Kaempferol acts on bile acid signaling and gut microbiota to attenuate the tumor burden in ApcMin/+ mice
Eur J Pharmacol. 2022 Jan 19:174773. doi: 10.1016/j.ejphar.2022.174773. Online ahead of print.ABSTRACTEmerging evidence points to a strong association between the bile acid (BA)-gut microbiota (GM) axis, and the risk of colorectal cancer (CRC). Kaempferol, a common polyphenol in the daily diet, shows various pharmacological activities. However, it remains unclear about the effect of kaempferol on the CRC development and the BA-GM homeostasis. Here, we found kaempferol effectively reduced tumor burden, restored the damaged intestinal barrier and downregulated antigen Ki67 and leucine-rich repeat-containing G-protein coupled...
Source: European Journal of Pharmacology - January 22, 2022 Category: Drugs & Pharmacology Authors: Xiaoyan Li Imran Khan Guoxin Huang Yiyan Lu Liping Wang Yuanyuan Liu Linlin Lu W L Wendy Hsiao Zhongqiu Liu Source Type: research

Kaempferol acts on bile acid signaling and gut microbiota to attenuate the tumor burden in ApcMin/+ mice
Eur J Pharmacol. 2022 Jan 19:174773. doi: 10.1016/j.ejphar.2022.174773. Online ahead of print.ABSTRACTEmerging evidence points to a strong association between the bile acid (BA)-gut microbiota (GM) axis, and the risk of colorectal cancer (CRC). Kaempferol, a common polyphenol in the daily diet, shows various pharmacological activities. However, it remains unclear about the effect of kaempferol on the CRC development and the BA-GM homeostasis. Here, we found kaempferol effectively reduced tumor burden, restored the damaged intestinal barrier and downregulated antigen Ki67 and leucine-rich repeat-containing G-protein coupled...
Source: European Journal of Pharmacology - January 22, 2022 Category: Drugs & Pharmacology Authors: Xiaoyan Li Imran Khan Guoxin Huang Yiyan Lu Liping Wang Yuanyuan Liu Linlin Lu W L Wendy Hsiao Zhongqiu Liu Source Type: research

Suppression of hippocampal GABAergic transmission impairs memory in rodent models of Alzheimer's disease
We report a suppressed hippocampal GABAergic strength, potentially resulting from the reduced expression of anion chloride co-transporter KCC2 and subsequent positive shift of GABAergic Cl-equilibrium potential (ECl-), which is attenuated by microinjection of BDNF with proBDNF inhibitor TAT-Pep5. We also show that normalization of proBDNF/BDNF signaling or GABAergic ECl-by intracerebroventricular (i.c.v.) administration of bumetanide remarkably improves the cognitive performance in Morris water maze test and fear conditioning test in rodent models of AD. These results demonstrate a critical role of hippocampal proBDNF/BDNF...
Source: European Journal of Pharmacology - January 18, 2022 Category: Drugs & Pharmacology Authors: Bihua Bie Jiang Wu Feng Lin Mohamed Naguib Jijun Xu Source Type: research

Suppression of hippocampal GABAergic transmission impairs memory in rodent models of Alzheimer's disease
We report a suppressed hippocampal GABAergic strength, potentially resulting from the reduced expression of anion chloride co-transporter KCC2 and subsequent positive shift of GABAergic Cl-equilibrium potential (ECl-), which is attenuated by microinjection of BDNF with proBDNF inhibitor TAT-Pep5. We also show that normalization of proBDNF/BDNF signaling or GABAergic ECl-by intracerebroventricular (i.c.v.) administration of bumetanide remarkably improves the cognitive performance in Morris water maze test and fear conditioning test in rodent models of AD. These results demonstrate a critical role of hippocampal proBDNF/BDNF...
Source: European Journal of Pharmacology - January 18, 2022 Category: Drugs & Pharmacology Authors: Bihua Bie Jiang Wu Feng Lin Mohamed Naguib Jijun Xu Source Type: research

Suppression of hippocampal GABAergic transmission impairs memory in rodent models of Alzheimer's disease
We report a suppressed hippocampal GABAergic strength, potentially resulting from the reduced expression of anion chloride co-transporter KCC2 and subsequent positive shift of GABAergic Cl-equilibrium potential (ECl-), which is attenuated by microinjection of BDNF with proBDNF inhibitor TAT-Pep5. We also show that normalization of proBDNF/BDNF signaling or GABAergic ECl-by intracerebroventricular (i.c.v.) administration of bumetanide remarkably improves the cognitive performance in Morris water maze test and fear conditioning test in rodent models of AD. These results demonstrate a critical role of hippocampal proBDNF/BDNF...
Source: European Journal of Pharmacology - January 18, 2022 Category: Drugs & Pharmacology Authors: Bihua Bie Jiang Wu Feng Lin Mohamed Naguib Jijun Xu Source Type: research

Suppression of hippocampal GABAergic transmission impairs memory in rodent models of Alzheimer's disease
We report a suppressed hippocampal GABAergic strength, potentially resulting from the reduced expression of anion chloride co-transporter KCC2 and subsequent positive shift of GABAergic Cl-equilibrium potential (ECl-), which is attenuated by microinjection of BDNF with proBDNF inhibitor TAT-Pep5. We also show that normalization of proBDNF/BDNF signaling or GABAergic ECl-by intracerebroventricular (i.c.v.) administration of bumetanide remarkably improves the cognitive performance in Morris water maze test and fear conditioning test in rodent models of AD. These results demonstrate a critical role of hippocampal proBDNF/BDNF...
Source: European Journal of Pharmacology - January 18, 2022 Category: Drugs & Pharmacology Authors: Bihua Bie Jiang Wu Feng Lin Mohamed Naguib Jijun Xu Source Type: research

