Pharmacological Reports最新文献

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Cannabidiol (CBD) modulates the serotonin-kynurenine metabolic balance in the brain of morphine-tolerant neuropathic rats. 大麻二酚(CBD)调节吗啡耐受神经病大鼠大脑中血清素-犬尿氨酸代谢平衡。
IF 3.8 3区 医学
Pharmacological Reports Pub Date : 2026-03-24 DOI: 10.1007/s43440-026-00850-w
Sofia Nasini, Leora Pearl-Dowler, Martha Lopez-Canul, Luca Posa, Antonella Bertazzo, Gabriella Gobbi, Stefano Comai
{"title":"Cannabidiol (CBD) modulates the serotonin-kynurenine metabolic balance in the brain of morphine-tolerant neuropathic rats.","authors":"Sofia Nasini, Leora Pearl-Dowler, Martha Lopez-Canul, Luca Posa, Antonella Bertazzo, Gabriella Gobbi, Stefano Comai","doi":"10.1007/s43440-026-00850-w","DOIUrl":"https://doi.org/10.1007/s43440-026-00850-w","url":null,"abstract":"","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":""},"PeriodicalIF":3.8,"publicationDate":"2026-03-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147513915","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery of a tetrazole-thiourea derivative as a potential active agent against multidrug-resistant Staphylococcus aureus and Mycobacterium tuberculosis. 发现一种四唑-硫脲衍生物作为抗耐多药金黄色葡萄球菌和结核分枝杆菌的潜在活性剂。
IF 3.8 3区 医学
Pharmacological Reports Pub Date : 2026-03-19 DOI: 10.1007/s43440-026-00848-4
Jolanta Szymańska-Majchrzak, Agnieszka Głogowska, Ewa Augustynowicz-Kopeć, Katarzyna Ewa Greber, Krzesimir Ciura, Wioletta Olejarz, Tomasz Szostek, Marta Struga, Daniel Szulczyk
{"title":"Discovery of a tetrazole-thiourea derivative as a potential active agent against multidrug-resistant Staphylococcus aureus and Mycobacterium tuberculosis.","authors":"Jolanta Szymańska-Majchrzak, Agnieszka Głogowska, Ewa Augustynowicz-Kopeć, Katarzyna Ewa Greber, Krzesimir Ciura, Wioletta Olejarz, Tomasz Szostek, Marta Struga, Daniel Szulczyk","doi":"10.1007/s43440-026-00848-4","DOIUrl":"https://doi.org/10.1007/s43440-026-00848-4","url":null,"abstract":"","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":""},"PeriodicalIF":3.8,"publicationDate":"2026-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147487009","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Hybrids of harmine and quinoline-based antimalarials show a strong antiproliferative effect on glioblastoma cells and reverse ATP-binding cassette transporter-mediated drug resistance. 以甘草碱和喹啉为基础的抗疟药杂交种对胶质母细胞瘤细胞具有较强的抗增殖作用,并能逆转atp结合盒转运体介导的耐药性。
IF 3.8 3区 医学
Pharmacological Reports Pub Date : 2026-03-17 DOI: 10.1007/s43440-026-00849-3
Marija Mioč, Kristina Pavić, Goran Poje, Zrinka Rajić, Marijeta Kralj
{"title":"Hybrids of harmine and quinoline-based antimalarials show a strong antiproliferative effect on glioblastoma cells and reverse ATP-binding cassette transporter-mediated drug resistance.","authors":"Marija Mioč, Kristina Pavić, Goran Poje, Zrinka Rajić, Marijeta Kralj","doi":"10.1007/s43440-026-00849-3","DOIUrl":"https://doi.org/10.1007/s43440-026-00849-3","url":null,"abstract":"","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":""},"PeriodicalIF":3.8,"publicationDate":"2026-03-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147474960","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
CC8, a heterodimeric disintegrin from Cerastes cerastes snake venom, triggers apoptosis and restrains the dissemination of human glioblastoma cells. CC8是一种异二聚体崩解素,来自于cerecastae蛇毒,可引发细胞凋亡并抑制人类胶质母细胞瘤细胞的传播。
IF 3.8 3区 医学
Pharmacological Reports Pub Date : 2026-03-11 DOI: 10.1007/s43440-026-00846-6
Maram Morjen, Khaoula Smati, Cyrine Souissi, Sahar Ben Lamine, Mbarka Barmet, Aurelie Chantome, Marie Potier-Cartereau, Christophe Vandier, Najet Srairi-Abid, Naziha Marrakchi, Jed Jebali
