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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2025 · IF 5.2

Oxytocin lipidation expanding therapeutics for long-term reversal of autistic behaviors in rats

Honglin Li,Ya Chen,Yue Qiu

Autism spectrum disorder (ASD) is a neurodevelopmental condition characterized by deficits in social interaction and repetitive, stereotyped behaviors. There is no universally effective pharmacological treatment targeting its core symptoms.   Oxytocin, an endogenous polypeptide known as the “social hormone”, has shown potential in improving emotional recognition and social interactions in individuals with ASD. However, its clinical application has been limited due to its short half-life and poor blood–brain barrier penetration. To address these challenges, we utilized peptide lipidation technology to enhance the pharmacokinetic properties and brain bioavailability of oxytocin. A series of lipidated oxytocin analogs was designed and synthesized, exhibiting superior brain distribution and pharmacokinetic profiles in valproic acid-induced autistic rat models compared to unmodified oxytocin. Among these   analogs, C16-modified oxytocin (C16-OT), administered intrathecally, achieved the most extensive brain distribution with limited presence in the blood, resulting in long-lasting improvements in autistic behaviors. These improvements, including enhanced social behaviors and reduced stereotypical actions, were sustained for up to 42 days, contrasting with the brief effects typically reported in previous studies. Furthermore, a comparison of administration routes revealed that intrathecal injection achieved higher brain concentrations and more prolonged social behavioral improvements than intranasal delivery. These findings provide robust preclinical evidence that C16-OT, through optimized lipidation and intrathecal delivery, offers sustained central nervous system activity and significant, long-term reversal of social behavioral deficits in rats with autism.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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NEW JOURNAL OF CHEMISTRY · 2018 ·Vol. 42 ·期 4 ·3097-3101 · IF 3.201

One-step microwave synthesis of carbon dots for highly sensitive and selective detection of copper ions in aqueous solution

Qiaoling Liu,Nan Zhang,Haoying Shi,Wenyan Ji,Xiaoqian Guo,Wen Yuan,Qin Hu

Highly fluorescent carbon dots (CDs) are prepared by a one-step microwave heating method using citric acid, L-cysteine and dextrin as the precursors. The average size of the CDs is 2.61 nm with good water dispersibility and photostability. Compared with undoped CDs, small amounts of nitrogen (N) and sulfur atom (S) co-doped CDs exhibit a red shift of the absorption spectra to the visible region and lead to a high quantum yield of 22%. Due to the large amount of carboxyl and hydroxyl groups (−COOH and −OH) on the surface of the CDs, Cu2+ is selectively detected in aqueous solution at pH 7.0 with a detection limit as low as 20 nM, which is much lower than the maximum concentration of Cu2+ in drinking water (∼20 μM) permitted by the US Environmental Protection Agency (EPA). Moreover, the application in tap water samples further demonstrates that the as-synthesized CDs are good candidates for the monitoring of Cu2+ in environmental water samples.

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ELECTROCHIMICA ACTA · 2018 · IF 5.116

Facile fabrication of a non-enzymatic nanocomposite of heteropolyacids and CeO2@Pt alloy nanoparticles doped reduced graphene oxide and its application towards the simultaneous determination of xanthine and uric acid

Di Zhu,Huiyuan Ma,Haijun Pang,Lichao Tan,Jia Jiao,Tao Chen

A non-enzymatic nanocomposite of 12-heteropolyacids and CeO 2 @Pt alloy nanoparticles decorated by reduced graphene oxide (RGO), was successfully developed by a facile and eco-friendly route for simultaneous determination of xanthine (XA) and uric acid (UA). The surface morphology and structure of the nanocomposite were investigated by scanning electron microscopy (SEM), energy dispersive X-ray spectroscopy (EDS), X-ray photoelectron spectroscopy (XPS) and fourier transform infrared spectroscopy (FT-IR), respectively. And then, the electrochemical properties of the nanocomposite were further examined by differential pulse voltammetry (DPV), cyclic voltammetry (CV) and electrochemical impedance spectroscopy (EIS). The as-prepared nanocomposite exhibited excellent sensing performance towards the determination of UA and XA simultaneously with a widely linear range from 4.43 × 10 −7  M to 4.52 × 10 −4  M and 1.25 × 10 −7  M to 5.73 × 10 −4  M, respectively, along with a relatively low detection limit of 5.13 × 10 −8  M and 1.34 × 10 −8  M, mainly because of the synergistic effect of the active components. Meanwhile, the nanocomposite also revealed a superb anti-interference property, as well as good stability and reproducibility. What's more, the nanocomposite was applied in detecting XA and UA in real samples with satisfactory results, demonstrating that the nanocomposite of PMo 6 W 6 /RGO-CeO 2 @Pt would be a good potential candidate sensor for practical detecting xanthine and uric acid.