Ursodesoxycholic acid is an FFA4 agonist and reduces hepatic steatosis via FFA4 signaling
This study not only identified a new skeleton of FFA4 agonists, but also demonstrated that FFA4 signal was accounting for the protective effects of UDCA in the NAFLD treatment.PMID:35033554 | DOI:10.1016/j.ejphar.2022.174760 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - January 16, 2022 Category: Drugs & Pharmacology Authors: Fangfang Xu Jun Wang Pan Wang Tao Hou Han Zhou Yaopeng Zhao Jixia Wang Yanfang Liu Xinmiao Liang Source Type: research

Ursodesoxycholic acid is an FFA4 agonist and reduces hepatic steatosis via FFA4 signaling
This study not only identified a new skeleton of FFA4 agonists, but also demonstrated that FFA4 signal was accounting for the protective effects of UDCA in the NAFLD treatment.PMID:35033554 | DOI:10.1016/j.ejphar.2022.174760 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - January 16, 2022 Category: Drugs & Pharmacology Authors: Fangfang Xu Jun Wang Pan Wang Tao Hou Han Zhou Yaopeng Zhao Jixia Wang Yanfang Liu Xinmiao Liang Source Type: research

2-Benzyllawsone protects against polymicrobial sepsis and vascular hyporeactivity in swiss albino mice
CONCLUSIONS: LT-9 showed potent biological activity against sepsis and was found to be well tolerated in the toxicity study in Swiss albino mice and showed promise for the benzyllawsone class of molecules against sepsis for the development of novel pharmacophore.PMID:35032484 | DOI:10.1016/j.ejphar.2022.174757 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - January 15, 2022 Category: Drugs & Pharmacology Authors: Pankaj Yadav Hina Iqbal Kapil Kumar Parmanand Kumar Divya Mishra Arjun Singh Anirban Pal Pradipto Mukhopadhyay Beena Vamadevan Dhirendra Singh Arvind Singh Negi Debabrata Chanda Source Type: research

Proteomic profiling reveals antitumor effects of RT2 peptide on a human colon carcinoma xenograft mouse model
Eur J Pharmacol. 2022 Jan 12:174753. doi: 10.1016/j.ejphar.2022.174753. Online ahead of print.ABSTRACTA comparative study of human colon HCT-116 xenograft in nude mice treated with and without peptide RT2 at high doses is performed along with a label-free proteomic analysis of the tissue in order to understand the potential mechanisms by which RT2 acts in vivo against colorectal tumors. RT2 displays no significant systematic toxicity, but reduces tumor growth after either intraperitoneal or intratumoral injection demonstrating it is a safe and efficacious antitumor agent in vivo. Of the 3196 proteins identified by label-fr...
Source: European Journal of Pharmacology - January 15, 2022 Category: Drugs & Pharmacology Authors: Surachai Maijaroen Sompong Klaynongsruang Somrudee Reabroi Arthit Chairoungdua Sittiruk Roytrakul Jureerut Daduang Lapatrada Taemaitree Nisachon Jangpromma Source Type: research

Role of Thioredoxin-1 and its inducers in human health and diseases
Eur J Pharmacol. 2022 Jan 12:174756. doi: 10.1016/j.ejphar.2022.174756. Online ahead of print.ABSTRACTThioredoxin-1 (Trx-1) is a small redox-active protein normally found in mammalian cells that responds to the changing redox environment by contributing electrons or regulating related proteins. There is growing evidence that Trx-1 has multiple functions, including cytoprotective, anti-apoptotic, antioxidant and anti-inflammatory effects. To date, researchers have found that Trx-1 deficiency leads to severe damage in various disease models, such as atherosclerosis, cerebral ischemia, diabetes and tumors. Conversely, activat...
Source: European Journal of Pharmacology - January 15, 2022 Category: Drugs & Pharmacology Authors: Yuanyuan Liu Nianyu Xue Boxi Zhang Hongming Lv Shize Li Source Type: research

Poncirin ameliorates cardiac ischemia-reperfusion injury by activating PI3K/AKT/PGC-1 α signaling
In conclusion, both in vitro and in vivo studies suggested that poncirin alleviates cardiac ischemia-reperfusion injury by mitigating oxidative stress, which is dependent on activation of the PI3K/AKT/PGC-1α signaling pathway.PMID:35032487 | DOI:10.1016/j.ejphar.2022.174759 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - January 15, 2022 Category: Drugs & Pharmacology Authors: Bingda Li Tianpeng Chen Wenfeng Hu Zhenhua Wang Ji Wu Qing Zhou Ping Li Source Type: research

Dichloroacetate reactivates pyruvate-supported peroxide removal by liver mitochondria and prevents NAFLD aggravation in NAD(P) < sup > + < /sup > transhydrogenase-null mice consuming a high-fat diet
Eur J Pharmacol. 2022 Jan 12:174750. doi: 10.1016/j.ejphar.2022.174750. Online ahead of print.ABSTRACTThe mechanisms by which a high-fat diet (HFD) promotes non-alcoholic fatty liver disease (NAFLD) appear to involve liver mitochondrial dysfunction and redox imbalance. The functional loss of the enzyme NAD(P)+ transhydrogenase, an essential source of mitochondrial NADPH, results in impaired mitochondrial peroxide removal, pyruvate dehydrogenase inhibition by phosphorylation, and progression of NAFLD in HFD-fed mice. The present study aimed to investigate whether pharmacological reactivation of pyruvate dehydrogenase by dic...
Source: European Journal of Pharmacology - January 15, 2022 Category: Drugs & Pharmacology Authors: Claudia D C Navarro Annelise Francisco Tiago R Figueira Juliana A Ronchi Helena C F Oliveira Anibal E Vercesi Roger F Castilho Source Type: research

