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The role of astrocytic γ-aminobutyric acid in the action of inhalational anesthetics Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-12 Dongwook Won, Elliot H. Lee, Jee-Eun Chang, Min-Ho Nam, Ki Duk Park, Soo-Jin Oh, Jin-Young Hwang
Inhalational anesthetics target the inhibitory extrasynaptic γ-aminobutyric acid type A (GABA) receptors. Both neuronal and glial GABA mediate tonic inhibition of the extrasynaptic GABA receptors. However, the role of glial GABA during inhalational anesthesia remains unclear. This study aimed to evaluate whether astrocytic GABA contributes to the action of different inhalational anesthetics. Gene knockout
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Blocking of FGFR4 signaling by F30 inhibits hepatocellular carcinoma cell proliferation through HMOX1-dependent ferroptosis pathway Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-12 Fengyu Huang, Xueqin Shi, Meng Hu, Hang Yan, Xiaohui Li, Yujie Ding, Xinxin Zheng, Xiaojun Cai, Shijie Dai, Qinqin Xia, Yuepiao Cai
Excessive activation of FGF19/fibroblast growth factor receptor 4 (FGFR4) signaling is associated with poor survival of patients with hepatocellular carcinoma (HCC). FGFR4 inhibitors show promise for HCC treatment. F30, an indazole derivative designed through computer-aided drug design targeting FGFR4, demonstrated anti-HCC activity as described in our previous studies. However, the precise molecular
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Targeting oncogenic kinases: Insights on FDA approved tyrosine kinase inhibitors Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-11 Sahil Hussain, Mohd Mursal, Garima Verma, Syed Misbahul Hasan, Mohemmed Faraz Khan
Protein kinases play pivotal roles in various biological functions, influencing cell differentiation, promoting survival, and regulating the cell cycle. The disruption of protein kinase activity is intricately linked to pathways in tumor development. This manuscript explores the transformative impact of protein kinase inhibitors on cancer therapy, particularly their efficacy in cases driven by targeted
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Arglabin: A mediator of inflammasome modulated and independent myocardial injury (PARA-AMI study) Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-11 Khushboo Bisht, Vipin Kumar Verma, Zia Abdullah, Vaishali Prajapati, Narang Rajiv, Jagriti Bhatia, Ruma Ray, Tapas Chandra Nag, Dharamvir Singh Arya
Arglabin is a plant alkaloid (sesquiterpene lactone) that is used as an anticancer drug. It has potential anti-diabetic and anti-atherogenic effects. Arglabin, has drawn particular attention because of its therapeutic effects as an anti-inflammatory agent in multiple diseases. Since arglabin inhibits Epidermal Growth Factor Receptor (EGFR) tyrosine kinase, concerns for cardiotoxic effects are valid
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Activation of CaMKII/HDAC4 by SDF1 contributes to pulmonary arterial hypertension via stabilization Runx2 Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-11 Yuqian Chen, Jin Liu, Qianqian Zhang, Limin Chai, Huan Chen, Danyang Li, Yan Wang, Yuanjie Qiu, Nirui Shen, Jia Zhang, Qingting Wang, Jian Wang, Xinming Xie, Shaojun Li, Manxiang Li
Stromal derived factor 1 (SDF1) has been shown to be involved in the pathogenesis of pulmonary artery hypertension (PAH). However, the detailed molecular mechanisms remain unclear. To address this, we utilized primary cultured rat pulmonary artery smooth muscle cells (PASMCs) and monocrotaline (MCT)-induced PAH rat models to investigate the mechanisms of SDF1 driving PASMCs proliferation and pulmonary
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Pyroptosis in myocardial ischemia/reperfusion and its therapeutic implications Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-09 Yin Liu, Xi Li, Tingting Sun, Tao Li, Qian Li
Ischemic heart disease, a prevalent cardiovascular disease with global significance, is associated with substantial morbidity. Timely and successful reperfusion is crucial for reducing infarct size and enhancing clinical outcomes. However, reperfusion may induce additional myocardium injury, manifesting as myocardial ischemia/reperfusion (MI/R) injury. Pyroptosis is a regulated cell death pathway,
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Pogostone attenuated high-fat diet–induced nonalcoholic fatty liver disease in mice through inhibition of NLRP3 inflammasome signaling Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-09 Shengzhao Tang, Shangyi Huang, Jiaxin Huang, Xinger Lai, Jingyi Guo, Jiawen Huang, Yanhua Zhong
Inhibition of inflammasome activation is a potential therapeutic strategy for treating nonalcoholic fatty liver disease (NAFLD). Pogostone (PO), an active ingredient in Pogostemon cablin, exhibits various pharmacological properties, including anti-inflammation. However, there are no reports of the hepatoprotective effects of PO in NAFLD induced by a high-fat diet (HFD). Molecular biology methods and