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ANALYTICA CHIMICA ACTA · 2017 · IF 4.95

Colorimetric logic gate for alkaline phosphatase based on copper (II)-based metal-organic frameworks with peroxidase-like activity

Caihong Wang,Jie Gao,Yili Cao,Hongliang Tan

Nanozymes have been extensively exploited in the construction of colorimetric sensors in the past decade. However, as lack of specific recognition element, these sensors are mostly limited in the detection of hydrogen peroxide and its related agents. In this work, a colorimetric assay for the detection of alkaline phosphatase (ALP) activity was developed by employing copper (II)-based metal-organic frameworks (Cu-MOFs) as peroxidase mimic and pyrophosphate (PPi) as recognition element. Benefiting from its intrinsic porosity, Cu-MOFs built from one-step self-assembly showed a superior catalytic activity over horseradish peroxidase. It was found that, in the presence of PPi, the catalytic activity of Cu-MOFs was greatly inhibited due to the ultrastrong binding ability of Cu 2+ with PPi, and no colorimetric signal was recorded. However, after incubation with ALP, such negative behavior of PPi can be suppressed as the hydrolysis of PPi into orthophosphates (Pi) with low affinity to Cu 2+ , producing a colorimetric signal depending on ALP level. On this basis, a way for quantitative analysis of ALP activity was paved accordingly. Compared with previously reported ALP assays based on nanomaterials , this assay is simple, cost-effective and visualized, which not only allows highly sensitive analysis of ALP activity with a detection limit of 0.19 U/L, but also exhibits a good sensing performance in serum samples. Furthermore, based on the distinct colorimetric signals induced by PPi and ALP, an IMPLICATION logic gate was constructed. We hope that this study could provide a new insight for designing nanozyme-based highly specific colorimetric sensors.

CAS / MDL: 7365-45-9 7722-88-5
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SENSORS AND ACTUATORS B-CHEMICAL · 2018 · IF 5.667

Visual detection of Pb2+ using strip biosensor based on PS2M aptamer and sensitivity enhancement probe

Hai-Bo Wang,Li-Hong Ma,Bi-Yun Fang,Fang Tan,Yuan-Cheng Cao,Yuan-Di Zhao,Xue-Bin Hu

PS2M aptamer was selected as sensing element to construct Pb 2+ strip biosensor, and for the first time, AuNP-DNA polymer was used as sensitivity enhancement probe (SEP) to improve sensitivity. Pb 2+ separated the double-strand formed by PS2M and its complementary sequence at Anti-PS2M and induced PS2M to form G-quadruplex structure, then single-strand Anti-PS2M was released. When migrated along the strip, sequence at one end of Anti-PS2M hybridized with AuNP-DNA probe G immobilized on conjugate pad, when the composite migrated to test zone (TZ), other end of Anti-PS2M hybridized with biotin-DNA probe T on TZ to form sandwich structure. Subsequent SEP hybridized with the remaining oligonucleotides of AuNP-DNA probe G on TZ thus enhanced the signal. After optimization, the false positive result could be eliminated and the best signal value could be obtained. The results showed that the limit of detection of Pb 2+ strip biosensor was 2.5 nM by adding the sensitivity enhancement probe, which was 40 times better than that strip without enhancement. The test strip showed good results in the direct detection of soil and lake samples, presenting good practical value. In addition, the cost of this strip biosensor was low, with good market prospect.

