Drug Research最新文献_第3页

Adverse Event Profile Differences Between Eliglustat and Miglustat: A Pharmacovigilance Study using the U.S. Food and Drug Administration Adverse Event Reporting System. 依格司他和米格司他不良事件概况差异：一项使用美国食品和药物管理局不良事件报告系统的药物警戒研究。

IF 2.4

Drug Research Pub Date : 2026-03-01 Epub Date: 2026-02-05 DOI: 10.1055/a-2791-0972

Ya Gan, Jie Liu, Chunyong Xia

{"title":"Adverse Event Profile Differences Between Eliglustat and Miglustat: A Pharmacovigilance Study using the U.S. Food and Drug Administration Adverse Event Reporting System.","authors":"Ya Gan, Jie Liu, Chunyong Xia","doi":"10.1055/a-2791-0972","DOIUrl":"10.1055/a-2791-0972","url":null,"abstract":"Both eliglustat and miglustat are substrate reduction therapies targeting glucosylceramide synthase; yet, their safety profile has not been comprehensively analyzed. This study analyzes adverse events associated with both drugs using the U.S. Food and Drug Administration Adverse Event Reporting System to provide insights for clinical safety.Adverse events were classified by MedDRA System Organ Class (SOC, v26.1). Adverse event signals were mined by disproportionality analyses, including the reporting odds ratio, the proportional reporting ratio, the multi-item gamma Poisson shrinker algorithms, and the Bayesian confidence propagation neural network.A total of 1,223 and 980 adverse event reports were retrieved from eliglustat and miglustat, respectively, involving 27 System Organ Class categories each. Some positive signals were consistent with the drug labels, including dyspepsia identified in eliglustat and diarrhoea identified in miglustat. We also identified unexpected signals not listed on the drug labels, such as paresthesia, dry skin, and ichthyosis for eliglustat and dysphagia for miglustat. For patients treated with eliglustat and miglustat, the majority of adverse events manifested more than 1 year after the initiation of therapy. Notably, male patients treated with eliglustat have the significantly higher incidence of weight increase and dry skin. Female patients treated with miglustat have the significantly higher incidence of dysphagia and cognitive disorder.In the clinical administration of eliglustat and miglustat, clinicians need to monitor the effects of adverse events varied by gender and to pay more attention to new adverse event signals.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":"82-90"},"PeriodicalIF":2.4,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146124166","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Treatment of K562 Cells with ABL Kinase Inhibitors Reveals Differential Metabolic Profiles. 用ABL激酶抑制剂治疗K562细胞揭示不同的代谢特征

IF 2.4

Drug Research Pub Date : 2026-03-01 Epub Date: 2026-01-22 DOI: 10.1055/a-2769-1965

Pranay Renukuntla, Sai Charitha Mullaguri, Divya Presingu, Rama Krishna Kancha, Jagadeshwar Reddy Thota

引用次数: 0

Translational Insights into Liposomal Drug Delivery: Recent Advances, Therapeutic Applications, and Clinical Trials. 转化洞察脂质体药物递送：最新进展，治疗应用和临床试验。

IF 2.1

Drug Research Pub Date : 2026-03-01 Epub Date: 2026-02-25 DOI: 10.1055/a-2795-7008

Abdul Shadab, Abdul Faiz Ansari

{"title":"Translational Insights into Liposomal Drug Delivery: Recent Advances, Therapeutic Applications, and Clinical Trials.","authors":"Abdul Shadab, Abdul Faiz Ansari","doi":"10.1055/a-2795-7008","DOIUrl":"10.1055/a-2795-7008","url":null,"abstract":"Liposomes are artificially constructed, phospholipid-based vesicular systems that have emerged as vital components in pharmaceutical nanotechnology and advanced drug delivery. Their flexible bilayered structure enables the encapsulation of a broad spectrum of therapeutic agents, enhancing drug stability and bioavailability. Since their discovery, liposomes have been widely explored as efficient drug carriers and diagnostic tools due to their superior capacity to deliver active pharmaceutical ingredients precisely to target sites. Their inherent advantages including high biocompatibility, the enhanced permeability and retention effect for passive tumor targeting, customizable surface modification for improved targeting efficiency, and enhanced physicochemical stability collectively position them as promising nanocarriers for cancer therapy and other biomedical applications. Liposomes, as synthetic nanoscale vesicles, offer significant promise for immunotherapeutic interventions due to their capability to codeliver antigens and adjuvants while modulating immune cell behavior. Specialized formulations such as immunoliposomes, virosomes, and other immunostimulatory complexes engineered with specific ligands or immune active moieties exhibit unique structural and functional profiles that enhance anticancer immune responses. Furthermore, liposomes facilitate targeted cargo delivery to immune cells, influencing their phenotype and functional activity. This review presents an integrated overview of liposomal composition, structural attributes, mechanisms of drug delivery, therapeutic applications, and clinical progress. The use of liposomes in delivering small molecules, macromolecules, and nucleic acids has demonstrated significant advancements, underscoring their expanding role in modern therapeutics. Overall, this article provides a comprehensive and up-to-date examination of liposome technology and its clinical translational potential.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":"65-81"},"PeriodicalIF":2.1,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147303518","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Gallic Acid Induces Apoptosis in Oral Squamous Cell Carcinoma via PI3K/AKT/mTOR Pathway Inhibition and PTEN Upregulation: an In Vitro Study. 没食子酸通过抑制PI3K/AKT/mTOR通路和上调PTEN诱导口腔鳞癌细胞凋亡的体外研究