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Retraction notice to “Evaluation of the treatment strategies on patient-derived xenograft mice of human breast tumor” [Eur. J. Pharmacol. 889 (2020) 173605] Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-07 Solmaz Khalighfard, Ali Mohammad Alizadeh, Amirhoushang Poorkhani, Mohammadmehdi Motahari, Arash Tahmasebifar, Ramesh Omranipour, Pedram Keshavarz, Peiman Haddad
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Retraction notice to “Enhancement of resistance to chemo-radiation by hsa-miR-1290 expression in glioblastoma cells” [Eur. J. Pharmacol. 880 (2020) 173144] Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-07 Solmaz Khalighfard, Mohammad Reza Kalhori, Peiman Haddad, Vahid Khori, Ali Mohammad Alizadeh
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Retraction notice to “Effects of salvianolic acid B on survival, self-renewal and neuronal differentiation of bone marrow derived neural stem cells” [Eur. J. Pharmacol. 697 (1–3) (2012) 32–39] Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-07 Nan Zhang, Tingguo Kang, Yang Xia, Qingping Wen, Xiaodan Zhang, Hongyan Li, Yv Hu, Haiguang Hao, Dan Zhao, Dong Sun, Yaping Yan, Guang-Xian Zhang, Jingxian Yang
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Role of sulfatide-reactive vNKT cells in promoting lung Treg cells via dendritic cell modulation in asthma models Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-07 Haiyang Ni, Qibin Lin, Jieying Zhong, Shaoding Gan, Hong Cheng, Yi Huang, Xuhong Ding, Hongying Yu, Yaqing Xu, Hanxiang Nie
Our previous studies have showed that sulfatide-reactive type II NKT (i.e. variant NKT, vNKT) cells inhibit the immunogenic maturation during the development of mature lung dendritic cells (LDCs), leading todeclined allergic airway inflammation in asthma. Nonetheless, the specific immunoregulatory roles of vNKT cells in LDC-mediated Th2 cell responses remain incompletely understood. Herein, we found
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Inhibition of Kv2.1 potassium channels by the antidepressant drug sertraline Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-06 Mayra Delgado-Ramírez, Ana Laura López-Serrano, Aldo A. Rodríguez-Menchaca
Sertraline is a commonly used antidepressant of the selective serotonin reuptake inhibitors (SSRIs) class. In this study, we have used the patch-clamp technique to assess the effects of sertraline on Kv2.1 channels heterologously expressed in HEK-293 cells and on the voltage-gated potassium currents (I) of Neuro 2a cells, which are predominantly mediated by Kv2.1 channels. Our results reveal that sertraline
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Synthesis and biological evaluation of folic acid-rotenol conjugate as a potent targeted anticancer prodrug Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-06 Min Hong, Juan Wang, Haobin Chen, Jiayu Qi, Qinghong Ji, Xiaoyan Liu, Qiaoli Yue, Lei li, Shuang Cheng
Rotenone, a plant-based agricultural insecticide, has been shown to have anti-tumor activity through targeting mitochondrial complex I in cancer cells. However, off-target toxic side effect on nervous systems have greatly restricted the application of rotenone as anticancer drugs. Here, a folic acid-rotenol (FA-rotenol) conjugate was prepared by covalent coupling of the tumor-targeting ligand folic
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Sildenafil, alone and in combination with imipramine or escitalopram, display antidepressant-like effects in an adrenocorticotropic hormone-induced (ACTH) rodent model of treatment-resistant depression Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-06 Juandré Lambertus Bernardus Saayman, Brian Herbert Harvey, Gregers Wegener, Christiaan Beyers Brink
Major depressive disorder (MDD) represents a challenge with high prevalence and limited effectiveness of existing treatments, particularly in cases of treatment-resistant depression (TRD). Innovative strategies and alternative drug targets are therefore necessary. Sildenafil, a selective phosphodiesterase type 5 (PDE5) inhibitor, is known to exert neuroplastic, anti-inflammatory, and antioxidant properties
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Sulforaphane's role in Redefining autophagic Responses in depression associated with polycystic ovarian syndrome: Unveiling the SIRT1/AMPK/LKB1 pathway connection Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-02 Ahmed S. Kamel, Sarah S. El-Sayed, Nesrine S. EL Sayed
Polycystic ovarian syndrome (PCOS) has been associated with depression and suicidal ideations in females. Studies have highlighted the role of autophagic deficiency in depression pathogenesis. Sulforaphane (SFN) is a natural product that improved autophagic deficiency and showed antidepressant activity in depressed patients. Herein, the study aimed to evaluate the impact of using SFN on depression-associated
