Nitazoxanide, an anti-parasitic drug, efficiently ameliorates learning and memory impairments in AD model mice
Nitazoxanide, an anti-parasitic drug, efficiently ameliorates learning and memory impairments in AD model mice, Published online: 18 April 2019; doi:10.1038/s41401-019-0220-1Nitazoxanide, an anti-parasitic drug, efficiently ameliorates learning and memory impairments in AD model mice (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - April 18, 2019 Category: Drugs & Pharmacology Authors: Lei Fan Xiao-xia Qiu Zhi-yuan Zhu Jian-lu Lv Jian Lu Fei Mao Jin Zhu Jia-ying Wang Xiao-wei Guan Jing Chen Jin Ren Ji-ming Ye Yong-hua Zhao Jian Li Xu Shen Source Type: research

Monocarbonyl curcumin analog A2 potently inhibits angiogenesis by inducing ROS-dependent endothelial cell death
Monocarbonyl curcumin analog A2 potently inhibits angiogenesis by inducing ROS-dependent endothelial cell death, Published online: 18 April 2019; doi:10.1038/s41401-019-0224-xMonocarbonyl curcumin analog A2 potently inhibits angiogenesis by inducing ROS-dependent endothelial cell death (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - April 18, 2019 Category: Drugs & Pharmacology Authors: Bin Liu Liu-su Cui Bo Zhou Ling-ling Zhang Zhi-hui Liu Lu Zhang Source Type: research

Sevoflurane promotes migration, invasion, and colony-forming ability of human glioblastoma cells possibly via increasing the expression of cell surface protein 44.
In conclusion, sevoflurane increases the migration, invasion, and colony-forming ability of human glioblastoma cells in vitro, and their tumor volume and invasion/migration in vivo. Sevoflurane enhances these cancer cell biology features via increasing the expression of CD44. PMID: 30967592 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - April 9, 2019 Category: Drugs & Pharmacology Authors: Lai RC, Shan WR, Zhou D, Zeng XQ, Zuo K, Pan DF, Zeng WA, Zuo ZY Tags: Acta Pharmacol Sin Source Type: research

Sevoflurane promotes migration, invasion, and colony-forming ability of human glioblastoma cells possibly via increasing the expression of cell surface protein 44
Sevoflurane promotes migration, invasion, and colony-forming ability of human glioblastoma cells possibly via increasing the expression of cell surface protein 44, Published online: 09 April 2019; doi:10.1038/s41401-019-0221-0Sevoflurane promotes migration, invasion, and colony-forming ability of human glioblastoma cells possibly via increasing the expression of cell surface protein 44 (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - April 9, 2019 Category: Drugs & Pharmacology Authors: Ren-chun Lai Wei-ran Shan Di Zhou Xiao-qing Zeng Kendrick Zuo Dong-feng Pan Wei-an Zeng Zhi-yi Zuo Source Type: research

Protective effects of specific cannabinoid receptor 2 agonist GW405833 on concanavalin A-induced acute liver injury in mice.
Abstract Cannabinoid receptor 2 (CB2R) is highly expressed in immune cells and plays an important role in regulating immune responses. In the current study, we investigated the effects of GW405833 (GW), a specific CB2R agonist, on acute liver injury induced by concanavalin A (Con A). In animal experiments, acute liver injury was induced in mice by injection of Con A (20 mg/kg, i.v.). The mice were treated with GW (20 mg/kg, i.p., 30 min after Con A injection) or GW plus the selective CB2R antagonist AM630 (2 mg/kg, i.p., 15 min after Con A injection). We found that Con A caused s...
Source: Acta Pharmacologica Sinica - March 27, 2019 Category: Drugs & Pharmacology Authors: Huang ZB, Zheng YX, Li N, Cai SL, Huang Y, Wang J, Hu XW, Wang Y, Wu J, Fan XG Tags: Acta Pharmacol Sin Source Type: research

