-3,4,6,7,9,10-hexahydroacridine-1,8(2H,5H)-dione derivatives 2 were synthesized by condensation of compounds 1 with amines, which the compounds 1 were synthesized by 5-phenylcyclohexane-1,3-dione and aromatic aldehydes according to Knoevenagel, Michael, and cyclization reactions in the presence of a very small amount of l-proline as catalyzed at room temperature. The structures of all the synthesized compounds were characterized by IR, 1H NMR, and MS. In addition, the molecular structures of compound 1a have been determined by single-crystal X-ray diffraction analysis.

研究领域: 有机化学 · 药物化学 · 生物化学
✓ 已验证 DOI 高影响因子
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JOURNAL OF NANOBIOTECHNOLOGY · 2025 · IF 12.6

Enzyme-assisted nanopore sensor for sensitive and multiplexed detection of microRNAs

Huang Xiaobin,Yi Yakun,Zhou Ke,Liu Lei,Wu Hai-Chen

MicroRNAs (miRNAs) play crucial roles in the pathogenesis of diverse diseases; however, their extremely low abundance in complex biological systems makes highly sensitive and specific multiplexed detection particularly challenging. Here, we report an enzyme-assisted nanopore sensor that enables simultaneous and ultrasensitive detection of multiple miRNAs. Capture DNA (cDNA) immobilized on streptavidin-coated magnetic beads specifically hybridizes with target miRNAs, opening the cDNA hairpin and facilitating the binding of alkaline phosphatase (ALP)-labeled detection DNA to form stable complexes. ALP catalyzes the dephosphorylation of designed phosphorylated peptide probes, inducing conformational and charge changes that yield distinct current blockade signatures in the presence of cucurbit [ 7 ]uril within the nanopore. This strategy reduces background interference via magnetic separation and amplifies detection signals through enzymatic reactions, thereby markedly improving sensitivity for low-abundance miRNAs. The sensor achieves a broad dynamic range from 10.0 fM to 10.0 nM across three target miRNAs, with femtomolar-level limits of detection. By integrating molecular separation, enzymatic amplification, and nanopore sensing, this platform provides a robust approach for precise miRNA analysis, offering strong potential for early disease diagnosis.

CAS / MDL: 60-00-4
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOORGANIC CHEMISTRY · 2020 · IF 4.831

Discovery of novel aminophosphonate derivatives containing pyrazole moiety as potential selective COX-2 inhibitors

Bo Zhang,Xiu-Ting Hu,Kang-Min Zhou,Yu-Shun Yang,Hai-Liang Zhu

Cyclooxygenase is critical for maintaining physiological functions, whereas overexpression of COX-2 was closely implicated in various cancers. In this study, a series of novel aminophosphonate derivatives containing pyrazole moiety were synthesized with their anti-cancer activity evaluated. In vitro assays of the target compounds showed that Z21 displayed excellent COX-2 inhibitory activity against COX-2 (IC 50  = 0.22 ± 0.04 µM) and anti-proliferative activity against MCF-7 cell (IC 50  = 4.37 ± 0.49 µM). The apoptosis induction of compound Z21 was confirmed by flow cytometry and polymerase chain reaction. Further investigation demonstrated that compound Z21 induced apoptosis of MCF-7 cells through a mitochondrion-dependent pathway and involved cell-cycle arrest in G2 phase. Overall, these results provided some new insights into the design of therapeutic drugs for COX-2 inhibitors and indicated the connection between selective COX-2 inhibition and the anti-tumor activity.

研究领域: 药理学 · 肿瘤学 · 药物化学
✓ 已验证 DOI PubMed 高影响因子
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Theranostics · 2019 · IF 8.063

Supramolecular therapeutics to treat the side effects induced by a depolarizing neuromuscular blocking agent

Xiangjun Zhang,Qian Cheng,Lanlan Li,Liqing Shangguan,Chenwen Li,Shengke Li,Feihe Huang,Jianxiang Zhang,Ruibing Wang