2-Benzyllawsone protects against polymicrobial sepsis and vascular hyporeactivity in swiss albino mice
CONCLUSIONS: LT-9 showed potent biological activity against sepsis and was found to be well tolerated in the toxicity study in Swiss albino mice and showed promise for the benzyllawsone class of molecules against sepsis for the development of novel pharmacophore.PMID:35032484 | DOI:10.1016/j.ejphar.2022.174757 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - January 15, 2022 Category: Drugs & Pharmacology Authors: Pankaj Yadav Hina Iqbal Kapil Kumar Parmanand Kumar Divya Mishra Arjun Singh Anirban Pal Pradipto Mukhopadhyay Beena Vamadevan Dhirendra Singh Arvind Singh Negi Debabrata Chanda Source Type: research

Proteomic profiling reveals antitumor effects of RT2 peptide on a human colon carcinoma xenograft mouse model
Eur J Pharmacol. 2022 Jan 12:174753. doi: 10.1016/j.ejphar.2022.174753. Online ahead of print.ABSTRACTA comparative study of human colon HCT-116 xenograft in nude mice treated with and without peptide RT2 at high doses is performed along with a label-free proteomic analysis of the tissue in order to understand the potential mechanisms by which RT2 acts in vivo against colorectal tumors. RT2 displays no significant systematic toxicity, but reduces tumor growth after either intraperitoneal or intratumoral injection demonstrating it is a safe and efficacious antitumor agent in vivo. Of the 3196 proteins identified by label-fr...
Source: European Journal of Pharmacology - January 15, 2022 Category: Drugs & Pharmacology Authors: Surachai Maijaroen Sompong Klaynongsruang Somrudee Reabroi Arthit Chairoungdua Sittiruk Roytrakul Jureerut Daduang Lapatrada Taemaitree Nisachon Jangpromma Source Type: research

Role of Thioredoxin-1 and its inducers in human health and diseases
Eur J Pharmacol. 2022 Jan 12:174756. doi: 10.1016/j.ejphar.2022.174756. Online ahead of print.ABSTRACTThioredoxin-1 (Trx-1) is a small redox-active protein normally found in mammalian cells that responds to the changing redox environment by contributing electrons or regulating related proteins. There is growing evidence that Trx-1 has multiple functions, including cytoprotective, anti-apoptotic, antioxidant and anti-inflammatory effects. To date, researchers have found that Trx-1 deficiency leads to severe damage in various disease models, such as atherosclerosis, cerebral ischemia, diabetes and tumors. Conversely, activat...
Source: European Journal of Pharmacology - January 15, 2022 Category: Drugs & Pharmacology Authors: Yuanyuan Liu Nianyu Xue Boxi Zhang Hongming Lv Shize Li Source Type: research

Poncirin ameliorates cardiac ischemia-reperfusion injury by activating PI3K/AKT/PGC-1 α signaling
In conclusion, both in vitro and in vivo studies suggested that poncirin alleviates cardiac ischemia-reperfusion injury by mitigating oxidative stress, which is dependent on activation of the PI3K/AKT/PGC-1α signaling pathway.PMID:35032487 | DOI:10.1016/j.ejphar.2022.174759 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - January 15, 2022 Category: Drugs & Pharmacology Authors: Bingda Li Tianpeng Chen Wenfeng Hu Zhenhua Wang Ji Wu Qing Zhou Ping Li Source Type: research

Dichloroacetate reactivates pyruvate-supported peroxide removal by liver mitochondria and prevents NAFLD aggravation in NAD(P) < sup > + < /sup > transhydrogenase-null mice consuming a high-fat diet
Eur J Pharmacol. 2022 Jan 12:174750. doi: 10.1016/j.ejphar.2022.174750. Online ahead of print.ABSTRACTThe mechanisms by which a high-fat diet (HFD) promotes non-alcoholic fatty liver disease (NAFLD) appear to involve liver mitochondrial dysfunction and redox imbalance. The functional loss of the enzyme NAD(P)+ transhydrogenase, an essential source of mitochondrial NADPH, results in impaired mitochondrial peroxide removal, pyruvate dehydrogenase inhibition by phosphorylation, and progression of NAFLD in HFD-fed mice. The present study aimed to investigate whether pharmacological reactivation of pyruvate dehydrogenase by dic...
Source: European Journal of Pharmacology - January 15, 2022 Category: Drugs & Pharmacology Authors: Claudia D C Navarro Annelise Francisco Tiago R Figueira Juliana A Ronchi Helena C F Oliveira Anibal E Vercesi Roger F Castilho Source Type: research

The macamide relieves fatigue by acting as inhibitor of inflammatory response in exercising mice: From central to peripheral
In this study, the anti-fatigue properties of N-benzyl-(9Z, 12Z)-octadecadienamide were further evaluated by a weight-loaded forced swimming test. Results indicated N-benzyl-(9Z, 12Z)-octadecadienamide supplementation increased the forelimb grip strength of mice and exercising time remaining on the Rota-rod test. Furthermore, significant decreases in pro-inflammatory factors and reactive oxygen species (ROS) contents were observed in mice receiving N-benzyl-(9Z, 12Z)-octadecadienamide treatment after a 30 min swimming test, which was equivalent to that of caffeine. Histological analysis also indicated that N-benzyl-(9Z, 12...
Source: European Journal of Pharmacology - January 13, 2022 Category: Drugs & Pharmacology Authors: Hongkang Zhu Ruoyong Wang Hanyi Hua Yuliang Cheng Yahui Guo He Qian Peng Du Source Type: research

Ovarian cancer and KiSS-1 gene expression: A consideration of the use of Kisspeptin plus Kisspeptin aptamers in diagnostics and therapy
Eur J Pharmacol. 2022 Jan 10:174752. doi: 10.1016/j.ejphar.2022.174752. Online ahead of print.ABSTRACTGynaecological cancers continue to present a significant health burden upon the health of the global female population. This deficit is most prominent with ovarian cancer which possesses the lowest survival rate compared to all other cancers occurring within this anatomical region, with an annual UK-mortality of 7,300. The poor tolerability and selectively of the treatment options that are currently available is likely to have contributed to this high mortality rate thus, demonstrating the need for the development of enhan...
Source: European Journal of Pharmacology - January 13, 2022 Category: Drugs & Pharmacology Authors: Navinder Singh Richard Hutson Nathaniel G N Milton Farideh A Javid Source Type: research

