Pharmacological Reports最新文献_第10页

Novel method of measurement of in vitro drug uptake in OATP1B3 overexpressing cells in the presence of dextran. 在存在葡聚糖的情况下测量 OATP1B3 过表达细胞体外药物吸收的新方法。

IF 4.4 3区医学

Pharmacological Reports Pub Date : 2024-04-01 Epub Date: 2024-03-26 DOI: 10.1007/s43440-024-00583-8

Anna Kowal-Chwast, Ewelina Gabor-Worwa, Nilesh Gaud, Dawid Gogola, Agnieszka Piątek, Adrian Zarębski, Peter Littlewood, Marek Smoluch, Krzysztof Brzózka, Kamil Kuś

{"title":"Novel method of measurement of in vitro drug uptake in OATP1B3 overexpressing cells in the presence of dextran.","authors":"Anna Kowal-Chwast, Ewelina Gabor-Worwa, Nilesh Gaud, Dawid Gogola, Agnieszka Piątek, Adrian Zarębski, Peter Littlewood, Marek Smoluch, Krzysztof Brzózka, Kamil Kuś","doi":"10.1007/s43440-024-00583-8","DOIUrl":"10.1007/s43440-024-00583-8","url":null,"abstract":"Background: In predictions about hepatic clearance (CLH), a number of studies explored the role of albumin and transporters in drug uptake by liver cells, challenging the traditional free-drug theory. It was proposed that liver uptake can occur for transporter substrate compounds not only from the drug's unbound form but also directly from the drug-albumin complex, a phenomenon known as uptake facilitated by albumin. In contrast to albumin, dextran does not exhibit binding properties for compounds. However, as a result of its inherent capacity for stabilization, it is widely used to mimic conditions within cells.Methods: The uptake of eight known substrates of the organic anion-transporting polypeptide 1B3 (OATP1B3) was assessed using a human embryonic kidney cell line (HEK293), which stably overexpresses this transporter. An inert polymer, dextran, was used to simulate cellular conditions, and the results were compared with experiments involving human plasma and human serum albumin (HSA).Results: This study is the first to demonstrate that dextran increases compound uptake in cells with overexpression of the OATP1B3 transporter. Contrary to the common theory that highly protein-bound ligands interact with hepatocytes to increase drug uptake, the results indicate that dextran's interaction with test compounds does not significantly increase concentrations near the cell membrane surface.Conclusions: We evaluated the effect of dextran on the uptake of known substrates using OATP1B3 overexpressed in the HEK293 cell line, and we suggest that its impact on drug concentrations in liver cells may differ from the traditional role of plasma proteins and albumin.","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":"400-415"},"PeriodicalIF":4.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140294259","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

Further proof on the role of accumbal nNOS in cocaine-seeking behavior in rats. 进一步证明蓄积性 nNOS 在大鼠可卡因寻求行为中的作用。

IF 4.4 3区医学

Pharmacological Reports Pub Date : 2024-04-01 Epub Date: 2024-03-14 DOI: 10.1007/s43440-024-00571-y

Małgorzata Frankowska, Irena Smaga, Kinga Gawlińska, Renata Pieniążek, Małgorzata Filip

{"title":"Further proof on the role of accumbal nNOS in cocaine-seeking behavior in rats.","authors":"Małgorzata Frankowska, Irena Smaga, Kinga Gawlińska, Renata Pieniążek, Małgorzata Filip","doi":"10.1007/s43440-024-00571-y","DOIUrl":"10.1007/s43440-024-00571-y","url":null,"abstract":"Background: Cocaine use disorder (CUD) remains a severe health problem with no effective pharmacological therapy. One of the potential pharmacological strategies for CUD pharmacotherapy includes manipulations of the brain glutamatergic (Glu) system which is particularly involved in drug withdrawal and relapse. Previous research indicated a pivotal role of ionotropic N-methyl-D-aspartate (NMDA) receptors or metabotropic receptors' type 5 (mGlu5) receptors in controlling the reinstatement of cocaine. Stimulation of the above molecules results in the activation of the downstream signaling targets such as neuronal nitric oxide synthase (nNOS) and the release of nitric oxide.Methods: In this paper, we investigated the molecular changes in nNOS in the prefrontal cortex and nucleus accumbens following 3 and 10 days of cocaine abstinence as well as the effectiveness of nNOS blockade with the selective enzyme inhibitor N-ω-propyl-L-arginine hydrochloride (L-NPA) on cocaine seeking in male rats. The effect of L-NPA on locomotor activity in drug-naïve animals was investigated.Results: Ten-day (but not 3-day) cocaine abstinence from cocaine self-administration increased nNOS gene and protein expression in the nucleus accumbens, but not in the prefrontal cortex. L-NPA (0.5-5 mg/kg) administered peripherally did not change locomotor activity but attenuated the reinstatement induced with cocaine priming or the drug-associated conditioned cue.Conclusions: Our findings support accumbal nNOS as an important molecular player for cocaine seeking while its inhibitors could be considered as anti-cocaine pharmacological tools in male rats.","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":"338-347"},"PeriodicalIF":4.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140120322","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