Donepezil, a drug for Alzheimer's disease, promotes oligodendrocyte generation and remyelination.
Abstract Myelin sheaths play important roles in neuronal functions. In the central nervous system (CNS), the myelin is formed by oligodendrocytes (OLs), which are differentiated from oligodendrocyte precursor cells (OPCs). In CNS demyelinating disorders such as multiple sclerosis (MS), the myelin sheaths are damaged and the remyelination process is hindered. Small molecule drugs that promote OPC to OL differentiation and remyelination may provide a new way to treat these demyelinating diseases. Here we report that donepezil, an acetylcholinesterase inhibitor (AChEI) developed for the treatment of Alzheimer's disea...
Source: Acta Pharmacologica Sinica - March 27, 2019 Category: Drugs & Pharmacology Authors: Cui X, Guo YE, Fang JH, Shi CJ, Suo N, Zhang R, Xie X Tags: Acta Pharmacol Sin Source Type: research

Donepezil, a drug for Alzheimer’s disease, promotes oligodendrocyte generation and remyelination
Donepezil, a drug for Alzheimer’s disease, promotes oligodendrocyte generation and remyelinationDonepezil, a drug for Alzheimer’s disease, promotes oligodendrocyte generation and remyelination, Published online: 27 March 2019; doi:10.1038/s41401-018-0206-4Donepezil, a drug for Alzheimer’s disease, promotes oligodendrocyte generation and remyelination (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - March 27, 2019 Category: Drugs & Pharmacology Authors: Xue Cui Yu-e Guo Jia-hui Fang Chang-jie Shi Na Suo Ru Zhang Xin Xie Source Type: research

Protective effects of specific cannabinoid receptor 2 agonist GW405833 on concanavalin A-induced acute liver injury in mice
Protective effects of specific cannabinoid receptor 2 agonist GW405833 on concanavalin A-induced acute liver injury in mice, Published online: 27 March 2019; doi:10.1038/s41401-019-0213-0Protective effects of specific cannabinoid receptor 2 agonist GW405833 on concanavalin A-induced acute liver injury in mice (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - March 27, 2019 Category: Drugs & Pharmacology Authors: Ze-bing Huang Yi-xiang Zheng Ning Li Sheng-lan Cai Yan Huang Juan Wang Xing-wang Hu Yang Wang Jie Wu Xue-gong Fan Source Type: research

Eukaryotic elongation factor-2 kinase regulates the cross-talk between autophagy and pyroptosis in doxorubicin-treated human melanoma cells in vitro.
In this study, we investigated the regulatory role of eEF-2K in pyroptosis (a new form of programmed necrosis) in doxorubicin-treated human melanoma cells. We found that doxorubicin (0.5-5 μmol/L) induced pyroptosis in melanoma cell lines SK-MEL-5, SK-MEL-28, and A-375 with high expression of DFNA5, but not in human breast cancer cell line MCF-7 with little expression of DFNA5. On the other hand, doxorubicin treatment activated autophagy in the melanoma cells; inhibition of autophagy by transfecting the cells with siRNA targeting Beclin1 or by pretreatment with chloroquine (20 μmol/L) significantly augm...
Source: Acta Pharmacologica Sinica - March 26, 2019 Category: Drugs & Pharmacology Authors: Yu P, Wang HY, Tian M, Li AX, Chen XS, Wang XL, Zhang Y, Cheng Y Tags: Acta Pharmacol Sin Source Type: research

Eukaryotic elongation factor-2 kinase regulates the cross-talk between autophagy and pyroptosis in doxorubicin-treated human melanoma cells in vitro
Eukaryotic elongation factor-2 kinase regulates the cross-talk between autophagy and pyroptosis in doxorubicin-treated human melanoma cells in vitro, Published online: 26 March 2019; doi:10.1038/s41401-019-0222-zEukaryotic elongation factor-2 kinase regulates the cross-talk between autophagy and pyroptosis in doxorubicin-treated human melanoma cells in vitro (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - March 26, 2019 Category: Drugs & Pharmacology Authors: Pian Yu Hai-yan Wang Min Tian Ao-xue Li Xi-sha Chen Xin-luan Wang Yi Zhang Yan Cheng Source Type: research