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SENSORS AND ACTUATORS B-CHEMICAL · 2018 · IF 5.667

The construction of a FRET assembly by using gold nanoclusters and carbon dots and their application as a ratiometric probe for cysteine detection

Xu Yu,Chun-Xia Zhang,Lening Zhang,Ya-Rong Xue,Hong-Wei Li,Yuqing Wu

Förster resonance energy transfer (FRET) is a powerful tool to study single molecular conformation and/or distance changes between two fluorophores, which is mainly depended on the combinations and spatial distance between the donor and acceptor. The present study has built a FRET assembly by using gold nanoclusters capped by glutathione (AuNCs@GSH) and carbon dots (CDs) prepared by polyethyleneimine (PEI) through supramolecular interactions. The assembly is characterized in detail by employing Zeta potential, UV–vis absorption and fluorescence spectra, the luminescent decay curves and TEM images, which indicate the AuNCs are adhered to the surface of CDs. In addition, the transfer efficiency between them has been calculated to be 65.7%, which is sufficient enough for practical applications, and particularly, the quantum yield (QY) of AuNCs@GSH is increased from 3.07% to 5.35% via the assembly. Moreover, the FRET assembly is used as a ratiometric probe for cysteine detection in showing a limit of detection (LOD) at 100 nM, a very high selectivity to cysteine among amino acids as well as a strong anti-interference on them, especially, it was feasible for cysteine detection in fetal calf serum, which showed very high potential in the diagnose of cysteine-related disease.

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International Journal of Nanomedicine · 2024 · IF 6.6

Dual-Sensitive Carbohydrate-Based Nanosystem for Targeted Drug Delivery to Potentiate the Therapeutic Efficacy of Ulcerative Colitis

Yuan Wang,Xiaoyu Song,Ru Cui,Xinlin Luo,Juntian Dong,Hanqi Wang,Chengcheng Song,Yifa Zhou,Sisi Cui

Purpose Conventional oral formulations for inflammatory bowel disease (IBD) treatment are less than satisfactory, due to the poor controllability of drug release and lack of specificity to the inflammation sites in the gastrointestinal (GI) tract. To overcome these limitations, we developed a multiple carbohydrate-based nanosystem with pH/ROS dual responsibility and charge-mediated targeting ability for IBD-specific drug delivery.Methods In view of the overproduction of ROS and overexpression of cationic proteins in the inflammatory colon, the designed nanosystem was composed of oxidation-sensitive cyclodextrin (OX-CD), chitosan (CS) and pectin (AHP). OX-CD was utilized to load dexamethasone (DM) by the solvent evaporation method. CS and AHP with opposite charges were sequentially coated onto OX-CD to generate the nanosystems by the electrostatic self-assembly method. The physicochemical properties, stability, dual-sensitive drug release behavior, cytotoxicity, cellular uptake and anti-inflammatory activity were investigated in vitro. In vivo bio-distribution and therapeutic efficacy of the nanosystem were further evaluated in the ulcerative colitis (UC) mice.Results The obtained AHP/CS/OX-CD-DM nanosystem (ACOC-DM) could maintain stability under the GI pH environments, and release drug in the inflammatory colon with pH/ROS sensitivity. Dual polysaccharide-coated ACOC-DM exhibited higher cellular uptake and anti-inflammatory efficacy in macrophages than single polysaccharide-coated CS/OX-CD-DM nanosystem (COC-DM). Orally administrated ACOC-DM could enhance inflammation targeting ability and therapeutic efficacy of DM in the UC mice.Conclusion This carbohydrate-based nanosystem with pH/ROS dual sensitivity and inflammation targeting capacity may serve as a safe and versatile nanoplatform for IBD therapy.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF CONTROLLED RELEASE · 2025 · IF 11.5

Dual-target nanotherapy for vascular endothelium and bone mesenchymal stem cells halt steroid-induced osteonecrosis of the femoral head progression

Wenbo Yang,Qing Pan,Yizhong Peng,Yuxiang Hu,Yongzhi Cui,Zengwu Shao,Chunqing Meng,Hong Wang,Wei Huang

