FDA compound library screening Baicalin upregulates TREM2 for the treatment of cerebral ischemia-reperfusion injury
In this study, we employed a high-throughput screening (HTS) strategy to evaluate 2625 compounds from the (Food and Drug Administration) FDA library in vitro to identify compounds that upregulate the TREM2 receptor on microglia. Through this screening, we identified Baicalin as a potential drug for AIS treatment. Baicalin, a flavonoid compound extracted and isolated from the root of Scutellaria baicalensis, demonstrated promising results. Next, we established an in vivo mouse model of cerebral ischemia-reperfusion injury (MCAO/R) and an in vitro microglia cell of oxygen-glucose deprivation reperfusion (OGD/R) to investigat...
Source: European Journal of Pharmacology - March 1, 2024 Category: Drugs & Pharmacology Authors: Hongxia Wang Jialiang Ma Xiaoling Li Yanhui Peng Manxia Wang Source Type: research

Punicalagin promotes mincle-mediated phagocytosis of macrophages via the NF- κB and MAPK signaling pathways
In this study, we found that pre-treatment with PUN significantly enhanced phagocytosis by macrophages in a time- and dose-dependent manner in vitro. Moreover, KEGG enrichment analysis by RNA-sequencing showed that differentially expressed genes following PUN treatment were significantly enriched in phagocyte-related receptors, such as the C-type lectin receptor signaling pathway. Among the C-type lectin receptor family, Mincle (Clec4e) significantly increased at the mRNA and protein level after PUN treatment, as shown by qRT-PCR and western blotting. Small interfering RNA (siRNA) mediated knockdown of Mincle in macrophage...
Source: European Journal of Pharmacology - March 1, 2024 Category: Drugs & Pharmacology Authors: 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 Source Type: research

Naringenin reduces oxidative stress and necroptosis, apoptosis, and pyroptosis in random-pattern skin flaps by enhancing autophagy
CONCLUSIONS: The findings indicated that naringenin treatment could promote flap survival by inhibiting pyroptosis, apoptosis, necroptosis, and alleviating oxidative stress, caused by the activation of autophagy.PMID:38423240 | DOI:10.1016/j.ejphar.2024.176455 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - February 29, 2024 Category: Drugs & Pharmacology Authors: Shuai Jiang Feixia Ma Junsheng Lou Jiafeng Li Xiushuai Shang Yifan Li Junsong Wu Sanzhong Xu Source Type: research

Ursolic acid alleviates cancer cachexia by inhibiting STAT3 signaling pathways in C2C12 myotube and CT26 tumor-bearing mouse model
This study aimed to assess the efficacy of UA in addressing muscle atrophy and organ dysfunction in cancer cachexia and reveal the mechanisms involved. UA dose-dependently ameliorated C2C12 myotube atrophy. Mechanistically, it inhibited the expression of muscle-specific RING finger containing protein 1 (MURF1) and the phosphorylation of signal transducer and activator of transcription 3 (STAT3), and upregulated the mRNA or protein levels of myogenic differentiation antigen and myogenin in cultured C2C12 myotubes treated with conditioned medium. In vivo, UA protected CT26 tumor-bearing mice against loss of body weight, as w...
Source: European Journal of Pharmacology - February 29, 2024 Category: Drugs & Pharmacology Authors: Li Chen Yan Chen Mengxia Wang Linglin Lai Linbo Zheng Huiqin Lu Source Type: research

Fluoroquinolones upregulate insulin-like growth factor-binding protein 3, inhibit cell growth and insulin-like growth factor signaling
This study elucidates the biological impact of FQs on insulin-like growth factor-binding protein 3 (IGFBP-3) productions in a p53-dependent manner. Cultured cells and mouse models treated with FQs demonstrated increased IGFBP-3 mRNA expression and protein secretion. The FQ-induced IGFBP-3 was identified to impede cell growth by inhibiting IGF-I signaling and exerting effects through an IGF-independent pathway. Notably, FQ-mediated suppression of cell proliferation was reversed in p53-null and p53 knockdown cells, suggesting the pivotal role of p53 in FQ-induced IGFBP-3 production and IGFBP-3-mediated growth inhibition. Add...
Source: European Journal of Pharmacology - February 29, 2024 Category: Drugs & Pharmacology Authors: Chih-Ling Chung Chun-Lin Chen Source Type: research

