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Frontiers in Pharmacology · 2024 · IF 4.4

Protective effect of baicalin on oxidative stress injury in retinal ganglion cells through the JAK/STAT signaling pathway in vitro and in vivo

Huan Yu,Dan Zhou,Wei Wang,Qingxia Wang,Min Li,Xiaoyun Ma

Background and Purpose: The damage or apoptosis of retinal ganglion cells (RGCs) is one of the leading causes of various blinding eye diseases, such as glaucoma, diabetic retinopathy, optic neuritis, and ischemic optic neuropathy. Oxidative stress is involved in RGCs death. Baicalin, a flavonoid compound extracted from Scutellaria baicalensis, has various beneficial effects, including anti-inflammatory, anti-apoptotic, and antioxidant properties. However, the effects of baicalin on RGCs and the underlying mechanisms require further investigation.Methods: In this study, a glutamate-induced oxidative stress damage model of R28 cells and a rat retinal injury model were established to investigate the effects of baicalin on oxidative stress damage to RGCs and try to elucidate the underlying mechanism.Results: In vitro experiments demonstrated that the survival rate of R28 cells after glutamate treatment dropped to 33.4%, while 10 μM baicalin significantly inhibited glutamate-induced damage in RGCs (P < 0.001) and enhanced cell viability through decreasing ROS levels, increasing antioxidant enzyme activity, and suppressing the expression of inflammatory factors iNOS, TNF-α, IL-6, and IL-1β (P < 0.001). In vivo, baicalin effectively mitigated structural damage to retinal tissue and RGCs morphology induced by glutamate, increasing the thickness of the retinal ganglion cell layer, improving RGCs density, and reducing overall retinal thinning in rats (P < 0.001) in a time- and dose-dependent effects. Mechanistic studies revealed that glutamate evaluated the phosphorylation levels of JAK/STAT, while baicalin effectively inhibited the activation of the JAK/STAT signaling pathway.Conclusion: This study confirmed that baicalin protects against glutamate-induced oxidative stress damage in RGCs. It effectively alleviates oxidative stress and inflammatory responses, reduces cell apoptosis, and improves the pathological changes in the retina of rat models of RGCs damage, thereby decreasing RGCs death. Further exploration of its mechanism revealed that baicalin effectively inhibits the JAK/STAT signaling pathway, protecting RGCs from oxidative stress damage. This provides an experimental basis for the application of baicalin in the treatment of RGCs damage.

CAS / MDL: 6461-04-7
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ANALYTICAL LETTERS · 2024 · IF 1.6

Rapid Determination of Flavorings in e-Cigarette Liquid by Direct Analysis in Real Time (DART) Mass Spectrometry (MS) in the Quick Strip Mode

Xuerui Lou,Minglei Li,Weiwei Guo,Yingjie Fu,Hui Xi,Peng Li,Wuduo Zhao,Shihao Sun

Electronic cigarettes (E-cigarettes) have become popular around the world. An important reason is the variety of available flavors. However, many countries have imposed restrictions on flavor substances in E-cigarettes due to their potential health risks. Therefore, it is necessary to develop an effective way to identify flavorings in E-cigarette liquids. In this work, direct analysis in real time-mass spectrometry (DART-MS) in the quick strip (QS) mode was developed and applied to determine flavorings in the E-cigarettes. Vanillin, ethyl vanillin, maltol, and ethyl maltol were quantified. Meanwhile, the ionization efficiency of flavorings in the different solvents was compared in the QS mode, which revealed that the solvent boiling point was related to the analyte ionization efficiency. The effect of endogenous matrix (propylene glycol and glycerol) on flavoring ionization was also investigated. Calibration curves with satisfactory linearity (R2 > 0.99) were established from 1 to 1000 μg L−1. Good sensitivity (limits of detection [LODs] < 0.3 μg L−1), recoveries (92.6% to 104.7%), and acceptable repeatability (relative standard deviations < 14.6%, n = 5) were obtained. The limits of quantification (LOQs; 10–50 μg g−1) for the E-cigarette liquid sample were much lower than the regulatory limits. The developed method provided a simple way for rapidly determining flavorings in E-cigarettes.