Diabetes inhibits corneal epithelial cell migration and tight junction formation in mice and human via increasing ROS and impairing Akt signaling.
Abstract Corneal wounds usually heal quickly; but diabetic patients have more fragile corneas and experience delayed and painful healing. In the present study, we compared the healing capacity of corneal epithelial cells (CECs) between normal and diabetic conditions and the potential mechanisms. Primary murine CEC derived from wild-type and diabetic (db/db) mice, as well as primary human CEC were prepared. Human CEC were exposed to high glucose (30 mM) to mimic diabetic conditions. Cell migration and proliferation were assessed using Scratch test and MTT assays, respectively. Reactive oxygen species (ROS) p...
Source: Acta Pharmacologica Sinica - March 13, 2019 Category: Drugs & Pharmacology Authors: Jiang QW, Kaili D, Freeman J, Lei CY, Geng BC, Tan T, He JF, Shi Z, Ma JJ, Luo YH, Chandler H, Zhu H Tags: Acta Pharmacol Sin Source Type: research

Diabetes inhibits corneal epithelial cell migration and tight junction formation in mice and human via increasing ROS and impairing Akt signaling
Diabetes inhibits corneal epithelial cell migration and tight junction formation in mice and human via increasing ROS and impairing Akt signaling, Published online: 13 March 2019; doi:10.1038/s41401-019-0223-yDiabetes inhibits corneal epithelial cell migration and tight junction formation in mice and human via increasing ROS and impairing Akt signaling (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - March 13, 2019 Category: Drugs & Pharmacology Authors: Qi-wei Jiang Denis Kaili Jonaye Freeman Chong-yang Lei Bing-chuan Geng Tao Tan Jian-feng He Zhi Shi Jian-jie Ma Yan-hong Luo Heather Chandler Hua Zhu Source Type: research

Temporal dynamics of immune response following prolonged myocardial ischemia/reperfusion with and without cyclosporine A.
This study aimed to determine the dynamics of the immune response following myocardial ischemia/reperfusion (I/R) and the effects of CSA in a mouse model of prolonged myocardial ischemia designated to represent the human condition of late reperfusion. Adult C57BL/6 mice were subjected to 90 min of closed-chest myocardial I/R, which induced severe myocardial injury and excessive inflammation in the heart. Multicomponent analysis of the immune response caused by prolonged I/R revealed that the peak of cytokines/chemokines in the systemic circulation was synchronized with the maximal influx of neutrophils and T-cells i...
Source: Acta Pharmacologica Sinica - March 11, 2019 Category: Drugs & Pharmacology Authors: Rusinkevich V, Huang Y, Chen ZY, Qiang W, Wang YG, Shi YF, Yang HT Tags: Acta Pharmacol Sin Source Type: research

Temporal dynamics of immune response following prolonged myocardial ischemia/reperfusion with and without cyclosporine A
Temporal dynamics of immune response following prolonged myocardial ischemia/reperfusion with and without cyclosporine A, Published online: 11 March 2019; doi:10.1038/s41401-018-0197-1Temporal dynamics of immune response following prolonged myocardial ischemia/reperfusion with and without cyclosporine A (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - March 11, 2019 Category: Drugs & Pharmacology Authors: Vitali Rusinkevich Yin Huang Zhong-yan Chen Wu Qiang Yi-gang Wang Yu-fang Shi Huang-tian Yang Source Type: research

Genetic variants in the PLS3 gene are associated with osteoporotic fractures in postmenopausal Chinese women.
Abstract Plastin 3 (PLS3) has been identified as a candidate gene for bone fragility in the Rotterdam study (RS) population. So far, however, whether PLS3 polymorphisms are genetic risk factors for osteoporosis in Asian population remains unclear. In order to investigate the association between genetic variants in PLS3 and the risk of fragility fracture and/or bone mineral density (BMD) in postmenopausal Chinese women, we conducted a case-control association study. A total of 1083 postmenopausal patients with osteoporotic fractures and 2578 unrelated non-fracture controls in Shanghai were enrolled. Seven SNPs, inc...
Source: Acta Pharmacologica Sinica - March 5, 2019 Category: Drugs & Pharmacology Authors: Shao C, Wang YW, He JW, Fu WZ, Wang C, Zhang ZL Tags: Acta Pharmacol Sin Source Type: research

Genetic variants in the PLS3 gene are associated with osteoporotic fractures in postmenopausal Chinese women
Genetic variants in the PLS3 gene are associated with osteoporotic fractures in postmenopausal Chinese women, Published online: 05 March 2019; doi:10.1038/s41401-019-0219-7Genetic variants in the PLS3 gene are associated with osteoporotic fractures in postmenopausal Chinese women (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - March 5, 2019 Category: Drugs & Pharmacology Authors: Chong Shao Yi-wen Wang Jin-wei He Wen-zhen Fu Chun Wang Zhen-lin Zhang Source Type: research