Dapagliflozin exerts anti-inflammatory effects via inhibition of LPS-induced TLR-4 overexpression and NF- κB activation in human endothelial cells and differentiated macrophages
Eur J Pharmacol. 2022 Jan 10:174715. doi: 10.1016/j.ejphar.2021.174715. Online ahead of print.ABSTRACTEvidence has demonstrated that a new class of anti-diabetic drugs, sodium-glucose co-transporter 2 (SGLT2) inhibitors, could exert beneficial effects on atherosclerotic complications of diabetes. Atherosclerosis is widely accepted as an inflammatory disease. Therefore, we aimed to assess the direct anti-inflammatory effects of SGLT2 inhibitors dapagliflozin (DAPA) on two cell types involved in the process of atherogenesis. Human umbilical vein endothelial cells (HUVECs) and macrophages were exposed to DAPA and lipopolysacc...
Source: European Journal of Pharmacology - January 13, 2022 Category: Drugs & Pharmacology Authors: Elaheh Abdollahi Fariborz Keyhanfar Ali-Akbar Delbandi Reza Falak Seyed Javad Hajimiresmaiel Massoumeh Shafiei Source Type: research

Electrophysiologic effects of sacubitril in different arrhythmia models
Eur J Pharmacol. 2022 Jan 10;917:174747. doi: 10.1016/j.ejphar.2022.174747. Online ahead of print.ABSTRACTBACKGROUND: Previous studies report conflicting data regarding anti- or proarrhythmic effects of sacubitril. Aim of this study was to assess the impact of acute sacubitril treatment in different arrhythmia models.METHODS: Sacubitril was administered (3, 5, 10 μM) in 12 isolated rabbit hearts. Further 12 hearts were treated with erythromycin to simulate long-QT-syndrome-2 (LQT2). Other 12 hearts were perfused with veratridine to mimic long-QT-syndrome-3 (LQT3). Both LQT-groups were treated with sacubitril (5 μM) a...
Source: European Journal of Pharmacology - January 13, 2022 Category: Drugs & Pharmacology Authors: Christian Ellermann Darian Dimanski Julian Wolfes Benjamin Rath Patrick Leitz Kevin Willy Felix K Wegner Lars Eckardt Gerrit Frommeyer Source Type: research

The macamide relieves fatigue by acting as inhibitor of inflammatory response in exercising mice: From central to peripheral
In this study, the anti-fatigue properties of N-benzyl-(9Z, 12Z)-octadecadienamide were further evaluated by a weight-loaded forced swimming test. Results indicated N-benzyl-(9Z, 12Z)-octadecadienamide supplementation increased the forelimb grip strength of mice and exercising time remaining on the Rota-rod test. Furthermore, significant decreases in pro-inflammatory factors and reactive oxygen species (ROS) contents were observed in mice receiving N-benzyl-(9Z, 12Z)-octadecadienamide treatment after a 30 min swimming test, which was equivalent to that of caffeine. Histological analysis also indicated that N-benzyl-(9Z, 12...
Source: European Journal of Pharmacology - January 13, 2022 Category: Drugs & Pharmacology Authors: Hongkang Zhu Ruoyong Wang Hanyi Hua Yuliang Cheng Yahui Guo He Qian Peng Du Source Type: research

Ovarian cancer and KiSS-1 gene expression: A consideration of the use of Kisspeptin plus Kisspeptin aptamers in diagnostics and therapy
Eur J Pharmacol. 2022 Jan 10:174752. doi: 10.1016/j.ejphar.2022.174752. Online ahead of print.ABSTRACTGynaecological cancers continue to present a significant health burden upon the health of the global female population. This deficit is most prominent with ovarian cancer which possesses the lowest survival rate compared to all other cancers occurring within this anatomical region, with an annual UK-mortality of 7,300. The poor tolerability and selectively of the treatment options that are currently available is likely to have contributed to this high mortality rate thus, demonstrating the need for the development of enhan...
Source: European Journal of Pharmacology - January 13, 2022 Category: Drugs & Pharmacology Authors: Navinder Singh Richard Hutson Nathaniel G N Milton Farideh A Javid Source Type: research

Dapagliflozin exerts anti-inflammatory effects via inhibition of LPS-induced TLR-4 overexpression and NF- κB activation in human endothelial cells and differentiated macrophages
Eur J Pharmacol. 2022 Jan 10:174715. doi: 10.1016/j.ejphar.2021.174715. Online ahead of print.ABSTRACTEvidence has demonstrated that a new class of anti-diabetic drugs, sodium-glucose co-transporter 2 (SGLT2) inhibitors, could exert beneficial effects on atherosclerotic complications of diabetes. Atherosclerosis is widely accepted as an inflammatory disease. Therefore, we aimed to assess the direct anti-inflammatory effects of SGLT2 inhibitors dapagliflozin (DAPA) on two cell types involved in the process of atherogenesis. Human umbilical vein endothelial cells (HUVECs) and macrophages were exposed to DAPA and lipopolysacc...
Source: European Journal of Pharmacology - January 13, 2022 Category: Drugs & Pharmacology Authors: Elaheh Abdollahi Fariborz Keyhanfar Ali-Akbar Delbandi Reza Falak Seyed Javad Hajimiresmaiel Massoumeh Shafiei Source Type: research