IF 2.1

Drug Research Pub Date : 2026-01-01 Epub Date: 2025-11-26 DOI: 10.1055/a-2724-9894

Sanaz Helli, Armin Heidari, Armin Tafvizi, Amir Valizadeh, Sona Rafieyan, Bahman Yousefi

{"title":"Gallic Acid Induces Apoptosis in Oral Squamous Cell Carcinoma via PI3K/AKT/mTOR Pathway Inhibition and PTEN Upregulation: an In Vitro Study.","authors":"Sanaz Helli, Armin Heidari, Armin Tafvizi, Amir Valizadeh, Sona Rafieyan, Bahman Yousefi","doi":"10.1055/a-2724-9894","DOIUrl":"10.1055/a-2724-9894","url":null,"abstract":"Oral squamous cell carcinoma is one of the most common head and neck cancers, which is associated with drug resistance and high mortality rates. The PI3K/AKT/mTOR pathway plays a crucial role in the survival, growth, and metastasis of cancer cells, making it a suitable target for targeted therapy.This study investigated the antitumor effects of gallic acid on CAL-27 cells, with a focus on the aforementioned pathway.CAL-27 cells were treated with different concentrations of gallic acid for 48 hours, and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay was performed to assess viability. The expression of key genes and proteins in the PI3K/AKT/mTOR pathway, as well as apoptosis-related genes, was evaluated using the quantitative real-time reverse transcription polymerase chain reaction and western blot. Also, the activity of caspase-3/7 enzymes and the level of apoptosis were measured by fluorometric methods and enzyme-linked immunosorbent assay.Gallic acid significantly decreased oral squamous cell carcinoma cell viability in a dose- and time-dependent manner. The expression of PI3K, AKT, and mTOR genes and proteins was decreased, while PTEN expression was increased. Also, the increase in Bax expression and caspase activity indicated a strong induction of apoptosis by gallic acid.Gallic acid exhibits significant anticancer effects in oral squamous cell carcinoma cells by inhibiting the PI3K/AKT/mTOR pathway and activating apoptotic pathways. This natural compound may contribute to the development of targeted therapies for oral cancer, pending further preclinical validation.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":"14-19"},"PeriodicalIF":2.1,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145631287","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Protective Effect of Boldine Against Diclofenac-Induced Renal Damage in Rats. 波定对双氯芬酸所致大鼠肾损伤的保护作用。

IF 2.1

Drug Research Pub Date : 2026-01-01 Epub Date: 2025-11-27 DOI: 10.1055/a-2749-3102

Luísa Nathália Bolda Mariano, Heloísa Roberti Cristofolini, Rita de Cássia Vilhena da Silva, Anelise Felício Macarini, Valdir Cechinel Filho, Priscila de Souza

{"title":"Protective Effect of Boldine Against Diclofenac-Induced Renal Damage in Rats.","authors":"Luísa Nathália Bolda Mariano, Heloísa Roberti Cristofolini, Rita de Cássia Vilhena da Silva, Anelise Felício Macarini, Valdir Cechinel Filho, Priscila de Souza","doi":"10.1055/a-2749-3102","DOIUrl":"10.1055/a-2749-3102","url":null,"abstract":"This study investigated the protective effect of alkaloid boldine against diclofenac-induced kidney damage in normotensive female rats. Animals were divided into three groups: naive, vehicle+diclofenac (50 mg/kg), and boldine+diclofenac (boldine 0.1 mg/kg+diclofenac 50 mg/kg). Treatments were administered orally once daily for 2 days. The vehicle+diclofenac group showed reduced urinary volume and sodium excretion. In contrast, the boldine+diclofenac group restored both parameters to levels similar to the naive group. Other urinary electrolytes indicated imbalance in diclofenac-treated animals, regardless of boldine co-treatment. Plasma analysis showed no alterations. Kidney tissue from diclofenac-treated groups revealed increased glutathione and decreased lipid hydroperoxides. Histology showed that vehicle+diclofenac resulted in a reduction in glomerular size, thickening of Bowman's capsule, and mesangial disarray, while these changes were less pronounced with boldine co-treatment. Molecular docking analysis indicated that boldine may interact with important proteins related to renal hemodynamics, sodium regulation, and inflammatory processes pointing to a multi-target mechanism. Boldine attenuated renal damage induced by diclofenac, improving urinary parameters and reducing histological alterations. Further studies are necessary to elucidate its protective mechanisms and impact on renal hemodynamics.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":"35-42"},"PeriodicalIF":2.1,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145631230","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

