Oroxylin A inhibits the migration of hepatocellular carcinoma cells by inducing NAG-1 expression
Acta Pharmacol Sin. 2021 Jun 11. doi: 10.1038/s41401-021-00695-4. Online ahead of print.ABSTRACTHepatocellular carcinoma (HCC), the most prevalent liver cancer, is considered one of the most lethal malignancies with a dismal outcome mainly due to frequent intrahepatic and distant metastasis. In the present study, we demonstrated that oroxylin A, a natural product extracted from Scutellaria radix, significantly inhibits transforming growth factor-beta1 (TGF-β1)-induced epithelial-mesenchymal transition (EMT) and metastasis in HCC. Oroxylin A blocked the TGF-β1/Smad signaling via upregulating the non-steroidal anti...
Source: Acta Pharmacologica Sinica - June 12, 2021 Category: Drugs & Pharmacology Authors: Tong-Xin Huo Xiao-Ping Wang Zhou Yu Bo Kong Yuan He Qing-Long Guo Xiao-Bo Zhang Lei Qiang Source Type: research

Oroxylin A inhibits the migration of hepatocellular carcinoma cells by inducing NAG-1 expression
Acta Pharmacol Sin. 2021 Jun 11. doi: 10.1038/s41401-021-00695-4. Online ahead of print.ABSTRACTHepatocellular carcinoma (HCC), the most prevalent liver cancer, is considered one of the most lethal malignancies with a dismal outcome mainly due to frequent intrahepatic and distant metastasis. In the present study, we demonstrated that oroxylin A, a natural product extracted from Scutellaria radix, significantly inhibits transforming growth factor-beta1 (TGF-β1)-induced epithelial-mesenchymal transition (EMT) and metastasis in HCC. Oroxylin A blocked the TGF-β1/Smad signaling via upregulating the non-steroidal anti...
Source: Acta Pharmacologica Sinica - June 12, 2021 Category: Drugs & Pharmacology Authors: Tong-Xin Huo Xiao-Ping Wang Zhou Yu Bo Kong Yuan He Qing-Long Guo Xiao-Bo Zhang Lei Qiang Source Type: research

ATF3 contributes to brucine-triggered glioma cell ferroptosis via promotion of hydrogen peroxide and iron
In this study, we showed that brucine inhibited glioma cell growth in vitro and in vivo, which was paralleled by nuclear translocation of ATF3, lipid peroxidation, and increases of iron and H2O2. Furthermore, brucine-induced lipid peroxidation was inhibited or exacerbated when intracellular iron was chelated by deferoxamine (500 μM) or improved by ferric ammonium citrate (500 μM). Suppression of lipid peroxidation with lipophilic antioxidants ferrostatin-1 (50 μM) or liproxstatin-1 (30 μM) rescued brucine-induced glioma cell death. Moreover, knockdown of ATF3 prevented brucine-induced accumulation of iron and H...
Source: Acta Pharmacologica Sinica - June 11, 2021 Category: Drugs & Pharmacology Authors: Shan Lu Xuan-Zhong Wang Chuan He Lei Wang Shi-Peng Liang Chong-Cheng Wang Chen Li Tian-Fei Luo Chun-Sheng Feng Zhen-Chuan Wang Guang-Fan Chi Peng-Fei Ge Source Type: research

ATF3 contributes to brucine-triggered glioma cell ferroptosis via promotion of hydrogen peroxide and iron
In this study, we showed that brucine inhibited glioma cell growth in vitro and in vivo, which was paralleled by nuclear translocation of ATF3, lipid peroxidation, and increases of iron and H2O2. Furthermore, brucine-induced lipid peroxidation was inhibited or exacerbated when intracellular iron was chelated by deferoxamine (500 μM) or improved by ferric ammonium citrate (500 μM). Suppression of lipid peroxidation with lipophilic antioxidants ferrostatin-1 (50 μM) or liproxstatin-1 (30 μM) rescued brucine-induced glioma cell death. Moreover, knockdown of ATF3 prevented brucine-induced accumulation of iron and H...
Source: Acta Pharmacologica Sinica - June 11, 2021 Category: Drugs & Pharmacology Authors: Shan Lu Xuan-Zhong Wang Chuan He Lei Wang Shi-Peng Liang Chong-Cheng Wang Chen Li Tian-Fei Luo Chun-Sheng Feng Zhen-Chuan Wang Guang-Fan Chi Peng-Fei Ge Source Type: research

Oroxylin A inhibits the migration of hepatocellular carcinoma cells by inducing NAG-1 expression
Acta Pharmacologica Sinica, Published online: 11 June 2021; doi:10.1038/s41401-021-00695-4Oroxylin A inhibits the migration of hepatocellular carcinoma cells by inducing NAG-1 expression (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - June 11, 2021 Category: Drugs & Pharmacology Authors: Tong-xin Huo Xiao-ping Wang Zhou Yu Bo Kong Yuan He Qing-long Guo Xiao-bo Zhang Lei Qiang Source Type: research

Role of TRPM2 in brain tumours and potential as a drug target
This article reviews the current understanding of TRPM2 in the context of brain tumours and overviews the effects of potential drug therapies targeting TRPM2 including hydrogen peroxide (H2O2), curcumin, docetaxel and selenium, paclitaxel and resveratrol, and botulinum toxin. It is long withstanding knowledge that gliomas are difficult to treat effectively, therefore investigating TRPM2 as a potential therapeutic target for brain tumours may be of considerable interest in the fields of ion channels and pharmacology.PMID:34108651 | DOI:10.1038/s41401-021-00679-4 (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - June 10, 2021 Category: Drugs & Pharmacology Authors: Delphine Ji Zheng-Wei Luo Andrea Ovcjak Rahmah Alanazi Mei-Hua Bao Zhong-Ping Feng Hong-Shuo Sun Source Type: research