Electrophysiologic effects of sacubitril in different arrhythmia models
Eur J Pharmacol. 2022 Jan 10:174747. doi: 10.1016/j.ejphar.2022.174747. Online ahead of print.ABSTRACTBACKGROUND: Previous studies report conflicting data regarding anti- or proarrhythmic effects of sacubitril. Aim of this study was to assess the impact of acute sacubitril treatment in different arrhythmia models.METHODS: Sacubitril was administered (3, 5, 10 μM) in 12 isolated rabbit hearts. Further 12 hearts were treated with erythromycin to simulate long-QT-syndrome-2 (LQT2). Other 12 hearts were perfused with veratridine to mimic long-QT-syndrome-3 (LQT3). Both LQT-groups were treated with sacubitril (5 μM) addit...
Source: European Journal of Pharmacology - January 13, 2022 Category: Drugs & Pharmacology Authors: Christian Ellermann Darian Dimanski Julian Wolfes Benjamin Rath Patrick Leitz Kevin Willy Felix K Wegner Lars Eckardt Gerrit Frommeyer Source Type: research

Aesculin offers increased resistance against oxidative stress and protective effects against A β-induced neurotoxicity in Caenorhabditis elegans
Eur J Pharmacol. 2022 Jan 8:174755. doi: 10.1016/j.ejphar.2022.174755. Online ahead of print.ABSTRACTAesculin, a coumarin compound, is one of the major active ingredients of traditional Chinese herbal medicine Qinpi (Cortex Fraxini), which has been reported to exhibit antioxidative, anti-inflammatory and neuroprotective properties against oxidative stress and cellular apoptosis. However, the regulatory mechanisms remain poorly characterized in vivo. This research was performed to explore the underlying molecular mechanisms behind aesculin response conferring oxidative stress resistance, and the protective effects on amyloi...
Source: European Journal of Pharmacology - January 12, 2022 Category: Drugs & Pharmacology Authors: Ying Wang Qiong Cheng Qina Su Xuesong Yu Tianqi Shen Xiaoling Yang Weizhang Jia Source Type: research

Targeted drug delivery in cervical cancer: Current perspectives
Eur J Pharmacol. 2022 Jan 9:174751. doi: 10.1016/j.ejphar.2022.174751. Online ahead of print.ABSTRACTCervical cancer is preventable yet one of the most prevalent cancers among women around the globe. Though regular screening has resulted in the decline in incidence, the disease claims a high number of lives every year, especially in the developing countries. Owing to rather aggressive and non-specific nature of the conventional chemotherapeutics, there is a growing need for newer treatment modalities. The advent of nanotechnology has assisted in this through the use of nanocarriers for targeted drug delivery. A number of n...
Source: European Journal of Pharmacology - January 12, 2022 Category: Drugs & Pharmacology Authors: Supriti Ghosh Pradyumna Jayaram Shama Prasada Kabekkodu Kapaettu Satyamoorthy Source Type: research

Aesculin offers increased resistance against oxidative stress and protective effects against A β-induced neurotoxicity in Caenorhabditis elegans
Eur J Pharmacol. 2022 Jan 8:174755. doi: 10.1016/j.ejphar.2022.174755. Online ahead of print.ABSTRACTAesculin, a coumarin compound, is one of the major active ingredients of traditional Chinese herbal medicine Qinpi (Cortex Fraxini), which has been reported to exhibit antioxidative, anti-inflammatory and neuroprotective properties against oxidative stress and cellular apoptosis. However, the regulatory mechanisms remain poorly characterized in vivo. This research was performed to explore the underlying molecular mechanisms behind aesculin response conferring oxidative stress resistance, and the protective effects on amyloi...
Source: European Journal of Pharmacology - January 12, 2022 Category: Drugs & Pharmacology Authors: Ying Wang Qiong Cheng Qina Su Xuesong Yu Tianqi Shen Xiaoling Yang Weizhang Jia Source Type: research

Targeted drug delivery in cervical cancer: Current perspectives
Eur J Pharmacol. 2022 Jan 9:174751. doi: 10.1016/j.ejphar.2022.174751. Online ahead of print.ABSTRACTCervical cancer is preventable yet one of the most prevalent cancers among women around the globe. Though regular screening has resulted in the decline in incidence, the disease claims a high number of lives every year, especially in the developing countries. Owing to rather aggressive and non-specific nature of the conventional chemotherapeutics, there is a growing need for newer treatment modalities. The advent of nanotechnology has assisted in this through the use of nanocarriers for targeted drug delivery. A number of n...
Source: European Journal of Pharmacology - January 12, 2022 Category: Drugs & Pharmacology Authors: Supriti Ghosh Pradyumna Jayaram Shama Prasada Kabekkodu Kapaettu Satyamoorthy Source Type: research

Glutamic oxaloacetic transaminase 1 as a potential target in human cancer
Eur J Pharmacol. 2022 Jan 7:174754. doi: 10.1016/j.ejphar.2022.174754. Online ahead of print.ABSTRACTGlutamic Oxaloacetic Transaminase 1 (GOT1) is one distinct isoenzyme of glutamic oxaloacetic transaminase in eukaryotic cells, which is located in the cytoplasm. To date, several studies have shown that GOT1 plays a critical role in regulating cell proliferation by participating in amino acid metabolism, especially in glutamine metabolism. In addition, GOT1 is overexpressed in many cancer, so GOT1 has been identified as a potentially therapeutic target. Herein, this review summarizes the structure and function of GOT1 and t...
Source: European Journal of Pharmacology - January 10, 2022 Category: Drugs & Pharmacology Authors: Zhuorui Song Yueying Yang Yanli Wu Mengzhu Zheng Dejuan Sun Hua Li Lixia Chen Source Type: research