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International Journal of Nanomedicine · 2024 · IF 6.6

Zeolitic Imidazolate Framework-8 Offers an Anti-Inflammatory and Antifungal Method in the Treatment of Aspergillus Fungal Keratitis in vitro and in vivo

Xueyun Fu,Xue Tian,Jing Lin,Qian Wang,Lingwen Gu,Ziyi Wang,Menghui Chi,Bing Yu,Zhuhui Feng,Wenyao Liu,Lina Zhang,Cui Li,Guiqiu Zhao

Background: Fungal keratitis is a serious blinding eye disease. Traditional drugs used to treat fungal keratitis commonly have the disadvantages of low bioavailability, poor dispersion, and limited permeability.Purpose: To develop a new method for the treatment of fungal keratitis with improved bioavailability, dispersion, and permeability.Methods: Zeolitic Imidazolate Framework-8 (ZIF-8) was formed by zinc ions and 2-methylimidazole linked by coordination bonds and characterized by Scanning electron microscopy (SEM), X-ray diffraction (XRD), and Zeta potential. The safety of ZIF-8 on HCECs and RAW 264.7 cells was detected by Cell Counting Kit-8 (CCK-8). Safety evaluation of ZIF-8 on mice corneal epithelium was conducted using the Draize corneal toxicity test. The effects of ZIF-8 on fungal growth, biofilm formation, and hyphae structure were detected by Minimal inhibit concentration (MIC), crystal violet staining, Propidium Iodide (PI) testing, and calcofluor white staining. The anti-inflammatory effects of ZIF-8 on RAW 246.7 cells were evaluated by Quantitative Real-Time PCR Experiments (qPCR) and Enzyme-linked immunosorbent assay (ELISA). Clinical score, Colony-Forming Units (CFU), Hematoxylin-eosin (HE) staining, and immunofluorescence were conducted to verify the therapeutic effect of ZIF-8 on C57BL/6 female mice with fungal keratitis.Results: In vitro, ZIF-8 showed outstanding antifungal effects, including inhibiting the growth of Aspergillus fumigatus over 90% at 64 μg/mL, restraining the formation of biofilm, and destroying cell membranes. In vivo, treatment with ZIF-8 reduced corneal fungal load and mitigated neutrophil infiltration in fungal keratitis, which effectively reduced the severity of keratitis in mice and alleviated the infiltration of inflammatory factors in the mouse cornea. In addition, ZIF-8 reduces the inflammatory response by downregulating the expression of pro-inflammatory cytokines TNF-α, IL-6, and IL-1β after Aspergillus fumigatus infection in vivo and in vitro.Conclusion: ZIF-8 has a significant anti-inflammatory and antifungal effect, which provides a new solution for the treatment of fungal keratitis.

CAS / MDL: 10196-18-6
✓ 已验证 产品关联 DOI PubMed 高影响因子
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EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS · 2025 · IF 4.3

Thymol@pro-phytomicelles as an antibiotic alternative in livestock and poultry farming: preparation, characterization, and in vitro and in vivo antimicrobial activity evaluation