Chitosan revokes controlled-cortical impact generated neurological aberrations in circadian disrupted mice via TLR4-NLRP3 axis
Eur J Pharmacol. 2024 Feb 27:176436. doi: 10.1016/j.ejphar.2024.176436. Online ahead of print.ABSTRACTThe 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 in mice by altering sporadic day-night cycles for 2 weeks. Then, CCI surgery was performed using a stereotaxic ImpactOne de...
Source: European Journal of Pharmacology - February 29, 2024 Category: Drugs & Pharmacology Authors: Mohd Rabi Bazaz Amit Asthana Manoj P Dandekar Source Type: research

Naringenin reduces oxidative stress and necroptosis, apoptosis, and pyroptosis in random-pattern skin flaps by enhancing autophagy
CONCLUSIONS: The findings indicated that naringenin treatment could promote flap survival by inhibiting pyroptosis, apoptosis, necroptosis, and alleviating oxidative stress, caused by the activation of autophagy.PMID:38423240 | DOI:10.1016/j.ejphar.2024.176455 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - February 29, 2024 Category: Drugs & Pharmacology Authors: Shuai Jiang Feixia Ma Junsheng Lou Jiafeng Li Xiushuai Shang Yifan Li Junsong Wu Sanzhong Xu Source Type: research

Ursolic acid alleviates cancer cachexia by inhibiting STAT3 signaling pathways in C2C12 myotube and CT26 tumor-bearing mouse model
This study aimed to assess the efficacy of UA in addressing muscle atrophy and organ dysfunction in cancer cachexia and reveal the mechanisms involved. UA dose-dependently ameliorated C2C12 myotube atrophy. Mechanistically, it inhibited the expression of muscle-specific RING finger containing protein 1 (MURF1) and the phosphorylation of signal transducer and activator of transcription 3 (STAT3), and upregulated the mRNA or protein levels of myogenic differentiation antigen and myogenin in cultured C2C12 myotubes treated with conditioned medium. In vivo, UA protected CT26 tumor-bearing mice against loss of body weight, as w...
Source: European Journal of Pharmacology - February 29, 2024 Category: Drugs & Pharmacology Authors: Li Chen Yan Chen Mengxia Wang Linglin Lai Linbo Zheng Huiqin Lu Source Type: research

Fluoroquinolones upregulate insulin-like growth factor-binding protein 3, inhibit cell growth and insulin-like growth factor signaling
This study elucidates the biological impact of FQs on insulin-like growth factor-binding protein 3 (IGFBP-3) productions in a p53-dependent manner. Cultured cells and mouse models treated with FQs demonstrated increased IGFBP-3 mRNA expression and protein secretion. The FQ-induced IGFBP-3 was identified to impede cell growth by inhibiting IGF-I signaling and exerting effects through an IGF-independent pathway. Notably, FQ-mediated suppression of cell proliferation was reversed in p53-null and p53 knockdown cells, suggesting the pivotal role of p53 in FQ-induced IGFBP-3 production and IGFBP-3-mediated growth inhibition. Add...
Source: European Journal of Pharmacology - February 29, 2024 Category: Drugs & Pharmacology Authors: Chih-Ling Chung Chun-Lin Chen Source Type: research

Chitosan revokes controlled-cortical impact generated neurological aberrations in circadian disrupted mice via TLR4-NLRP3 axis
Eur J Pharmacol. 2024 Feb 27:176436. doi: 10.1016/j.ejphar.2024.176436. Online ahead of print.ABSTRACTThe 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 in mice by altering sporadic day-night cycles for 2 weeks. Then, CCI surgery was performed using a stereotaxic ImpactOne de...
Source: European Journal of Pharmacology - February 29, 2024 Category: Drugs & Pharmacology Authors: Mohd Rabi Bazaz Amit Asthana Manoj P Dandekar Source Type: research