Isovitexin protects against acute liver injury by targeting PTEN, PI3K and BiP via modification of m6A
Eur J Pharmacol. 2022 Jan 7:174749. doi: 10.1016/j.ejphar.2022.174749. Online ahead of print.ABSTRACTIsovitexin (IVT) has been shown to have a potential therapeutic effect on acute liver injury (ALI), but its underlying mechanisms especially the targets remain unclear, which was investigated in the present study. Briefly, the targets of IVT were predicted by bioinformatics and then were verified by multiple examinations using molecular docking, cellular thermal shift assay (CETSA), and Lipopolysaccharide/D-Galactosamine (LPS/D-GalN)-induced ALI animal model. The bioinformatic analysis predicted that the target genes of IVT...
Source: European Journal of Pharmacology - January 10, 2022 Category: Drugs & Pharmacology Authors: Yushen Huang Siyun Chen Lijun Pang Zhongwen Feng Hongmei Su Wuchang Zhu Jinbin Wei Source Type: research

Glutamic oxaloacetic transaminase 1 as a potential target in human cancer
Eur J Pharmacol. 2022 Jan 7:174754. doi: 10.1016/j.ejphar.2022.174754. Online ahead of print.ABSTRACTGlutamic Oxaloacetic Transaminase 1 (GOT1) is one distinct isoenzyme of glutamic oxaloacetic transaminase in eukaryotic cells, which is located in the cytoplasm. To date, several studies have shown that GOT1 plays a critical role in regulating cell proliferation by participating in amino acid metabolism, especially in glutamine metabolism. In addition, GOT1 is overexpressed in many cancer, so GOT1 has been identified as a potentially therapeutic target. Herein, this review summarizes the structure and function of GOT1 and t...
Source: European Journal of Pharmacology - January 10, 2022 Category: Drugs & Pharmacology Authors: Zhuorui Song Yueying Yang Yanli Wu Mengzhu Zheng Dejuan Sun Hua Li Lixia Chen Source Type: research

Isovitexin protects against acute liver injury by targeting PTEN, PI3K and BiP via modification of m6A
Eur J Pharmacol. 2022 Jan 7:174749. doi: 10.1016/j.ejphar.2022.174749. Online ahead of print.ABSTRACTIsovitexin (IVT) has been shown to have a potential therapeutic effect on acute liver injury (ALI), but its underlying mechanisms especially the targets remain unclear, which was investigated in the present study. Briefly, the targets of IVT were predicted by bioinformatics and then were verified by multiple examinations using molecular docking, cellular thermal shift assay (CETSA), and Lipopolysaccharide/D-Galactosamine (LPS/D-GalN)-induced ALI animal model. The bioinformatic analysis predicted that the target genes of IVT...
Source: European Journal of Pharmacology - January 10, 2022 Category: Drugs & Pharmacology Authors: Yushen Huang Siyun Chen Lijun Pang Zhongwen Feng Hongmei Su Wuchang Zhu Jinbin Wei Source Type: research

Corrigendum to "siRNA: Mechanism of action, challenges, and therapeutic approaches" [Eur. J. Pharmacol. 905 (2021) 174178]
Eur J Pharmacol. 2022 Jan 5:174741. doi: 10.1016/j.ejphar.2022.174741. Online ahead of print.NO ABSTRACTPMID:34998574 | DOI:10.1016/j.ejphar.2022.174741 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - January 9, 2022 Category: Drugs & Pharmacology Authors: Walhan Alshaer Hadil Zureigat Arwa Al Karaki Abdulfattah Al-Kadash Lobna Gharaibeh Ma'mon M Hatmal Alaa A A Aljabali Abdalla Awidi Source Type: research

Role of high-fat diet on letrozole-induced polycystic ovarian syndrome in rats
Eur J Pharmacol. 2022 Jan 5;917:174746. doi: 10.1016/j.ejphar.2022.174746. Online ahead of print.ABSTRACTPolycystic ovary syndrome (PCOS) is one of the most prevalent hormonal disorders in women of reproductive age. Letrozole (LET)-induced PCOS is a good model but has drawbacks such as the absence of metabolic changes. Hence, in the present study, we aimed to develop a new animal model combining a high-fat diet (HFD) and LET. Female Wistar rats were divided into a control group, LET group, and LET + HFD (45% energy from fat) group. Compared with the control group, the LET and LET + HFD groups showed ovarian cysts and eleva...
Source: European Journal of Pharmacology - January 9, 2022 Category: Drugs & Pharmacology Authors: Nazia Begum Kandavalli Manipriya B Veeresh Source Type: research

Endoplasmic reticulum stress-dependent activation of TRB3-FoxO1 signaling pathway exacerbates hyperglycemic nephrotoxicity: Protection accorded by naringenin
This study unravels the critical role of Tribbles 3 (TRB3)-Forkhead box O1 (FoxO1) signaling pathway during hyperglycemic renal toxicity. It also uncovers the novel role of Naringenin, a flavanone, in regulating ER stress in proximal tubular cells, NRK 52E, and kidneys of streptozotocin/nicotinamide induced experimental diabetic Wistar rats. Results demonstrate that expression of ER stress marker proteins including phosphorylated protein kinase ER like kinase (p-PERK), phosphorylated eukaryotic Initiation Factor 2α (p-eIF2α), X Box Binding Protein 1 spliced (XBP1s), Activating Transcription Factor 4 (ATF4) and ...
Source: European Journal of Pharmacology - January 9, 2022 Category: Drugs & Pharmacology Authors: Mohammad Fareed Khan Alpana Mathur Vivek Kumar Pandey Poonam Kakkar Source Type: research