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Sodium valproate treatment reverses endothelial dysfunction in aorta from rabbits with acute myocardial infarction Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-02 Sol Guerra-Ojeda, Andrea Suarez, Begoña Belmonte, Patricia Marchio, Patricia Genovés, Oscar Julian Arias, Martin Aldasoro, José M. Vila, Eva Serna, Maria D. Mauricio
Sodium valproate (VPA), a histone deacetylase (HDAC) inhibitor, could be a promising candidate to treat acute myocardial infarction (AMI). In this study, AMI was induced in New Zealand White rabbits by occluding the left circumflex coronary artery for 1 h, followed by reperfusion. The animals were distributed into three experimental groups: the sham-operated group (SHAM), the AMI group and the AMI + VPA
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Tetrandrine alleviates pulmonary fibrosis by inhibiting alveolar epithelial cell senescence through PINK1/Parkin-mediated mitophagy Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-02 Lanhe Chu, Jinzhong Zhuo, Haohua Huang, Weimou Chen, Wenshan Zhong, Jinming Zhang, Xiaojing Meng, Fei Zou, Shaoxi Cai, Mengchen Zou, Hangming Dong
Idiopathic pulmonary fibrosis (IPF) is a fatal and insidious interstitial lung disease. So far, there are no effective drugs for preventing the disease process. Cellular senescence plays a critical role in the development of IPF, with the senescence and insufficient mitophagy of alveolar epithelial cells being implicated in its pathogenesis. Tetrandrine is a natural alkaloid which is now produced synthetically
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The psychomotor, reinforcing, and discriminative stimulus effects of synthetic cathinone mexedrone in male mice and rats Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-01 Kyung Oh Jeon, Oc-Hee Kim, Su Yeon Seo, Jaesuk Yun, Choon-Gon Jang, Ri-Na Lim, Tae Wan Kim, Chae Ha Yang, Seong Shoon Yoon, Eun Young Jang
The chronic use of the novel synthetic cathinone mexedrone, like other psychoactive drugs, can be considered addictive, with a high potential for abuse and the ability to cause psychological dependence in certain users. However, little is known about the neurobehavioral effects of mexedrone in association with its potential for abuse. We investigated the abuse potential for mexedrone abuse through
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siRNA as potential therapeutic strategy for hypertension Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-01 Srushti Tanna, Gaurav Doshi, Angel Godad
Hypertension, a well-known cardiovascular disorder noticed by rise in blood pressure, poses a significant global health challenge. The development RNA interfering (RNAi)-based therapies offers a ground-breaking molecular tool, holds promise for addressing hypertension's intricate molecular mechanisms. Harnessing the power of small interfering RNA (siRNA), researchers aim to selectively target and modulate
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Inhibition of spinal BRD4 alleviates pyroptosis and M1 microglia polarization via STING-IRF3 pathway in morphine-tolerant rats Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-03-01 Xiaoqian Jia, Jie Ju, Zheng Li, Xiaoling Peng, Jihong Wang, Feng Gao
Morphine tolerance has been a challenging medical issue. Neuroinflammation is considered as a critical mechanism for the development of morphine tolerance. Bromodomain-containing protein 4 (BRD4), a key regulator in cell damage and inflammation, participates in the development of chronic pain. However, whether BRD4 is involved in morphine tolerance and the underlying mechanisms remain unknown. The
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MFG-E8 induces epithelial-mesenchymal transition and anoikis resistance to promote the metastasis of pancreatic cancer cells Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-29 Wuming Liu, Yifan Ren, Tao Wang, Mengzhou Wang, Yujia Xu, Jia Zhang, Jianbin Bi, Zheng Wu, Yi Lv, Rongqian Wu
Pancreatic cancer is an extremely malignant tumor, and only a few clinical treatment options exist. MFG-E8 and kindlin-2 all play an important role in cancer progression. However, the specific mechanism occurring between MFG-E8, kindlin-2 and the migration and invasion of pancreatic cancer cells remains unelucidated. To unravel the specific mechanism, this study assessed the potential association between
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Punicalagin promotes mincle-mediated phagocytosis of macrophages via the NF-κB and MAPK signaling pathways. Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-29 Shuangqin Yin, Weihong Dai, Tianyin Kuang, Jing Zhou, Li Luo, Shengxiang Ao, Xue Yang, Hongyan Xiao, Lin Qiao, Rixing Wang, Fei Wang, Caihong Yun, Shaowen Cheng, Junyu Zhu, Huaping Liang
Punicalagin (PUN) is a polyphenol derived from the pomegranate peel. It has been reported to have many beneficial effects, including anti-inflammatory, anti-oxidant, and anti-proliferation. However, the role of PUN in macrophage phagocytosis is currently unknown. In this study, we found that pre-treatment with PUN significantly enhanced phagocytosis by macrophages in a time- and dose-dependent manner
