Telmisartan Ameliorates Nephropathy and Restores the Hippo Pathway in Rats with Metabolic Syndrome
Eur J Pharmacol. 2024 Apr 21:176605. doi: 10.1016/j.ejphar.2024.176605. Online ahead of print.ABSTRACTThe main objective of this study was to determine if the telmisartan-ameliorative effects of metabolic syndrome (MetS)-evoked nephropathy are attributed to the Hippo pathway. A secondary objective was to investigate the potential of vitamin D3 to enhance telmisartan-favourable effects. A diet composed of 24% fat and 3% salt, along with drinking water containing 10% fructose, was administered for 12 weeks to induce MetS. MetS-rats were given telmisartan (5 mg/kg/day), vitamin D3 (10 μg/kg/day) or both by gavage, starting i...
Source: European Journal of Pharmacology - April 23, 2024 Category: Drugs & Pharmacology Authors: Badria Mohamed Salah A Ghareib Amira Ebrahim Alsemeh Shaimaa S El-Sayed Source Type: research

Therapeutic effects of ginsenosides on osteoporosis for novel drug applications
Eur J Pharmacol. 2024 Apr 20:176604. doi: 10.1016/j.ejphar.2024.176604. Online ahead of print.ABSTRACTOsteoporosis (OP) is a metabolic bone disease with a high incidence rate worldwide. Its main features are decreased bone mass, increased bone fragility and deterioration of bone microstructure. It is caused by an imbalance between bone formation and bone resorption. Ginsenoside is a safe and effective traditional Chinese medicine (TCM) usually extracted from ginseng plants, having various therapeutic effects, of which the effect against osteoporosis has been extensively studied. We searched a total of 44 relevant articles ...
Source: European Journal of Pharmacology - April 22, 2024 Category: Drugs & Pharmacology Authors: Rui Liu Li-Xia Xu Lin-Jian Tong Hai-Yang Wu Qiang Guo Zhi-Ming Sun Hua Yan Source Type: research

Therapeutic effects of ginsenosides on osteoporosis for novel drug applications
Eur J Pharmacol. 2024 Apr 20:176604. doi: 10.1016/j.ejphar.2024.176604. Online ahead of print.ABSTRACTOsteoporosis (OP) is a metabolic bone disease with a high incidence rate worldwide. Its main features are decreased bone mass, increased bone fragility and deterioration of bone microstructure. It is caused by an imbalance between bone formation and bone resorption. Ginsenoside is a safe and effective traditional Chinese medicine (TCM) usually extracted from ginseng plants, having various therapeutic effects, of which the effect against osteoporosis has been extensively studied. We searched a total of 44 relevant articles ...
Source: European Journal of Pharmacology - April 22, 2024 Category: Drugs & Pharmacology Authors: Rui Liu Li-Xia Xu Lin-Jian Tong Hai-Yang Wu Qiang Guo Zhi-Ming Sun Hua Yan Source Type: research

Dabrafenib mitigates the neuroinflammation caused by ferroptosis in experimental autoimmune encephalomyelitis by up regulating Axl receptor
In this study, we preliminarily studied the possible mechanism of dabrafenib in the treatment of multiple sclerosis from the perspective of ferroptosis. First, we observed that dabrafenib significantly improved symptoms of gait abnormalities, limb weakness or paralysis, and down-regulated levels of spinal cord inflammation in an experimental autoimmune encephalitis (EAE) model. Meanwhile, we also observed that dabrafenib could inhibit the proteins of ferroptosis in spinal cord tissue of EAE mice by western blot. The results of immunohistochemical analysis showed that the effect of dabrafenib on ferroptosis mainly occurred ...
Source: European Journal of Pharmacology - April 21, 2024 Category: Drugs & Pharmacology Authors: Ning Liu Wuhan Yu Mengjiao Sun Xiaoling Li Wenjing Zhang Manxia Wang Source Type: research

IP3R1 dysregulation via miR-200c-3p/SSFA2 axis contributes to taxol resistance in head and neck cancer
Eur J Pharmacol. 2024 Apr 18:176592. doi: 10.1016/j.ejphar.2024.176592. Online ahead of print.ABSTRACTHead and neck cancer (HNC) is the sixth most common malignancy worldwide. Although current modalities offer a wide variety of therapy choices, head and neck carcinoma has poor prognosis due to its diagnosis at later stages and development of resistance to current therapeutic tools. In the current study, we aimed at exploring the roles of miR-200c-3p during head and neck carcinogenesis and acquisition of taxol resistance. We analyzed miR-200c-3p levels in HNC clinical samples and cell lines using quantitative real-time poly...
Source: European Journal of Pharmacology - April 20, 2024 Category: Drugs & Pharmacology Authors: Fatma Sanli Arzu Tatar Betul Gundogdu Omer Faruk Karatas Source Type: research