Antiandrogenic activity of Riboflavin 5'-phosphate (FMN) in 22Rv1 and LNCaP human prostate cancer cell lines
In this study, the antiandrogenic effects of FMN were investigated in 22Rv1 and LNCaP prostate cancer cells. FMN inhibited dihydrotestosterone (DHT)-induced protein expression of androgen receptor in 22Rv1cells. In another prostate cancer LNCaP cells, FMN decreased the protein level of DHT-induced prostate specific antigen (PSA). In addition, FMN downregulated DHT-induced mRNA expression of androgen regulated genes in both cell lines, showing less prominent inhibition in 22Rv1cells where androgen receptor had been significantly decreased by FMN. FMN was found to bind androgen receptor, demonstrating that it acted as a comp...
Source: European Journal of Pharmacology - January 9, 2022 Category: Drugs & Pharmacology Authors: Yun-Ho Choi Jaeyoon Kim Jae Young Shin Nae-Gyu Kang Sanghwa Lee Source Type: research

γ-mangostin attenuates amyloid-β42-induced neuroinflammation and oxidative stress in microglia-like BV2 cells via the mitogen-activated protein kinases signaling pathway
CONCLUSION: This study demonstrated that γ-mangostin could attenuate OS and inflammation resulting from Aβ42 oligomers, which also protect neurons against toxic medium-induced injury, suggesting that it may exert a protective effect in AD.PMID:34998794 | DOI:10.1016/j.ejphar.2022.174744 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - January 9, 2022 Category: Drugs & Pharmacology Authors: Chaojun Kong Longfei Jia Jianping Jia Source Type: research

Isoorientin protects lipopolysaccharide-induced acute lung injury in mice via modulating Keap1/Nrf2-HO-1 and NLRP3 inflammasome pathways
Eur J Pharmacol. 2022 Jan 6;917:174748. doi: 10.1016/j.ejphar.2022.174748. Online ahead of print.ABSTRACTAcute lung injury (ALI) is a pulmonary disease with high mortality. The present study investigated the protective effect of isoorientin (ISO) on lipopolysaccharide (LPS)-induced ALI compared with Thalictrum minus L. (TML). The experimental ALI was achieved by LPS via endotracheal drip, ISO and TML (40 mg/kg) were administered orally 1 h prior to LPS. ISO treatment significantly protected mice from ALI and exhibited similar efficacy as TML. Administration of ISO markedly corrected weight loss and improved lung pathologic...
Source: European Journal of Pharmacology - January 9, 2022 Category: Drugs & Pharmacology Authors: Lu Zhang Xiao-Zhou Zhu Rentsen Badamjav Jia-Zhi Zhang Jun-Ping Kou Bo-Yang Yu Fang Li Source Type: research

Ginsenoside Rg1 ameliorated experimental colitis by regulating the balance of M1/M2 macrophage polarization and the homeostasis of intestinal flora
Eur J Pharmacol. 2022 Jan 6:174742. doi: 10.1016/j.ejphar.2022.174742. Online ahead of print.ABSTRACTAberrant M1/M2 macrophage polarization and dysbiosis are involved in the pathogenesis of ulcerative colitis (UC). Ginsenoside Rg1 exhibits optimal immunomodulatory and anti-inflammatory effects in treating UC of humans and animals, but the action mechanism through the regulation of M1/M2 macrophage polarization and intestinal flora composition remain unclear. Here, experimental colitis was induced in BALB/c mice using dextran sulfate sodium, and Rock1 inhibitor Y27632 was used to explore the action mechanism of ginsenoside ...
Source: European Journal of Pharmacology - January 9, 2022 Category: Drugs & Pharmacology Authors: Jian Long Xue-Ke Liu Zeng-Ping Kang Meng-Xue Wang Hai-Mei Zhao Jia-Qi Huang Qiu-Ping Xiao Duan-Yong Liu You-Bao Zhong Source Type: research

Corrigendum to "siRNA: Mechanism of action, challenges, and therapeutic approaches" [Eur. J. Pharmacol. 905 (2021) 174178]
Eur J Pharmacol. 2022 Jan 5:174741. doi: 10.1016/j.ejphar.2022.174741. Online ahead of print.NO ABSTRACTPMID:34998574 | DOI:10.1016/j.ejphar.2022.174741 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - January 9, 2022 Category: Drugs & Pharmacology Authors: Walhan Alshaer Hadil Zureigat Arwa Al Karaki Abdulfattah Al-Kadash Lobna Gharaibeh Ma'mon M Hatmal Alaa A A Aljabali Abdalla Awidi Source Type: research

Role of high-fat diet on letrozole-induced polycystic ovarian syndrome in rats
Eur J Pharmacol. 2022 Jan 5;917:174746. doi: 10.1016/j.ejphar.2022.174746. Online ahead of print.ABSTRACTPolycystic ovary syndrome (PCOS) is one of the most prevalent hormonal disorders in women of reproductive age. Letrozole (LET)-induced PCOS is a good model but has drawbacks such as the absence of metabolic changes. Hence, in the present study, we aimed to develop a new animal model combining a high-fat diet (HFD) and LET. Female Wistar rats were divided into a control group, LET group, and LET + HFD (45% energy from fat) group. Compared with the control group, the LET and LET + HFD groups showed ovarian cysts and eleva...
Source: European Journal of Pharmacology - January 9, 2022 Category: Drugs & Pharmacology Authors: Nazia Begum Kandavalli Manipriya B Veeresh Source Type: research

Endoplasmic reticulum stress-dependent activation of TRB3-FoxO1 signaling pathway exacerbates hyperglycemic nephrotoxicity: Protection accorded by naringenin
This study unravels the critical role of Tribbles 3 (TRB3)-Forkhead box O1 (FoxO1) signaling pathway during hyperglycemic renal toxicity. It also uncovers the novel role of Naringenin, a flavanone, in regulating ER stress in proximal tubular cells, NRK 52E, and kidneys of streptozotocin/nicotinamide induced experimental diabetic Wistar rats. Results demonstrate that expression of ER stress marker proteins including phosphorylated protein kinase ER like kinase (p-PERK), phosphorylated eukaryotic Initiation Factor 2α (p-eIF2α), X Box Binding Protein 1 spliced (XBP1s), Activating Transcription Factor 4 (ATF4) and ...
Source: European Journal of Pharmacology - January 9, 2022 Category: Drugs & Pharmacology Authors: Mohammad Fareed Khan Alpana Mathur Vivek Kumar Pandey Poonam Kakkar Source Type: research