Prolame produces anxiolytic- and antidepressant-like effects in middle-aged female rats with less uterotrophic effects than 17 β-estradiol
This study aimed to identify the antidepressant- and anxiolytic-like effects of prolame and E2 (used as a reference estrogen treatment) in middle-aged female rats coursing with irregular cycles, in two different conditions: ovariectomized or gonadally intact. Results were compared with those from young adult ovariectomized rats. Prolame (60 or 120 μg/kg), 17β-estradiol (E2, 40 or 80 μg/kg), or vehicle were chronically administered, and their effects were evaluated in the elevated plus-maze, defensive burying behavior test, open field test, and forced swimming test. Uterotrophic actions were estimated by uterine weight r...
Source: European Journal of Pharmacology - February 28, 2024 Category: Drugs & Pharmacology Authors: C Lemini E Garc ía-Albor B Cruz-L ópez G Matamoros-Trejo S M árquez-Baltazar J J Herrera-P érez L Mart ínez-Mota Source Type: research

Drug repurposing screen identifies novel anti-inflammatory activity of sunitinib in macrophages
This study validates drug repurposing as a strategy for the identification of novel anti-inflammatory medicines and highlights sunitinib as a potential drug repurposing candidate for inflammatory disease via inhibition of NF-κB signalling.PMID:38417608 | DOI:10.1016/j.ejphar.2024.176437 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - February 28, 2024 Category: Drugs & Pharmacology Authors: Laura E Chaffey Annabell Roberti Amelia Bowman Conan Jo O'Brien Liliana Som Gareth Sd Purvis David R Greaves Source Type: research

Cellular and molecular mechanisms of oroxylin A in cancer therapy: Recent advances
Eur J Pharmacol. 2024 Feb 26:176452. doi: 10.1016/j.ejphar.2024.176452. Online ahead of print.ABSTRACTSeeking 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. Studies have shown that OA has a wide range of powerful biological activities and plays an important role in neuroprotection,...
Source: European Journal of Pharmacology - February 28, 2024 Category: Drugs & Pharmacology Authors: Peng-Xin Wang Xiao-Nan Mu Shu-Hong Huang Kang Hu Zhi-Gang Sun Source Type: research

Prolame produces anxiolytic- and antidepressant-like effects in middle-aged female rats with less uterotrophic effects than 17 β-estradiol
This study aimed to identify the antidepressant- and anxiolytic-like effects of prolame and E2 (used as a reference estrogen treatment) in middle-aged female rats coursing with irregular cycles, in two different conditions: ovariectomized or gonadally intact. Results were compared with those from young adult ovariectomized rats. Prolame (60 or 120 μg/kg), 17β-estradiol (E2, 40 or 80 μg/kg), or vehicle were chronically administered, and their effects were evaluated in the elevated plus-maze, defensive burying behavior test, open field test, and forced swimming test. Uterotrophic actions were estimated by uterine weight r...
Source: European Journal of Pharmacology - February 28, 2024 Category: Drugs & Pharmacology Authors: C Lemini E Garc ía-Albor B Cruz-L ópez G Matamoros-Trejo S M árquez-Baltazar J J Herrera-P érez L Mart ínez-Mota Source Type: research

Drug repurposing screen identifies novel anti-inflammatory activity of sunitinib in macrophages
This study validates drug repurposing as a strategy for the identification of novel anti-inflammatory medicines and highlights sunitinib as a potential drug repurposing candidate for inflammatory disease via inhibition of NF-κB signalling.PMID:38417608 | DOI:10.1016/j.ejphar.2024.176437 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - February 28, 2024 Category: Drugs & Pharmacology Authors: Laura E Chaffey Annabell Roberti Amelia Bowman Conan Jo O'Brien Liliana Som Gareth Sd Purvis David R Greaves Source Type: research