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2026 Volume 36 Issue 5  Published: 2026-05-25
  • Guangdong Pharmaceutical Association
    doi: 10.12048/j.issn.1674-229X.2026.05.001
  • Yiyun WANG , Yibo LIANG , Wei SHEN , Yuanyi ZHOU , Zongming LUO , Dong LV
    doi: 10.12048/j.issn.1674-229X.2026.05.002
    OBJECTIVE

    To evaluate the analgesic and anti-inflammatory effects of gout pills using animal experiments.

    METHODS

    The mice were randomly divided into low-medium and high-dose gout pill groups, the model control group and positive control group. The analgesic and anti-inflammatory effects of gout pills were initially evaluated through the acetic acid-induced writhing test, ear swelling test, capillary permeability test and measurement of certain inflammatory factors.

    RESULTS

    Gout pills significantly reduce the number of writhes, auricular swelling degree and capillary permeability, serum levels of IL-6 and TH1 levels in mice, and elevated the levels of TH2 and IgG.

    CONCLUSION

    Gout pills have good anti-inflammatory and analgesic effects.

  • Ke WEI , Junfeng ZHOU , Zhongyin WEI , Weifeng MA , Guangyuan ZHOU
    doi: 10.12048/j.issn.1674-229X.2026.05.003
    OBJECTIVE

    To explore the potential molecular mechanism by which saffron exerts its antidepressant effect by regulating the expression of angiotensinogen (Agt) in the nucleus accumbens (NAc) and regulating synaptic remodeling.

    METHODS

    Fifty mice were randomly divided into five groups: blank control group, model group, fluoxetine group, low-dose saffron group, and high-dose saffron group. The chronic unpredictable stress (CUMS) model was established in mice (except the blank control group), and continuous intragastric administration was performed for 7 days after modeling.. Depressive-like behaviors of mice were evaluated using the forced swimming test (FST), sucrose preference test (SPT), and tail suspension test (TST). The mRNA and protein expression levels of Agt in the NAc were detected. The mRNA levels of angiotensin II (Ang-Ⅱ), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α) in mouse brain tissues were measured. The content of malondialdehyde (MDA) and the activity of superoxide dismutase (SOD) in mouse brain tissues were assayed. Additionally, the protein expression levels of synaptophysin (Syp), postsynaptic density protein 95 (Psd-95), and brain-derived neurotrophic factor (Bdnf) in mouse brain tissues were determined.

    RESULTS

    Compared with the model group, the fluoxetine group, low-dose saffron group, and high-dose saffron group showed improved depressive-like behaviors, with a significant increase in SPT and a significant decrease in immobility time in FST and TST (P<0.05). Compared with the model group, the high-dose saffron group exhibited significantly reduced mRNA levels of Agt, Ang-Ⅱ, IL-6, and TNF-α (P<0.05), decreased MDA content, and significantly increased SOD activity in brain tissues (P<0.05). The protein expression of Syp, Psd-95, and Bdnf in brain tissues was significantly upregulated in the high-dose saffron group (P<0.05).

    CONCLUSION

    Crocetin exerts its antidepressant effect by inhibiting the expression of Agt in the NAc, regulating the renin-angiotensin system (RAS), alleviating neuroinflammation and oxidative stress, and promoting synaptic remodeling mediated by Syp, Psd-95, and Bdnf.

  • Keqin FAN , Fangyu SONG , Liangjing XIA , Jiaqi SUN , Yuehui ZHANG , Liangming ZHANG , Tong CHEN , Zijun YAN
    doi: 10.12048/j.issn.1674-229X.2026.05.004
    OBJECTIVE

    To systematically analyze the polymorphic characteristics of the ITGA2 gene and the impact of the rs1126643 F253L mutation on the biological function of the ITGA2 protein and the antiplatelet effect of aspirin, thereby providing a theoretical foundation and potential genetic biomarkers for the individualized diagnosis and treatment of aspirin resistance (AR).

    METHODS

    The ITGA2 gene and encoded protein sequences were obtained from NCBI and UniProt databases. Physicochemical properties and hydrophobicity profiles of the encoded protein were analyzed using ProtParam and Protscale, respectively. Protein-protein interaction networks were constructed via STRING, secondary structure elements were predicted using SOPMA and DNAStar, and tertiary structural models were generated using SWISS-MODEL, with detailed analysis of conformational differences at the mutation site. Functional and pathogenicity impacts of wild-type versus mutant proteins were assessed in silico, followed by validation through molecular docking and molecular dynamics simulations.

