Demotion of canonical/non-canonical inflammasome and pyroptosis alleviates ischemia/reperfusion-induced acute kidney injury: Novel role of the D2/D3 receptor agonist ropinirole
In conclusion, ropinirole has the potential to be a reno-therapeutic treatment against I/R insult by abating the inflammatory NLRP3 inflammasome signal, pyroptosis, and oxidative stress.PMID:38402931 | DOI:10.1016/j.ejphar.2024.176460 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - February 25, 2024 Category: Drugs & Pharmacology Authors: Nada T Henedak Hanan S El-Abhar Dalaal M Abdallah Kawkab A Ahmed Ayman A Soubh Source Type: research

The natural compounds, Magnolol or Honokiol, promote adipose tissue browning and resist obesity through modulating PPAR α/γ activity
In this study, our objective was to examine the effects of phenolic extracts derived from Magnolia officinalis on the regulation of NAFLD. Specifically, we investigated the impact of Magnolol or Honokiol treatment on high-fat diet (HFD)-induced obese C57BL6/J male mice. Firstly, we monitored energy metabolism, dissected tissues, and analyzed tissue sections. Additionally, we conducted experiments on HepG2 and primary adipocytes to gain insights into the roles of Magnolol or Honokiol. To further understand the effects of these compounds on related signaling pathways and marker genes, we performed molecular docking, dual-luc...
Source: European Journal of Pharmacology - February 25, 2024 Category: Drugs & Pharmacology Authors: Yi Chu Sisi Gui Yazhen Zheng Jingwu Zhao Yaxiang Zhao Yingying Li Xiaodong Chen Source Type: research

Pharmacological insights on novel oral selective estrogen receptor degraders in breast cancer
Eur J Pharmacol. 2024 Feb 23:176424. doi: 10.1016/j.ejphar.2024.176424. Online ahead of print.ABSTRACTThe 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 parental administration stimulated the search for new oral SERDs opening a new therapeutic era in ER + breast cancer. Elaces...
Source: European Journal of Pharmacology - February 25, 2024 Category: Drugs & Pharmacology Authors: Giorgio Guglielmi Marzia Del Re Leila Sadeghi Gol Carmelo Bengala Romano Danesi Stefano Fogli Source Type: research

Semaglutide alleviates gut microbiota dysbiosis induced by a high-fat diet
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 model and the intervention was lasted for 18 days. The results showed Semaglutide significantly reduced body weight gain, areas under the curve (AUC) of glucose tolerance test and insulin resistance test, as well as adipose tissu...
Source: European Journal of Pharmacology - February 25, 2024 Category: Drugs & Pharmacology Authors: Xinhao Duan Lei Zhang Yi Liao Zijing Lin Changxin Guo Sen Luo Fu Wang Zhen Zou Zhijun Zeng Chengzhi Chen Jingfu Qiu Source Type: research

Demotion of canonical/non-canonical inflammasome and pyroptosis alleviates ischemia/reperfusion-induced acute kidney injury: Novel role of the D2/D3 receptor agonist ropinirole
In conclusion, ropinirole has the potential to be a reno-therapeutic treatment against I/R insult by abating the inflammatory NLRP3 inflammasome signal, pyroptosis, and oxidative stress.PMID:38402931 | DOI:10.1016/j.ejphar.2024.176460 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - February 25, 2024 Category: Drugs & Pharmacology Authors: Nada T Henedak Hanan S El-Abhar Dalaal M Abdallah Kawkab A Ahmed Ayman A Soubh Source Type: research

Sophoricoside ameliorates cerebral ischemia-reperfusion injury dependent on activating AMPK
CONCLUSION: SOP inhibits cerebral I/R injury by promoting the phosphorylation of AMPK.PMID:38401605 | DOI:10.1016/j.ejphar.2024.176439 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - February 24, 2024 Category: Drugs & Pharmacology Authors: Zhaoshuo Li Mi Zhang Lixia Yang Ding Fan Peng Zhang Li Zhang Jianqing Zhang Zhigang Lu Source Type: research

Sophoricoside ameliorates cerebral ischemia-reperfusion injury dependent on activating AMPK
CONCLUSION: SOP inhibits cerebral I/R injury by promoting the phosphorylation of AMPK.PMID:38401605 | DOI:10.1016/j.ejphar.2024.176439 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - February 24, 2024 Category: Drugs & Pharmacology Authors: Zhaoshuo Li Mi Zhang Lixia Yang Ding Fan Peng Zhang Li Zhang Jianqing Zhang Zhigang Lu Source Type: research

Alantolactone derivatives inhibit the tumor necrosis factor α-induced nuclear factor κB pathway by a different mechanism from alantolactone
Eur J Pharmacol. 2024 Feb 21:176458. doi: 10.1016/j.ejphar.2024.176458. Online ahead of print.ABSTRACTAlantolactone 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 cytokines and Toll-like receptor ligands. In human lung adenocarcinoma A549 cells stimulated with tumor necrosis ...
Source: European Journal of Pharmacology - February 23, 2024 Category: Drugs & Pharmacology Authors: Quy Van Vu Kosuke Baba Saki Sasaki Koichiro Kawaguchi Hiroyuki Hirano Hiroyuki Osada Takao Kataoka Source Type: research

