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Pharmacological Potential and Molecular Targets of Tetrahydrofurofuranoid Lignans From Magnoliae Flos. 木兰四氢呋喃类木脂素的药理潜力及分子靶点。
IF 5.1 2区 医学
Drug Design, Development and Therapy Pub Date : 2025-10-03 eCollection Date: 2025-01-01 DOI: 10.2147/DDDT.S547924
Xiaohan Yi, Zixuan Xiao, Jiaxue Chen, Guoren Chen, Ping Ma
{"title":"Pharmacological Potential and Molecular Targets of Tetrahydrofurofuranoid Lignans From <i>Magnoliae Flos</i>.","authors":"Xiaohan Yi, Zixuan Xiao, Jiaxue Chen, Guoren Chen, Ping Ma","doi":"10.2147/DDDT.S547924","DOIUrl":"https://doi.org/10.2147/DDDT.S547924","url":null,"abstract":"<p><p>Tetrahydrofurofuranoid lignans (TFLs) are lignans extracted from the dried flower buds of <i>Magnoliae Flos (MF)</i>. The chemical structures of the seven major constituents, magnolin, fargesin, aschantin, lirirresinol B dimethyl ether, epimognolin, eudesmin, and kobusin, are strikingly similar. Despite their potential therapeutic effects against various pathological conditions, their underlying mechanisms have not been systematically analyzed. The primary objective of this review was to examine the mechanisms by which TFLs exert therapeutic effects on inflammation, allergies, cancer, cardiovascular diseases, metabolic disorders and osteoarticular diseases. Data were retrieved from scientific databases, including PubMed, Web of Science, and Google Scholar, up to November 2024. The search terms employed included \"Magnoliae Flos\" or \"Magnolia\" and \"Lignans\" \"Tetrahydrofurofuranoid\" \"Magnolin\" \"Fargesin\" \"Aschantin\" \"Lirirresinol B dimethyl ether\" \"Epimagnolin\" \"Eudesmin\" and \"Kobusin.\" TFLs have been demonstrated to treat various inflammatory diseases through inhibition of signaling pathways, including NF-κB and MAPK. Additionally, allergic reactions are suppressed via inhibition of mast cell degranulation-related receptors. Furthermore, anticancer activity is achieved by triggering signaling pathways such as PI3K/AKT/mTOR, ERK/MEK, and P53. Besides enhancing glucose metabolism, TFLs suppress adipogenesis through downregulation of pathways involving PI3K/Akt, Akt/AMPK, and P-selectin expression. Fargesin, a notable compound derived from <i>MF</i>, exerts cardioprotective effects by inhibiting the cAMP/PKA pathway and counteracts atherosclerosis through the downregulation of the TLR4/NF-κB signaling pathway. Notably, TFLs also demonstrate the ability to reduce melanin synthesis by suppressing tyrosinase, associated proteins, MITF, and enzymes involved in melanogenesis. Growing research highlights diverse pharmacological attributes of TFLs, providing critical insights for future studies aimed at developing novel therapeutics exhibiting enhanced efficacy and minimal toxicity for inflammation, cancer, cardiovascular disorders, diabetes, skin ultraviolet damage and osteoporosis.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"9011-9027"},"PeriodicalIF":5.1,"publicationDate":"2025-10-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12502963/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145250176","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Efficacy of QP002 for the Treatment of Post-Operative Pain After Tension-Free Repair of Open Unilateral Inguinal Hernia. 一项评估QP002治疗开放性单侧腹股沟疝无张力修复术后疼痛的安全性、耐受性、药代动力学和疗效的I期研究。
IF 5.1 2区 医学
Drug Design, Development and Therapy Pub Date : 2025-10-02 eCollection Date: 2025-01-01 DOI: 10.2147/DDDT.S518200
Lina Yang, Jinyu Liu, Shaoxing Liu, Dejun Cao, Keyu Xie, Xianjie Zhang, Mengchang Yang