Ligand-induced activation of ERK1/2 signaling by constitutively active Gs-coupled 5-HT receptors.
In this study, we investigated these two signaling pathways originating from the three Gs-coupled 5-HT receptors in AD293 cells. We found that the phosphorylation and activation of ERK1/2 are ligand-induced, in contrast to the constitutively active Gs signaling. This indicates that Gs signaling alone is not sufficient for ERK1/2 activation in these three 5-HT receptors. In addition to Gs, we found that β-arrestin and Fyn are essential for the activation of ERK1/2. Together, these results put forth a novel mechanism for ERK1/2 activation involving the cooperative action of Gs, β-arrestin, and Fyn. PMID: 30833...
Source: Acta Pharmacologica Sinica - March 4, 2019 Category: Drugs & Pharmacology Authors: Liu P, Yin YL, Wang T, Hou L, Wang XX, Wang M, Zhao GG, Shi Y, Xu HE, Jiang Y Tags: Acta Pharmacol Sin Source Type: research

Nicotinamide phosphoribosyltransferase aggravates inflammation and promotes atherosclerosis in ApoE knockout mice.
In this study, we crossed global Nampt transgenic mice (Nampt-Tg) with a well-established atherosclerosis animal model (ApoE knockout mice, ApoE-/-) to generate ApoE-/-;Nampt-Tg mice and investigated the effects of Nampt overexpression on atherosclerosis development in ApoE-/- mice. Both ApoE-/- and ApoE-/-;Nampt-Tg mice were fed with a pro-atherosclerotic high-fat diet (HFD) for 16 weeks. Their serum lipid contents and atherosclerotic lesion were assessed. The results showed that there was no significant difference in body weight or serum levels of glucose, total cholesterol, triglycerides, high-density lipoprotein choles...
Source: Acta Pharmacologica Sinica - March 4, 2019 Category: Drugs & Pharmacology Authors: Kong YY, Li GQ, Zhang WJ, Hua X, Zhou CC, Xu TY, Li ZY, Wang P, Miao CY Tags: Acta Pharmacol Sin Source Type: research

Small molecule IVQ, as a prodrug of gluconeogenesis inhibitor QVO, efficiently ameliorates glucose homeostasis in type 2 diabetic mice.
Abstract Gluconeogenesis is a major source of hyperglycemia in patients with type 2 diabetes mellitus (T2DM), thus targeting gluconeogenesis to suppress glucose production is a promising strategy for anti-T2DM drug discovery. In our preliminary in vitro studies, we found that a small-molecule (E)-3-(2-(quinoline-4-yl)vinyl)-1H-indol-6-ol (QVO) inhibited the hepatic glucose production (HGP) in primary hepatocytes. We further revealed that QVO suppressed hepatic gluconeogenesis involving calmodulin-dependent protein kinase kinase β- and liver kinase B1-adenosine monophosphate-activated protein kinase (AMPK) pat...
Source: Acta Pharmacologica Sinica - March 4, 2019 Category: Drugs & Pharmacology Authors: Zhou TT, Zhao T, Ma F, Zhang YN, Jiang J, Ruan Y, Yan QY, Wang GH, Ren J, Guan XW, Guo J, Zhao YH, Ye JM, Hu LH, Chen J, Shen X Tags: Acta Pharmacol Sin Source Type: research

Ligand-induced activation of ERK1/2 signaling by constitutively active Gs-coupled 5-HT receptors
Ligand-induced activation of ERK1/2 signaling by constitutively active Gs-coupled 5-HT receptors, Published online: 04 March 2019; doi:10.1038/s41401-018-0204-6Ligand-induced activation of ERK1/2 signaling by constitutively active Gs-coupled 5-HT receptors (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - March 4, 2019 Category: Drugs & Pharmacology Authors: Ping Liu Yu-ling Yin Ting Wang Li Hou Xiao-xi Wang Man Wang Guan-guan Zhao Yi Shi H. Eric Xu Yi Jiang Source Type: research