An In-Depth Exploration of Natural and Herbal Tooth Whitening Agents: Efficacy, Safety, and Clinical Applications. 天然和草药牙齿增白剂的深入探索：疗效、安全性和临床应用。

IF 2.1

Drug Research Pub Date : 2026-01-01 Epub Date: 2025-12-29 DOI: 10.1055/a-2762-7875

Sowmya Halasabalu Kalgeri, SunilKumar Bheemasamudra Balaraj, Vidya G Doddawad, Ashwini Tumkur Shivakumar, Deepa Basapur Vijayakumar, Parinitha Mysore Shankar

引用次数: 0

Investigating the Protective Role of Vitamin D Supplementation on Cyclophosphamide-Induced Liver Enzyme Alterations in Adult Male Rats. 研究补充维生素D对环磷酰胺诱导的成年雄性大鼠肝酶改变的保护作用。

IF 2.1

Drug Research Pub Date : 2026-01-01 Epub Date: 2025-11-25 DOI: 10.1055/a-2734-1920

Tania Nazem, Ali Hosseini-Sharifabad, Mohammad Reza Mofid, Mohammad Hashemnia, Habib-Allah Nazem, Adel Mohammadalipour

{"title":"Investigating the Protective Role of Vitamin D Supplementation on Cyclophosphamide-Induced Liver Enzyme Alterations in Adult Male Rats.","authors":"Tania Nazem, Ali Hosseini-Sharifabad, Mohammad Reza Mofid, Mohammad Hashemnia, Habib-Allah Nazem, Adel Mohammadalipour","doi":"10.1055/a-2734-1920","DOIUrl":"10.1055/a-2734-1920","url":null,"abstract":"Cyclophosphamide is known to cause liver dysfunction. This study investigated the protective role of vitamin D supplementation against cyclophosphamide -induced liver dysfunction in adult male rats. The rats receiving cyclophosphamide were treated with vitamin D at doses of 1,000 and 3,000 IU/kg. At the end of the study period, biochemical and histopathological evaluations were conducted after the animals were sacrificed. The levels of aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, lactate dehydrogenase, nitric oxide, and bilirubin were significantly elevated in the cyclophosphamide group compared to the control group (p<0.001). Conversely, these levels were significantly decreased in the vitamin D treatment groups (p<0.01). Additionally, the activities of the catalase and glutathione peroxidase were significantly lower in the cyclophosphamide group than in controls (p<0.01), while they increased significantly in the vitamin D groups (p<0.001). According to a semi-quantitative scoring system, the highest scores for pathological lesions were observed in the cyclophosphamide group, with lower scores in the vitamin D groups. The differences between the cyclophosphamide group and both treated groups were statistically significant (p<0.05). These results indicate that vitamin D, through its antioxidant properties, positively influenced liver enzyme levels altered by cyclophosphamide.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":"20-27"},"PeriodicalIF":2.1,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145603231","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Correction: Treatment of K562 Cells with ABL Kinase Inhibitors Reveals Differential Metabolic Profiles. 更正：用ABL激酶抑制剂治疗K562细胞揭示了不同的代谢特征。

IF 2.1

Drug Research Pub Date : 2026-01-01 Epub Date: 2026-02-11 DOI: 10.1055/a-2798-3571

Pranay Renukuntla, Sai Charitha Mullaguri, Divya Presingu, Rama Krishna Kancha, Jagadeshwar Reddy Thota

引用次数: 0

Anticancer Activity of Alectinib through Hydroxypropyl-β-Cyclodextrin Complexation: In Vitro Evaluation on A549 Lung Cancer Cells. 羟丙基-β-环糊精络合Alectinib抗癌活性：对A549肺癌细胞的体外评价

IF 2.1

Drug Research Pub Date : 2026-01-01 Epub Date: 2025-12-29 DOI: 10.1055/a-2764-8938