{"title":"A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Efficacy of QP002 for the Treatment of Post-Operative Pain After Tension-Free Repair of Open Unilateral Inguinal Hernia.","authors":"Lina Yang, Jinyu Liu, Shaoxing Liu, Dejun Cao, Keyu Xie, Xianjie Zhang, Mengchang Yang","doi":"10.2147/DDDT.S518200","DOIUrl":"https://doi.org/10.2147/DDDT.S518200","url":null,"abstract":"<p><strong>Background: </strong>QP002 Long-acting local anaesthetic with bupivacaine and low-dose meloxicam as active ingredients for postoperative regional analgesia. The objective of the present study was to evaluate the safety, tolerability, and pharmacokinetics (PK) and pharmacodynamics (PD) of QP002 for postoperative analgesia following tension-free repair of an open unilateral inguinal hernia.</p><p><strong>Methods: </strong>This was a multicentre, randomised, double-blind, positive-controlled trial. Patients were randomly assigned to receive a single injection of QP002 (five dose groups) with 0.25% bupivacaine hydrochloride 75 mg after open unilateral tension-free repair of an inguinal hernia. Pharmacokinetic parameters were evaluated by obtaining pharmacokinetic characteristic blood samples before and 120 hours after administration, at a total of 20 sampling points. Adverse events occurring after treatment were recorded from baseline to postoperative day 27 follow-up.</p><p><strong>Results: </strong>A total of 40 patients with unilateral inguinal hernia were included in this study. In comparison to 0.25% bupivacaine hydrochloride 75 mg, the results demonstrate that QP002 was well tolerated, with no additional adverse events (AEs) observed and no instances of serious adverse events (SAEs). QP002 demonstrated prolonged absorption and clearance of bupivacaine, including a longer time to reach peak plasma concentration and a terminal elimination half-life. The peak plasma concentrations of 240 mg/7.2 mg QP002 (C<sub>max</sub> 250.33 ng/mL) were similar to those of 0.25% bupivacaine hydrochloride 75 mg (C<sub>max</sub> 258.40 ng/mL). Cumulative pain intensity scores at 24 hours postoperatively in the exercise state (NRS-A-AUC<sub>0-24</sub>) were lower in the QP002 dose groups than in the 0.25% bupivacaine hydrochloride 75 mg, with P = 0.0165 in the 320 mg/9.6 mg QP002 and P = 0.0435 in the 400 mg/12 mg QP002.</p><p><strong>Conclusion: </strong>QP002 demonstrated favorable safety profiles and exhibited distinct extended-release pharmacokinetic (PK) characteristics in single-ascending-dose administration. High doses of QP002 showed potential for postoperative incisional infiltration to control pain. Future studies will further explore its efficacy and safety in broader clinical applications.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"8985-8995"},"PeriodicalIF":5.1,"publicationDate":"2025-10-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12499247/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145244001","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Modified Sijunzi Decoction Inhibits Pancreatic Cancer Progression and Improves Immune Suppression: Network Pharmacology and Experimental Validation. 加减四君子汤抑制胰腺癌进展及改善免疫抑制:网络药理学及实验验证。
IF 5.1 2区 医学
Drug Design, Development and Therapy Pub Date : 2025-10-02 eCollection Date: 2025-01-01 DOI: 10.2147/DDDT.S520390
Yuan Zhang, Linjie Ruan, Xin Li, Waimei Si, Peiwen Yang, He Ba, Zhen Chen
{"title":"Modified Sijunzi Decoction Inhibits Pancreatic Cancer Progression and Improves Immune Suppression: Network Pharmacology and Experimental Validation.","authors":"Yuan Zhang, Linjie Ruan, Xin Li, Waimei Si, Peiwen Yang, He Ba, Zhen Chen","doi":"10.2147/DDDT.S520390","DOIUrl":"https://doi.org/10.2147/DDDT.S520390","url":null,"abstract":"<p><strong>Purpose: </strong>This study aimed to assess the effectiveness of Modified Sijunzi Decoction (MSJZD) in pancreatic cancer (PC) treatment. Molecular mechanisms were elucidated and active ingredients were screened using network pharmacology, RNA sequencing, and in vivo experiments, providing a scientific foundation for the clinical application of MSJZD in PC treatment.</p><p><strong>Methods: </strong>We established an orthotopic PC mouse model and treated it with different MSJZD concentrations to evaluate its efficacy. Ultra-high-performance liquid chromatography Q-Exactive mass spectrometry was used to identify MSJZD components. Through integrated pharmacology analyses, the active ingredients, core targets, and signaling pathways were determined, and active ingredients targeting the core targets were screened using molecular docking simulations. RNA-sequencing analyses of the molecular mechanism of MSJZD in PC treatment were verified using immunohistochemistry and Western blotting. A multiplex immunofluorescence assay was used to detect macrophage and CD8<sup>+</sup> T cell infiltration levels.