Role of TRPM2 in brain tumours and potential as a drug target
This article reviews the current understanding of TRPM2 in the context of brain tumours and overviews the effects of potential drug therapies targeting TRPM2 including hydrogen peroxide (H2O2), curcumin, docetaxel and selenium, paclitaxel and resveratrol, and botulinum toxin. It is long withstanding knowledge that gliomas are difficult to treat effectively, therefore investigating TRPM2 as a potential therapeutic target for brain tumours may be of considerable interest in the fields of ion channels and pharmacology.PMID:34108651 | DOI:10.1038/s41401-021-00679-4 (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - June 10, 2021 Category: Drugs & Pharmacology Authors: Delphine Ji Zheng-Wei Luo Andrea Ovcjak Rahmah Alanazi Mei-Hua Bao Zhong-Ping Feng Hong-Shuo Sun Source Type: research

ATF3 contributes to brucine-triggered glioma cell ferroptosis via promotion of hydrogen peroxide and iron
Acta Pharmacologica Sinica, Published online: 10 June 2021; doi:10.1038/s41401-021-00700-wATF3 contributes to brucine-triggered glioma cell ferroptosis via promotion of hydrogen peroxide and iron (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - June 10, 2021 Category: Drugs & Pharmacology Authors: Shan Lu Xuan-zhong Wang Chuan He Lei Wang Shi-peng Liang Chong-cheng Wang Chen Li Tian-fei Luo Chun-sheng Feng Zhen-chuan Wang Guang-fan Chi Peng-fei Ge Source Type: research

Epac activation ameliorates tubulointerstitial inflammation in diabetic nephropathy
Acta Pharmacol Sin. 2021 Jun 8. doi: 10.1038/s41401-021-00689-2. Online ahead of print.ABSTRACTTubulointerstitial inflammation plays an important role in the progression of diabetic nephropathy (DN), and tubular epithelial cells (TECs) are crucial promoters of the inflammatory cascade. Exchange protein activated by cAMP (Epac) has been shown to suppress the angiotensin II (Ang-II)-induced release of inflammatory cytokines in tubular cells. However, the role of Epac in TEC-mediated tubulointerstitial inflammation in DN remains unknown. We found that administering the Epac agonist 8-pCPT-2'-O-Me-cAMP (8-O-cAMP) to db/db mice...
Source: Acta Pharmacologica Sinica - June 9, 2021 Category: Drugs & Pharmacology Authors: Wen-Xia Yang Yu Liu Shu-Min Zhang Hua-Fen Wang Yi-Fei Liu Jia-Lu Liu Xiao-Hui Li Meng-Ru Zeng Yu-Zhang Han Fu-You Liu Lin Sun Li Xiao Source Type: research

Inhibition of Nav1.7 channel by a novel blocker QLS-81 for alleviation of neuropathic pain
Acta Pharmacol Sin. 2021 Jun 8. doi: 10.1038/s41401-021-00682-9. Online ahead of print.ABSTRACTVoltage-gated sodium channel Nav1.7 robustly expressed in peripheral nociceptive neurons has been considered as a therapeutic target for chronic pain, but there is no selective Nav1.7 inhibitor available for therapy of chronic pain. Ralfinamide has shown anti-nociceptive activity in animal models of inflammatory and neuropathic pain and is currently under phase III clinical trial for neuropathic pain. Based on ralfinamide, a novel small molecule (S)-2-((3-(4-((2-fluorobenzyl) oxy) phenyl) propyl) amino) propanamide (QLS-81) was s...
Source: Acta Pharmacologica Sinica - June 9, 2021 Category: Drugs & Pharmacology Authors: He-Ling Niu Ya-Ni Liu Deng-Qi Xue Li-Ying Dong Hui-Jie Liu Jing Wang Yi-Lin Zheng An-Ruo Zou Li-Ming Shao KeWei Wang Source Type: research

Rg1 exerts protective effect in CPZ-induced demyelination mouse model via inhibiting CXCL10-mediated glial response
In conclusion, CXCL10 mediates the protective role of Rg1 in CPZ-induced demyelination mouse model. This study provides new insight into potential disease-modifying therapies for myelin abnormalities.PMID:34103690 | DOI:10.1038/s41401-021-00696-3 (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - June 9, 2021 Category: Drugs & Pharmacology Authors: Yi-Xiao Dong Shi-Feng Chu Sha-Sha Wang Ya-Juan Tian Wen-Bin He Yu-Sheng Du Zhen-Zhen Wang Xu Yan Zhao Zhang Nai-Hong Chen Source Type: research

Role of TRPM2 in brain tumours and potential as a drug target
Acta Pharmacologica Sinica, Published online: 09 June 2021; doi:10.1038/s41401-021-00679-4The role of TRPM2 in the pathways of various inhibitors and activators. (a) A schematic illustration of the TRPM2 channel which includes 4 N-terminal MHR domains, six transmembrane helices labelled S1–S6, a TRP domain, a coiled-coil domain and NUDT9-H domain. (b) BTX increases mitochondrial ROS leading to increased caspase 9 and 3. (c) The pathway of TNF-α, increasing ROS, activating the caspase 8 cascade, increasing ROS in the mitochondria, finally leading to increased PARP. PARP converts NAD+ to ADPR, activating TRPM2 at...
Source: Acta Pharmacologica Sinica - June 9, 2021 Category: Drugs & Pharmacology Authors: Delphine Ji Zheng-wei Luo Andrea Ovcjak Rahmah Alanazi Mei-Hua Bao Zhong-Ping Feng Hong-Shuo Sun Source Type: research