    RESULTS

    The ITGA2 gene spans 105 428 base pairs and encodes a 1 181 amino-acid protein, classifying it as an acidic, hydrophilic protein. Secondary structure analysis revealed that α-helices constitute 14.39%, extended strands 27.35%, and random coils 58.26% of the protein structure. Although the F253L substitution does not significantly alter the fundamental physicochemical properties of the protein, stability prediction tools including DUET and MUpro consistently indicated reduced structural stability. Six out of seven pathogenicity prediction algorithms classified the variant as highly pathogenic. MutPred2 analysis suggested that the mutation may disrupt protein function by decreasing relative solvent accessibility and altering ordered interfacial regions. The ITGA2 protein is involved in critical biological processes such as cell-matrix adhesion, and the F253L mutation may contribute to pathological mechanisms through structural and functional perturbations. These findings were further substantiated by molecular docking and molecular dynamics simulations.

    CONCLUSION

    The ITGA2 F253L mutation represents a core molecular mechanism underlying aspirin resistance, acting through destabilization of the ITGA2 protein structure, reduction in solvent accessibility, reduced binding affinity to aspirin, and thereby attenuating the antiplatelet effect of aspirin. This study highlights the pivotal role of the ITGA2 F253L polymorphism in modulating aspirin responsiveness and provides potential biomarkers and mechanistic insights for genetic profiling and personalized antiplatelet therapy in patients with AR.

  • Jianbiao LI , Shangjie GUO , Xian'en FA
    doi: 10.12048/j.issn.1674-229X.2026.05.005
    OBJECTIVE

    This study aimed to identify novel ligands targeting Site C of Nur77-LBD (ligand binding domain), a critical regulatory binding site of inflammation, using computational approaches.

    METHODS

    A structure-based virtual screening of 9 371 DrugBank compounds was conducted against the Nur77 ligand-binding domain (PDB ID:4JGV) using molecular docking. Top-scoring hits were subjected to 500-ns molecular dynamics (MD) simulations using Schrödinger Desmond module. Binding stability was assessed by root mean square deviation (RMSD), root mean square fluctuation (RMSF), Protein-ligand interaction analysis, and MM-GBSA calculations.

    RESULTS

    Five candidate compounds were identified to potentially bind to Nur77-LBD. Among them, compounds 1, 2, and 3 demonstrated stable binding, with low RMSD fluctuations and persistent protein-ligand interactions comparable to reference ligands 13 and 29.

    CONCLUSION

    These findings highlight compound 1 as the most promising candidate, showing comprehensive binding stability and interaction strength, and provide new chemical scaffolds for further optimization of Nur77 modulators.

  • Fangyu SONG , Keqin FAN , Liangjing XIA , Yuehui ZHANG , Haizhu ZHANG , Liangming ZHANG , Tong CHEN , Jiaqi SUN , Zijun YAN
    doi: 10.12048/j.issn.1674-229X.2026.05.006
    OBJECTIVE

    Based on the US FDA Adverse Event Reporting System (FAERS), this study comprehensively evaluated the adverse reaction characteristics of cephalosporins on the gastrointestinal system, and analyzed the risk heterogeneity among different drug varieties and the influence of patients' baseline characteristics.

    METHODS

    The data from the FAERS database from 1994 to 2024 were extracted, and disproportionality analysis combined with Bayesian method was used to mine the correlation signals between cephalosporins and gastrointestinal adverse events.

    RESULTS

    A total of 54.249 6 million adverse event reports were included, and 793 gastrointestinal system adverse events related to signal-positive cephalosporins were screened out.The signal intensity of cefdinir [ROR=2.69 (2.52-2.88)] was significantly higher than that of other drugs. The Bayesian method verified the association of high-risk events, such as the megacolon signal of cefixime [EBGM=75.21 (95%CI:23.54)]. The risk of signal-negative cephalosporin was low, and very few had a certain intensity of PT signal values.

    CONCLUSION

    This study analyzed the risk of gastrointestinal adverse reactions associated with the use of different types of cephalosporins. Among them, cefdinir had the highest risk of gastrointestinal-related adverse events (AEs), while non-oral signal-negative ceped drugs.

  • Xixi ZHAO , Yang TAO , Hong ZHANG , Zengqing MA
    doi: 10.12048/j.issn.1674-229X.2026.05.007
    OBJECTIVE

    To explore the characteristics and development trends of asthma drug clinical trials in China, and to provide references for promoting the research of new asthma drugs.

    METHODS

    Using "asthma" as the keyword, we searched the Chinese Clinical Trial Registry and Information Disclosure Platform. Data regarding clinical trials of asthma drugs registered from January 2013 to December 2025 were collected, and statistical analyses were performed on registration time, geographic information, investigational drugs and other relevant information.