Small molecule IVQ, as a prodrug of gluconeogenesis inhibitor QVO, efficiently ameliorates glucose homeostasis in type 2 diabetic mice
Small molecule IVQ, as a prodrug of gluconeogenesis inhibitor QVO, efficiently ameliorates glucose homeostasis in type 2 diabetic mice, Published online: 04 March 2019; doi:10.1038/s41401-018-0208-2Small molecule IVQ, as a prodrug of gluconeogenesis inhibitor QVO, efficiently ameliorates glucose homeostasis in type 2 diabetic mice (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - March 4, 2019 Category: Drugs & Pharmacology Authors: Ting-ting Zhou Tong Zhao Fei Ma Yi-nan Zhang Jing Jiang Yuan Ruan Qiu-ying Yan Gai-hong Wang Jin Ren Xiao-wei Guan Jun Guo Yong-hua Zhao Ji-ming Ye Li-hong Hu Jing Chen Xu Shen Source Type: research

Nicotinamide phosphoribosyltransferase aggravates inflammation and promotes atherosclerosis in ApoE knockout mice
Nicotinamide phosphoribosyltransferase aggravates inflammation and promotes atherosclerosis in ApoE knockout mice, Published online: 04 March 2019; doi:10.1038/s41401-018-0207-3Nicotinamide phosphoribosyltransferase aggravates inflammation and promotes atherosclerosis in ApoE knockout mice (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - March 4, 2019 Category: Drugs & Pharmacology Authors: Yuan-yuan Kong Guo-qiang Li Wen-jie Zhang Xia Hua Can-can Zhou Tian-ying Xu Zhi-yong Li Pei Wang Chao-yu Miao Source Type: research

Structural insight into the serotonin (5-HT) receptor family by molecular docking, molecular dynamics simulation and systems pharmacology analysis
Structural insight into the serotonin (5-HT) receptor family by molecular docking, molecular dynamics simulation and systems pharmacology analysis, Published online: 27 February 2019; doi:10.1038/s41401-019-0217-9Structural insight into the serotonin (5-HT) receptor family by molecular docking, molecular dynamics simulation and systems pharmacology analysis (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 27, 2019 Category: Drugs & Pharmacology Authors: Yuan-qiang Wang Wei-wei Lin Nan Wu Si-yi Wang Mao-zi Chen Zhi-hua Lin Xiang-Qun Xie Zhi-wei Feng Source Type: research

Structural insight into the serotonin (5-HT) receptor family by molecular docking, molecular dynamics simulation and systems pharmacology analysis.
Abstract Serotonin (5-HT) receptors are proteins involved in various neurological and biological processes, such as aggression, anxiety, appetite, cognition, learning, memory, mood, sleep, and thermoregulation. They are commonly associated with drug abuse and addiction due to their importance as targets for various pharmaceutical and recreational drugs. However, due to a high sequence similarity/identity among 5-HT receptors and the unavailability of the 3D structure of the different 5-HT receptor, no report was available so far regarding the systematical comparison of the key and selective residues involved in th...
Source: Acta Pharmacologica Sinica - February 27, 2019 Category: Drugs & Pharmacology Authors: Wang YQ, Lin WW, Wu N, Wang SY, Chen MZ, Lin ZH, Xie XQ, Feng ZW Tags: Acta Pharmacol Sin Source Type: research

The inhibitory mechanism of aurintricarboxylic acid targeting serine/threonine phosphatase Stp1 in Staphylococcus aureus: insights from molecular dynamics simulations.
This study indicated the inhibitory mechanism of ATA targeting Stp1 using MD simulations and sheds light on the future design of allosteric Stp1 inhibitors. PMID: 30796354 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 22, 2019 Category: Drugs & Pharmacology Authors: Liu TT, Yang T, Gao MN, Chen KX, Yang S, Yu KQ, Jiang HL Tags: Acta Pharmacol Sin Source Type: research