</p><p><strong>Results: </strong>MSJZD effectively inhibited the growth of orthotopic pancreatic tumors in mice via JAK1-STAT3 pathway and reduced Ki-67 expression, with no discernible toxicity to the liver and kidneys. MSJZD relieved immunosuppression by decreasing M2 macrophage infiltration, increasing CD8<sup>+</sup> T cell infiltration, and lowering the expression of immunosuppressive cytokines (interleukins 10 and 6). Network pharmacology analysis revealed that EGFR, SRC, AKT1, and STAT3 were the core MSJZD targets in PC treatment. Molecular docking revealed a strong binding affinity between wedelolactone and its core target proteins (EGFR, SRC, AKT1).</p><p><strong>Conclusion: </strong>MSJZD is a safe and effective decoction for PC that exerts anti-tumor effects by inhibiting JAK1-STAT3 pathway and improving immunosuppressive microenvironment by reducing M2 macrophage infiltration and increasing CD8<sup>+</sup> T cell infiltration. This study reveals MSJZD therapeutic potential and offers a reference for further research.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"8949-8966"},"PeriodicalIF":5.1,"publicationDate":"2025-10-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12499272/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145244096","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The Comparison of the Efficacy of Esketamine Over Sufentanil to Reduce Postoperative Nausea and Vomiting in Gynecological Laparoscopic Surgery: A Prospective, Double-Blind, Randomized Controlled Trial. 艾氯胺酮与舒芬太尼减少妇科腹腔镜手术术后恶心呕吐的疗效比较:一项前瞻性、双盲、随机对照试验。
IF 5.1 2区 医学
Drug Design, Development and Therapy Pub Date : 2025-10-02 eCollection Date: 2025-01-01 DOI: 10.2147/DDDT.S533198
Zhuolin Qiu, Yue Guo, Weilong Zhong, Weiqiang Chen, Ping Xiang, Jianfen Liang, Jingyi Du, Xiang Li
{"title":"The Comparison of the Efficacy of Esketamine Over Sufentanil to Reduce Postoperative Nausea and Vomiting in Gynecological Laparoscopic Surgery: A Prospective, Double-Blind, Randomized Controlled Trial.","authors":"Zhuolin Qiu, Yue Guo, Weilong Zhong, Weiqiang Chen, Ping Xiang, Jianfen Liang, Jingyi Du, Xiang Li","doi":"10.2147/DDDT.S533198","DOIUrl":"https://doi.org/10.2147/DDDT.S533198","url":null,"abstract":"<p><strong>Background: </strong>Postoperative nausea and vomiting (PONV) affect 40-80% of patients undergoing gynecological laparoscopy (GLS). Opioids, though effective for analgesia, may exacerbate PONV. Esketamine, the dextrorotatory form of ketamine with analgesic, sedation and anti-inflammatory properties, was evaluated for PONV prophylaxis compared to sufentanil.</p><p><strong>Methods: </strong>In this single-center, double-blind trial, 150 patients undergoing elective GLS were randomized to receive esketamine (0.25mg/kg, n=75) or sufentanil (0.1μg/kg, n=75) at the incision closing. Primary outcomes were PONV incidence and severity in Postanesthesia care unit (PACU) and during 48 hours postoperation. Secondary outcomes included pain scores, supplemental analgesia use, sore throat and bucking at excubation. Statistical analyses utilized t-tests, Mann-Whitney U, and <i>χ²</i>-tests (significance: p < 0.05) with Friedman test for within-group comparisons and generalized estimating equations (GEE) for group-time interaction evaluation.</p><p><strong>Results: </strong>The esketamine group demonstrated significantly lower PONV incidence (in PACU: 57.3% vs 36%, p=0.014; 24h: 53.3% vs 36%, p=0.048) and reduced severity within 24 hours (in PACU, p<0.001; 6h, P=0.042; 24h, p=0.029). Secondary outcomes favored esketamine: lower dynamic pain scores during coughing (in PACU, p=0.017; 6h, P=0.021; 24h, p=0.012), lower severity of sore throat (6h, P=0.019; 24h, p=0.028), reduced rescue analgesia needs (6h: RD=0.12, p=0.037), and decreased incidence of bucking reflex (RD=0.21, p=0.014).