Epac activation ameliorates tubulointerstitial inflammation in diabetic nephropathy
Acta Pharmacologica Sinica, Published online: 08 June 2021; doi:10.1038/s41401-021-00689-2Epac activation ameliorates tubulointerstitial inflammation in diabetic nephropathy (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - June 8, 2021 Category: Drugs & Pharmacology Authors: Wen-xia Yang Yu Liu Shu-min Zhang Hua-fen Wang Yi-fei Liu Jia-lu Liu Xiao-hui Li Meng-ru Zeng Yu-zhang Han Fu-you Liu Lin Sun Li Xiao Source Type: research

Inhibition of Nav1.7 channel by a novel blocker QLS-81 for alleviation of neuropathic pain
Acta Pharmacologica Sinica, Published online: 08 June 2021; doi:10.1038/s41401-021-00682-9Inhibition of Nav1.7 channel by a novel blocker QLS-81 for alleviation of neuropathic pain (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - June 8, 2021 Category: Drugs & Pharmacology Authors: He-ling Niu Ya-ni Liu Deng-qi Xue Li-ying Dong Hui-jie Liu Jing Wang Yi-lin Zheng An-ruo Zou Li-ming Shao KeWei Wang Source Type: research

Rg1 exerts protective effect in CPZ-induced demyelination mouse model via inhibiting CXCL10-mediated glial response
Acta Pharmacologica Sinica, Published online: 08 June 2021; doi:10.1038/s41401-021-00696-3Rg1 exerts protective effect in CPZ-induced demyelination mouse model via inhibiting CXCL10-mediated glial response (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - June 8, 2021 Category: Drugs & Pharmacology Authors: Yi-xiao Dong Shi-feng Chu Sha-sha Wang Ya-juan Tian Wen-bin He Yu-sheng Du Zhen-zhen Wang Xu Yan Zhao Zhang Nai-hong Chen Source Type: research

Targeting HMGB1 for the treatment of sepsis and sepsis-induced organ injury
Acta Pharmacol Sin. 2021 May 26. doi: 10.1038/s41401-021-00676-7. Online ahead of print.ABSTRACTHigh mobility group box 1 (HMGB1) is a ubiquitous nuclear protein that is present in almost all cells and regulates the activity of innate immune responses in both intracellular and extracellular settings. Current evidence suggests that HMGB1 plays a pivotal role in human pathological and pathophysiological processes such as the inflammatory response, immune reactions, cell migration, aging, and cell death. Sepsis is a systemic inflammatory response syndrome (SIRS) that occurs in hosts in response to microbial infections with a ...
Source: Acta Pharmacologica Sinica - May 27, 2021 Category: Drugs & Pharmacology Authors: Chao Deng Lin Zhao Zhi Yang Jia-Jia Shang Chang-Yu Wang Ming-Zhi Shen Shuai Jiang Tian Li Wen-Cheng Di Ying Chen He Li Ye-Dong Cheng Yang Yang Source Type: research

Targeting HMGB1 for the treatment of sepsis and sepsis-induced organ injury
Acta Pharmacol Sin. 2021 May 26. doi: 10.1038/s41401-021-00676-7. Online ahead of print.ABSTRACTHigh mobility group box 1 (HMGB1) is a ubiquitous nuclear protein that is present in almost all cells and regulates the activity of innate immune responses in both intracellular and extracellular settings. Current evidence suggests that HMGB1 plays a pivotal role in human pathological and pathophysiological processes such as the inflammatory response, immune reactions, cell migration, aging, and cell death. Sepsis is a systemic inflammatory response syndrome (SIRS) that occurs in hosts in response to microbial infections with a ...
Source: Acta Pharmacologica Sinica - May 27, 2021 Category: Drugs & Pharmacology Authors: Chao Deng Lin Zhao Zhi Yang Jia-Jia Shang Chang-Yu Wang Ming-Zhi Shen Shuai Jiang Tian Li Wen-Cheng Di Ying Chen He Li Ye-Dong Cheng Yang Yang Source Type: research

Targeting HMGB1 for the treatment of sepsis and sepsis-induced organ injury
Acta Pharmacol Sin. 2021 May 26. doi: 10.1038/s41401-021-00676-7. Online ahead of print.ABSTRACTHigh mobility group box 1 (HMGB1) is a ubiquitous nuclear protein that is present in almost all cells and regulates the activity of innate immune responses in both intracellular and extracellular settings. Current evidence suggests that HMGB1 plays a pivotal role in human pathological and pathophysiological processes such as the inflammatory response, immune reactions, cell migration, aging, and cell death. Sepsis is a systemic inflammatory response syndrome (SIRS) that occurs in hosts in response to microbial infections with a ...
Source: Acta Pharmacologica Sinica - May 27, 2021 Category: Drugs & Pharmacology Authors: Chao Deng Lin Zhao Zhi Yang Jia-Jia Shang Chang-Yu Wang Ming-Zhi Shen Shuai Jiang Tian Li Wen-Cheng Di Ying Chen He Li Ye-Dong Cheng Yang Yang Source Type: research

Targeting HMGB1 for the treatment of sepsis and sepsis-induced organ injury
Acta Pharmacol Sin. 2021 May 26. doi: 10.1038/s41401-021-00676-7. Online ahead of print.ABSTRACTHigh mobility group box 1 (HMGB1) is a ubiquitous nuclear protein that is present in almost all cells and regulates the activity of innate immune responses in both intracellular and extracellular settings. Current evidence suggests that HMGB1 plays a pivotal role in human pathological and pathophysiological processes such as the inflammatory response, immune reactions, cell migration, aging, and cell death. Sepsis is a systemic inflammatory response syndrome (SIRS) that occurs in hosts in response to microbial infections with a ...
Source: Acta Pharmacologica Sinica - May 27, 2021 Category: Drugs & Pharmacology Authors: Chao Deng Lin Zhao Zhi Yang Jia-Jia Shang Chang-Yu Wang Ming-Zhi Shen Shuai Jiang Tian Li Wen-Cheng Di Ying Chen He Li Ye-Dong Cheng Yang Yang Source Type: research