Linrong Yu,Yunchun Pan,Qingqian Meng,Xianggen Wu,Mengshuang Li

Antibiotic abuse in livestock and poultry farming poses significant threats to human health, including the emergence of drug-resistant bacteria. Thus, antibiotic alternatives are highly required in this field. Thymol (THY) demonstrates significant potential as an antibiotic alternative, but its commercial application is limited due to its high volatility and low water solubility. In this study, a novel nanoformulation of pro-phytomicelles, with glycyrrhizin and rebaudioside A as mixed-nanocarriers that load THY (called “THY@pro-phytomicelles”), was designed and tested as a potent antibiotic alternative. The optimized THY@pro-phytomicelles had an encapsulation efficiency of 99.75 ± 0.37 % and a particle size of 3.83 ± 0.44 nm after they were dispersed in water. Following THY’s formulation into THY@pro-phytomicelles, its water solubility, volatility stability, and antioxidant activity significantly improved. In vitro, the THY@pro-phytomicelles showed better antimicrobial activity than THY. Their antibacterial mechanism appeared to involve destruction of the integrity of the bacterial cell wall and biomembrane, leading to alkaline phosphatase (AKP) leakage and inhibition of biofilm formation. In the animal evaluation in this study, they showed excellent in vivo antibacterial capacities against Salmonella enteritidis -induced enteritis, including improvement of the liver bacterial abscess, alleviation of the oxidative stress and inflammatory cytokine levels, reduction of the bacterial load of the liver, and alleviation of the inflammation and damage caused by bacteria in the cecum. Overall, the THY@pro-phytomicelles showed excellent in vitro and in vivo antibacterial activity, making them a potentially effective antibiotic alternative in livestock and poultry farming, with broad potential application in the breeding industry.

CAS / MDL: 89-83-8
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF MOLECULAR STRUCTURE · 2025 · IF 4.7

Effects of conformation of excipients succinic acid and maleic acid in molecular salts on in vitro/in vivo properties of marine drug cytarabine

Yue-Ming Yu,Xue-Jie Li,Zhi-Long Zhao,Qiu-Tong Chen,Fan-Zhi Bu,Zhi-Yong Wu,Yan-Tuan Li

A salification-actuated cocrystalline strategy has been proposed to allow full play to structural and property advantages of pharmaceutical excipients succinic acid (H 2 SA) and maleic acid (H 2 MA) in perfecting in vitro/vivo properties of marine antitumor drug cytarabine (ARC). Utilizing the acidity of H 2 SA/H 2 MA, and the alkalinity of ARC can generate strong charge-assisted complementary hydrogen-bond by proton transfer reaction, for one thing, it is conducive to protecting the amino active site of ARC and reducing its inactivation, eventually heightening the bioavailability. For another, the properties of ARC are raised by playing the superiorities of these excipients, thus increasing its therapeutic effect. Along this line, two new pharmaceutical molecular salts are achieved structurally characterized. The structure data display that both compounds are cytarabine monocarboxylate salt, namely HARC + -HAS – ( 1 ) and HARC + -HMA – ( 2 ), featuring with the charge-assisted hydrogen bonds. Thereinto, 1 has an open three-dimensional hydrogen-bonding skeleton, while 2 is closed into independent one-dimensional belts, which can ascribe to the configurations of these excipients. The structural features can regulate the poor permeability of ARC supported by theoretical and experimental data. While the meliorative properties have further promoted stronger antitumor activity and optimal pharmacokinetic behavior, with 2 showcasing greater superiority than that of 1 . These results offer new crystalline forms for ARC, also open an innovative avenue to the application of aliphatic diacid pharmaceutical excipients in the realm of marine antitumor drugs.

✓ 已验证 DOI 高影响因子
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ACS Applied Nano Materials · 2022 · IF 6.14

In Situ Dynamic Study of Color-Changing in Liquid Colloidal Crystals for Electrophoretic Displays

Yiquan Fang,Huateng Li,Xiuli Wang,Mengjing Zhu,Jia Guo,Changchun Wang

Reflective display devices, especially for electrochromic photonic crystals (ECPCs), are of great interest to researchers due to their convenient control approach, wide color regulation range, fast response, and low power consumption. Herein, liquid colloidal crystals (LCCs) of SiO2 nanospheres were prepared through an evaporation-induced self-assembly method and used as a reflective unit for fabricating dynamic ECPC devices. The ECPC device exhibited brilliant controllable structural color across the visible spectrum under low voltages (<3.5 V). Based on the in situ ultra-small-angle X-ray scattering results and reflective spectra, regulatory rules of the dynamic ECPC device concerning a color tunable range, reflectance intensity, response speed, and cyclic performance were set up, and the relationship between slurry concentration, electrode spacing, and viewing angle was established. Furthermore, a dynamic mechanism was revealed for explaining the responsive behaviors of reflection spectra during the electrical modulation, which is significant for the development of ECPC devices in the future. Based on the parameter optimization and structure design of the dynamic ECPC device, a pressure-responsive electrochromic prototype device was constructed with rapid response, dynamic structural color, and good reversibility, which demonstrated its great potential in reflective display units and multifunctional sensors.