</p><p><strong>Conclusion: </strong>Single-dose esketamine significantly reduces PONV incidence and severity in GLS, improves dynamic analgesia, and mitigates extubation complications. These results support the single dose use of esketamine as an opioid-sparing adjunct to prevent PONV in gynecological laparoscopy.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"8919-8929"},"PeriodicalIF":5.1,"publicationDate":"2025-10-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12499367/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145244061","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Dexmedetomidine's Effect on Catecholamine and Inflammation in Reducing In-Hospital Adverse Events for Older Patients with STEMI Undergoing Primary PCI. 右美托咪定对儿茶酚胺和炎症的影响减少老年STEMI患者行初次PCI的住院不良事件
IF 5.1 2区 医学
Drug Design, Development and Therapy Pub Date : 2025-10-02 eCollection Date: 2025-01-01 DOI: 10.2147/DDDT.S542160
Guang-An Liu, Wanglong Wu, Linxiao Zhou, Ruoxi Zhang, Feng Liu
{"title":"Dexmedetomidine's Effect on Catecholamine and Inflammation in Reducing In-Hospital Adverse Events for Older Patients with STEMI Undergoing Primary PCI.","authors":"Guang-An Liu, Wanglong Wu, Linxiao Zhou, Ruoxi Zhang, Feng Liu","doi":"10.2147/DDDT.S542160","DOIUrl":"https://doi.org/10.2147/DDDT.S542160","url":null,"abstract":"<p><strong>Objective: </strong>This study aimed to assess the effects of dexmedetomidine (DEX) on anxiety and inflammation, and its potential in reducing in-hospital adverse events in older patients with ST-elevation myocardial infarction (STEMI) undergoing primary percutaneous coronary intervention (PCI).</p><p><strong>Methods: </strong>We conducted a retrospective, real-world cohort study, enrolling 160 elderly patients with STEMI admitted to the cardiac care unit (CCU) between September 2020 and December 2024. Patients were divided into two groups: DEX and non-DEX. Propensity score matching (PSM, 1:1 ratio) was applied based on demographic and clinical variables, ensuring balanced groups for comparison. We evaluated catecholamine and inflammation levels, anxiety using the Amsterdam Preoperative Anxiety and Information Scale (APAIS), and cognitive function at four time points (T0-T3). The incidence of cumulative MACE (20.00% vs 38.8%, <i>P</i> = 0.015) and VT/VF (1.3% vs 10.0%, <i>P</i> = 0.034) was significantly lower in the DEX group compared to the non-DEX group. Multivariable logistic regression was performed to identify risk factors for in-hospital major adverse cardiac events (MACE).</p><p><strong>Results: </strong>The DEX group had significantly lower catecholamine (norepinephrine, <i>P</i> < 0.001; epinephrine, <i>P</i> = 0.001; dopamine, <i>P</i> < 0.001) and inflammation levels (hs-CRP, <i>P</i> < 0.001) post-PCI compared to the non-DEX group. Additionally, heart rate (HR) (T1, <i>P</i> < 0.001; T2, <i>P</i> < 0.001; T3, <i>P</i> = 0.007) and respiratory rate (RR) (T1, <i>P</i> < 0.001; T2, <i>P</i> < 0.001) were lower, while blood oxygen saturation (SpO<sub>2</sub>) (T1, <i>P</i> = 0.045; T2, <i>P</i> < 0.001; T3, <i>P</i> < 0.001; T4, <i>P</i> = 0.016) was higher in the DEX group at various time points. In the DEX group, Ramsay Sedation Scores were higher at T1 (<i>P</i> = 0.007) and T2 (<i>P</i> < 0.001) than at T0, and anxiety scores decreased significantly from T1 (<i>P</i> = 0.021), T1 (<i>P</i> = 0.017) to T3 (<i>P</i> = 0.015) compared with the preceding time point. DEX was identified as an independent predictor of reduced in-hospital MACE [odds ratio (OR) = 0.244, 95% confidence interval (CI) = 0.082-0.728, <i>P</i> = 0.011].</p><p><strong>Conclusion: </strong>DEX was associated with lower catecholamine and inflammation levels, provided adequate sedation, and appeared safety, feasibility, and effectiveness for older patients with STEMI undergoing primary PCI.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"8935-8947"},"PeriodicalIF":5.1,"publicationDate":"2025-10-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12499248/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145244071","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Astragaloside IV Alleviates Systemic Lupus Erythematosus by Modulating ITGB1/PTK2/p38 Pathway: Integrated Network Pharmacology and Experimental Validation. 黄芪甲苷通过调节ITGB1/PTK2/p38通路缓解系统性红斑狼疮:综合网络药理学及实验验证