Targeting HMGB1 for the treatment of sepsis and sepsis-induced organ injury
Acta Pharmacol Sin. 2021 May 26. doi: 10.1038/s41401-021-00676-7. Online ahead of print.ABSTRACTHigh mobility group box 1 (HMGB1) is a ubiquitous nuclear protein that is present in almost all cells and regulates the activity of innate immune responses in both intracellular and extracellular settings. Current evidence suggests that HMGB1 plays a pivotal role in human pathological and pathophysiological processes such as the inflammatory response, immune reactions, cell migration, aging, and cell death. Sepsis is a systemic inflammatory response syndrome (SIRS) that occurs in hosts in response to microbial infections with a ...
Source: Acta Pharmacologica Sinica - May 27, 2021 Category: Drugs & Pharmacology Authors: Chao Deng Lin Zhao Zhi Yang Jia-Jia Shang Chang-Yu Wang Ming-Zhi Shen Shuai Jiang Tian Li Wen-Cheng Di Ying Chen He Li Ye-Dong Cheng Yang Yang Source Type: research

Targeting HMGB1 for the treatment of sepsis and sepsis-induced organ injury
Acta Pharmacol Sin. 2021 May 26. doi: 10.1038/s41401-021-00676-7. Online ahead of print.ABSTRACTHigh mobility group box 1 (HMGB1) is a ubiquitous nuclear protein that is present in almost all cells and regulates the activity of innate immune responses in both intracellular and extracellular settings. Current evidence suggests that HMGB1 plays a pivotal role in human pathological and pathophysiological processes such as the inflammatory response, immune reactions, cell migration, aging, and cell death. Sepsis is a systemic inflammatory response syndrome (SIRS) that occurs in hosts in response to microbial infections with a ...
Source: Acta Pharmacologica Sinica - May 27, 2021 Category: Drugs & Pharmacology Authors: Chao Deng Lin Zhao Zhi Yang Jia-Jia Shang Chang-Yu Wang Ming-Zhi Shen Shuai Jiang Tian Li Wen-Cheng Di Ying Chen He Li Ye-Dong Cheng Yang Yang Source Type: research

Targeting HMGB1 for the treatment of sepsis and sepsis-induced organ injury
Acta Pharmacol Sin. 2021 May 26. doi: 10.1038/s41401-021-00676-7. Online ahead of print.ABSTRACTHigh mobility group box 1 (HMGB1) is a ubiquitous nuclear protein that is present in almost all cells and regulates the activity of innate immune responses in both intracellular and extracellular settings. Current evidence suggests that HMGB1 plays a pivotal role in human pathological and pathophysiological processes such as the inflammatory response, immune reactions, cell migration, aging, and cell death. Sepsis is a systemic inflammatory response syndrome (SIRS) that occurs in hosts in response to microbial infections with a ...
Source: Acta Pharmacologica Sinica - May 27, 2021 Category: Drugs & Pharmacology Authors: Chao Deng Lin Zhao Zhi Yang Jia-Jia Shang Chang-Yu Wang Ming-Zhi Shen Shuai Jiang Tian Li Wen-Cheng Di Ying Chen He Li Ye-Dong Cheng Yang Yang Source Type: research

Targeting HMGB1 for the treatment of sepsis and sepsis-induced organ injury
Acta Pharmacol Sin. 2021 May 26. doi: 10.1038/s41401-021-00676-7. Online ahead of print.ABSTRACTHigh mobility group box 1 (HMGB1) is a ubiquitous nuclear protein that is present in almost all cells and regulates the activity of innate immune responses in both intracellular and extracellular settings. Current evidence suggests that HMGB1 plays a pivotal role in human pathological and pathophysiological processes such as the inflammatory response, immune reactions, cell migration, aging, and cell death. Sepsis is a systemic inflammatory response syndrome (SIRS) that occurs in hosts in response to microbial infections with a ...
Source: Acta Pharmacologica Sinica - May 27, 2021 Category: Drugs & Pharmacology Authors: Chao Deng Lin Zhao Zhi Yang Jia-Jia Shang Chang-Yu Wang Ming-Zhi Shen Shuai Jiang Tian Li Wen-Cheng Di Ying Chen He Li Ye-Dong Cheng Yang Yang Source Type: research

Targeting HMGB1 for the treatment of sepsis and sepsis-induced organ injury
Acta Pharmacol Sin. 2021 May 26. doi: 10.1038/s41401-021-00676-7. Online ahead of print.ABSTRACTHigh mobility group box 1 (HMGB1) is a ubiquitous nuclear protein that is present in almost all cells and regulates the activity of innate immune responses in both intracellular and extracellular settings. Current evidence suggests that HMGB1 plays a pivotal role in human pathological and pathophysiological processes such as the inflammatory response, immune reactions, cell migration, aging, and cell death. Sepsis is a systemic inflammatory response syndrome (SIRS) that occurs in hosts in response to microbial infections with a ...
Source: Acta Pharmacologica Sinica - May 27, 2021 Category: Drugs & Pharmacology Authors: Chao Deng Lin Zhao Zhi Yang Jia-Jia Shang Chang-Yu Wang Ming-Zhi Shen Shuai Jiang Tian Li Wen-Cheng Di Ying Chen He Li Ye-Dong Cheng Yang Yang Source Type: research