Muathe Najim, Israa Al-Ani, Ibraheem Al-Deeb, Bashar J M Majeed, Tha'er Ata, Enass Daoud

{"title":"Anticancer Activity of Alectinib through Hydroxypropyl-β-Cyclodextrin Complexation: In Vitro Evaluation on A549 Lung Cancer Cells.","authors":"Muathe Najim, Israa Al-Ani, Ibraheem Al-Deeb, Bashar J M Majeed, Tha'er Ata, Enass Daoud","doi":"10.1055/a-2764-8938","DOIUrl":"10.1055/a-2764-8938","url":null,"abstract":"Alectinib is an effective inhibitor of anaplastic lymphoma kinase utilized in the treatment of anaplastic lymphoma kinase-positive non-small-cell lung cancer. Nonetheless, its limited solubility in water restricts its therapeutic effectiveness. This research seeks to improve the anticancer efficacy of alectinib through the formation of an inclusion complex with hydroxypro-pyl-β-cyclodextrin. The alectinib-hydroxypro-pyl-β-cyclodextrin complex was synthesized via the kneading method and characterized according to established studies. In vitro assays, such as cell viability (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay), colony formation, scratch wound healing, and tube formation assays, were conducted to assess the antiproliferative, antimigratory, and antiangiogenic activities of the complex in comparison to free alectinib. The alectinib-hydroxypro-pyl-β-cyclodextrin complex exhibited markedly increased cy-totoxicity, diminished colony formation, inhibited cell migration, and impaired tube formation compared to free alectinib. The findings indicate that hydroxypro-pyl-β-cyclodextrin complexation enhances the solubility and anticancer efficacy of alectinib, presenting a viable strategy for improving its therapeutic potential in the treatment of non-small-cell lung cancer. Alectinib, in conjunction with hydroxypropyl-β-cyclodextrin, was evaluated for its effects on A549 cells, which are representative of non-small-cell lung cancer. This study focused on its anticancer activity and its influence on cell migration. Angiogenesis refers to the physiological process through which new blood vessels form from pre-existing vessels.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":"28-34"},"PeriodicalIF":2.1,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145854871","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Evaluation of the Migrastatic Properties of Selective MMP-2 Inhibitors in Colorectal Cancer: An In Ovo Approach. 评价选择性MMP-2抑制剂在结直肠癌中的迁移特性：一种卵内方法。

IF 2.1

Drug Research Pub Date : 2026-01-01 Epub Date: 2025-11-28 DOI: 10.1055/a-2724-6878

Nikunj Parekh, Mansi Patel, Praysha Patel, Disha Patel, Kirtan Patel, Krishna Thakkar, Aarti Parmar, Umang Shah, Sahil Panjvani, Samir Patel, Alkeshkumar Kiritbhai Patel

{"title":"Evaluation of the Migrastatic Properties of Selective MMP-2 Inhibitors in Colorectal Cancer: An In Ovo Approach.","authors":"Nikunj Parekh, Mansi Patel, Praysha Patel, Disha Patel, Kirtan Patel, Krishna Thakkar, Aarti Parmar, Umang Shah, Sahil Panjvani, Samir Patel, Alkeshkumar Kiritbhai Patel","doi":"10.1055/a-2724-6878","DOIUrl":"10.1055/a-2724-6878","url":null,"abstract":"Colorectal cancer accounts for about 10% of all cancer diagnoses and is the second leading cause of cancer-related death. Until the cancer has progressed to an advanced stage, colorectal cancer typically shows no symptoms. The medications currently utilized to treat colorectal cancer have serious drawbacks. The aim of the study was to evaluate the ability of newly developed synthetic matrix metalloprotease-2 inhibitors to prevent metastases. This study used computational models to evaluate pharmacokinetic characteristics and ligand-binding affinities for preliminary screening. Later, we used the human colorectal cancer cell line SW620 in an in ovo approach to assess its anti-migratory properties. The chorioallantoic membrane was used to transplant tumor cells. In order to assess migrastatic activity in a preclinical model using an in ovo technique, we measured changes in the chick embryo's total body weight, colon length and body weight, complete blood count and histopathology of the colon, liver and stomach. In addition, the histology of the stomach, liver, colon, and chorioallantoic membrane was taken into account while assessing the activity. We discovered that compound N5 ({4-[(3'-amino[1,1'-biphenyl]-4-carbonyl) amino] phenyl~acetic acid) had the best migrastatic action by blocking matrix metalloprotease-2. The new compound showed potential as a matrix metalloprotease-2 inhibitor compared to doxycycline. A more robust platform was needed for further investigation and progress of novel compound towards clinical setting.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":"5-13"},"PeriodicalIF":2.1,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145631251","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0