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Drug repurposing screen identifies novel anti-inflammatory activity of sunitinib in macrophages Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-28 Laura E. Chaffey, Annabell Roberti, Amelia Bowman, Conan JO. O'Brien, Liliana Som, Gareth SD. Purvis, David R. Greaves
Inflammation is a driver of human disease and an unmet clinical need exists for new anti-inflammatory medicines. As a key cell type in both acute and chronic inflammatory pathologies, macrophages are an appealing therapeutic target for anti-inflammatory medicines. Drug repurposing – the use of existing medicines for novel indications – is an attractive strategy for the identification of new anti-inflammatory
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Cellular and molecular mechanisms of oroxylin A in cancer therapy: Recent advances Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-28 Peng-Xin Wang, Xiao-Nan Mu, Shu-Hong Huang, Kang Hu, Zhi-Gang Sun
Seeking an effective and safe scheme is the common goal of clinical treatment of tumor patients. In recent years, traditional Chinese medicine has attracted more and more attention in order to discover new drugs with good anti-tumor effects. Oroxylin A (OA) is a compound found in natural Oroxylum indicum and Scutellaria baicalensis Georgi plants and has been used in the treatment of various cancers
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FDA compound library screening Baicalin upregulates TREM2 for the treatment of cerebral ischemia-reperfusion injury Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-28 Hongxia Wang, Jialiang Ma, Xiaoling Li, Yanhui Peng, Manxia Wang
Acute ischemic stroke (AIS) is a leading cause of global incidence and mortality rates. Oxidative stress and inflammation are key factors in the pathogenesis of AIS neuroinjury. Therefore, it is necessary to develop drugs that target neuroinflammation and oxidative stress in AIS. The Triggering Receptor Expressed on Myeloid Cells 2 (TREM2), primarily expressed on microglial cell membranes, plays a
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Chitosan revokes controlled-cortical impact generated neurological aberrations in circadian disrupted mice via TLR4-NLRP3 axis Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-27 Mohd Rabi Bazaz, Amit Asthana, Manoj P. Dandekar
The severity of inevitable neurological deficits and long-term psychiatric disorders in the aftermath of traumatic brain injury is influenced by pre-injury biological factors. Herein, we investigated the therapeutic effect of chitosan lactate on neurological and psychiatric aberrations inflicted by circadian disruption (CD) and controlled-cortical impact (CCI) injury in mice. Firstly, CD was developed
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Fluoroquinolones upregulate insulin-like growth factor–binding protein 3, inhibit cell growth and insulin-like growth factor signaling Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-27 Chih-Ling Chung, Chun-Lin Chen
Fluoroquinolones (FQs), commonly known for their antibiotic properties, exhibit additional pharmacological potential with anti-proliferative effects on various malignant cell types and immunomodulatory responses. Despite these observed effects, the precise mechanisms of action remain elusive. This study elucidates the biological impact of FQs on insulin-like growth factor–binding protein 3 (IGFBP-3)
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Ursolic acid alleviates cancer cachexia by inhibiting STAT3 signaling pathways in C2C12 myotube and CT26 tumor-bearing mouse model Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-27 Li Chen, Yan Chen, Mengxia Wang, Linglin Lai, Linbo Zheng, Huiqin Lu
Cancer cachexia, a multi-organ disorder resulting from tumor and immune system interactions, prominently features muscle wasting and affects the survival of patients with cancer. Ursolic acid (UA) is known for its antioxidant, anti-inflammatory, and anticancer properties. However, its impact on cancer cachexia remains unexplored. This study aimed to assess the efficacy of UA in addressing muscle atrophy
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Prolame produces anxiolytic- and antidepressant-like effects in middle-aged female rats with less uterotrophic effects than 17β-estradiol Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-27 C. Lemini, E. García-Albor, B. Cruz-López, G. Matamoros-Trejo, S. Márquez-Baltazar, J.J. Herrera-Pérez, L. Martínez-Mota
Estrogen hormone replacement therapy (EHRT), improving women's life quality at menopause, reduces anxiety and depression symptoms associated with ovarian hormonal decline. However, its potential adverse effects, like thromboembolism and cancer risk, limit its use. Prolame is a synthetic 17β-amino estrogen with antithrombotic actions that exerts anxiolytic- and antidepressant-like effects on young adult