Targeting HMGB1 for the treatment of sepsis and sepsis-induced organ injury
Acta Pharmacol Sin. 2021 May 26. doi: 10.1038/s41401-021-00676-7. Online ahead of print.ABSTRACTHigh mobility group box 1 (HMGB1) is a ubiquitous nuclear protein that is present in almost all cells and regulates the activity of innate immune responses in both intracellular and extracellular settings. Current evidence suggests that HMGB1 plays a pivotal role in human pathological and pathophysiological processes such as the inflammatory response, immune reactions, cell migration, aging, and cell death. Sepsis is a systemic inflammatory response syndrome (SIRS) that occurs in hosts in response to microbial infections with a ...
Source: Acta Pharmacologica Sinica - May 27, 2021 Category: Drugs & Pharmacology Authors: Chao Deng Lin Zhao Zhi Yang Jia-Jia Shang Chang-Yu Wang Ming-Zhi Shen Shuai Jiang Tian Li Wen-Cheng Di Ying Chen He Li Ye-Dong Cheng Yang Yang Source Type: research

Targeting HMGB1 for the treatment of sepsis and sepsis-induced organ injury
Acta Pharmacol Sin. 2021 May 26. doi: 10.1038/s41401-021-00676-7. Online ahead of print.ABSTRACTHigh mobility group box 1 (HMGB1) is a ubiquitous nuclear protein that is present in almost all cells and regulates the activity of innate immune responses in both intracellular and extracellular settings. Current evidence suggests that HMGB1 plays a pivotal role in human pathological and pathophysiological processes such as the inflammatory response, immune reactions, cell migration, aging, and cell death. Sepsis is a systemic inflammatory response syndrome (SIRS) that occurs in hosts in response to microbial infections with a ...
Source: Acta Pharmacologica Sinica - May 27, 2021 Category: Drugs & Pharmacology Authors: Chao Deng Lin Zhao Zhi Yang Jia-Jia Shang Chang-Yu Wang Ming-Zhi Shen Shuai Jiang Tian Li Wen-Cheng Di Ying Chen He Li Ye-Dong Cheng Yang Yang Source Type: research

Amygdala dynorphin/ κ opioid receptor system modulates depressive-like behavior in mice following chronic social defeat stress
In this study we investigated the role of dynorphin/κ opioid receptor system in the development of depression. Mice were subjected to chronic social defeat stress for 14 days. Chronic social defeat stress induced significant social avoidance in mice characterized by decreased time duration in the interaction zone and increased time duration in the corner zone. Pre-administration of a κ opioid receptor antagonist norBNI (10 mg/kg, i.p.) could prevent the development of social avoidance induced by chronic social defeat stress. Social avoidance was not observed in κ opioid receptor knockout mice subjected to...
Source: Acta Pharmacologica Sinica - May 26, 2021 Category: Drugs & Pharmacology Authors: Gui-Ying Zan Xiang Sun Yu-Jun Wang Rui Liu Chen-Yao Wang Wei-Jia Du Liu-Bin Guo Jing-Rui Chai Qing-Lin Li Zhi-Qiang Liu Jing-Gen Liu Source Type: research

Exogenous glutathione exerts a therapeutic effect in ischemic stroke rats by interacting with intrastriatal dopamine
Acta Pharmacol Sin. 2021 May 25. doi: 10.1038/s41401-021-00650-3. Online ahead of print.ABSTRACTWe previously showed that oral administration of exogenous glutathione (GSH) exerted a direct and/or indirect therapeutic effect on ischemic stroke rats, but the underlying mechanisms remain elusive. In the current study, we conducted a quantitative proteomic analysis to explore the pathways mediating the therapeutic effect of GSH in cerebral ischemia/reperfusion (I/R) model rats. Rats were subjected to middle cerebral artery occlusion (MCAO) for 2 h followed by reperfusion. The rats were treated with GSH (250 mg/kg, ig) or levo...
Source: Acta Pharmacologica Sinica - May 26, 2021 Category: Drugs & Pharmacology Authors: He Wang Yi-Sha Du Wen-Shuo Xu Chang-Jian Li Hong Sun Kang-Rui Hu Yuan-Zhuo Hu Teng-Jie Yu Hui-Min Guo Lin Xie Guang-Ji Wang Yan Liang Source Type: research

Kanglexin delays heart aging by promoting mitophagy
In conclusion, this study identifies KLX and emodin as effective anti-heart aging drugs that activate Parkin-mediated mitophagy and outlines their putative therapeutic importance.PMID:34035486 | DOI:10.1038/s41401-021-00686-5 (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - May 26, 2021 Category: Drugs & Pharmacology Authors: Hui-Min Li Xin Liu Zi-Yu Meng Lei Wang Li-Min Zhao Hui Chen Zhi-Xia Wang Hao Cui Xue-Qing Tang Xiao-Han Li Wei-Na Han Xue Bai Yuan Lin Heng Liu Yong Zhang Bao-Feng Yang Source Type: research

Upregulation of wild-type p53 by small molecule-induced elevation of NQO1 in non-small cell lung cancer cells
Acta Pharmacol Sin. 2021 May 25. doi: 10.1038/s41401-021-00691-8. Online ahead of print.ABSTRACTThe tumor suppressor p53 is usually inactivated by somatic mutations in malignant neoplasms, and its reactivation represents an attractive therapeutic strategy for cancers. Here, we reported that a new quinolone compound RYL-687 significantly inhibited non-small cell lung cancer (NSCLC) cells which express wild type (wt) p53, in contract to its much weaker cytotoxicity on cells with mutant p53. RYL-687 upregulated p53 in cells with wt but not mutant p53, and ectopic expression of wt p53 significantly enhanced the anti-NSCLC acti...
Source: Acta Pharmacologica Sinica - May 26, 2021 Category: Drugs & Pharmacology Authors: Hong Yu Hong-Ying Gao Hua Guo Gui-Zhen Wang Yi-Qing Yang Qian Hu Li-Jun Liang Qun Zhao Da-Wei Xie Yu Rao Guang-Biao Zhou Source Type: research