研究领域: 材料科学 · 显示技术 · 纳米科技
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JOURNAL OF LUMINESCENCE · 2019 · IF 2.961

Strong red emission in Bi3+ and Mn4+ codoped Mg3.5Ge1.25O6 phosphors applied in optical agriculture

Qiying Huang,Weihao Ye,Guangqi Hu,Xiaotang Liu

Bi 3+ and Mn 4+ co-activated Mg 3.5 Ge 1.25 O 6 phosphors were synthesized via a solid-state method in air. Codoping Bi 3+ into the matrix leads to effective enhancement of the deep-red emssion (659 nm) compared to Bi 3+ -free samples. The spectroscopic properties are discussed based on the Bi 3+ (6s 2 )→Ge 4+ (3d 10 ) metal-to-metal charge transfer and energy transfer between Bi 3+ and Mn 4+ . All samples emit deep-red emission ascribed to 2 E g → 4 A 2g transition of Mn 4+ . We have carried out the X-ray power diffraction (XRD), photoluminescence spectrum (PL), field emission scanning electron microscope (FESEM), fourier transform infrared spectroscopy (FT-IR) and UV–Vis absorption measurement to investigate the influences induced by Bi 3+ incorporation.

研究领域: 材料科学 · 光学农业
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Asian Biomedicine · 2020 ·Vol. 14 ·期 1 ·19-26 · IF 0.324

Variation in contents of active components and antibacterial activity in different parts of Thunb

Luyun Yan,Yulei Xie,Youyou Wang,Jinhua Zhu,Mingjing Li,Xiuhua Liu,Dongbao Zhao

BackgroundLonicera japonica Thunb has been comprehensively used as a traditional Chinese medicine which contains a variety of medicinally active substances.ObjectivesThe active constituents in various parts of L. japonica Thunb (leaves [LE], flowers fl, and green buds [GB]) were studied to rational and efficient use of this medicinal plant.MethodsUV–vis spectrophotometry was used for the determination of the total flavonoids; gas chromatography–mass spectrometric method was employed for the analysis of volatile components; and high-performance liquid chromatography technology was applied to detect nine bioactive components including chlorogenic acid, neochlorogenic acid, isochlorogenic acid C, caffeic acid, luteolin, galuteolin, hyperoside, rutin, and quercetin in different parts of L. japonica Thunb. The antimicrobial effects of LE, FL, and GB were further measured using agar plate drilling method.ResultsThe content of the total flavonoids in different portions of L. japonica Thunb has significant difference, and the content with the decreasing sequence is found in GB, LE, and FL. The contents of main volatile components were highest in FL, followed by GB and LE. Besides, the contents of galuteolin, luteolin, rutin, and isochlorogenic acid C were higher in LE than those in FL and GB, and neochlorogenic acid content was similar in LE and FL. The antimicrobial effects showed

研究领域: 中药学 · 植物化学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Durable adhesion in flexible sensors via synergistic interactions in tannic acid/thiosemicarbazide-chitosan networks

Yu Liu,Jie Chen,Chunyan Hu,Baojiang Liu

Adhesive conductive hydrogels have a broad application prospect in the field of flexible sensors, but existing adhesive hydrogels often struggle to balance adhesion performance and mechanical strength, and their adhesion stability is poor, which limits their long-term applications. In this study, a dual-network-structured hydrogel with durability, conductivity, and adhesion was prepared using a photoinitiated polymerization process, and its potential application in flexible sensors was explored. The hydrogel is based on thiosemicarbazone-modified chitosan (CS-SCM) as the backbone, introducing a reducible group into the system, acrylic acid (AA), tannic acid (TA), and Fe3+ are incorporated, endowing the hydrogel with excellent electrical conductivity and adhesion durability through multiple hydrogen bonds, electrostatic interactions, and metal-phenol complexation effects. The experimental results show that the hydrogel is able to maintain stable and long-lasting adhesion on the surface of various substrates, and its adhesion to plank remains above 90 kPa after 5 days of storage and more than 20 kPa after 13 days, which is significantly better than traditional hydrogels. Moreover, the durable adhesion of this hydrogel is highly valuable for research and applications in flexible sensors, smart wearables, and bioelectronic devices.