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Naringenin reduces oxidative stress and necroptosis, apoptosis, and pyroptosis in random-pattern skin flaps by enhancing autophagy Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-27 Shuai Jiang, Feixia Ma, Junsheng Lou, Jiafeng Li, Xiushuai Shang, Yifan Li, Junsong Wu, Sanzhong Xu
Random skin flap grafting is one of the most commonly used techniques in plastic and orthopedic surgery. However, necrosis resulting from ischemia and ischemia-reperfusion injury in the distal part of the flap can severely limit the clinical application of the flap. Studies have revealed that naringenin reduces pyroptosis, apoptosis, and necroptosis, inhibits oxidative stress, and promotes autophagy
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Semaglutide alleviates gut microbiota dysbiosis induced by a high-fat diet Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-24 Xinhao Duan, Lei Zhang, Yi Liao, Zijing Lin, Changxin Guo, Sen Luo, Fu Wang, Zhen Zou, Zhijun Zeng, Chengzhi Chen, Jingfu Qiu
This study investigated the effects of semaglutide (Sema) on the gut microbiota of obese mice induced with high-fat diet (HFD). Male C57BL/6 J mice aged 6 weeks were enrolled and randomly distributed to four groups, which were provided with a normal control diet (NCD,NCD + Sema) and a 60% proportion of a high-fat diet (HFD,HFD + Sema), respectively. HFD was given for 10 weeks to develop an obesity
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The natural compounds, Magnolol or Honokiol, promote adipose tissue browning and resist obesity through modulating PPARα/γ activity Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-24 Yi Chu, Sisi Gui, Yazhen Zheng, Jingwu Zhao, Yaxiang Zhao, Yingying Li, Xiaodong Chen
Non-alcoholic fatty liver disease (NAFLD) is closely associated with the body's energy metabolism. A potential strategy to regulate energy metabolism, combat obesity, and reduce NAFLD is by enhancing adipocyte thermogenesis and increasing energy expenditure. In this study, our objective was to examine the effects of phenolic extracts derived from Magnolia officinalis on the regulation of NAFLD. Specifically
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A new era of immune therapeutics for pancreatic cancer: Monoclonal antibodies paving the way Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-24 Pankti C. Balar, Vasso Apostolopoulos, Vivek P. Chavda
Pancreatic cancer, particularly pancreatic ductal adenocarcinoma, remains a devastating disease with a dismal prognosis and limited survival rates. Despite various drug treatments and regimens showing promise in managing the disease, the clinical outcomes have not significantly improved. Immunotherapy however, has become a forefront area in pancreatic cancer treatment. This approach comprises a range
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Demotion of canonical/non-canonical inflammasome and pyroptosis alleviates ischemia/reperfusion-induced acute kidney injury: Novel role of the D2/D3 receptor agonist ropinirole Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-24 Nada T. Henedak, Hanan S. El-Abhar, Dalaal M. Abdallah, Kawkab A. Ahmed, Ayman A. Soubh
Ropinirole used to treat Parkinson's disease highly targets the dopaminergic receptor D3 over the D2 receptor but although both are expressed in the kidneys the ropinirole potential to treat kidney injury provoked by ischemia/reperfusion (I/R) is undraped. We investigated whether ropinirole can alleviate renal I/R by studying its anti-inflammatory, antioxidant, and anti-pyroptotic effects targeting
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Tyrosol attenuates NASH features by reprogramming the hepatic immune milieu Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-24 Daniela Gabbia, Katia Sayaf, Ilaria Zanotto, Martina Colognesi, Yahima Frion-Herrera, Maria Carrara, Francesco Paolo Russo, Sara De Martin
Nonalcoholic steatohepatitis (NASH) is a leading cause of chronic liver disease, and no drugs have been approved for its therapy. Among plant-derived molecules, phenolic compounds of extra virgin olive oil like tyrosol (Tyr) had demonstrated multiple beneficial actions for liver health, including the modulation of inflammation in fibrosis. This study aims at assessing the protective effect and mechanism
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Pharmacological insights on novel oral selective estrogen receptor degraders in breast cancer Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-23 Giorgio Guglielmi, Marzia Del Re, Leila Sadeghi Gol, Carmelo Bengala, Romano Danesi, Stefano Fogli
The therapeutic landscape of estrogen receptor (ER)-positive breast cancer includes endocrine treatments with aromatase inhibitors (AIs), selective estrogen receptor modulators (SERMs), and selective estrogen receptor degraders (SERDs). Fulvestrant is the first approved SERD with proven efficacy and good tolerability in clinical practice. However, secondary drug resistance, low receptor affinity, and