Diagnostic, prognostic, and therapeutic potential of exosomal microRNAs in renal cancer. 肾癌外泌体 microRNA 的诊断、预后和治疗潜力。

IF 4.4 3区医学

Pharmacological Reports Pub Date : 2024-04-01 Epub Date: 2024-02-22 DOI: 10.1007/s43440-024-00568-7

Xiaodong Yu, Zhongbo Du, Pingyu Zhu, Bo Liao

{"title":"Diagnostic, prognostic, and therapeutic potential of exosomal microRNAs in renal cancer.","authors":"Xiaodong Yu, Zhongbo Du, Pingyu Zhu, Bo Liao","doi":"10.1007/s43440-024-00568-7","DOIUrl":"10.1007/s43440-024-00568-7","url":null,"abstract":"Renal cell carcinoma (RCC) arises from the tubular epithelial cells of the nephron. It has the highest mortality rate among urological cancers. There are no effective therapeutic approaches and no non-invasive biomarkers for diagnosis and follow-up. Thus, suitable novel biomarkers and therapeutic targets are essential for improving RCC diagnosis/prognosis and treatment. Circulating exosomes such as exosomal microRNAs (Exo-miRs) provide non-invasive prognostic/diagnostic biomarkers and valuable therapeutic targets, as they can be easily isolated and quantified and show high sensitivity and specificity. Exosomes secreted by an RCC can exhibit alterations in the miRs' profile that may reflect the cellular origin and (patho)physiological state, as a ''signature'' or ''fingerprint'' of the donor cell. It has been shown that the transportation of renal-specific miRs in exosomes can be rapidly detected and measured, holding great potential as biomarkers in RCC. The present review highlights the studies reporting tumor microenvironment-derived Exo-miRs with therapeutic potential as well as circulating Exo-miRs as potential diagnostic/prognostic biomarkers in patients with RCC.","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":"273-286"},"PeriodicalIF":4.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139932377","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 protective effects of statins in traumatic brain injury. 他汀类药物对创伤性脑损伤的保护作用。

IF 4.4 3区医学

Pharmacological Reports Pub Date : 2024-04-01 Epub Date: 2024-03-07 DOI: 10.1007/s43440-024-00582-9

Safoora Pordel, Alice P McCloskey, Wael Almahmeed, Amirhossein Sahebkar

{"title":"The protective effects of statins in traumatic brain injury.","authors":"Safoora Pordel, Alice P McCloskey, Wael Almahmeed, Amirhossein Sahebkar","doi":"10.1007/s43440-024-00582-9","DOIUrl":"10.1007/s43440-024-00582-9","url":null,"abstract":"Traumatic brain injury (TBI), often referred to as the \"silent epidemic\", is the most common cause of mortality and morbidity worldwide among all trauma-related injuries. It is associated with considerable personal, medical, and economic consequences. Although remarkable advances in therapeutic approaches have been made, current treatments and clinical management for TBI recovery still remain to be improved. One of the factors that may contribute to this gap is that existing therapies target only a single event or pathology. However, brain injury after TBI involves various pathological mechanisms, including inflammation, oxidative stress, blood-brain barrier (BBB) disruption, ionic disturbance, excitotoxicity, mitochondrial dysfunction, neuronal necrosis, and apoptosis. Statins have several beneficial pleiotropic effects (anti-excitotoxicity, anti-inflammatory, anti-oxidant, anti-thrombotic, immunomodulatory activity, endothelial and vasoactive properties) in addition to promoting angiogenesis, neurogenesis, and synaptogenesis in TBI. Supposedly, using agents such as statins that target numerous and diverse pathological mechanisms, may be more effective than a single-target approach in TBI management. The current review was undertaken to investigate and summarize the protective mechanisms of statins against TBI. The limitations of conducted studies and directions for future research on this potential therapeutic application of statins are also discussed.","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":"235-250"},"PeriodicalIF":4.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140050079","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