Steroid-induced osteonecrosis of the femoral head (SANFH) is a common hip joint disease that imposes a heavy economic burden on society. Patients continue to experience bone necrosis even after discontinuing glucocorticoid therapy, and the specific mechanisms require further investigation. The results of this study demonstrate that exosomes secreted by damaged vascular endothelial cells in SANFH lesions may be a crucial factor leading to abnormal adipogenic differentiation of bone marrow stromal cells (BMSCs). We also found that adipogenically differentiated BMSCs can secrete increased pro-inflammatory factors, which contribute to the maintenance of endothelial cell damage, thereby creating a vicious cycle. Due to endothelial damage and abnormal differentiation of BMSCs, insufficient bone repair occurs, leading to spontaneous disease progression. Based on our newly explored mechanism, we designed a nanomaterial, M-SiO 2 @Icariin@EBHM, that simultaneously targets the repair of damaged vascular endothelium and re-regulation of BMSCs, and we assessed its role in delaying SANFH progression. We found that the M-SiO 2 @Icariin@EBHM nanomaterial can target SANFH lesions when applied systemically, effectively clearing the elevated reactive oxygen species in vascular endothelial cells caused by glucocorticoids and regulating the osteogenic differentiation of BMSCs. This process breaks the vicious cycle while promoting bone repair and significantly inhibiting SANFH progression, revealing its potential as a promising treatment strategy for SANFH.

CAS / MDL: 23491-52-3
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Advanced Biology · 2024 · IF 3.2

Development of a pH-Responsive Antimicrobial and Potent Antioxidant Hydrogel for Accelerated Wound Healing: A Game Changer in Drug Delivery

Qixiang Gui,Neng Ding,Haimei Wu,Jinyue Liu,Yingnan Geng,Jie Zhu,Mingyue Gao,Antong Du,Bingbing Yue,Lie Zhu

Stimuli-responsive hydrogels have the capability to alter their state in response to changes in physiological signals within their application environment, providing distinct benefits in drug delivery applications. Here, the acidic pH typically found in acutely infected wounds can be effectively managed by incorporating a pH-responsive Ag + loaded system within the hydrogel, thereby ensuring efficient drug use and preventing potential toxicity from the sudden release of silver ions. The antimicrobial composite hydrogel HAMA/GelMA-CA/Ag + provides some tissue adhesion and accelerates wound healing. GelMA-CA is synthesized by modifying gelatin methacryloyl (GelMA) with caffeic acid (CA), while hyaluronic acid methacryloyl (HAMA) is introduced to prepare a double network hydrogel. Silver nitrate is then introduced to make it pH-responsive through the formation of coordination between the polyphenolic structure of caffeic acid and the silver ions. The composite hydrogel exhibited excellent antioxidant properties and strong antimicrobial activity against both Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli). Furthermore, the composite hydrogel accelerated the promotion of wound healing in a rat model of S. aureus-infected wounds. In conclusion, the HAMA/GelMA-CA/Ag + hydrogel is a promising bioactive material that can be used as a wound dressing to promote the healing of acutely infected wounds.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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CARBOHYDRATE POLYMERS · 2024 · IF 10.7

Different polysaccharide-enhanced probiotic and polyphenol dual-functional factor co-encapsulated microcapsules demonstrate acute colitis alleviation efficacy and food fortification

Rui Sun,Zhongyi Lv,Ying Wang,Menghui Li,Jianrui Qi,Kai Wang,Haihua Yang,Tianli Yue,Yahong Yuan

Probiotics and polyphenols have multiple bioactivities, and developing co-encapsulated microcapsules (CM) is a novel strategy to enhance their nutritional diversity. However, the development of CMs is challenged by complicated processing, single types, and unclear in vivo effects and applications. In this study, the co -microencapsulations of polyphenol and probiotic were constructed using pectin, alginate (WGCA@LK), and Fu brick tea polysaccharides (WGCF@LK), respectively, with chitosan-whey isolate proteins by layer-by-layer coacervation reaction, and their protective effects, in vivo effectiveness, and application potential were evaluated. WGCA@LK improved the encapsulation rate of polyphenols (42.41 %), and remained high viability of probiotics after passing through gastric acidic environment (8.79 ± 0.04 log CFU/g) and storage for 4 weeks (4.59 ± 0.06 log CFU/g). WGCF@LK exhibited the highest total antioxidant activity (19.40 ± 0.25 μmol/mL) and its prebiotic activity removed the restriction on probiotic growth. WGCA@LK showed strong in vitro colonic adhesion, but WGCF@LK promoted in vivo retention of probiotics at 48 h. WGCF@LK showed excellent anti-inflammatory effects and alleviated symptoms of acute colitis in mice. These findings provide unique insights into the fortification of probiotic-polyphenol CMs by different polysaccharides and the development of novel health foods with rich functional hierarchies and superior therapeutic effects.