{"title":"CC8, a heterodimeric disintegrin from Cerastes cerastes snake venom, triggers apoptosis and restrains the dissemination of human glioblastoma cells.","authors":"Maram Morjen, Khaoula Smati, Cyrine Souissi, Sahar Ben Lamine, Mbarka Barmet, Aurelie Chantome, Marie Potier-Cartereau, Christophe Vandier, Najet Srairi-Abid, Naziha Marrakchi, Jed Jebali","doi":"10.1007/s43440-026-00846-6","DOIUrl":"https://doi.org/10.1007/s43440-026-00846-6","url":null,"abstract":"<p><strong>Background: </strong>Glioblastoma (GBM) is the most aggressive and frequent primary malignant brain tumor and remains highly resistant to existing therapies. Snake-venom disintegrins possess potent anticancer activities, yet their pharmacological potential against GBM is not fully explored. In this work, we aimed to evaluate the therapeutic potential of the disintegrin CC8 from Cerastes cerastes snake venom, toward the development of a novel anti-GBM drug.</p><p><strong>Methods: </strong>The effects of CC8 on the viability and proliferation of human GBM cell lines U87, U251, LN229, and LN18 were assessed using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and crystal violet assays. Apoptosis induction was examined by annexin V-fluorescein isothiocyanate (FITC)/propidium iodide (PI) staining and reverse transcription-quantitative polymerase chain reaction (RT-qPCR) analysis of pro- and anti-apoptotic gene expression. The effect of CC8 on cell-extracellular matrix (ECM) interactions was evaluated through adhesion assays and integrin-blocking antibodies. GBM cell infiltration potential was further explored using cell invasion assays and spheroid-based migration models.</p><p><strong>Results: </strong>CC8 significantly reduced the viability of U87, LN18, and LN229 cells and inhibited the proliferation of U87, whereas U251 cells showed resistance up to 200 nM. CC8 induced caspase-dependent apoptosis, as evidenced by downregulation of BCL2 apoptosis regulator (BCL2) and upregulation of BCL2-associated X, apoptosis regulator (BAX), caspase 3 (CASP3), and caspase 8 (CASP8) expression. CC8 also disrupted cell adhesion to fibrinogen (Fg) and fibronectin (Fn) through integrin interference. Furthermore, it markedly decreased GBM cell invasion and reduced U87 spheroid migration.</p><p><strong>Conclusions: </strong>These findings identify CC8 as a promising venom-derived candidate for GBM drug development, with potential to improve therapeutic outcomes for this aggressive and treatment-resistant cancer.</p><p><strong>Clinical trial number: </strong>Not applicable.</p>","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":""},"PeriodicalIF":3.8,"publicationDate":"2026-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147433671","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The effect of salidroside, an active component of Rhodiola rosea, on the metabolic activity of rat and human cytochromes P450 in preclinical studies. 红景天有效成分红景天苷对大鼠和人细胞色素P450代谢活性的影响。
IF 3.8 3区 医学
Pharmacological Reports Pub Date : 2026-03-11 DOI: 10.1007/s43440-026-00842-w
Eva Klaskova, Jan Jurica, Przemysław Jan Danek, Natalie Mlcuchova, Saltuk Mustafa Eyrilmez, Petra Borilova Linhartova, David Bednar, Rajamanikkam Kamaraj, Władysława Anna Daniel, Ondrej Zendulka