    RESULTS

    A total of 663 clinical trials of asthma drugs were included in this study. Over the past decade, the number of clinical trials of asthma drugs has shown an upward trend. In terms of trial phases, bioequivalence trials accounted for the largest proportion (n=398, 60.03%). Regarding the categories of investigational drugs, there were 527 chemical drugs, 110 biological agents, and 26 traditional Chinese medicines/natural medicines. The geographical distribution of clinical trial sites was generally characterized by a concentration in eastern China and a scarcity in central and western regions. Regarding pharmacological mechanisms, glucocorticoids were the most widely studied drug category (n=131, 19.76%), while there were 105 biotargeted drugs (15.84%). Among them, domestic innovative drugs have been growing rapidly in recent years.

    CONCLUSION

    Significant progress has been made in clinical trials of asthma drugs in China, particularly with the rapid development of biotargeted drugs. However, problems such as uneven regional distribution of clinical trials and low proportion of innovative drugs still exist. It is necessary to strengthen policy support, optimize the allocation of regional medical and pharmaceutical resources, and continuously promote the research and development of asthma drugs and the advancement of related clinical trials.

  • Hao LI , Lingyun ZUO , Jiahui LIN , Mengying PI , Xiaobin LIN , Xiao CHEN , Guoping ZHONG , Kejing TANG , Changjie CAI , Pan CHEN , Yanzhe XIA
    doi: 10.12048/j.issn.1674-229X.2026.05.008
    OBJECTIVE

    To investigate the relationship between intravenous polymyxin B (PMB) exposure and clinical outcome in septic patients, and to explore the pharmacokinetic target.

    METHODS

    This single-center observational study enrolled septic patients who received PMB therapy between July 2021 and July 2025. Primary outcome was the clinical success rate. Secondary outcomes included 28-day all-cause mortality, 90-day survival time, bacterial clearance, 28-day ventilator/ICU/hospital-free days and incidence of PMB-related acute kidney injury (AKI). The AUCss, 0-12 h and Css, avg were analyzed for associations with outcomes, and cut-off value was determined by receiver-operating characteristic (ROC) curves. Subgroup analysis was conducted among patients receiving continuous renal replacement therapy (CRRT).

    RESULTS

    Of 82 septic patients, clinical success rate was 37.8%. The AUCss, 0-12 h cut-off value was 27.10 mg·h-1·L-1 (Css, avg 2.26 mg·L-1). AUCss, 0-12 h > 27.10 mg·h-1·L-1 was associated with longer 90-day survival time (ETR=1.92, P=0.039). In the CRRT subgroup, increased loading dose was associated with longer 90-day survival time (ETR=1.38, P=0.015). The incidence of PMB-related AKI was 40.54% (15/37).. Patients with AKI had higher AUCss, 0-12 h (43.51 vs. 27.23 mg·h-1·L-1, P=0.006).

    CONCLUSION

    PMB exposure is associated with clinical efficacy in septic patients. Maintaining an AUCss, 0-12 h > 27.10 mg·h-1·L-1 (Css, avg of 2.26 mg·L-1) enhances clinical success. Higher AUCss, 0-12 h is an independent risk factor for PMB-related AKI. Therapeutic drug monitoring is recommended to ensure efficacy and safety.

  • Zhongshun OU , Xuemin LIU , Mingjian CHENG , Qingshang ZHANG , Bang CAI , Xiaofeng ZHU
    doi: 10.12048/j.issn.1674-229X.2026.05.009
    OBJECTIVE

    To analyze the rationality and safety of clinical use of PD-1 inhibitors as novel antitumor drugs, providing guidance for their standardized and safe clinical application.

    METHODS

    This study randomly selected inpatient medical records from April to June 2024 (before clinical pharmacist intervention) as the control group, and records from July 2024 to June 2025 (after intervention) as the intervention group. The rationality and safety of PD-1 inhibitor use were analyzed, with each 3-month period constituting a cycle. Results from each cycle were compared with those of the preceding cycle. Statistical analysis was performed to compare the rationality and safety of PD-1 inhibitor use between the first, second, third, and fourth intervention cycles and the pre-intervention cycle.

    RESULTS

    Post-intervention improvements were observed in prescription qualified rate, proportion of off-label use rate, and number of adverse drug reaction reports for PD-1 inhibitors. For prescription compliance and expanded clinical use indicators, the differences between the first, second, third, and fourth intervention cycles versus the pre-intervention cycle showed statistical significance (P<0.05).

    CONCLUSION

    Clinical pharmacist intervention enhances the rationality and standardization of PD-1 inhibitor use in clinical practice, facilitates timely identification of new or severe adverse reactions, and enables appropriate treatment measures, thereby reducing patient mortality, prolonging survival time, and reducing patients'medical costs.