Rapid elucidation of agonist-driven regulation of the neurokinin 1 receptor using a GPCR phosphorylation immunoassay
Eur J Pharmacol. 2024 Apr 18:176587. doi: 10.1016/j.ejphar.2024.176587. Online ahead of print.ABSTRACTAgonist-induced phosphorylation is a crucial step in the activation/deactivation cycle of G protein-coupled receptors (GPCRs), but direct determination of individual phosphorylation events has remained a major challenge. We have recently developed a bead-based immunoassay for the quantitative assessment of agonist-induced GPCR phosphorylation that can be performed entirely in 96-well plates, thus eliminating the need for western blot analysis. In the present study, we adapted this assay to three novel phosphosite-specific ...
Source: European Journal of Pharmacology - April 20, 2024 Category: Drugs & Pharmacology Authors: Nina K Blum Anne Schaffner Julia Drube Falko Nagel Rainer K Reinscheid Carsten Hoffmann Stefan Schulz Source Type: research

Gastrodin alleviates the deterioration of depressive-like behavior and glucolipid metabolism promoted by chronic stress in type 2 diabetic mice
In this study, we performed 5 weeks CUMS intervention and simultaneously administered gastrodin (140 mg/kg, once daily) on T2DM mice, to investigate the potential protective effects of gastrodin. The protective effect of gastrodin was evaluated by behavioral tests, biochemical analysis, histopathological examination, RT-qPCR and gut microbiota analysis. We found that the depressive-like behavior and glucolipid metabolism could be deteriorated by chronic stress in type 2 diabetic mice, while gastrodin showed a protective effect against these exacerbations by regulating HPA hormones, activating FXR and Cyp7a1, reducing infla...
Source: European Journal of Pharmacology - April 20, 2024 Category: Drugs & Pharmacology Authors: Canye Li Jinming Cao Zhicong Chen Zuanjun Su Huimin Bao Xue Li Luping Liu Zhijun Xiao Jingjing Duan Ting Zhou Feng Xu Source Type: research

Angiotensin-converting enzyme inhibition prevents L-dopa-induced dyskinesia in a 6-OHDA-induced mouse model of Parkinson's disease
In conclusion, co-treatment with ACEIs and L-dopa, such as perindopril, captopril, and enalapril, may mitigate the severity of L-DOPA-induced dyskinesia in a mouse model of PD.PMID:38642669 | DOI:10.1016/j.ejphar.2024.176573 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - April 20, 2024 Category: Drugs & Pharmacology Authors: Hye-Yeon Park Ga Seul Lee Jun Go Young-Kyoung Ryu Chul-Ho Lee Jeong Hee Moon Kyoung-Shim Kim Source Type: research

Osteoporosis: Emerging Targets on the Classical Signaling Pathways of Bone Formation
Eur J Pharmacol. 2024 Apr 18:176574. doi: 10.1016/j.ejphar.2024.176574. Online ahead of print.ABSTRACTOsteoporosis is a multifaceted skeletal disorder characterized by reduced bone mass and structural deterioration, posing a significant public health challenge, particularly in the elderly population. Treatment strategies for osteoporosis primarily focus on inhibiting bone resorption and promoting bone formation. However, the effectiveness and limitations of current therapeutic approaches underscore the need for innovative methods. This review explores emerging molecular targets within crucial signaling pathways, including ...
Source: European Journal of Pharmacology - April 20, 2024 Category: Drugs & Pharmacology Authors: Si-Yan Li Si-Tu Xue Zhuo-Rong Li Source Type: research

Stachydrine hydrochloride protects the ischemic heart by ameliorating endoplasmic reticulum stress through a SERCA2a dependent way and maintaining intracellular Ca < sup > 2+ < /sup > homeostasis
This study aimed to explore the effects and mechanism of action of stachydrine hydrochloride (Sta) against myocardial infarction (MI) through sarcoplasmic/endoplasmic reticulum stress-related injury. The targets of Sta against MI were screened using network pharmacology. C57BL/6 J mice after MI were treated with saline, Sta (6 or 12 mg kg-1) for 2 weeks, and adult mouse and neonatal rat cardiomyocytes (AMCMs and NRCMs) were incubated with Sta (10-4-10-6 M) under normoxia or hypoxia for 2 or 12 h, respectively. Echocardiography, Evans blue, and 2,3,5-triphenyltetrazolium chloride (TTC) staining were used for morphological a...
Source: European Journal of Pharmacology - April 18, 2024 Category: Drugs & Pharmacology Authors: Minghui Feng Yuwen Chen Jingzhi Chen Wei Guo Pei Zhao Chen Zhang Xiaoli Shan Huihua Chen Ming Xu Rong Lu Source Type: research