Suppression of hypoxia-induced CAV1 autophagic degradation enhances nanoalbumin-paclitaxel transcytosis and improves therapeutic activity in pancreatic cancer
Eur J Pharmacol. 2024 Feb 21:176431. doi: 10.1016/j.ejphar.2024.176431. Online ahead of print.ABSTRACTNanoalbumin-paclitaxel (nab-paclitaxel) is a standard chemotherapy for pancreatic cancer but has shown limited efficacy. However, the mechanism through which circulating nab-paclitaxel passes through the tumour vascular endothelium has not been determined. In our study, a new nonradioactive and highly sensitive method for analysing nab-paclitaxel transcytosis was established. Based on these methods, we found that hypoxia significantly enhanced the autophagic degradation of CAV1 and therefore attenuated caveolae-mediated na...
Source: European Journal of Pharmacology - February 23, 2024 Category: Drugs & Pharmacology Authors: Xiangli Bai Jia Xiong Lin Li Chao Yu Chengyi Sun Source Type: research

The blockade of neuropeptide FF receptor 1 and 2 differentially contributed to the modulating effects on fentanyl-induced analgesia and hyperalgesia in mice
In this study, we employed pharmacological and genetic inhibition of NPFFR to investigate the modulating roles of central NPFFR1 and NPFFR2 in opioid-induced analgesia and hyperalgesia, using a male mouse model of acute fentanyl-induced analgesia and secondary hyperalgesia. Our findings revealed that intrathecal (i.t.) injection of the nonselective NPFFR antagonist RF9 significantly enhanced fentanyl-induced analgesia, whereas intracerebroventricular (i.c.v.) injection did not show the same effect. Moreover, NPFFR2 deficient (npffr2-/-) mice exhibited stronger analgesic responses to fentanyl compared to wild type (WT) or N...
Source: European Journal of Pharmacology - February 23, 2024 Category: Drugs & Pharmacology Authors: Dan Chen Mengna Zhang Qinqin Zhang Shuyuan Wu Bowen Yu Xiaodi Zhang Xuanran Hu Shichao Zhang Zhenyun Yang Junzhe Kuang Biao Xu Quan Fang Source Type: research

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. 2024 Feb 22:176456. doi: 10.1016/j.ejphar.2024.176456. Online ahead of print.NO ABSTRACTPMID:38395694 | DOI:10.1016/j.ejphar.2024.176456 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - February 23, 2024 Category: Drugs & Pharmacology Authors: Anbo Gao Jin Zou Zhenjiang Mao Hong Zhou Gaofeng Zeng Source Type: research

Inhibition of colon C5a/C5a receptor signalling pathway confers protection against LPS-induced acute kidney injury via gut microbiota-kidney axis
In conclusion, W54011 alleviates LPS-induced AKI by modulating the interplay between the colon, gut microbiota, and kidneys. It preserves the integrity of the intestinal barrier and reinstates gut microbiota, thereby mitigating AKI symptoms. These findings suggest that targeting the colon and gut microbiota could be a promising therapeutic strategy for AKI treatment.PMID:38387717 | DOI:10.1016/j.ejphar.2024.176425 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - February 22, 2024 Category: Drugs & Pharmacology Authors: 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 Source Type: research

Pharmacological characterization of seven human histamine H < sub > 3 < /sub > receptor isoforms
In this study, we pharmacologically characterized for the first time all seven H3R isoforms by determining their binding affinities for reference histamine H3 receptor agonists and inverse agonists. The H3R-453, H3R-415, and H3R-413 isoforms display similar binding affinities for all ligands as the H3R-445. However, increased agonist binding affinities were observed for the three shorter isoforms H3R-329, H3R-365, and H3R-373, whereas inverse agonists such as the approved anti-narcolepsy drug pitolisant (Wakix®) displayed significantly decreased binding affinities for the latter two isoforms. This opposite change in bindi...
Source: European Journal of Pharmacology - February 22, 2024 Category: Drugs & Pharmacology Authors: Meichun Gao Mabel E Dekker Rob Leurs Henry F Vischer Source Type: research

Effects of nitrous oxide and ketamine on electrophysiological and molecular responses in the prefrontal cortex of mice: A comparative study
Eur J Pharmacol. 2024 Feb 20:176426. doi: 10.1016/j.ejphar.2024.176426. Online ahead of print.ABSTRACTNitrous oxide (N2O; laughing gas) has recently reported to produce rapid antidepressant effects, but little is known about the underlying mechanisms. We performed transcriptomics, in situ hybridization, and electrophysiological studies to examine the potential shared signatures induced by 1 h inhalation of 50% N2O and a single subanesthetic dose of ketamine (10 mg/kg, i.p.) in the medial prefrontal cortex (mPFC) in adult mice. Both treatments similarly affected the transcription of several negative regulators of mitogen-ac...
Source: European Journal of Pharmacology - February 22, 2024 Category: Drugs & Pharmacology Authors: Stanislav Rozov Roosa Saarreharju Stanislav Khirug Markus Storvik Claudio Rivera Tomi Rantam äki Source Type: research

Inhibition of colon C5a/C5a receptor signalling pathway confers protection against LPS-induced acute kidney injury via gut microbiota-kidney axis
In conclusion, W54011 alleviates LPS-induced AKI by modulating the interplay between the colon, gut microbiota, and kidneys. It preserves the integrity of the intestinal barrier and reinstates gut microbiota, thereby mitigating AKI symptoms. These findings suggest that targeting the colon and gut microbiota could be a promising therapeutic strategy for AKI treatment.PMID:38387717 | DOI:10.1016/j.ejphar.2024.176425 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - February 22, 2024 Category: Drugs & Pharmacology Authors: 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 Source Type: research