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Sophoricoside ameliorates cerebral ischemia-reperfusion injury dependent on activating AMPK Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-23 Zhaoshuo Li, Mi Zhang, Lixia Yang, Ding Fan, Peng Zhang, Li Zhang, Jianqing Zhang, Zhigang Lu
Ischemic stroke accounts for 87% of all strokes, and its death and disability bring a huge burden to society. Brain injury caused by ischemia-reperfusion (I/R) is also a major difficulty in clinical treatment and prognosis. Sophoricoside (SOP) is an isoflavone glycoside isolated from the seed of medical herb L. Previously, SOP was found to be effective in anti-inflammation and glucose-lipid metabolism-related
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Alantolactone derivatives inhibit the tumor necrosis factor α-induced nuclear factor κB pathway by a different mechanism from alantolactone Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-22 Quy Van Vu, Kosuke Baba, Saki Sasaki, Koichiro Kawaguchi, Hiroyuki Hirano, Hiroyuki Osada, Takao Kataoka
Alantolactone is an eudesmane-type sesquiterpene lactone that exerts various biological effects, including anti-inflammatory activity. In the present study, screening using the RIKEN Natural Products Depository chemical library identified alantolactone derivatives that inhibited the expression of intercellular adhesion molecule-1 (ICAM-1) on human umbilical vein endothelial cells stimulated with proinflammatory
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Corrigendum to “SUMO2-mediated SUMOylation of SH3GLB1 promotes ionizing radiation-induced hypertrophic cardiomyopathy through mitophagy activation”[Eur. J. Pharmacol. 924 (2022) 174980] Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-22 Anbo Gao, Jin Zou, Zhenjiang Mao, Hong Zhou, Gaofeng Zeng
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The blockade of neuropeptide FF receptor 1 and 2 differentially contributed to the modulating effects on fentanyl-induced analgesia and hyperalgesia in mice Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-22 Dan Chen, Mengna Zhang, Qinqin Zhang, Shuyuan Wu, Bowen Yu, Xiaodi Zhang, Xuanran Hu, Shichao Zhang, Zhenyun Yang, Junzhe Kuang, Biao Xu, Quan Fang
Neuropeptide FF (NPFF) plays a critical role in various physiological processes through the activation of neuropeptide FF receptor 1 and 2 (NPFFR1 and NPFFR2). Numerous evidence has indicated that NPFF exhibits opposite opioid-modulating effects on opioid-induced analgesia after supraspinal and spinal administrations, while the detailed role of NPFFR1 and NPFFR2 remains unclear. In this study, we employed
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Suppression of hypoxia-induced CAV1 autophagic degradation enhances nanoalbumin-paclitaxel transcytosis and improves therapeutic activity in pancreatic cancer Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-22 Xiangli Bai, Jia Xiong, Lin Li, Chao Yu, Chengyi Sun
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Pharmacological characterization of seven human histamine H3 receptor isoforms Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-21 Meichun Gao, Mabel E. Dekker, Rob Leurs, Henry F. Vischer
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Effects of nitrous oxide and ketamine on electrophysiological and molecular responses in the prefrontal cortex of mice: A comparative study Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-21 Stanislav Rozov, Roosa Saarreharju, Stanislav Khirug, Markus Storvik, Claudio Rivera, Tomi Rantamäki
Nitrous oxide (NO; laughing gas) has recently reported to produce rapid antidepressant effects, but little is known about the underlying mechanisms. We performed transcriptomics, hybridization, and electrophysiological studies to examine the potential shared signatures induced by 1 h inhalation of 50% NO and a single subanesthetic dose of ketamine (10 mg/kg, i.p.) in the medial prefrontal cortex (mPFC)
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Inhibition of colon C5a/C5a receptor signalling pathway confers protection against LPS-induced acute kidney injury via gut microbiota-kidney axis Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-20 Rong-Cheng Xie, Jin-Cheng Zhang, Xiao-Ming Lin, Ting Huang, Yu-Ting Wang, Lian-Fang Zhang, Xiang-Yu Hong, Xue-Feng Lin, Hong-Jun Zheng, Zhe Luo, Li-Tao Yi, Jie-Fei Ma
Acute kidney injury (AKI) is a critical condition often associated with systemic inflammation and dysregulated gut microbiota. This study aimed to investigate the effects of the C5a receptor antagonist W54011 on lipopolysaccharide (LPS)-induced AKI, focusing on the colon's C5a/C5a receptor pathway, intestinal barrier integrity, and gut microbiota. Our findings demonstrate that W54011 effectively ameliorated
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Ginsenoside Rg1 promotes fetal hemoglobin production in vitro: A potential therapeutic avenue for β-thalassemia Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-19 Dong-Ling Cai, Ying Chan, Ya-Min Kong, Yi-Ze Liu, Yan Guo, Ai-Qi Cai, Bao-Sheng Zhu