{"title":"The effect of salidroside, an active component of Rhodiola rosea, on the metabolic activity of rat and human cytochromes P450 in preclinical studies.","authors":"Eva Klaskova, Jan Jurica, Przemysław Jan Danek, Natalie Mlcuchova, Saltuk Mustafa Eyrilmez, Petra Borilova Linhartova, David Bednar, Rajamanikkam Kamaraj, Władysława Anna Daniel, Ondrej Zendulka","doi":"10.1007/s43440-026-00842-w","DOIUrl":"https://doi.org/10.1007/s43440-026-00842-w","url":null,"abstract":"","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":""},"PeriodicalIF":3.8,"publicationDate":"2026-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147434115","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Ketamine for comorbid treatment-resistant depression and substance use disorders: balancing risks and opportunities. 氯胺酮治疗共病难治性抑郁症和物质使用障碍:平衡风险和机会。
IF 3.8 3区 医学
Pharmacological Reports Pub Date : 2026-03-11 DOI: 10.1007/s43440-026-00843-9
Benjamin D Brody, Dora Kanellopoulos
{"title":"Ketamine for comorbid treatment-resistant depression and substance use disorders: balancing risks and opportunities.","authors":"Benjamin D Brody, Dora Kanellopoulos","doi":"10.1007/s43440-026-00843-9","DOIUrl":"https://doi.org/10.1007/s43440-026-00843-9","url":null,"abstract":"","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":""},"PeriodicalIF":3.8,"publicationDate":"2026-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147434100","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
New molecules candidates with a semicarbazide scaffold - anticancer potential in view of research on their physicochemical properties, antioxidant activity, and preliminary biological activity. 从物理化学性质、抗氧化活性和初步生物活性的研究来看,具有缩氨基脲支架的新候选分子具有抗癌潜力。
IF 3.8 3区 医学
Pharmacological Reports Pub Date : 2026-03-05 DOI: 10.1007/s43440-026-00844-8
Łucja Justyna Walczak, Marta Arczewska, Zbigniew Karczmarzyk, Monika Gawrońska-Grzywacz, Agnieszka Wieleba, Daniel Kamiński, Monika Pitucha, Waldemar Wysocki, Mariola Herbet
{"title":"New molecules candidates with a semicarbazide scaffold - anticancer potential in view of research on their physicochemical properties, antioxidant activity, and preliminary biological activity.","authors":"Łucja Justyna Walczak, Marta Arczewska, Zbigniew Karczmarzyk, Monika Gawrońska-Grzywacz, Agnieszka Wieleba, Daniel Kamiński, Monika Pitucha, Waldemar Wysocki, Mariola Herbet","doi":"10.1007/s43440-026-00844-8","DOIUrl":"https://doi.org/10.1007/s43440-026-00844-8","url":null,"abstract":"","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":""},"PeriodicalIF":3.8,"publicationDate":"2026-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147355750","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Isoxazole derivatives as multi-target agents: virucidal, antibacterial, and antiproliferative effects on skin cancer cells. 异恶唑衍生物作为多靶点药物:对皮肤癌细胞的杀毒、抗菌和抗增殖作用。
IF 3.8 3区 医学
Pharmacological Reports Pub Date : 2026-03-04 DOI: 10.1007/s43440-026-00839-5
Izabela Jęśkowiak-Kossakowska, Paulina Nowotarska, Elżbieta Gębarowska, Barbara Bażanów, Tomasz Gębarowski, Roman Szafran, Aleksandra Chwirot, Edward Krzyżak, Adam Szeląg, Marcin Mączyński, Maciej Janeczek, Benita Wiatrak
{"title":"Isoxazole derivatives as multi-target agents: virucidal, antibacterial, and antiproliferative effects on skin cancer cells.","authors":"Izabela Jęśkowiak-Kossakowska, Paulina Nowotarska, Elżbieta Gębarowska, Barbara Bażanów, Tomasz Gębarowski, Roman Szafran, Aleksandra Chwirot, Edward Krzyżak, Adam Szeląg, Marcin Mączyński, Maciej Janeczek, Benita Wiatrak","doi":"10.1007/s43440-026-00839-5","DOIUrl":"https://doi.org/10.1007/s43440-026-00839-5","url":null,"abstract":"<p><strong>Background: </strong>The convergence of microbial infections and cancer risk in inflammatory skin diseases demands novel, multi-functional therapeutics. This challenge is exacerbated by the rise in antimicrobial resistance and the lack of approved drugs for pathogens like human adenovirus (HAdV).