IF 5.1 2区 医学
Drug Design, Development and Therapy Pub Date : 2025-10-02 eCollection Date: 2025-01-01 DOI: 10.2147/DDDT.S554510
Zhongfu Tang, Lili Cheng, Ming Li, Chuanbing Huang
{"title":"Astragaloside IV Alleviates Systemic Lupus Erythematosus by Modulating ITGB1/PTK2/p38 Pathway: Integrated Network Pharmacology and Experimental Validation.","authors":"Zhongfu Tang, Lili Cheng, Ming Li, Chuanbing Huang","doi":"10.2147/DDDT.S554510","DOIUrl":"https://doi.org/10.2147/DDDT.S554510","url":null,"abstract":"<p><strong>Purpose: </strong>Systemic lupus erythematosus (SLE) features immune cell dysfunction, causing immune - complex and inflammatory - factor formation that damages organs. Astragaloside IV (AS-IV), a cyclic triterpene saponin from Astragalus membranaceus, has strong anti-inflammatory and immunomodulatory effects. This study aimed to evaluate AS-IV's therapeutic potential for SLE and uncover its mechanism.</p><p><strong>Methods: </strong>MRL/lpr mice were divided into MRL/lpr, low - medium - high - dose AS-IV, and Pred groups, with C57BL/6 mice as controls. Renal damage was assessed by histopathology and electron microscopy. Immune parameters were analyzed using ELISA, flow cytometry, immunofluorescence, and immunohistochemistry. Network pharmacology was used to find AS-IV's SLE targets, and molecular docking was employed to clarify its mechanism, with multiple methods used to measure target expression.</p><p><strong>Results: </strong>AS-IV ameliorated renal pathology by reducing glomerular and vascular wall lesion scores while attenuating immune complex deposition. It significantly decreased podocyte foot process fusion rates, alleviated overall renal damage, and reduced key renal inflammatory cytokines. Systemically, AS-IV reduced spleen index and lowered anti-dsDNA, IgG levels, while restoring complement components C3 and C4, akin to the effects observed in the Pred group. AS-IV notably downregulated the expression of ITGB1, PTK2, p38, IL-4, IL-21, IL-17, and the Th1/Th2 and Th17 ratios, while upregulating the Treg ratio compared to the MRL/lpr group. Molecular docking and Western blot analyses further validated the interaction between AS-IV and the ITGB1/PTK2/p38 axis.</p><p><strong>Conclusion: </strong>AS-IV can modulate the ITGB1/PTK2/p38 axis to suppress immune inflammatory responses, thereby ameliorating SLE progression. These findings suggest the certain therapeutic value of AS-IV in managing SLE.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"8967-8984"},"PeriodicalIF":5.1,"publicationDate":"2025-10-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12499577/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145244043","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Methodological Considerations in the Evaluation of Ciprofol's Effect on Postoperative Delirium in Elderly Patients [Letter]. 评价环丙酚对老年患者术后谵妄疗效的方法学考虑[信]。
IF 5.1 2区 医学
Drug Design, Development and Therapy Pub Date : 2025-10-01 eCollection Date: 2025-01-01 DOI: 10.2147/DDDT.S566568
Yanfei Lu, Fang Cai
{"title":"Methodological Considerations in the Evaluation of Ciprofol's Effect on Postoperative Delirium in Elderly Patients [Letter].","authors":"Yanfei Lu, Fang Cai","doi":"10.2147/DDDT.S566568","DOIUrl":"https://doi.org/10.2147/DDDT.S566568","url":null,"abstract":"","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"8933-8934"},"PeriodicalIF":5.1,"publicationDate":"2025-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12497654/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145244122","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