β-thalassemia, a globally prevalent genetic disorder, urgently requires innovative treatment options. Fetal hemoglobin (HbF) induction stands as a key therapeutic approach. This investigation focused on Ginsenoside Rg1 from the Panax genus for HbF induction. Employing K562 cells and human erythroid precursor cells (ErPCs) derived from neonatal cord blood, the study tested Rg1 at different concentrations
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A peripheral blood mononuclear cell-based in vitro model: A tool to explore indoleamine 2, 3-dioxygenase-1 (IDO1) Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-16 Milene Gonçalves, Alessia Furgiuele, Emanuela Rasini, Massimiliano Legnaro, Marco Ferrari, Alessandra Luini, Paulo Rodrigues-Santos, Francisco Caramelo, Franca Marino, Frederico C. Pereira, Marco Cosentino
Proinflammatory cytokines powerfully induce the rate-limiting enzyme indoleamine 2, 3-dioxygenase-1 (IDO-1) in dendritic cells (DCs) and monocytes, it converts tryptophan (Trp) into L-kynurenine (KYN), along the kynurenine pathway (KP). This mechanism represents a crucial innate immunity regulator that can modulate T cells. This work explores the role of IDO1 in lymphocyte proliferation within a specific
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Metformin improves obesity-related oligoasthenospermia via regulating the expression of HSL in testis in mice Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-16 Jinhui Dong, Xiaohui Tong, Jing Xu, Min Pan, Lei Wang, Fei Xu, Yajuan Wang, Li Li, Tongsheng Wang
Researches have proposed that obesity might contribute to development of oligoasthenospermia. This study was performed to confirm whether obesity contributes to oligoasthenospermia as well as the underlying mechanisms in mice fed with a high fat diet (HFD). Meanwhile, the actions of metformin, a drug of well-known weight-lowering effect, on sperm quality in obese mice were investigated. Our results
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Tetrahydroberberine alleviates high-fat diet-induced hyperlipidemia in mice via augmenting lipoprotein assembly-induced clearance of low-density lipoprotein and intermediate-density lipoprotein Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-16 Guilan Wei, Ning Huang, Mengyao Li, Fengkun Guan, Liping Chen, Yingyi Liao, Xingyu Xie, Yucui Li, Ziren Su, Jiannan Chen, Yuhong Liu
The promotion of excess low-density lipoprotein (LDL) clearance stands as an effective clinical approach for treating hyperlipidemia. Tetrahydroberberine, a metabolite of berberine, exhibits superior bioavailability compared to berberine and demonstrates a pronounced hypolipidemic effect. Despite these characteristics, the impact of tetrahydroberberine on improving excessive LDL clearance in hyperlipidemia
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Inhibition of Alzheimer's disease by 4-octyl itaconate revealed by RNA-seq transcriptome analysis Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-16 Yingchao Liu, Pengcheng Xia, Shuai Zong, Ni Zheng, Xiaolin Cui, Cuicui Wang, Miaomiao Wang, Xueying Wang, Shuyi Yu, Hao Zhao, Zhiming Lu
This study aimed to examine the therapeutic effects and response mechanisms of 4-OI in Alzheimer's disease (AD). In this study, network pharmacology was employed to analyze potential targets for AD drug therapy. Immunofluorescence and quantitative reverse transcription polymerase chain reaction (qRT-PCR) techniques were utilized to detect inflammatory phenotypes in a 4-OI-resistant mouse microglia
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Regulation mechanisms of sea cucumber peptides against scopolamine-induced memory disorder and novel memory-improving peptides identification Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-16 Zhiqiang Lu, Jingqi Yang, Xiaomeng Xu, Ruowen Liu, Songyi Lin
Memory impairment affects cognition and information processing, and attention, leading to a decline in life quality of patients. Previous studies have shown the memory-improving effects of sea cucumber peptides. This study further explored the memory-improving mechanisms of sea cucumber peptides using scopolamine-induced memory-impaired mice and identified novel memory-improving peptides within low
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Parecoxib sodium attenuates acute lung injury following burns by regulating M1/M2 macrophage polarization through the TLR4/NF-κB pathway Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-15 Dongxiao Huang, Zhongjun Zhang, Jinjin Jian, Xuliang Jiang, Jie Gao, Minlie Yang, Xian Ding
High temperature-induced burn injury often leads to an excessive inflammatory cascade resulting in multiple organ dysfunction syndrome, such as acute lung injury (ALI), in addition to skin tissue damage. As a specific COX2 inhibitor, parecoxib sodium suppresses the inflammatory response during burn injury. The effect of parecoxib sodium on ALI induced by burn injury and the associated molecular mechanism