Cannabinoids in the treatment of glioblastoma. 治疗胶质母细胞瘤的大麻素。

IF 4.4 3区医学

Pharmacological Reports Pub Date : 2024-04-01 Epub Date: 2024-03-08 DOI: 10.1007/s43440-024-00580-x

Barbara Buchalska, Katarzyna Kamińska, Maja Owe-Larsson, Agnieszka Cudnoch-Jędrzejewska

{"title":"Cannabinoids in the treatment of glioblastoma.","authors":"Barbara Buchalska, Katarzyna Kamińska, Maja Owe-Larsson, Agnieszka Cudnoch-Jędrzejewska","doi":"10.1007/s43440-024-00580-x","DOIUrl":"10.1007/s43440-024-00580-x","url":null,"abstract":"Glioblastoma (GBM) is the most prevalent primary malignant tumor of the nervous system. While the treatment of other neoplasms is increasingly more efficacious the median survival rate of GBM patients remains low and equals about 14 months. Due to this fact, there are intensive efforts to find drugs that would help combat GBM. Nowadays cannabinoids are becoming more and more important in the field of cancer and not only because of their properties of antiemetic drugs during chemotherapy. These compounds may have a direct cytotoxic effect on cancer cells. Studies indicate GBM has disturbances in the endocannabinoid system-changes in cannabinoid metabolism as well as in the cannabinoid receptor expression. The GBM cells show expression of cannabinoid receptors 1 and 2 (CB1R and CB2R), which mediate various actions of cannabinoids. Through these receptors, cannabinoids inhibit the proliferation and invasion of GBM cells, along with changing their morphology. Cannabinoids also induce an intrinsic pathway of apoptosis in the tumor. Hence the use of cannabinoids in the treatment of GBM may be beneficial to the patients. So far, studies focusing on using cannabinoids in GBM therapy are mainly preclinical and involve cell lines and mice. The results are promising and show cannabinoids inhibit GBM growth. Several clinical studies are also being carried out. The preliminary results show good tolerance of cannabinoids and prolonged survival after administration of these drugs. In this review, we describe the impact of cannabinoids on GBM and glioma cells in vitro and in animal studies. We also provide overview of clinical trials on using cannabinoids in the treatment of GBM.","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":"223-234"},"PeriodicalIF":4.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140060168","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

Mechanisms of norcantharidin against renal tubulointerstitial fibrosis. 去甲斑蝥素抗肾小管间质纤维化的机制

IF 4.4 3区医学

Pharmacological Reports Pub Date : 2024-04-01 Epub Date: 2024-03-12 DOI: 10.1007/s43440-024-00578-5

Qin-Su Yun, Yu-Xin Bao, Jie-Bing Jiang, Qian Guo

引用次数: 0

The study of platelet aggregation using a microtiter plate reader ‒ methodological considerations. 使用微孔板阅读器研究血小板聚集--方法上的考虑。

IF 4.4 3区医学

Pharmacological Reports Pub Date : 2024-04-01 Epub Date: 2024-03-05 DOI: 10.1007/s43440-024-00576-7

Magdalena Boncler, Jacek Golański

引用次数: 0

Ginsenoside Rg5 as an anticancer drug: a comprehensive review on mechanisms, structure-activity relationship, and prospects for clinical advancement. 作为抗癌药物的人参皂苷 Rg5：关于机理、结构-活性关系和临床应用前景的全面综述。

IF 4.4 3区医学

Pharmacological Reports Pub Date : 2024-04-01 Epub Date: 2024-03-25 DOI: 10.1007/s43440-024-00586-5

Tilal Elsaman, Ali Mahmoud Muddathir, Ebtihal A M Mohieldin, Irmanida Batubara, Min Rahminiwati, Kosei Yamauchi, Magdi Awadalla Mohamed, Shadila Fira Asoka, Dietrich Büsselberg, Solomon Habtemariam, Javad Sharifi-Rad

