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Table of Content

    02 June 2025, Volume 34 Issue 5
    Original articles
    Evaluation of different solvents for phytochemical compounds, antioxidant activities, cholinesterase inhibition, and anti-HepG2 cell proliferation of three plant parts in Elaeagnus mollis
    Hao Zhong, Jingmiao Li, Changle Li, Yulin Liu
    2025, 34(5):  411-422.  DOI: 10.5246/jcps.2025.05.031
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    To explore the potential utilization of Elaeagnus mollis, we conducted a comprehensive assessment of its phytochemical composition, antioxidant properties, cholinesterase inhibition, and anti-HepG2 cell proliferation activity across different plant parts (branch wood, branch bark, and pericarp) using various solvents (water, methanol, ethanol, and n-hexane). Our findings revealed that water extracts displayed superior antioxidant activities in ABTS and RP assays, while methanol extracts exhibited better performance in DPPH and FRAP assays. Moreover, methanol extracts demonstrated the highest effectiveness against anti-HepG2 cell proliferation, whereas n-hexane extracts showed greater efficiency in cholinesterase inhibition. Notably, branch bark extracts exhibited the highest levels of phytochemical compounds, with both branch bark and pericarp extracts demonstrating significant effects in cholinesterase inhibition and anti-HepG2 cell proliferation. Correlation analysis indicated that phytochemical compounds were primarily responsible for the observed biological activities. Overall, extracts from the branch bark and pericarp of E. mollis showed promising potential for antioxidant and anticancer activities, suggesting their suitability for applications in the pharmaceutical industry as health-promoting products.

    Comparative analysis of UPLC-MS/MS and chemiluminescence microparticle immunoassay for serum methotrexate measurement in pediatric intracranial tumor patients
    Zhengyuan Shi, Jingfeng Li, Chunjing Yang, Xiqiao Xu, Dechun Jiang
    2025, 34(5):  423-431.  DOI: 10.5246/jcps.2025.05.032
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    This study aimed to establish a highly accurate method for quantifying methotrexate (MTX) concentrations in serum using an ultra-high performance liquid chromatography-tandem mass spectrometry system (UPLC-MS/MS) and to compare its performance with the chemiluminescence microparticle immunoassay (CMIA). A total of 211 serum samples from pediatric patients with intracranial tumors undergoing high-dose MTX treatment were analyzed using both techniques. Correlation and agreement analyses were performed to assess the level of concordance between these methods. The results demonstrated a significant correlation (P < 0.05) between the two methods, with correlation coefficients of 0.9913 and 0.9893, respectively. However, a statistical difference was noted in MTX serum concentrations at lower levels (0.04–1.5 μmol/L), while no significant difference was observed at higher concentrations (1.5–400 μmol/L). Specifically, in the 0.04–1.5 μmol/L range (107 cases), Bland-Altman analysis indicated a bias of 0.018 between the two methods. Given the observed discrepancies, particularly at lower concentrations, it is advised that the UPLC-MS/MS method should not be used interchangeably with the CMIA assay for therapeutic drug monitoring in patients receiving high-dose MTX treatment.

    Quantitative analysis of related substances in polyvinyl alcohol eye drops using HPLC-UV
    Yongfei Li, Wenfen Gao, Jihua Liu, Zheyuan Li, Zhiyuan Li
    2025, 34(5):  432-442.  DOI: 10.5246/jcps.2025.05.033
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    The current quality standard for polyvinyl alcohol eye drops lacks an impurity assessment, despite the potential impact of raw material impurities on product safety. To strengthen quality control and ensure drug safety, an investigation into the impurity profile of the formulation was conducted, and an HPLC-UV method was developed for impurity quantification. The method validation was performed using an H-type cation exchange column. A total of 116 batches of polyvinyl alcohol eye drops from four manufacturers and two batches of the innovator drug were analyzed. Formic acid was detected exclusively in 0.4 mL samples from Company A and the innovator drug, with concentrations below 0.002% in both cases. Acetic acid was identified in samples from all manufacturers, with levels not exceeding 0.1%. The method demonstrated high specificity and sensitivity, making it well-suited for the quantification of formic and acetic acids in polyvinyl alcohol eye drops. The presence of formic acid was attributed to excipients, whereas acetic acid originated from raw materials and was further generated during pH adjustment in manufacturing. Although the overall impurity levels were low and posed minimal risk to drug safety, manufacturers should remain vigilant regarding impurity control to maintain product quality.