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γ-Glutamylcysteine ameliorates blood-brain barrier permeability and neutrophil extracellular traps formation after ischemic stroke by modulating Wnt/β-catenin signalling in mice Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-15 Xinya Gu, Mengqi Dong, Shengnan Xia, Huiqin Li, Xinyu Bao, Xiang Cao, Yun Xu
During the inflammatory response after stroke, the blood-brain barrier (BBB) is significantly disrupted, compromising its integrity. This disruption allows many peripheral neutrophils to infiltrate the injury site in the brain and release neutrophil extracellular traps (NETs), which further increase BBB permeability. In this study, we aimed to investigate the protective effects of γ-Glutamylcysteine
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Toxicology, pharmacokinetics, and immunogenicity studies of CCR4-IL2 bispecific immunotoxin in rats and minipigs Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-15 Zhaohui Wang, Rashmi Ramakrishna, Yong Wang, Yue Qiu, Jihong Ma, Danielle Mintzlaff, Huiping Zhang, Bing Li, Benjamin Hammell, M. Scott Lucia, Elizabeth Pomfret, An-Jey A. Su, Kia M. Washington, David W. Mathes, Zhirui Wang
We have developed a diphtheria toxin-based recombinant human CCR4-IL2 bispecific immunotoxin (CCR4-IL2-IT) for targeted therapy of cutaneous T-cell lymphoma (CTCL). CCR4-IL2-IT demonstrated superior efficacy in an immunodeficient mouse CTCL model. Recently, we have compared the efficacy of CCR4-IL2-IT versus Brentuximab (FDA approved leading drug in CTCL market) in the same immunodeficient mouse CTCL
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Suramin inhibits phenotypic transformation of vascular smooth muscle cells and neointima hyperplasia by suppressing transforming growth factor beta receptor 1 /Smad2/3 pathway activation Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-15 Yingjie Xu, Luning Ge, Yanan Rui, Yuchen Wang, Zhonghua Wang, Jiemei Yang, Yuanqi Shi, Zengxiang Dong, Yu Zhang, Rongzhen Zhang, Tao Yang, Lin Lv, Fei Xiang, Sixuan Chen, Aoliang Song, Tiankai Li, Mingyu Liu, Yuanyuan Guo
Vascular smooth muscle cells (VSMCs) contribute to neointimal hyperplasia (NIH) after vascular injury, a common feature of vascular remodelling disorders. Suramin is known to exert antitumour effects by inhibiting the proliferation of various tumour cells; however, its effects and mechanism on VSMCs remain unclear. This study investigated the effects of suramin on human aortic smooth muscle cells (HASMCs)
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MiR-145–5p reduced ANG II-induced ACE2 shedding and the inflammatory response in alveolar epithelial cells by targeting ADAM17 and inhibiting the AT1R/ADAM17 pathway Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-15 Xu'an Wang, Jun Ma, Duomao Lin, Yang Bai, Dongni Zhang, Xiaotong Jia, Junwei Gao
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SIRT6-mediated Runx2 downregulation inhibits osteogenic differentiation of human aortic valve interstitial cells in calcific aortic valve disease Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-14 Jiaqi Xiong, Wenfeng Lin, Chunze Yuan, Jinhui Bian, Yifei Diao, Xinyang Xu, Buqing Ni, Hui Zhang, Yongfeng Shao
Calcific aortic valve disease (CAVD) is a progressive cardiovascular disorder involving multiple pathogenesis. Effective pharmacological therapies are currently unavailable. Sirtuin6 (SIRT6) has been shown to protect against aortic valve calcification in CAVD. The exact regulatory mechanism of SIRT6 in osteoblastic differentiation remains to be determined, although it inhibits osteogenic differentiation
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Distinct roles of the extracellular surface residues of glucagon-like peptide-1 receptor in β-arrestin 1/2 signaling Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-13 Saifei Lei, Qian Meng, Yanyun Liu, Qiaofeng Liu, Antao Dai, Xiaoqing Cai, Ming-Wei Wang, Qingtong Zhou, Hu Zhou, Dehua Yang
Glucagon-like peptide-1 receptor (GLP-1R) is a prime drug target for type 2 diabetes and obesity. The ligand initiated GLP-1R interaction with G protein has been well studied, but not with β-arrestin 1/2. Therefore, bioluminescence resonance energy transfer (BRET), mutagenesis and an operational model were used to evaluate the roles of 85 extracellular surface residues on GLP-1R in β-arrestin 1/2 recruitment
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Ruxolitinib attenuates microglial inflammatory response by inhibiting NF-κB/MAPK signaling pathway Eur. J. Pharmacol. (IF 5.0) Pub Date : 2024-02-12 Jingli Min, Hongmei Zheng, Heye Xia, Xuejun Tian, Meihao Liang, Jing Zhang, Wenhai Huang
Neuroinflammation is involved in the physiological and pathological processes of numerous neurological diseases, and its inhibition seems to be a promising therapeutic direction for these diseases. Ruxolitinib is a classical Janus kinase (JAK) inhibitor that is oral, highly potent and bioavailable, which has recently gained approval from the US Food and Drug Administration (FDA) for the treatment of