Succinylcholine (Sch) is the only depolarizing neuromuscular blocking agent widely used for rapid sequence induction in emergency rooms. Unfortunately, a variety of (sometimes lethal) adverse effects, such as hyperkalemia and cardiac arrest, are associated with its use, and currently there are no specific antidotes to reverse Sch or to treat these side-effects. Methods: The binding behaviors of Sch and several synthetic receptors, including cucurbit[7]uril, sulfo-calix[4]arene and water-soluble carboxylatopillar[6]arene (WP[6]), were first investigated. With a mouse model, a leathal dose of Sch was selected for evaluation of the antidotal effects of these synthetic receptors on Sch induced mortality. The antidotal effects of a selected synthetic receptor, WP[6], on Sch induced cardiac arrhythmias, hyperkalemia, rhabdomyolysis and paralysis were subsequently evaluated with rat and mouse models. The reversal mechanism was also investigated at a cellular level. Results: All of these macrocyclic molecules exhibited relatively high binding affinities with Sch in vitro . In a Sch-overdosed mouse model, immediate injection of these synthetic receptors right after Sch administration increased the overall survival rate, with WP[6] standing out with the most effective antidotal effects. In addition, administration of WP[6] also reversed the paralysis induced by Sch in a mouse model. Moreover, infusion of WP[6] to Sch-overdosed rats reduced the incidence of cardiac arrhythmia, inhibited the otherwise abnormally high serum potassium levels, and relieved the muscular damage. At the cellular level, WP[6] reversed the Sch induced depolarization and reduced the efflux of intracellular potassium. Conclusion: Synthetic receptors, particularly WP[6], exhibited high binding affinities towards Sch, and presented a significant potential as supramolecular therapeutics to treat the various side effects of Sch by specifically sequestering Sch in vivo .

研究领域: 药理学 · 药物化学 · 治疗学
✓ 已验证 DOI PubMed 高影响因子
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Inorganic Chemistry Frontiers · 2019 ·Vol. 6 ·期 10 ·2837-2849 · IF 5.934

Mixing the valence control of Eu2+/Eu3+ and energy transfer construction of Eu2+/Mn2+ in the solid solution (1 − x)Ca3(PO4)2–xCa9Y(PO4)7 for multichannel photoluminescence tuning

Peipei Dang,Dongjie Liu,Guogang Li,Sisi Liang,Hongzhou Lian,Mengmeng Shang,Jun Lin

Recently, controllable photoluminescence tuning by devising a solid solution framework, adjusting the valence mixing of Eu2+/Eu3+ and designing efficient energy transfer between activator ions has been extensively investigated and reported due to its significant advantages in the improvement and regulation of the luminescence performances of white light-emitting diodes (W-LEDs). In this study, we designed a series of novel Eu2+-doped (1 − x)Ca3(PO4)2–xCa9Y(PO4)7 (x = 0–1.0) isostructural solid solution phosphors with a β-Ca3(PO4)2-type structure, and powder samples were prepared via the traditional high-temperature solid-state reaction process. The crystal field variation around the Eu2+ ions causes superposition of linear luminescence and induces optical property tuning with a change in the solid solution ratio, x, values. Besides the high-energy emission peak at 418 nm in Ca3(PO4)2:0.03Eu2+, another low-energy emission peak at 486 nm was observed with the formation of the solid solution. Moreover, the corresponding high-energy emission peaks shifted from 418 to 430 nm, and the luminescence intensity of the low-energy emission at 486 nm increased with an increase in x, which was attributed to the combined effect of crystal field splitting of the local lattice and superposition of linear luminescence. In addition, tunable emission across the whole white light region could be realized by constructing a solid solution and adjusting the overall Eu concentration in (1 − x)Ca3(PO4)2–xCa9Y(PO4)7:Eu (x = 0.5, 0.7, 0.9, and 1.0), and the corresponding luminescence mechanisms have been proposed and discussed in detail. In the pursuit of precise color tuning, we also tested the Eu2+ → Mn2+ energy transfer in different compositions (x = 0.2, 0.5, 0.7, and 0.9) of the solid solution phosphors, and successive emission tuning from the blue and cyan range and then the red range was successfully achieved. Finally, the temperature-dependent photoluminescence and decay time were revealed systematically, and the corresponding mechanisms for the thermal quenching behavior have been discussed. This study provides a new perspective for color tuning originating from the simultaneous isostructural solid solution, valence mixing of Eu2+/Eu3+ and efficient energy transfer.