Dl-3-n-Butylphthalide Improves Stroke Outcomes after Focal Ischemic Stroke in Mouse Model by Inhibiting the Pyroptosis-regulated Cell Death and Ameliorating Neuroinflammation
Eur J Pharmacol. 2024 Apr 16:176593. doi: 10.1016/j.ejphar.2024.176593. Online ahead of print.ABSTRACTRecent studies have highlighted the involvement of pyroptosis-mediated cell death and neuroinflammation in ischemic stroke (IS) pathogenesis. DL-3-n-butylphthalide (NBP), a synthesized compound based on an extract from seeds of Apium graveolens, possesses a broad range of biological effects. However, the efficacy and the underlying mechanisms of NBP in IS remain contentious. Herein, we investigated the therapeutic effects of NBP and elucidated its potential mechanisms in neuronal cell pyroptosis and microglia inflammatory ...
Source: European Journal of Pharmacology - April 18, 2024 Category: Drugs & Pharmacology Authors: Mengru Ge Lingting Jin Can Cui Yingying Han Hongxia Li Xue Gao Gang Li Hongxiang Yu Bei Zhang Source Type: research

Wogonoside alleviates microglia-mediated neuroinflammation via TLR4/MyD88/NF- κB signaling axis after spinal cord injury
This study employed in silico, in vitro, and in vivo methodologies to investigate the impact of WG on microglia-mediated neuroinflammation after SCI. In the in silico experiment, we identified 15 potential target genes of WG associated with SCI. These genes were linked to the regulation of inflammatory response and immune defense. Molecular docking maps revealed toll-like receptor 4 as a molecular target for WG, demonstrating binding through a hydrogen bond (Lys263, Ser120). In lipopolysaccharide-stimulated BV2 cells and SCI mice, WG significantly attenuated microglial activation and facilitated a phenotype shift from M1 t...
Source: European Journal of Pharmacology - April 18, 2024 Category: Drugs & Pharmacology Authors: Ruyi Zhu Yaling Zhang Weitai He Yanan Sun Xin Zhao Yaping Yan Qian Zhang Source Type: research

The antidiabetic drug ipragliflozin induces vasorelaxation of rabbit femoral artery by activating a Kv channel, the SERCA pump, and the PKA signaling pathway
Eur J Pharmacol. 2024 Apr 16;972:176589. doi: 10.1016/j.ejphar.2024.176589. Online ahead of print.ABSTRACTWe explored the vasorelaxant effects of ipragliflozin, a sodium-glucose cotransporter-2 inhibitor, on rabbit femoral arterial rings. Ipragliflozin relaxed phenylephrine-induced pre-contracted rings in a dose-dependent manner. Pre-treatment with the ATP-sensitive K+ channel inhibitor glibenclamide (10 μM), the inwardly rectifying K+ channel inhibitor Ba2+ (50 μM), or the Ca2+-sensitive K+ channel inhibitor paxilline (10 μM) did not influence the vasorelaxant effect. However, the voltage-dependent K+ (Kv) channel inhi...
Source: European Journal of Pharmacology - April 17, 2024 Category: Drugs & Pharmacology Authors: Minju Park Seo-Yeong Mun Wenwen Zhuang Junsu Jeong Hye Ryung Kim Hongzoo Park Eun-Taek Han Jin-Hee Han Wanjoo Chun Hongliang Li Won Sun Park Source Type: research

The antidiabetic drug ipragliflozin induces vasorelaxation of rabbit femoral artery by activating a Kv channel, the SERCA pump, and the PKA signaling pathway
Eur J Pharmacol. 2024 Apr 15:176589. doi: 10.1016/j.ejphar.2024.176589. Online ahead of print.ABSTRACTWe explored the vasorelaxant effects of ipragliflozin, a sodium-glucose cotransporter-2 inhibitor, on rabbit femoral arterial rings. Ipragliflozin relaxed phenylephrine-induced pre-contracted rings in a dose-dependent manner. Pre-treatment with the ATP-sensitive K+ channel inhibitor glibenclamide (10 μM), the inwardly rectifying K+ channel inhibitor Ba2+ (50 μM), or the Ca2+-sensitive K+ channel inhibitor paxilline (10 μM) did not influence the vasorelaxant effect. However, the voltage-dependent K+ (Kv) channel inhibito...
Source: European Journal of Pharmacology - April 17, 2024 Category: Drugs & Pharmacology Authors: Minju Park Seo-Yeong Mun Wenwen Zhuang Junsu Jeong Hye Ryung Kim Hongzoo Park Eun-Taek Han Jin-Hee Han Wanjoo Chun Hongliang Li Won Sun Park Source Type: research

Single Nucleotide Polymorphism-based Biomarker in Primary Hypertension
In conclusion, SNP research in primary hypertension is rapidly evolving with emerging technologies and methodologies that have the potential to transform the knowledge about genetic basis related to the condition. These advances hold promise for personalized prevention and treatment strategies tailored to an individual's genetic profile ultimately improving patient outcomes and reducing healthcare costs.PMID:38621507 | DOI:10.1016/j.ejphar.2024.176584 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - April 15, 2024 Category: Drugs & Pharmacology Authors: None Laxmi Pougang Golmei Shriyansh Srivastava Sachin Kumar Source Type: research