Antiandrogenic activity of Riboflavin 5'-phosphate (FMN) in 22Rv1 and LNCaP human prostate cancer cell lines
In this study, the antiandrogenic effects of FMN were investigated in 22Rv1 and LNCaP prostate cancer cells. FMN inhibited dihydrotestosterone (DHT)-induced protein expression of androgen receptor in 22Rv1cells. In another prostate cancer LNCaP cells, FMN decreased the protein level of DHT-induced prostate specific antigen (PSA). In addition, FMN downregulated DHT-induced mRNA expression of androgen regulated genes in both cell lines, showing less prominent inhibition in 22Rv1cells where androgen receptor had been significantly decreased by FMN. FMN was found to bind androgen receptor, demonstrating that it acted as a comp...
Source: European Journal of Pharmacology - January 9, 2022 Category: Drugs & Pharmacology Authors: Yun-Ho Choi Jaeyoon Kim Jae Young Shin Nae-Gyu Kang Sanghwa Lee Source Type: research

γ-mangostin attenuates amyloid-β42-induced neuroinflammation and oxidative stress in microglia-like BV2 cells via the mitogen-activated protein kinases signaling pathway
CONCLUSION: This study demonstrated that γ-mangostin could attenuate OS and inflammation resulting from Aβ42 oligomers, which also protect neurons against toxic medium-induced injury, suggesting that it may exert a protective effect in AD.PMID:34998794 | DOI:10.1016/j.ejphar.2022.174744 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - January 9, 2022 Category: Drugs & Pharmacology Authors: Chaojun Kong Longfei Jia Jianping Jia Source Type: research

Isoorientin protects lipopolysaccharide-induced acute lung injury in mice via modulating Keap1/Nrf2-HO-1 and NLRP3 inflammasome pathways
Eur J Pharmacol. 2022 Jan 6:174748. doi: 10.1016/j.ejphar.2022.174748. Online ahead of print.ABSTRACTAcute lung injury (ALI) is a pulmonary disease with high mortality. The present study investigated the protective effect of isoorientin (ISO) on lipopolysaccharide (LPS)-induced ALI compared with Thalictrum minus L. (TML). The experimental ALI was achieved by LPS via endotracheal drip, ISO and TML (40 mg/kg) were administered orally 1 h prior to LPS. ISO treatment significantly protected mice from ALI and exhibited similar efficacy as TML. Administration of ISO markedly corrected weight loss and improved lung pathological d...
Source: European Journal of Pharmacology - January 9, 2022 Category: Drugs & Pharmacology Authors: Lu Zhang Xiao-Zhou Zhu Rentsen Badamjav Jia-Zhi Zhang Jun-Ping Kou Bo-Yang Yu Fang Li Source Type: research

Ginsenoside Rg1 ameliorated experimental colitis by regulating the balance of M1/M2 macrophage polarization and the homeostasis of intestinal flora
Eur J Pharmacol. 2022 Jan 6:174742. doi: 10.1016/j.ejphar.2022.174742. Online ahead of print.ABSTRACTAberrant M1/M2 macrophage polarization and dysbiosis are involved in the pathogenesis of ulcerative colitis (UC). Ginsenoside Rg1 exhibits optimal immunomodulatory and anti-inflammatory effects in treating UC of humans and animals, but the action mechanism through the regulation of M1/M2 macrophage polarization and intestinal flora composition remain unclear. Here, experimental colitis was induced in BALB/c mice using dextran sulfate sodium, and Rock1 inhibitor Y27632 was used to explore the action mechanism of ginsenoside ...
Source: European Journal of Pharmacology - January 9, 2022 Category: Drugs & Pharmacology Authors: Jian Long Xue-Ke Liu Zeng-Ping Kang Meng-Xue Wang Hai-Mei Zhao Jia-Qi Huang Qiu-Ping Xiao Duan-Yong Liu You-Bao Zhong Source Type: research

Corrigendum to "Protective effects of cortex fraxini coumarines against oxonate-induced hyperuricemia and renal dysfunction in mice" [Eur. J. Pharmacol. 666 (2011) 196-204]
Eur J Pharmacol. 2022 Jan 4:174740. doi: 10.1016/j.ejphar.2022.174740. Online ahead of print.NO ABSTRACTPMID:34996605 | DOI:10.1016/j.ejphar.2022.174740 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - January 8, 2022 Category: Drugs & Pharmacology Authors: Jian-Mei Li Xian Zhang Xing Wang Yong-Chang Xie Ling-Dong Kong Source Type: research

Berbamine reduces body weight via suppression of small GTPase Rab8a activity and activation of paraventricular hypothalamic neurons in obese mice
Eur J Pharmacol. 2022 Jan 1;916:174679. doi: 10.1016/j.ejphar.2021.174679. Online ahead of print.ABSTRACTSmall GTPase Rab8a is involved in fat-specific protein 27 (Fsp27) mediated lipid droplet accumulation in adipocytes. By screening inhibitors of Rab8a GTPase from a natural compound library, berbamine (BBM), a marketing drug for treatment of leukopenia in China, was identified to inhibit the activity of Rab8a GTPase and block the differentiation of 3T3-L1 adipocytes. Animal study showed that BBM could reduce body weight, improved glucose and lipid metabolic homeostasis in high-fat diet-induced obesity (DIO) C57BL/6 mice ...
Source: European Journal of Pharmacology - January 4, 2022 Category: Drugs & Pharmacology Authors: Liufang Yin Lijun Zhang Lingling Luo Yalei Liu Fei Wang Yaru Feng Hongqing Wang Yongli Han Yingxuan Yan Cheng Huang Shengjie Fan Source Type: research