    Proteomic alterations in the cortex and hippocampus of APP/PS1 mice: insights into potential mechanisms of Alzheimer's disease
    Hongyan Yin, Sihan You, Jiayi Zhang, Luyao Sun, Jinmeng Cao, Xinxing Liu, Shuang Li, Chunyan Guo
    2025, 34(5):  443-457.  DOI: 10.5246/jcps.2025.05.034
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    Alzheimer's disease (AD) stands as the principal cause of dementia globally, influenced by myriad risk factors. Despite extensive research, the pathogenesis of AD remains elusive. This study aimed to identify differentially expressed proteins in the cortex and hippocampus that are associated with AD. Our comparative analysis revealed significant impairments in spatial memory, cognitive function, and mobility in APPswe/PSEN1dE9 (APP/PS1) mice. Proteomic analysis of cortex tissues revealed 6405 proteins, with 283 showing significant alterations. In the hippocampus, 5574 proteins were identified, among which 244 were significantly altered, suggesting a connection to AD pathology. Through bioinformatics, functional analysis, and protein-protein interaction (PPI) network mapping, we demonstrated that AD progression in the cortex was predominantly driven by inflammation-related pathways, including neutrophil extracellular trap formation, as well as complement and coagulation cascades. Additionally, PPI analysis linked AD progression in the cortex to ribosome-associated proteins. Moreover, several proteins, including APP, IDE, SDHB, and RB1CC1, exhibited alterations in both the cortex and hippocampus. These findings offered novel insights into the diagnostics and therapeutic strategies for AD.

    Comparative effectiveness of sacubitril/valsartan versus valsartan in patients with newly diagnosed hypertensive acute heart failure
    Chengxia Gong, Hui Wang, Xiaoyun Shi, Wenwen Wang, Huiping Gong
    2025, 34(5):  458-469.  DOI: 10.5246/jcps.2025.05.035
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    In the present study, we aimed to investigate the clinical potential of sacubitril/valsartan compared with valsartan in patients with newly diagnosed hypertensive acute heart failure (H-AHF). A total of 63 patients were retrospectively enrolled from our hospital, with 32 patients assigned to the sacubitril/valsartan group and 31 patients to the valsartan group. Clinical characteristics, laboratory examinations, and echocardiographic data at baseline, during hospitalization, and follow-up were collected to assess. The results demonstrated that patients treated with sacubitril/valsartan achieved better control of systolic and diastolic blood pressures than those treated with valsartan. Sacubitril/valsartan also resulted in more significant reductions in N-terminal pro-brain natriuretic peptide (NT-proBNP), high-sensitivity troponin I (hs-TnI), and creatinine, as well as an increase in estimated glomerular filtration rate (eGFR). Moreover, sacubitril/valsartan significantly improved left ventricular ejection fraction (LVEF), the E/e' ratio [the ratio between the early diastolic filling velocity (E-wave) and early diastolic mitral annular velocity (E')], and reduced left atrial dimension (LAD) and left ventricular mass index (LVMI). Additionally, sacubitril/valsartan might offer potential benefits in managing cardiac arrhythmias such as atrial fibrillation, ventricular or supraventricular premature beats, and left bundle branch block (LBBB). No fatal or nonfatal adverse effects were observed in the sacubitril/valsartan group, although one patient in the valsartan group experienced angioedema. In conclusion, after short-term administration, sacubitril/valsartan proved to be more effective than valsartan in lowering blood pressure, improving cardiac function and remodeling, and enhancing biomarker profiles. Furthermore, it had favorable effects on renal function and cardiac arrhythmias in newly diagnosed H-AHF patients.