Furmonertinib (Alflutinib, AST2818) is a potential positive control drug comparable to rifampin for evaluation of CYP3A4 induction in sandwich-cultured primary human hepatocytes
This study investigated two important evaluation criteria of CYP3A4 induction by furmonertinib through quantitative proteomics and probe metabolite formation: simultaneous (1) protein expression and (2) enzyme activity with sandwich-cultured primary human hepatocytes in the same well of cell culture plates. Results confirmed that furmonertinib was a potent CYP3A4 inducer comparable with rifampin and could be used as a positive model drug in in vitro studies to evaluate the induction potential of other drug candidates in preclinical studies. In addition, inconsistencies were observed between the protein expression and enzym...
Source: Acta Pharmacologica Sinica - May 26, 2021 Category: Drugs & Pharmacology Authors: Ya-Li Wu Ya-Ru Xue Zi-Tao Guo Zhen-Dong Chen Xin-Yu Ge Da-Fang Zhong Xing-Xing Diao Source Type: research

Targeting HMGB1 for the treatment of sepsis and sepsis-induced organ injury
Acta Pharmacologica Sinica, Published online: 26 May 2021; doi:10.1038/s41401-021-00676-7Targeting HMGB1 for the treatment of sepsis and sepsis-induced organ injury (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - May 26, 2021 Category: Drugs & Pharmacology Authors: Chao Deng Lin Zhao Zhi Yang Jia-jia Shang Chang-yu Wang Ming-zhi Shen Shuai Jiang Tian Li Wen-cheng Di Ying Chen He Li Ye-dong Cheng Yang Yang Source Type: research

Furmonertinib (Alflutinib, AST2818) is a potential positive control drug comparable to rifampin for evaluation of CYP3A4 induction in sandwich-cultured primary human hepatocytes
Acta Pharmacologica Sinica, Published online: 25 May 2021; doi:10.1038/s41401-021-00692-7Furmonertinib (Alflutinib, AST2818) is a potential positive control drug comparable to rifampin for evaluation of CYP3A4 induction in sandwich-cultured primary human hepatocytes (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - May 25, 2021 Category: Drugs & Pharmacology Authors: Ya-li Wu Ya-ru Xue Zi-tao Guo Zhen-dong Chen Xin-yu Ge Da-fang Zhong Xing-xing Diao Source Type: research

Kanglexin delays heart aging by promoting mitophagy
Acta Pharmacologica Sinica, Published online: 25 May 2021; doi:10.1038/s41401-021-00686-5Kanglexin delays heart aging by promoting mitophagy (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - May 25, 2021 Category: Drugs & Pharmacology Authors: Hui-min Li Xin Liu Zi-yu Meng Lei Wang Li-min Zhao Hui Chen Zhi-xia Wang Hao Cui Xue-qing Tang Xiao-han Li Wei-na Han Xue Bai Yuan Lin Heng Liu Yong Zhang Bao-feng Yang Source Type: research

Exogenous glutathione exerts a therapeutic effect in ischemic stroke rats by interacting with intrastriatal dopamine
Acta Pharmacologica Sinica, Published online: 25 May 2021; doi:10.1038/s41401-021-00650-3Exogenous glutathione exerts a therapeutic effect in ischemic stroke rats by interacting with intrastriatal dopamine (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - May 25, 2021 Category: Drugs & Pharmacology Authors: He Wang Yi-sha Du Wen-shuo Xu Chang-jian Li Hong Sun Kang-rui Hu Yuan-zhuo Hu Teng-jie Yu Hui-min Guo Lin Xie Guang-ji Wang Yan Liang Source Type: research

Upregulation of wild-type p53 by small molecule-induced elevation of NQO1 in non-small cell lung cancer cells
Acta Pharmacologica Sinica, Published online: 25 May 2021; doi:10.1038/s41401-021-00691-8Upregulation of wild-type p53 by small molecule-induced elevation of NQO1 in non-small cell lung cancer cells (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - May 25, 2021 Category: Drugs & Pharmacology Authors: Hong Yu Hong-ying Gao Hua Guo Gui-zhen Wang Yi-qing Yang Qian Hu Li-jun Liang Qun Zhao Da-wei Xie Yu Rao Guang-biao Zhou Source Type: research

Amygdala dynorphin/κ opioid receptor system modulates depressive-like behavior in mice following chronic social defeat stress
Acta Pharmacologica Sinica, Published online: 25 May 2021; doi:10.1038/s41401-021-00677-6Amygdala dynorphin/κ opioid receptor system modulates depressive-like behavior in mice following chronic social defeat stress (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - May 25, 2021 Category: Drugs & Pharmacology Authors: Gui-ying Zan Xiang Sun Yu-jun Wang Rui Liu Chen-yao Wang Wei-jia Du Liu-bin Guo Jing-rui Chai Qing-lin Li Zhi-qiang Liu Jing-gen Liu Source Type: research

AKR1C1 connects autophagy and oxidative stress by interacting with SQSTM1 in a catalytic-independent manner
Acta Pharmacol Sin. 2021 May 20. doi: 10.1038/s41401-021-00673-w. Online ahead of print.ABSTRACTTargeting autophagy might be a promising anticancer strategy; however, the dual roles of autophagy in cancer development and malignancy remain unclear. NSCLC (non-small cell lung cancer) cells harbour high levels of SQSTM1 (sequestosome 1), the autophagy receptor that is critical for the dual roles of autophagy. Therefore, mechanistic insights into SQSTM1 modulation may point towards better approaches to treat NSCLC. Herein, we used multiple autophagy flux models and autophagy readouts to show that aldo-keto reductase family 1 m...
Source: Acta Pharmacologica Sinica - May 21, 2021 Category: Drugs & Pharmacology Authors: Lin-Lin Chang Yue-Kang Li Chen-Xi Zhao Chen-Ming Zeng Fu-Jing Ge Jia-Min Du Wen-Zhou Zhang Pei-Hua Lu Qiao-Jun He Hong Zhu Bo Yang Source Type: research