</p><p><strong>Methods: </strong>Here, we investigated a series of isoxazole derivatives to identify lead candidates with combined antibacterial, antiviral, and anticancer properties for dermatological applications. The tests performed include antibacterial agar diffusion assay, antiviral quantitative suspension test, in silico and in vitro assays such as MTT, Rho-123, DCF-DA, Griess, as well as ELISA tests (Caspase-3, IL-6, TNF-α, COX), and detection of apoptosis in a microchip.</p><p><strong>Results: </strong>Our study identified compound MO3 with significant antibacterial action against Staphylococcus aureus and the zoonotic pathogen Staphylococcus pseudintermedius. In antiviral assays, MO10 and MO7 demonstrated exceptionally high virucidal potency against HSV-1 (100-fold greater than the threshold) and AdV-5 (10-fold greater than the threshold), respectively, while remaining non-toxic to human fibroblasts. Critically, MO10 also exhibited multi-modal anticancer effects in melanoma, inducing NO-mediated apoptosis, reducing pro-inflammatory cytokines, and acting in strong synergy with doxorubicin to enhance its chemotherapeutic effect.</p><p><strong>Conclusion: </strong>In conclusion, this work validates specific isoxazole derivatives as highly promising candidates for development: MO3 for resistant bacterial infections, MO7 for otherwise untreatable adenovirus infections, and MO10 as a dual-action agent against HSV-1 and an adjunct to melanoma chemotherapy.</p>","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":""},"PeriodicalIF":3.8,"publicationDate":"2026-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147355801","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Propafenone-mediated gap junctional uncoupling results from aberrant connexin-43 trafficking. 普罗帕酮介导的间隙连接解耦是由异常连接蛋白-43贩运引起的。
IF 3.8 3区 医学
Pharmacological Reports Pub Date : 2026-03-02 DOI: 10.1007/s43440-026-00845-7
Encan Li, Najla Boujeddaine, Britt Mol, Emmy Penning de Vries, Marcel A G van der Heyden
{"title":"Propafenone-mediated gap junctional uncoupling results from aberrant connexin-43 trafficking.","authors":"Encan Li, Najla Boujeddaine, Britt Mol, Emmy Penning de Vries, Marcel A G van der Heyden","doi":"10.1007/s43440-026-00845-7","DOIUrl":"https://doi.org/10.1007/s43440-026-00845-7","url":null,"abstract":"","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":""},"PeriodicalIF":3.8,"publicationDate":"2026-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147326637","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Achieving target plasma concentrations of beta-lactam antibiotics in critically ill patients: a retrospective study of full-dose administration in the first 24 hours. 实现危重患者β -内酰胺类抗生素的目标血浆浓度:最初24小时全剂量给药的回顾性研究
IF 3.8 3区 医学
Pharmacological Reports Pub Date : 2026-02-25 DOI: 10.1007/s43440-026-00836-8
Milada Halačová, Marie Mieresová, Jan Kubele, Eva Klapková, Dalibor Černý, Petr Waldauf, František Duška
{"title":"Achieving target plasma concentrations of beta-lactam antibiotics in critically ill patients: a retrospective study of full-dose administration in the first 24 hours.","authors":"Milada Halačová, Marie Mieresová, Jan Kubele, Eva Klapková, Dalibor Černý, Petr Waldauf, František Duška","doi":"10.1007/s43440-026-00836-8","DOIUrl":"https://doi.org/10.1007/s43440-026-00836-8","url":null,"abstract":"","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":""},"PeriodicalIF":3.8,"publicationDate":"2026-02-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147284305","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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