Predicted secreted protein analysis reveals synaptogenic function of Clstn3 during WAT browning and BAT activation in mice.
In conclusion, our study demonstrates that the secretion pattern was somewhat different between WAT browning and BAT activation. We reveal that Clstn3 may be a key gene mediating the neuro-adipose junction formation or remodeling in WAT browning and BAT activation process. PMID: 30796355 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 22, 2019 Category: Drugs & Pharmacology Authors: Chen SQ, Niu Q, Ju LP, Alimujiang M, Yan H, Bai NN, Xu J, Fang QC, Han JF, Yang Y, Jia WP Tags: Acta Pharmacol Sin Source Type: research

mTORC1 inhibitor RAD001 (everolimus) enhances non-small cell lung cancer cell radiosensitivity in vitro via suppressing epithelial-mesenchymal transition.
In this study we explored whether mTORC1 regulated NSCLC cell radiosensitivity by altering EMT. We performed immunohistichemical analysis using tumor, adjacent and normal tissues from 50 NSCLC patients, which confirmed significantly elevated mTOR protein expression in NSCLC tissue. Then we used NCI-H460 and NCI-H661 cell lines to examine the effects of the mTORC1 inhibitor RAD001 (everolimus) on in vitro radiosensitivity, protein expression and dose-survival curves. RAD001 (10 nmol/L) significantly inhibited the mTORC1 pathway in both the cell lines. Pretreatment with RAD001 (0.1 nmol/L) enhanced the radiosen...
Source: Acta Pharmacologica Sinica - February 22, 2019 Category: Drugs & Pharmacology Authors: Chen Y, Li WW, Peng P, Zhao WH, Tian YJ, Huang Y, Xia S, Chen Y Tags: Acta Pharmacol Sin Source Type: research

The inhibitory mechanism of aurintricarboxylic acid targeting serine/threonine phosphatase Stp1 in Staphylococcus aureus: insights from molecular dynamics simulations
The inhibitory mechanism of aurintricarboxylic acid targeting serine/threonine phosphatase Stp1 in Staphylococcus aureus: insights from molecular dynamics simulations, Published online: 22 February 2019; doi:10.1038/s41401-019-0216-xThe inhibitory mechanism of aurintricarboxylic acid targeting serine/threonine phosphatase Stp1 in Staphylococcus aureus: insights from molecular dynamics simulations (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 22, 2019 Category: Drugs & Pharmacology Authors: Ting-ting Liu Teng Yang Mei-na Gao Kai-xian Chen Song Yang Kun-qian Yu Hua-liang Jiang Source Type: research

Predicted secreted protein analysis reveals synaptogenic function of Clstn3 during WAT browning and BAT activation in mice
Predicted secreted protein analysis reveals synaptogenic function of Clstn3 during WAT browning and BAT activation in mice, Published online: 22 February 2019; doi:10.1038/s41401-019-0211-2Predicted secreted protein analysis reveals synaptogenic function of Clstn3 during WAT browning and BAT activation in mice (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 22, 2019 Category: Drugs & Pharmacology Authors: Shu-qin Chen Qiang Niu Li-ping Ju Miriayi Alimujiang Han Yan Ning-ning Bai Jun Xu Qi-chen Fang Jun-feng Han Ying Yang Wei-ping Jia Source Type: research

mTORC1 inhibitor RAD001 (everolimus) enhances non-small cell lung cancer cell radiosensitivity in vitro via suppressing epithelial–mesenchymal transition
mTORC1 inhibitor RAD001 (everolimus) enhances non-small cell lung cancer cell radiosensitivity in vitro via suppressing epithelial–mesenchymal transitionmTORC1 inhibitor RAD001 (everolimus) enhances non-small cell lung cancer cell radiosensitivity in vitro via suppressing epithelial–mesenchymal transition, Published online: 22 February 2019; doi:10.1038/s41401-019-0215-ymTORC1 inhibitor RAD001 (everolimus) enhances non-small cell lung cancer cell radiosensitivity in vitro via suppressing epithelial–mesenchymal transition (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 22, 2019 Category: Drugs & Pharmacology Authors: Yu Chen Wen-wen LI Ping Peng Wei-heng Zhao Yi-jun Tian Yu Huang Shu Xia Yuan Chen Source Type: research