研究领域: 材料科学 · 光学材料 · 无机化学 · 固体物理 · 发光学
✓ 已验证 DOI 高影响因子
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Journal of Macromolecular Science Part B-Physics · 2024 · IF 1.2

Novel Design of Protein-functionalized Gold Nanoparticles Loaded with Dichlororuthenium (II) (p-cymene) (1,3,5-triaza-7-phosphaadamantane) (RAPTA-C) to Induce Reactive Oxygen Species (ROS)-mediated Apoptosis in Ovarian Cancer Cells

Chunbo Pan,Guanghua Gu

Potentially beneficial novel approaches to cancer treatment, particularly for drug-resistant malignancies, include synergistic therapies that combine chemotherapy with photothermal therapy. In our research described here we developed a unique silk protein-functionalized gold nanoparticles (AuNP) formulation for effective combinatorial photothermal therapy (PTT) and chemotherapy against ovarian cancer cells. The main goal of the present investigation was the fabrication of silk protein-functionalized gold nanoparticles (AuNPs) embedded with Dichlororuthenium (II) (p-cymene) (1,3,5-triaza-7-phosphaadamantane) (RAPTA-C) molecules (RC@Au-SF NPs) to improve apoptosis in ovarian cancer cells. The structural and morphological analyses of the prepared nanoformulations confirmed the successful fabrication and uniform distributions of Au-SF NPs with RAPTA-C. We observed the RC@Au-SF NPs showed enhanced toxicity to ovarian cancer cell lines with near infrared (NIR)-light exposure. The RAPTA-C loaded Au-SF NPs significantly improved the internalization of the nanoparticles inside the cells resulting in intracellular reactive oxygen species (ROS) generation, mitochondrial membrane potential (MMP) and cell apoptosis on ovarian cancer (SKOV-3 & A2780) cells. We suggest the outcome of the developed formulation for anti-ovarian cancer action will be highly promising for future cancer control research.

研究领域: 纳米医学 · 肿瘤学 · 药学 · 生物无机化学 · 光热治疗
✓ 已验证 DOI 高影响因子
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MICROCHEMICAL JOURNAL · 2025 · IF 5.1

An environmentally friendly cucurbit[7]uril-mediated magnetic-assisted matrix solid-phase dispersion extraction combined with HPLC-MS/MS for multiple analysis of pharmaceuticals and personal care products in aquatic organisms

Huiyu He,Rui Wang,Rongbin Nie,Nan Dong

Trace amounts of pharmaceuticals and personal care products (PPCPs) in aquatic environment poses a non-negligible risk to human health. Here, an environmentally friendly cucurbit[7]uril-mediated magnetic-assisted matrix solid phase dispersion (Q[7]- m -MSPD) extraction method was developed for extracting PPCPs from complex aquatic organisms. The extraction of PPCPs were achieved via the host-guest interaction between Q[7] and targets, significantly reducing the matrix interference. Gold magnetic nanoparticles (AuMNPs) were chelated to Q[7]-target complexes and used for purification and enrichment via magnetic solid-phase extraction (MSPE), effectively replacing the complex operation of sample loading and elution on SPE columns in MSPD. Coupled with high performance liquid chromatography-tandem mass spectrometry, multiple analysis of 14 PPCPs in 3 aquatic plants and an aquatic animal were achieved, with detection limits ranging from 0.0015 to 0.0179 μg/kg, recoveries ranging from 71.06 to 113.6 %, and enrichment factors within 46 to 152. The green chemistry assessment confirmed the environmental friendliness, economic feasibility, and application potential of the Q[7]- m -MSPD, with an AGREE score of 0.63 and a BAGI score of 72.5. By integrating the merits of MSPD and MSPE, the proposed approach exhibited high sensitivity and anti-interference capability, simple operation, and great environmental friendliness. Therefore, the approach provided a green method for simultaneously detecting multiple hazardous residues in complex matrices owing to the broad-spectrum molecular recognition capability of Q[7] , which has a good application prospect in food safety and environmental monitoring.