{"title":"Ginsenoside Rg5 as an anticancer drug: a comprehensive review on mechanisms, structure-activity relationship, and prospects for clinical advancement.","authors":"Tilal Elsaman, Ali Mahmoud Muddathir, Ebtihal A M Mohieldin, Irmanida Batubara, Min Rahminiwati, Kosei Yamauchi, Magdi Awadalla Mohamed, Shadila Fira Asoka, Dietrich Büsselberg, Solomon Habtemariam, Javad Sharifi-Rad","doi":"10.1007/s43440-024-00586-5","DOIUrl":"10.1007/s43440-024-00586-5","url":null,"abstract":"Cancer remains one of the leading causes of death in the world. Despite the considerable success of conventional treatment strategies, the incidence and mortality rates are still high, making developing new effective anticancer therapies an urgent priority. Ginsenoside Rg5 (Rg5) is a minor ginsenoside constituent obtained exclusively from ginseng species and is known for its broad spectrum of pharmacological activities. This article aimed to comprehensively review the anticancer properties of Rg5, focusing on action mechanisms, structure-activity relationship (SAR), and pharmacokinetics attributes. The in vitro and in vivo activities of Rg5 have been proven against several cancer types, such as breast, liver, lung, bone, and gastrointestinal (GI) cancers. The modulation of multiple signaling pathways critical for cancer growth and survival mediates these activities. Nevertheless, human clinical studies of Rg5 have not been addressed before, and there is still considerable ambiguity regarding its pharmacokinetics properties. In addition, a significant shortage in the structure-activity relationship (SAR) of Rg5 has been identified. Therefore, future efforts should focus on further optimization by performing extensive SAR studies to uncover the structural features essential for the potent anticancer activity of Rg5. Thus, this review highlights the value of Rg5 as a potential anticancer drug candidate and identifies the research areas requiring more investigation.","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":" ","pages":"287-306"},"PeriodicalIF":4.4,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140288748","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

Migraine and the microbiota. Can probiotics be beneficial in its prevention? - a narrative review 偏头痛与微生物群。益生菌对偏头痛的预防有益吗？- 综述

IF 4.4 3区医学

Pharmacological Reports Pub Date : 2024-03-19 DOI: 10.1007/s43440-024-00584-7

Aneta Kiecka, Marian Szczepanik

引用次数: 0

Effect of polyphenols against complications of COVID-19: current evidence and potential efficacy 多酚对 COVID-19 并发症的影响：现有证据和潜在疗效

IF 4.4 3区医学

Pharmacological Reports Pub Date : 2024-03-18 DOI: 10.1007/s43440-024-00585-6

Mahdi Vajdi, Arash Karimi, Shirin Hassanizadeh, Mahdieh Abbasalizad Farhangi, Mohammad Bagherniya, Gholamreza Askari, Basil D. Roufogalis, Neal M. Davies, Amirhossein Sahebkar

{"title":"Effect of polyphenols against complications of COVID-19: current evidence and potential efficacy","authors":"Mahdi Vajdi, Arash Karimi, Shirin Hassanizadeh, Mahdieh Abbasalizad Farhangi, Mohammad Bagherniya, Gholamreza Askari, Basil D. Roufogalis, Neal M. Davies, Amirhossein Sahebkar","doi":"10.1007/s43440-024-00585-6","DOIUrl":"https://doi.org/10.1007/s43440-024-00585-6","url":null,"abstract":"The COVID-19 pandemic that started in 2019 and resulted in significant morbidity and mortality continues to be a significant global health challenge, characterized by inflammation, oxidative stress, and immune system dysfunction.. Developing therapies for preventing or treating COVID-19 remains an important goal for pharmacology and drug development research. Polyphenols are effective against various viral infections and can be extracted and isolated from plants without losing their therapeutic potential. Researchers have developed methods for separating and isolating polyphenols from complex matrices. Polyphenols are effective in treating common viral infections, including COVID-19, and can also boost immunity. Polyphenolic-based antiviral medications can mitigate SARS-CoV-2 enzymes vital to virus replication and infection. Individual polyphenolic triterpenoids, flavonoids, anthraquinonoids, and tannins may also inhibit the SARS-CoV-2 protease. Polyphenol pharmacophore structures identified to date can explain their action and lead to the design of novel anti-COVID-19 compounds. Polyphenol-containing mixtures offer the advantages of a well-recognized safety profile with few known severe side effects. However, studies to date are limited, and further animal studies and randomized controlled trials are needed in future studies. The purpose of this study was to review and present the latest findings on the therapeutic impact of plant-derived polyphenols on COVID-19 infection and its complications. Exploring alternative approaches to traditional therapies could aid in developing novel drugs and remedies against coronavirus infection.","PeriodicalId":19947,"journal":{"name":"Pharmacological Reports","volume":"8 1","pages":""},"PeriodicalIF":4.4,"publicationDate":"2024-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140149810","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