LC-MS/MS Method for Simultaneous Quantification of Three Oxazolidinone Antimicrobials in Human Plasma: Application to Therapeutic Drug Monitoring. LC-MS/MS法同时定量人血浆中三种恶唑烷酮类抗菌药:在治疗药物监测中的应用。
IF 5.1 2区 医学
Drug Design, Development and Therapy Pub Date : 2025-10-01 eCollection Date: 2025-01-01 DOI: 10.2147/DDDT.S547979
Na Zhang, Nan Bai, Ying Wang, Beibei Liang, Yun Cai
{"title":"LC-MS/MS Method for Simultaneous Quantification of Three Oxazolidinone Antimicrobials in Human Plasma: Application to Therapeutic Drug Monitoring.","authors":"Na Zhang, Nan Bai, Ying Wang, Beibei Liang, Yun Cai","doi":"10.2147/DDDT.S547979","DOIUrl":"10.2147/DDDT.S547979","url":null,"abstract":"<p><strong>Background: </strong>Oxazolidinone antimicrobials, which are effective against multidrug-resistant gram-positive pathogens, face challenges of variable efficacy and safety owing to patient pharmacokinetic differences.</p><p><strong>Purpose: </strong>This study aimed to establish a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method to simultaneously quantify multiple oxazolidinone antimicrobials, including linezolid, tedizolid, and contezolid, for therapeutic drug monitoring (TDM) applications.</p><p><strong>Methods: </strong>Chromatographic separation was achieved on a C18 column (100 × 2.1 mm, 3.5 μm) with gradient elution. Detection was performed via positive electrospray ionization (ESI+) in multiple reaction monitoring (MRM) mode, targeting transitions: m/z 338.14→162.8 (linezolid); m/z 371→343.1 (tedizolid) and m/z 409.15→269.14 (contezolid), with voriconazole-d3 as the internal standard.</p><p><strong>Results: </strong>The method was validated using <i>Bioanalytical Method Validation (M10)</i>. The method demonstrated high selectivity and wide linear ranges of 50.0-15,000.0 ng/mL for linezolid and contezolid, and 25.0-7500.0 ng/mL for tedizolid, respectively, with a good linearity (R<sup>2</sup> > 0.993). The intra- and inter-day accuracy and precision were within acceptable limits. Recovery ranged from 94.4% to 104.2% in plasma, and matrix effects were negligible (CV%<3.6%). Stability experiments confirmed analyte integrity under short-term (8 h at room temperature), long-term (34 days at -80°C for linezolid; 40 days for tedizolid and contezolid), and freeze-thaw conditions. No carry-over contamination was exhibited. This method has been successfully applied to monitor the concentrations of both drugs during the transition between linezolid and contezolid therapy.</p><p><strong>Conclusion: </strong>This validated LC-MS/MS method enables the simultaneous determination of linezolid, tedizolid, and contezolid in human plasma, rendering it promising for pharmacokinetic studies and TDM, and contributing to optimized patient care in complex therapeutic scenarios.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"8903-8917"},"PeriodicalIF":5.1,"publicationDate":"2025-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12497388/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145238112","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Erratum: Natural Products from Traditional Chinese Medicine: Potential Therapeutic Agents in Cancer Therapy-Induced Cardiotoxicity [Corrigendum]. 来自传统中药的天然产物:癌症治疗引起的心脏毒性的潜在治疗剂[勘误]。
IF 5.1 2区 医学
Drug Design, Development and Therapy Pub Date : 2025-10-01 eCollection Date: 2025-01-01 DOI: 10.2147/DDDT.S571097
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引用次数: 0
Estimation of ED50 and ED95 of Oliceridine Required to Suppress the Bronchoscopy Response in Patients Undergoing Fiberoptic Bronchoscopy Under Sedation with Cipepofol: An Up-and-Down Sequential Allocation Trial. 估计丙泊酚镇静下行纤维支气管镜检查患者所需的奥利啶ED50和ED95:一项上下顺序分配试验
IF 5.1 2区 医学
Drug Design, Development and Therapy Pub Date : 2025-09-30 eCollection Date: 2025-01-01 DOI: 10.2147/DDDT.S535435
Dongxue Wu, Yeqing Liao, Yanlin Qin, Yafeng Wang, Bing Xu, Qiuling Chen, Xianting Wang, Xiaoshan Wu, Yalan Li, Xuehai Guan
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引用次数: 0
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