  • Yanyu LI , Qing LIU , Hongbing HUANG , Tao LIU , Jie ZHOU
    doi: 10.12048/j.issn.1674-229X.2026.05.010
    OBJECTIVE

    To study the efficacy of PD-1 monoclonal antibody in treating microsatellite instability-high (MSI-H) colorectal cancer with different Kras gene point mutations.

    METHODS

    Clinical data of patients with confirmed MSI-H colorectal cancer combined with Kras mutations were collected. Patients were divided into four groups based on different Kras mutation types: A146T, G12C, G12D, and G12V. Treatment efficacy was evaluated using the RECIST 1.1 criteria. Event-free survival (EFS) was calculated with the first administration of PD-1 monoclonal antibody as the starting point for survival time. The detection results of tumor markers (CEA, CA19-9, and CA72-4) were compared before and after treatment. The incidence of adverse reactions during treatment across groups was statistically analyzed.

    RESULTS

    The ORR (overall response rate) was highest in the G12V group (33.33%), followed by the G12D group (25.00%), the G12C group (20.00%), and the A146T group (12.50%). The DCR (disease control rate) was highest in the A146T group (100%), followed by the G12D group (91.66%), the G12V group (86.66%), the G12C group (70.00%), no statistically significant differences in ORR and DCR were observed among all groups (P>0.05). The average EFS duration was 19.25±12.19 months in the G12V group, 17.60±10.46 months in the A146T group, 15.36±9.32 months in the G12C group, and 12.15±7.36 months in the G12D group, with no significant differences among the groups (P>0.05). The median EFS duration was 15.12 months in the G12V group, 12.76 months in the A146T group, 10.65 months in the G12C group, and 10.20 months in the G12D group. In the G12V group, the levels of CEA and CA19-9 decreased significantly after treatment (P<0.05). During treatment, patients experienced immune-related adverse reactions such as rash, thyroid dysfunction, elevated transaminases, immune-related pneumonia, colitis, and peripheral neuritis, but no statistically significant differences in the incidence rates were found among the groups (P>0.05).

    CONCLUSION

    PD-1 monoclonal antibody showed better efficacy in patients with MSI-H colorectal cancer combined with Kras G12V mutation.

  • Yawen WANG , Guojin ZHOU , Weiheng LIU , Kejing TANG , Jing XU , Jie CHEN
    doi: 10.12048/j.issn.1674-229X.2026.05.011
    OBJECTIVE

    To investigate the efficacy and safety of first-line osimertinib in the treatment of epidermal growth factor receptor (EGFR)-mutated non-small cell lung cancer (NSCLC), and to analyze the influencing factors of progression-free survival (PFS).

    METHODS

    The clinical data of patients with EGFR-mutated NSCLC who received first-line osimertinib monotherapy only from January 2019 to December 2022 were collected retrospectively. The primary endpoint was PFS. Survival analysis was performed using the Kaplan-Meier method, and univariate and multivariate Cox regression models were used to analyze the influencing factors of PFS. Meanwhile, the occurrence of adverse events (AEs) was described.

    RESULTS

    A total of 74 patients were included, with a median PFS of 16.3 months (95%CI=13.2-20.3 months). Subgroup analysis showed that the median PFS of patients with stage ⅢA/ⅣA was significantly longer than that of patients with stage ⅣB (25.1 months vs. 15.0 months, P=0.035). The median PFS of patients with prognostic nutritional index (PNI)≥39.4 was significantly longer than that of patients with PNI <39.4 (17.2 months vs. 10.7 months, P=0.030). Multivariate Cox regression analysis showed that disease stage and PNI were independent influencing factors of PFS. Common AEs included rash, oral ulcer, diarrhea, decreased white blood cell count, and paronychia, mostly grades 1-2.

    CONCLUSION

    First-line osimertinib shows favorable efficacy with manageable safety in patients with EGFR-mutated NSCLC. Baseline disease stage and PNI are independent factors for disease progression in NSCLC patients receiving first-line osimertinib.

  • Hongxin LI , Jun WANG , Lingjun KONG , Qingwang WEI , Chengwu SHEN , Dongna ZOU
    doi: 10.12048/j.issn.1674-229X.2026.05.012

    Inhalation therapy is one of the common treatment methods in respiratory department, and it is clinically commonly used for the treatment of asthma, laryngitis, chronic obstructive pulmonary disease and other diseases. Special populations have attracted widespread attention because of their pathophysiological characteristics or inappropriate use methods, which may lead to improper drug selection or reduced drug effectiveness, and in severe cases, it will endanger patients' lives. According to the physiological characteristics of special populations, the pharmacological characteristics of inhaled drugs are analyzed, and the problems related to the standardized use and rational use of drugs in special populations were summarized, so as to provide a theoretical basis for clinical pharmacists to monitor the use of drugs in special groups of patients undergoing inhalation therapy.