Mitochondrial proteome of mouse oocytes and cisplatin-induced shifts in protein profile
Acta Pharmacol Sin. 2021 May 20. doi: 10.1038/s41401-021-00687-4. Online ahead of print.ABSTRACTMitochondria are essential organelles that provide energy for mammalian cells and participate in multiple functions, such as signal transduction, cellular differentiation, and regulation of apoptosis. Compared with the mitochondria in somatic cells, oocyte mitochondria have an additional level of importance since they are required for germ cell maturation, dysfunction in which can lead to severe inherited disorders. Thus, a systematic proteomic profile of oocyte mitochondria is urgently needed to support the basic and clinical r...
Source: Acta Pharmacologica Sinica - May 21, 2021 Category: Drugs & Pharmacology Authors: Na Zhang An-di Sun Si-Man Sun Rui Yang Yan-Yan Shi Qi-Long Wang Xin-Yu Li Ji-Hong Ma Wei Yue Bing-Teng Xie Jie Qiao Mo Li Source Type: research

Author Correction: Bmal1 inhibits phenotypic transformation of hepatic stellate cells in liver fibrosis via IDH1/ α-KG-mediated glycolysis
Acta Pharmacol Sin. 2021 May 20. doi: 10.1038/s41401-021-00685-6. Online ahead of print.NO ABSTRACTPMID:34017068 | DOI:10.1038/s41401-021-00685-6 (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - May 21, 2021 Category: Drugs & Pharmacology Authors: Lei Xu Tian-Yu Yang Yi-Wen Zhou Mei-Fei Wu Jie Shen Jie-Ling Cheng Qing-Xue Liu Shi-Yang Cao Jian-Qing Wang Lei Zhang Source Type: research

AKR1C1 connects autophagy and oxidative stress by interacting with SQSTM1 in a catalytic-independent manner
Acta Pharmacol Sin. 2021 May 20. doi: 10.1038/s41401-021-00673-w. Online ahead of print.ABSTRACTTargeting autophagy might be a promising anticancer strategy; however, the dual roles of autophagy in cancer development and malignancy remain unclear. NSCLC (non-small cell lung cancer) cells harbour high levels of SQSTM1 (sequestosome 1), the autophagy receptor that is critical for the dual roles of autophagy. Therefore, mechanistic insights into SQSTM1 modulation may point towards better approaches to treat NSCLC. Herein, we used multiple autophagy flux models and autophagy readouts to show that aldo-keto reductase family 1 m...
Source: Acta Pharmacologica Sinica - May 21, 2021 Category: Drugs & Pharmacology Authors: Lin-Lin Chang Yue-Kang Li Chen-Xi Zhao Chen-Ming Zeng Fu-Jing Ge Jia-Min Du Wen-Zhou Zhang Pei-Hua Lu Qiao-Jun He Hong Zhu Bo Yang Source Type: research

Mitochondrial proteome of mouse oocytes and cisplatin-induced shifts in protein profile
Acta Pharmacol Sin. 2021 May 20. doi: 10.1038/s41401-021-00687-4. Online ahead of print.ABSTRACTMitochondria are essential organelles that provide energy for mammalian cells and participate in multiple functions, such as signal transduction, cellular differentiation, and regulation of apoptosis. Compared with the mitochondria in somatic cells, oocyte mitochondria have an additional level of importance since they are required for germ cell maturation, dysfunction in which can lead to severe inherited disorders. Thus, a systematic proteomic profile of oocyte mitochondria is urgently needed to support the basic and clinical r...
Source: Acta Pharmacologica Sinica - May 21, 2021 Category: Drugs & Pharmacology Authors: Na Zhang An-di Sun Si-Man Sun Rui Yang Yan-Yan Shi Qi-Long Wang Xin-Yu Li Ji-Hong Ma Wei Yue Bing-Teng Xie Jie Qiao Mo Li Source Type: research

Author Correction: Bmal1 inhibits phenotypic transformation of hepatic stellate cells in liver fibrosis via IDH1/ α-KG-mediated glycolysis
Acta Pharmacol Sin. 2021 May 20. doi: 10.1038/s41401-021-00685-6. Online ahead of print.NO ABSTRACTPMID:34017068 | DOI:10.1038/s41401-021-00685-6 (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - May 21, 2021 Category: Drugs & Pharmacology Authors: Lei Xu Tian-Yu Yang Yi-Wen Zhou Mei-Fei Wu Jie Shen Jie-Ling Cheng Qing-Xue Liu Shi-Yang Cao Jian-Qing Wang Lei Zhang Source Type: research

AKR1C1 connects autophagy and oxidative stress by interacting with SQSTM1 in a catalytic-independent manner
Acta Pharmacol Sin. 2021 May 20. doi: 10.1038/s41401-021-00673-w. Online ahead of print.ABSTRACTTargeting autophagy might be a promising anticancer strategy; however, the dual roles of autophagy in cancer development and malignancy remain unclear. NSCLC (non-small cell lung cancer) cells harbour high levels of SQSTM1 (sequestosome 1), the autophagy receptor that is critical for the dual roles of autophagy. Therefore, mechanistic insights into SQSTM1 modulation may point towards better approaches to treat NSCLC. Herein, we used multiple autophagy flux models and autophagy readouts to show that aldo-keto reductase family 1 m...
Source: Acta Pharmacologica Sinica - May 21, 2021 Category: Drugs & Pharmacology Authors: Lin-Lin Chang Yue-Kang Li Chen-Xi Zhao Chen-Ming Zeng Fu-Jing Ge Jia-Min Du Wen-Zhou Zhang Pei-Hua Lu Qiao-Jun He Hong Zhu Bo Yang Source Type: research

