Parecoxib sodium attenuates acute lung injury following burns by regulating M1/M2 macrophage polarization through the TLR4/NF- κB pathway
Eur J Pharmacol. 2024 Feb 14:176407. doi: 10.1016/j.ejphar.2024.176407. Online ahead of print.ABSTRACTHigh 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 still need to be investigated. The role of parecoxib sodium in burn injury-induced ALI through the TLR4/NF-κB pathway w...
Source: European Journal of Pharmacology - February 16, 2024 Category: Drugs & Pharmacology Authors: Dongxiao Huang Zhongjun Zhang Jinjin Jian Xuliang Jiang Jie Gao Minlie Yang Xian Ding Source Type: research

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
In conclusion, our present study demonstrates the role and mechanism of miR-145-5p in alleviating ANG II-induced acute lung injury, providing a new insight into miRNA therapy for reducing lung injury in patients with aortic dissection.PMID:38365107 | DOI:10.1016/j.ejphar.2024.176392 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - February 16, 2024 Category: Drugs & Pharmacology Authors: Xu'an Wang Jun Ma Duomao Lin Yang Bai Dongni Zhang Xiaotong Jia Junwei Gao Source Type: research

Suramin inhibits phenotypic transformation of vascular smooth muscle cells and neointima hyperplasia by suppressing transforming growth factor beta receptor 1 /Smad2/3 pathway activation
This study investigated the effects of suramin on human aortic smooth muscle cells (HASMCs), rat aortic smooth muscle cells (RASMCs) and NIH to examine its suitability for the prevention of vascular remodelling disorders. In vitro, suramin administration reduced platelet-derived growth factor type BB (PDGF-BB)-stimulated proliferation, migration, and dedifferentiation of VSMCs through a transforming growth factor beta receptor 1 (TGFBR1)/Smad2/3-dependent pathway. Suramin dramatically inhibited NIH ligation in the left common carotid artery (LCCA) vivo. Therefore, our results indicate that suramin protects against the deve...
Source: European Journal of Pharmacology - February 16, 2024 Category: Drugs & Pharmacology Authors: 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 Source Type: research

SIRT6-mediated Runx2 downregulation inhibits osteogenic differentiation of human aortic valve interstitial cells in calcific aortic valve disease
Eur J Pharmacol. 2024 Feb 14:176423. doi: 10.1016/j.ejphar.2024.176423. Online ahead of print.ABSTRACTCalcific 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 of aortic valve interstitial cells. We demonstrated that SIRT6 was markedly downregulated in calcific human aortic valves...
Source: European Journal of Pharmacology - February 16, 2024 Category: Drugs & Pharmacology Authors: Jiaqi Xiong Wenfeng Lin Chunze Yuan Jinhui Bian Yifei Diao Xinyang Xu Buqing Ni Hui Zhang Yongfeng Shao Source Type: research

Distinct roles of the extracellular surface residues of glucagon-like peptide-1 receptor in β-arrestin 1/2 signaling
Eur J Pharmacol. 2024 Feb 13:176419. doi: 10.1016/j.ejphar.2024.176419. Online ahead of print.ABSTRACTGlucagon-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 triggered by three representative GLP-1R agonists (GLP-1, exendin-4 and oxyntomodulin). Residues selectively regul...
Source: European Journal of Pharmacology - February 15, 2024 Category: Drugs & Pharmacology Authors: Saifei Lei Qian Meng Yanyun Liu Qiaofeng Liu Antao Dai Xiaoqing Cai Ming-Wei Wang Qingtong Zhou Hu Zhou Dehua Yang Source Type: research

Distinct roles of the extracellular surface residues of glucagon-like peptide-1 receptor in β-arrestin 1/2 signaling
Eur J Pharmacol. 2024 Feb 13:176419. doi: 10.1016/j.ejphar.2024.176419. Online ahead of print.ABSTRACTGlucagon-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 triggered by three representative GLP-1R agonists (GLP-1, exendin-4 and oxyntomodulin). Residues selectively regul...
Source: European Journal of Pharmacology - February 15, 2024 Category: Drugs & Pharmacology Authors: Saifei Lei Qian Meng Yanyun Liu Qiaofeng Liu Antao Dai Xiaoqing Cai Ming-Wei Wang Qingtong Zhou Hu Zhou Dehua Yang Source Type: research