    Efficacy and safety of tyrosine kinase inhibitors in treating refractory thyroid cancer: A network meta-analysis
    Yixiao Zhu, Lirong Zhang, Wenhua Wu, Huiting Lin, Xiaoxia Wei
    2025, 34(5):  470-484.  DOI: 10.5246/jcps.2025.05.036
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    Refractory thyroid cancer is frequently associated with a poor prognosis, necessitating alternative therapeutic approaches. Tyrosine kinase inhibitors (TKIs) have emerged as a promising treatment option, showing generally favorable clinical outcomes in these challenging cancer subtypes. However, the existing body of research is constrained by small sample sizes and variable findings, limiting the ability to directly compare the efficacy of different TKI agents. This study aimed to bridge that gap through a network meta-analysis, evaluating the relative efficacy and safety of various TKIs in managing refractory thyroid cancer. Utilizing systematic keyword searches in databases such as PubMed, Cochrane Library, Embase, Scopus, Web of Science, and ClinicalTrials.gov, we identified studies that met predefined inclusion criteria. Extracted data were analyzed using Bayesian network meta-analysis methods via R software to ensure a comprehensive assessment. Our findings highlighted specific advantages of certain TKIs for various clinical outcomes. In terms of progression-free survival (PFS), Anlotinib and Apatinib showed notable efficacy. For the objective response rate (ORR), Cabozantinib and Lenvatinib demonstrated superior effectiveness, while for disease control rate (DCR), Apatinib and Lenvatinib were advantageous. Regarding safety profiles, Cabozantinib emerged as the safest option for all-grade adverse events (AEs), with Anlotinib showing a higher risk. For severe AEs (grade 3 or higher), Sorafenib proved to be the safest, while Apatinib carried the highest risk. In summary, Anlotinib, Apatinib, Lenvatinib, and Cabozantinib offered significant benefits for PFS, ORR, and DCR in patients with refractory thyroid cancer. However, Anlotinib and Apatinib were associated with higher AE rates, underlining the importance of balancing efficacy with safety. Cabozantinib and Vandetanib, while exhibiting comparatively safer profiles, showed moderate efficacy. These insights underscored the necessity for tailored treatment decisions that carefully weigh the benefits and risks of each TKI agent.

    Optimization of automated patch-clamp technique and comparative analysis with manual patch-clamp: A case study on the TRPV1 channel
    Guifang Duan, Yue Li, Xia Yuan, Shuxiang Song, Yingli Xu, Jianchun Zhou
    2025, 34(5):  485-492.  DOI: 10.5246/jcps.2025.05.037
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    Patch-clamp technique serve as a powerful tool for precisely measuring and characterizing ion channel currents, offering critical molecular-level insights essential for drug screening and optimization. By enabling a deeper understanding of ion channel behavior, these techniques significantly accelerate the process of drug discovery and development. In recent years, automated patch-clamp technique has undergone substantial advancements, surpassing traditional manual methods with its high throughput, improved data consistency, and automation. However, fully harnessing these advantages requires meticulous optimization of experimental conditions tailored to specific targets. Without such refinement, the high cost of consumables and operational expenses could severely hinder the widespread adoption of this technique. This study focused on the TRPV1 channel, detailing the establishment of an automated patch-clamp detection system for TRPV1 currents, optimization of experimental parameters, and a comparative evaluation of the results against manual patch-clamp techniques.

    News
    New progress in the research team of Prof. Zhenjun Yang at Peking University on "Mannosylated peptidyl lipid CManDA doped into cytidinyl/cationic lipids efficiently delivers siG12Ss to lung cancer in vivo"
    State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center
    2025, 34(5):  493-495. 
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    Reshape the fates of Treg and CD8+ T cells through IL-2Rα by synergizing divergent receptor-biased IL-2 PEGylates
    Department of Molecular and Cellular Pharmacology, School of Pharmaceutical Sciences, Peking University Health Science Center
    2025, 34(5):  496-496. 
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    The research team of Prof. Xiaodong Guan and Prof. Yang Xu has made research progress on Statin use and risk of intracerebral hemorrhage in Chinese population
    Department of Pharmacy Administration and Clinical Pharmacy, School of Pharmaceutical Sciences, Peking University Health Science Center
    2025, 34(5):  497-498. 
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    The research team of Prof. Jing Wang developed a new probe to analyze the spatiotemporal dynamic changes and regulatory mechanisms of intracellular adenosine in vivo
    State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center
    2025, 34(5):  499-502. 
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    The research team of Prof. Jing Wang developed a new probe to analyze the spatiotemporal dynamic changes and regulatory mechanisms of intracellular adenosine in vivo.