CAS / MDL: 9012-76-4 79-10-7
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF CONTROLLED RELEASE · 2012 · IF 6.499

Novel SN38 conjugate-forming nanoparticles as anticancer prodrug: In vitro and in vivo studies

Hongfang Zhang,Jinqiang Wang,Weiwei Mao,Jian Huang,Xianguo Wu,Youqing Shen,Meihua Sui

The clinical utility of CPT-11 is restricted by factors such as the low conversion rate to SN38 , high interpatient variability and dose-limiting toxicity. SN38 is significantly more potent than CPT-11, but parental administration of SN38 is impossible due to its poor solubility and low stability. This study aimed to develop a novel SN38 prodrug (OEG-SN38) that may overcome the various drawbacks of CPT-11 and SN38 and be useful for clinics. We attached a very low molecular weight oligo (ethylene glycol) (OEG) chain selected as the hydrophilic part to hydrophobic SN38 via ester bond at the C20 position to form the amphiphilic OEG-SN38. In aqueous solution OEG-SN38 formed micelles with diameter of 28.74   ±   2.51   nm, and showed greatly improved drug loading, solubility and stability, with drug loading as high as 36% (wt.%). Moreover, these micelles were stable in PBS with only 4.71% SN38 released from the prodrug even after 35   h incubation, but released SN38 promptly by esterase hydrolysis. Most importantly, OEG-SN38 exhibited potent antitumor activity against a panel of human tumor cell lines, as well as favorable antitumor activity and high safety in human xenograft models. These encouraging data merit further preclinical and clinical investigation on this novel SN38 delivery system.

研究领域: 药学 · 肿瘤学 · 生物医学工程
✓ 已验证 DOI PubMed 高影响因子
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EUROPEAN JOURNAL OF PHARMACOLOGY · 2020 · IF 3.263

Involvement of FGF-2 modulation in the antidepressant-like effects of liquiritin in mice

Min Chen,Qiu-Ping Zhang,Ji-Xiao Zhu,Jie Cheng,Qing Liu,Guang-Hui Xu,Cheng-Fu Li,Li-Tao Yi

It has been reported that liquiritin produced an antidepressant-like effect in rodents. However, little information is known regarding its antidepressant activity with the regulation of fibroblast growth factor 2 (FGF-2), a protein maintaining development and maturation of the nervous central system . Therefore, the aim of the present study was to investigate the underlying FGF-2 modulation involved in the antidepressant-like effects of liquiritin. In the present study, mice were orally administrated with liquiritin for 7 days prior to LPS injection. The depressive-like behaviors , levels of FGF-2, number of Iba1 positive cells, expression of proinflammatory cytokines and density of dendritic spines were evaluated. The results showed that liquiritin significantly ameliorated the depressive-like behaviors in mice response to LPS injection. Liquiritin reversed the reduction of FGF-2 levels in the hippocampus of LPS induced mice. In addition, the microglial activation caused by LPS was attenuated by liquiritin, in accordance with downregulation in mRNA levels of proinflammatory cytokines. Moreover, liquiritin also increased the density of dendritic spines in the hippocampus, which was suppressed by LPS. In conclusion, our findings demonstrated that liquiritin exerted the antidepressant-like effects in LPS-induced depression through FGF-2 enhancement by inhibiting neuroinflammation and maintaining synaptogenesis .

研究领域: 药理学 · 神经科学 · 免疫学
✓ 已验证 DOI PubMed 高影响因子
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