Ruxolitinib attenuates microglial inflammatory response by inhibiting NF- κB/MAPK signaling pathway
Eur J Pharmacol. 2024 Feb 12:176403. doi: 10.1016/j.ejphar.2024.176403. Online ahead of print.ABSTRACTNeuroinflammation 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 inflammatory disorders. The potential inhibitory effect of ruxolitinib on neuroinflammation has not been fully studied. In th...
Source: European Journal of Pharmacology - February 14, 2024 Category: Drugs & Pharmacology Authors: Jingli Min Hongmei Zheng Heye Xia Xuejun Tian Meihao Liang Jing Zhang Wenhai Huang Source Type: research

Ruxolitinib attenuates microglial inflammatory response by inhibiting NF- κB/MAPK signaling pathway
Eur J Pharmacol. 2024 Feb 12:176403. doi: 10.1016/j.ejphar.2024.176403. Online ahead of print.ABSTRACTNeuroinflammation 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 inflammatory disorders. The potential inhibitory effect of ruxolitinib on neuroinflammation has not been fully studied. In th...
Source: European Journal of Pharmacology - February 14, 2024 Category: Drugs & Pharmacology Authors: Jingli Min Hongmei Zheng Heye Xia Xuejun Tian Meihao Liang Jing Zhang Wenhai Huang Source Type: research

Licochalcone A induces mitochondria-dependent apoptosis and interacts with venetoclax in acute myeloid leukemia
Eur J Pharmacol. 2024 Feb 11:176418. doi: 10.1016/j.ejphar.2024.176418. Online ahead of print.ABSTRACTThe management of patients with acute myeloid leukemia (AML) remains a challenge because of the complexity and heterogeneity of this malignancy. Despite the recent approval of several novel targeted drugs, resistance seems inevitable, and clinical outcomes are still suboptimal. Increasing evidence supports the use of natural plants as an important source of anti-leukemic therapeutics. Licochalcone A (LCA) is an active flavonoid isolated from the roots of licorice, Glycyrrhiza uralensis Fisch., possessing extensive anti-tum...
Source: European Journal of Pharmacology - February 13, 2024 Category: Drugs & Pharmacology Authors: Youhong Li Mengting Zhao Ye Lin Xia Jiang Lili Jin Peipei Ye Ying Lu Renzhi Pei Lei Jiang Source Type: research

Gabapentin attenuates cardiac remodeling after myocardial infarction by inhibiting M1 macrophage polarization through the peroxisome proliferator-activated receptor- γ pathway
CONCLUSION: Gabapentin attenuates cardiac remodeling by inhibiting inflammation via peroxisome proliferator-activated receptor-γ activation and preventing calcium overload.PMID:38350591 | DOI:10.1016/j.ejphar.2024.176398 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - February 13, 2024 Category: Drugs & Pharmacology Authors: Zhenjun Li Shaoxian Wang Ying Qin Bo Yang Chengcheng Wang Tianyi Lu Jie Xu Lige Zhu Chen Yuan Wei Han Source Type: research

Palmatine alleviates cardiac fibrosis by inhibiting fibroblast activation through the STAT3 pathway
This study investigated the potential therapeutic value and mechanism of palmatine against cardiac fibrosis. Adult male C57BL/6 mice were treated with vehicle, isoproterenol (ISO), or ISO plus palmatine for one week. After echocardiography assessment, mice hearts were collected for histopathology, real-time polymerase chain reaction, and Western blot analyses. Primary rat CFs were utilized in vitro. Compared to control, ISO-treated mice exhibited cardiac hypertrophy and structural abnormalities; however, treatment with palmatine ameliorated these effects of ISO. Moreover, palmatine treatment mitigated ISO-induced cardiac f...
Source: European Journal of Pharmacology - February 13, 2024 Category: Drugs & Pharmacology Authors: Shaoling Lin Shengxi Zhang Angyu Zhan Jiaojiao Feng Qianqian Yang Tongjun Li Zijian Liu Quqian Mo Hui Fan Keke Wang Lexun Wang Source Type: research