✓ 已验证 产品关联 DOI 高影响因子
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Food Bioscience · 2025 · IF 5.9

Human FABP7 selectively captures docosahexaenoic acid over eicosapentaenoic acid: A potential protein-based platform for affinity purification of ω-3 lipids

Yuling Tang,Xunjiao Wei,Yonghua Wang,Wen Chen

Docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA) are principal omega-3 polyunsaturated fatty acids (PUFAs) nutritional and pharmaceutical interest. However, their near-isomeric structures render large-scale separation technically demanding and costly. Here we evaluate human fatty-acid-binding protein 7 (FABP7) as a biorecognition element capable of discriminating between these two lipids. Recombinant FABP7, expressed and purified from Escherichia coli , was analyzed for its binding affinity toward DHA and EPA by bio-layer interferometry (BLI). FABP7 bound DHA with an equilibrium dissociation constant K d  = 80.18 ± 3.71 mmol/m 3 , whereas binding to EPA was 7.5-fold weaker (K d  = 600.2 ± 30.2 mmol/m 3 ). Competitive BLI experiments confirmed that DHA efficiently displaced pre-bound EPA, while EPA was largely unable to remove DHA even at millimolar excess. These findings demonstrate that FABP7 possesses intrinsic molecular selectivity for DHA over EPA and could therefore serve as the affinity component of bio-based fractionation platforms. This work establishes a quantitative framework for engineering FABP-derived resins or sensors aimed at sustainable, low-energy purification of high-value ω-3 lipids.

CAS / MDL: 10417-94-4 6217-54-5
研究领域: 分子生物学 · 脂质代谢 · 生物化学 · 结构生物学 · 生物分离工程
✓ 已验证 产品关联 DOI 高影响因子
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DRUG DELIVERY · 2023 · IF 6

Tumor microenvironment-responsive micelles assembled from a prodrug of mitoxantrone and 1-methyl tryptophan for enhanced chemo-immunotherapy

Ru Wang,Nuannuan Li,Tianyu Zhang,Yiying Sun,Xiaoyan He,Xiaoyan Lu,Liuxiang Chu,Kaoxiang Sun

Mitoxantrone (MX) can induce the immunogenic-cell death (ICD) of tumor cells and activate anti-tumor immune responses. However, it can also cause high expression of indole amine 2, 3-dioxygenase (IDO) during ICD, leading to T-cell apoptosis and a weakened immune response. An IDO inhibitor, 1-methyl tryptophan (1-MT), can inhibit the activity of IDO caused by MX, resulting in enhanced chemo-immunotherapy. Here, MX-1-MT was connected by ester bond which could be broken in an acidic tumor microenvironment. MX-1-MT was combined with polyethylene glycol (PEG) via a disulfide bond which could be reduced by glutathione overexpressed in tumors, thereby accelerating drug release at target sites. Folic acid-modified distearoyl phosphoethanolamine-polyethylene glycol (DSPE-PEG-FA) was introduced to form targeting micelles. The micelles were of uniform particle size, high stability, and high responsiveness. They could be taken-up by drug-resistant MCF-7/ADR cells, displayed high targeting ability, and induced enhanced cytotoxicity and ICD. Due to 1-MT addition, micelles could inhibit IDO. In vivo studies demonstrated that micelles could accumulate in the tumor tissues of nude mice, resulting in an enhanced antitumor effect and few side-effects.

研究领域: 药学 · 癌症研究 · 纳米技术 · 免疫学 · 药物递送系统
✓ 已验证 DOI PubMed 高影响因子
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Inorganic Chemistry Frontiers · 2026 · IF 6.2

Ba 2+ Co-doping Enhances Phase Purity and Enables Narrow-Band Green Emission in Sr 5/6 Li 17/6 Al 7/6 O 4 :Eu 2+ Phosphor for Backlight Display Applications

Chenyang Zhan,Zihao Wang,Sisi Liang,Zhi-Ying Zhao,Hanru Chen,Jiahe Yu,Haomiao Zhu

Alkaline earth lithoaluminates with the UCr4C4-type structure have demonstrated considerable potential in achieving narrow-band emissions from Eu 2+ . However, obtaining single-phase powder samples with green-emitting remains challenging. In this study, we address this issue by co-doping Ba 2+ into the novel UCr4C4-type system Sr5/6-xBaxLi17/6Al7/6O4:Eu 2+ , which significantly enhances phase purity and structural homogeneity. This approach not only reduces the emission bandwidth from 66 nm (2241 cm -1 ) to 51 nm (1830 cm -1 ) but also induces a blue shift to 529 nm, fine-tuning the emission into the desired deep green region. Through detailed mechanistic studies-including low-temperature spectroscopy and luminescence decay analysis-we identify the presence of multiple Eu 2+ emission centers associated with distinct Sr 2+ sites. Ba 2+ doping is shown to promote dominant Eu 2+ emission in the green spectral region, thereby facilitating spectral narrowing.The optimized phosphor achieves a high absorption efficiency of 64.6% and an external quantum yield of 22.2%. When integrated into a white LED prototype, it enables a color gamut covering 97.6% of the NTSC (National Television System Committee) standard, outperforming a commercial β-SiAlON:Eu 2+ -based device. This study provides an effective cationic codoping strategy for designing high-performance narrow-band oxide phosphors and highlights a promising candidate for nextgeneration display technologies.