CAS / MDL: 23491-52-3 9012-76-4
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Scientific Reports · 2024 ·Vol. 14 ·期 1 ·1-9 · IF 3.8

Efficient and rapid digestion of proteins with a dual-enzyme microreactor featuring 3-D pores formed by dopamine/polyethyleneimine/acrylamide-coated KIT-6 molecular sieve

Yuan Fang-Fang,Wang Pei,Han Xiao-Jie,Qin Ting-Ting,Lu Xin,Bai Hai-Jiao

The microreactor with two types of immobilized enzymes, exhibiting excellent orthogonal performance, represents an effective approach to counteract the reduced digestion efficiency resulting from the absence of a single enzyme cleavage site, thereby impacting protein identification. In this study, we developed a hydrophilic dual-enzyme microreactor characterized by rapid mass transfer and superior enzymatic activity. Initially, we selected KIT-6 molecular sieve as the carrier for the dual-IMER due to its three-dimensional network pore structure. Modification involved co-deposition of polyethyleneimine (PEI) and acrylamide (AM) as amine donors, along with dopamine to enhance material hydrophilicity. Remaining amino and double bond functional groups facilitated stepwise immobilization of trypsin and Glu-C. Digestion times for bovine serum albumin (BSA) and bovine hemoglobin (BHb) on the dual-IMER were significantly reduced compared to solution-based digestion (1 min vs. 36 h), resulting in improved sequence coverage (91.30% vs. 82.7% for BSA; 90.24% vs. 89.20% for BHb). Additionally, the dual-IMER demonstrated excellent durability, retaining 96.08% relative activity after 29 reuse cycles. Enhanced protein digestion efficiency can be attributed to several factors: (1) KIT-6’s large specific surface area, enabling higher enzyme loading capacity; (2) Its three-dimensional network pore structure, facilitating faster mass transfer and substance diffusion; (3) Orthogonality of trypsin and Glu-C enzyme cleavage sites; (4) The spatial effect introduced by the chain structure of PEI and glutaraldehyde’s spacing arm, reducing spatial hindrance and enhancing enzyme–substrate interactions; (5) Mild and stable enzyme immobilization. The KIT-6-based dual-IMER offers a promising technical tool for protein digestion, while the PDA/PEI/AM-KIT-6 platform holds potential for immobilizing other proteins or active substances.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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Processes · 2025 ·Vol. 13 ·期 2 ·530 · IF 2.8

Characterization of Key Odorants in Hemp Seed Oil Extracted from the Hemp Seeds Roasted Under Various Conditions

Yuchen Bai,Ningke You,Hongyu Tian,Xuebing Zhao

Hemp seed oil is nutritious. Besides cannabinoids, it has a higher Omega-3 fatty acid content, making it an ideal and healthy edible oil. Roasting is a key factor affecting the flavor of hemp seed oil. In this study, solvent-assisted flavor evaporation (SAFE) combined with gas chromatography–mass spectrometry (GC-O-MS) was used to analyze the volatile compounds of hemp seed oil after the hemp seeds were roasted at different temperatures (120 °C, 140 °C, 160 °C, 180 °C). α-pinene, (1S)-(1)-β-pinene, myrcene, and (E)-β-ocimene, which are typical odorants for herbs and fresh flavors, had an active odor value (OAV) ≥ 1. The sweet, nutty, and toasty flavors became more pronounced as the temperature increased. 2-pentylfuran provided the caramel flavor, and 2,5-dimethylpyrazine, 2-ethyl-6-methylpyrazine, and 2-ethyl-5-methylpyrazine provided the toasty flavor. The combination of sensory evaluation and data analysis was effective in differentiating the odors of hemp seed oil extracted at different temperatures. Reconstitution and deletion experiments showed that these odorants could mimic the overall aroma profile. This article provides a theoretical basis for the effect of over-roasting on the flavor of hemp seed oil.

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