Mitochondrial proteome of mouse oocytes and cisplatin-induced shifts in protein profile
Acta Pharmacol Sin. 2021 May 20. doi: 10.1038/s41401-021-00687-4. Online ahead of print.ABSTRACTMitochondria are essential organelles that provide energy for mammalian cells and participate in multiple functions, such as signal transduction, cellular differentiation, and regulation of apoptosis. Compared with the mitochondria in somatic cells, oocyte mitochondria have an additional level of importance since they are required for germ cell maturation, dysfunction in which can lead to severe inherited disorders. Thus, a systematic proteomic profile of oocyte mitochondria is urgently needed to support the basic and clinical r...
Source: Acta Pharmacologica Sinica - May 21, 2021 Category: Drugs & Pharmacology Authors: Na Zhang An-di Sun Si-Man Sun Rui Yang Yan-Yan Shi Qi-Long Wang Xin-Yu Li Ji-Hong Ma Wei Yue Bing-Teng Xie Jie Qiao Mo Li Source Type: research

Author Correction: Bmal1 inhibits phenotypic transformation of hepatic stellate cells in liver fibrosis via IDH1/ α-KG-mediated glycolysis
Acta Pharmacol Sin. 2021 May 20. doi: 10.1038/s41401-021-00685-6. Online ahead of print.NO ABSTRACTPMID:34017068 | DOI:10.1038/s41401-021-00685-6 (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - May 21, 2021 Category: Drugs & Pharmacology Authors: Lei Xu Tian-Yu Yang Yi-Wen Zhou Mei-Fei Wu Jie Shen Jie-Ling Cheng Qing-Xue Liu Shi-Yang Cao Jian-Qing Wang Lei Zhang Source Type: research

AKR1C1 connects autophagy and oxidative stress by interacting with SQSTM1 in a catalytic-independent manner
Acta Pharmacol Sin. 2021 May 20. doi: 10.1038/s41401-021-00673-w. Online ahead of print.ABSTRACTTargeting autophagy might be a promising anticancer strategy; however, the dual roles of autophagy in cancer development and malignancy remain unclear. NSCLC (non-small cell lung cancer) cells harbour high levels of SQSTM1 (sequestosome 1), the autophagy receptor that is critical for the dual roles of autophagy. Therefore, mechanistic insights into SQSTM1 modulation may point towards better approaches to treat NSCLC. Herein, we used multiple autophagy flux models and autophagy readouts to show that aldo-keto reductase family 1 m...
Source: Acta Pharmacologica Sinica - May 21, 2021 Category: Drugs & Pharmacology Authors: Lin-Lin Chang Yue-Kang Li Chen-Xi Zhao Chen-Ming Zeng Fu-Jing Ge Jia-Min Du Wen-Zhou Zhang Pei-Hua Lu Qiao-Jun He Hong Zhu Bo Yang Source Type: research

Mitochondrial proteome of mouse oocytes and cisplatin-induced shifts in protein profile
Acta Pharmacol Sin. 2021 May 20. doi: 10.1038/s41401-021-00687-4. Online ahead of print.ABSTRACTMitochondria are essential organelles that provide energy for mammalian cells and participate in multiple functions, such as signal transduction, cellular differentiation, and regulation of apoptosis. Compared with the mitochondria in somatic cells, oocyte mitochondria have an additional level of importance since they are required for germ cell maturation, dysfunction in which can lead to severe inherited disorders. Thus, a systematic proteomic profile of oocyte mitochondria is urgently needed to support the basic and clinical r...
Source: Acta Pharmacologica Sinica - May 21, 2021 Category: Drugs & Pharmacology Authors: Na Zhang An-di Sun Si-Man Sun Rui Yang Yan-Yan Shi Qi-Long Wang Xin-Yu Li Ji-Hong Ma Wei Yue Bing-Teng Xie Jie Qiao Mo Li Source Type: research

Author Correction: Bmal1 inhibits phenotypic transformation of hepatic stellate cells in liver fibrosis via IDH1/ α-KG-mediated glycolysis
Acta Pharmacol Sin. 2021 May 20. doi: 10.1038/s41401-021-00685-6. Online ahead of print.NO ABSTRACTPMID:34017068 | DOI:10.1038/s41401-021-00685-6 (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - May 21, 2021 Category: Drugs & Pharmacology Authors: Lei Xu Tian-Yu Yang Yi-Wen Zhou Mei-Fei Wu Jie Shen Jie-Ling Cheng Qing-Xue Liu Shi-Yang Cao Jian-Qing Wang Lei Zhang Source Type: research

S-nitrosylation of c-Jun N-terminal kinase mediates pressure overload-induced cardiac dysfunction and fibrosis
Acta Pharmacol Sin. 2021 May 19. doi: 10.1038/s41401-021-00674-9. Online ahead of print.ABSTRACTCardiac fibrosis (CF) is an irreversible pathological process that occurs in almost all kinds of cardiovascular diseases. Phosphorylation-dependent activation of c-Jun N-terminal kinase (JNK) induces cardiac fibrosis. However, whether S-nitrosylation of JNK mediates cardiac fibrosis remains an open question. A biotin-switch assay confirmed that S-nitrosylation of JNK (SNO-JNK) increased significantly in the heart tissues of hypertrophic patients, transverse aortic constriction (TAC) mice, spontaneously hypertensive rats (SHRs), ...
Source: Acta Pharmacologica Sinica - May 20, 2021 Category: Drugs & Pharmacology Authors: Miao Zhou Ji-Yu Chen Meng-Lin Chao Chao Zhang Zhi-Guang Shi Xue-Chun Zhou Li-Ping Xie Shi-Xiu Sun Zheng-Rong Huang Shan-Shan Luo Yong Ji Source Type: research