✓ 已验证 产品关联 DOI 高影响因子
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SEPARATION AND PURIFICATION TECHNOLOGY · 2022 · IF 9.136

Synergistic reduction and oxidation system using 4,7-dihydroxycoumarin as a green photocatalyst for efficient nitrobenzene degradation

Jiajie Xu,Changyu Yan,Zhaojiang Wu,Miaoling Xu,Tuo Wei,Tingchao He,Wenhua Zhou,Yi Zhang,Junmin Zhang,Bo Yang

In this study, a synergistic reduction–oxidation process was proposed using natural organic matters (NOMs) as an organic photocatalyst for complete degradation of nitrobenzene (NB) that was difficult to oxidative decomposition directly. It has been verified by electron spin resonance (ESR) that both reductive organic free radical (4H-chromene-2,4,7-triol radical, S 2 ) and oxidative OH radicals could be generated sustainably by using 4,7-dihydroxycoumarin (4,7-DHC) as a green photocatalyst under UV light irradiation, and 95.07% of NB degradation efficiency was achieved after 4-h irradiation with 40 µM 4,7-DHC. The formation of aniline as a reductive product was convenient for the attack of OH radicals, making it easier for the complete degradation of NB. In addition, 4,7-DHC showed high photocatalytic activity in a wide range of pH from 1 to 13, and the best photocatalytic activity was achieved with a pH value of 4.56. Besides, the effect of common coexisted ions (SO 4 2− , Cl − and NO 3 − ) on the NB degradation was discussed, and the highest k value was obtained with SO 4 2− (80 µM), NO 3 − (120 µM) or Cl − (20 µM). Moreover, 4,7-DHC exhibited extensive degradability to the frequently coexisted pollutants in NB-contaminated wastewater including humic acid (HA), aniline (AN) and m-dinitrobenzene (m-DNB), which might be extended into a potential approach for environmental remediation of NB-contaminated water due to its low cost and accessibility of 4,7-DHC as NOMs.

研究领域: 环境科学 · 化学工程 · 光催化
✓ 已验证 DOI 高影响因子
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ACS Applied Bio Materials · 2018 · IF 0

Fluorescent Conjugated Polymer/Quarternary Ammonium Salt Co-assembly Nanoparticles: Applications in Highly Effective Antibacteria and Bioimaging

Lianqi Wang,Qi Zhao,Ziqi Zhang,Zhuanning Lu,Yantao Zhao,Yanli Tang

Bacterial resistance is one of the very severe factors that threaten human health. It is of great significance to construct a simple, highly effective, biocompatible, and cost-efficient therapeutic route. In this paper, a new method was constructed to prepare cationic nanoparticles, and fluorescent conjugated polymer coassembly nanoparticles CA-CPNs were designed and synthesized on the basis of the model conjugated polymers, PFVBT, and the model quarternary ammonium salts, cationic surfactant cetyltrimethylammonium bromide CTAB. PFVBTs were designed and synthesized in only three steps. CTAB is commercially available. By the reprecipitation method, the PFVBTs form the core and CTAB forms a shell on the surface of CA-CPNs by hydrophobic interaction. Importantly, when incubated with bacteria, the positively charged CA-CPNs can combine with bacteria, physically destroy the bacterial membrane, and kill bacteria without the requirement of light or chemical energy. When 0.80 μg/mL CA-CPNs were incubated for 30 min with Escherichia coli, more than 91% bacteria were killed. Also, more than 96% Staphylococcus aureus were dead when incubated with 1.0 μg/mL CA-CPNs. In virtue of the bright red fluorescence, CA-CPNs were also successfully applied to image MCF-7 cell with good biocompatibility. Overall, a simple, cost-effective, and universal method was provided to prepare cationic fluorescent nanoparticles that are a promising nanomaterial for biomedical applications.

研究领域: 材料科学 · 纳米技术 · 生物医学工程 · 微生物学
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