PARP-1 inhibitor alleviates cerebral ischemia/reperfusion injury by reducing PARylation of HK-1 and LDH in mice
Eur J Pharmacol. 2024 Feb 10:176377. doi: 10.1016/j.ejphar.2024.176377. Online ahead of print.ABSTRACTPoly (ADP-ribose) polymerase-1 (PARP-1) activity significantly increases during cerebral ischemia/reperfusion. PARP-1 is an NAD+-consumption enzyme. PARP-1 hyperactivity causes intracellular NAD+ deficiency and bioenergetic collapse, contributing to neuronal death. Besides, the powerful trigger of PARP-1 causes the catalyzation of poly (ADP-ribosyl)ation (PARylation), a posttranslational modification of proteins. Here, we found that PARP-1 was activated in the ischemic brain tissue during middle-cerebral-artery occlusion a...
Source: European Journal of Pharmacology - February 12, 2024 Category: Drugs & Pharmacology Authors: Ya-Ling Chen Yi Wang Qiu-Yu Fang Tong Wang Cong Chen Tong-Yao Gao Ming Wu Wei-Ping Zhang Yun-Bi Lu Source Type: research

Tet1/DLL3/Notch1 signal pathway affects hippocampal neurogenesis and regulates depression-like behavior in mice
In this study, the chronic social defeat stress (CSDS) paradigm was constructed by overexpressing Tet1 protein in the mouse hippocampus, and 5-ethynyl-2'-deoxyuridine (EdU, 50 mg/kg) was injected on the seventh day to explore the mechanism of the regulation of the Tet1/Delta-like protein 3 (DLL3)/Notch1 protein pathway in mice hippocampal neurogenesis and its influence on depression-like behaviour. Following CSDS, the expression level of Tet1 decreased significantly. Moreover, due to the downregulation of Tet1 protein, the maintenance of the DNA methylation and demethylation balance was affected, resulting in a significant...
Source: European Journal of Pharmacology - February 12, 2024 Category: Drugs & Pharmacology Authors: Ruonan Shuang Tiantian Gao Zhongwen Sun Yue Tong Keke Zhao Hanqing Wang Source Type: research

Effect of ABT-639 on Cav3.2 channel activity and its analgesic actions in mouse models of inflammatory and neuropathic pain
Eur J Pharmacol. 2024 Feb 9:176416. doi: 10.1016/j.ejphar.2024.176416. Online ahead of print.ABSTRACTCav3.2 T-type calcium channels are important targets for pain relief in rodent models of inflammatory and neuropathic pain. Even though many T-type channel blockers have been tested in mice, only one molecule, ABT-639, has been tested in phase II clinical studies and did not produce analgesic effects over placebo. Here we examined the effects of ABT-639 on Cav3.2 channel activity in tsA-201 cells and dorsal root ganglion (DRG) neurons, in comparison with another established Cav3.2 inhibitor Z944. These experiments revealed ...
Source: European Journal of Pharmacology - February 11, 2024 Category: Drugs & Pharmacology Authors: Flavia Tasmin Techera Antunes Sun Huang Lina Chen Gerald W Zamponi Source Type: research

Contribution of chemical and electrical transmission to the low delta-like intrinsic retinal oscillation in mice: A role for daylight-activated neuromodulators
Eur J Pharmacol. 2024 Feb 9:176384. doi: 10.1016/j.ejphar.2024.176384. Online ahead of print.ABSTRACTBasal electroretinogram (ERG) oscillations have shown predictive value for modifiable risk factors for type 2 diabetes. However, their origin remains unknown. Here, we seek to establish the pharmacological profile of the low delta-like (δ1) wave in the mouse because it shows light sensitivity in the form of a decreased peak frequency upon photopic exposure. Applying neuropharmacological drugs by intravitreal injection, we eliminated the δ1 wave using lidocaine or by blocking all chemical and electrical synapses. The δ1 w...
Source: European Journal of Pharmacology - February 11, 2024 Category: Drugs & Pharmacology Authors: Pamela Reyes-Ortega Alejandra Rodr íguez-Arzate Rams és Noguez-Imm Edith Arnold St éphanie C Thébault Source Type: research