Minocycline protects against myocardial ischemia/reperfusion injury in rats by upregulating MCPIP1 to inhibit NF- κB activation.
Minocycline protects against myocardial ischemia/reperfusion injury in rats by upregulating MCPIP1 to inhibit NF-κB activation. Acta Pharmacol Sin. 2019 Feb 21;: Authors: Yi Q, Tan FH, Tan JA, Chen XH, Xiao Q, Liu YH, Zhang GP, Luo JD Abstract Minocycline is a tetracycline antibiotic and has been shown to play a protective role in cerebral and myocardial ischemia/reperfusion (I/R). However, the underlying mechanism remains unclear. Herein, we investigated whether monocyte chemotactic protein-induced protein-1 (MCPIP1), a negative regulator of inflammation, was involved in the minocycline-induced...
Source: Acta Pharmacologica Sinica - February 21, 2019 Category: Drugs & Pharmacology Authors: Yi Q, Tan FH, Tan JA, Chen XH, Xiao Q, Liu YH, Zhang GP, Luo JD Tags: Acta Pharmacol Sin Source Type: research

Characteristics of β-oxidative and reductive metabolism on the acyl side chain of cinnamic acid and its analogues in rats.
In this study, we characterized the β-oxidative and reductive metabolism on acyl side chain of cinnamic acid and its analogues using primary rat hepatocytes, hepatic mitochondrial, and microsomal systems. A compartmental model including parent compounds and metabolites was developed to characterize in vivo β-oxidative and reductive metabolism following an intravenous dose of parent compounds to rats. The fitted total in vivo clearance values were further compared with the in vitro values predicted by the well-stirred model. We showed that hepatic microsomal CYP450s did not catalyze β-oxidative or reductive m...
Source: Acta Pharmacologica Sinica - February 21, 2019 Category: Drugs & Pharmacology Authors: Zhao KJ, Chen Y, Hong SJ, Yang YT, Xu J, Yang HY, Zhu L, Liu M, Xie QS, Tang XG, Yang TT, Zhou YQ, Liu L, Liu XD Tags: Acta Pharmacol Sin Source Type: research

Minocycline protects against myocardial ischemia/reperfusion injury in rats by upregulating MCPIP1 to inhibit NF-κB activation
Minocycline protects against myocardial ischemia/reperfusion injury in rats by upregulating MCPIP1 to inhibit NF-κB activationMinocycline protects against myocardial ischemia/reperfusion injury in rats by upregulating MCPIP1 to inhibit NF-κB activation, Published online: 21 February 2019; doi:10.1038/s41401-019-0214-zMinocycline protects against myocardial ischemia/reperfusion injury in rats by upregulating MCPIP1 to inhibit NF-κB activation (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 21, 2019 Category: Drugs & Pharmacology Authors: Quan Yi Fang-hui Tan Jia-an Tan Xiu-hui Chen Qing Xiao Ying-hua Liu Gui-ping Zhang Jian-dong Luo Source Type: research

Characteristics of β-oxidative and reductive metabolism on the acyl side chain of cinnamic acid and its analogues in rats
Characteristics of β-oxidative and reductive metabolism on the acyl side chain of cinnamic acid and its analogues in ratsCharacteristics of β-oxidative and reductive metabolism on the acyl side chain of cinnamic acid and its analogues in rats, Published online: 21 February 2019; doi:10.1038/s41401-019-0218-8Characteristics of β-oxidative and reductive metabolism on the acyl side chain of cinnamic acid and its analogues in rats (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 21, 2019 Category: Drugs & Pharmacology Authors: Kai-jing Zhao Yang Chen Shi-jin Hong Yi-ting Yang Jiong Xu Han-yu Yang Liang Zhu Ming Liu Qiu-shi Xie Xian-ge Tang Ting-ting Yang Ya-qian Zhou Li Liu Xiao-dong Liu Source Type: research

Inhibition of G9a by a small molecule inhibitor, UNC0642, induces apoptosis of human bladder cancer cells.
Abstract Urinary bladder cancer (UBC) is characterized by frequent recurrence and metastasis despite the standard chemotherapy with gemcitabine and cisplatin combination. Histone modifiers are often dysregulated in cancer development, thus they can serve as an excellent drug targets for cancer therapy. Here, we investigated whether G9a, one of the histone H3 methyltransferases, was associated with UBC development. We first analyzed clinical data from public databases and found that G9a was significantly overexpressed in UBC patients. The TCGA Provisional dataset showed that the average expression level of G9a in p...
Source: Acta Pharmacologica Sinica - February 14, 2019 Category: Drugs & Pharmacology Authors: Cao YP, Sun JY, Li MQ, Dong Y, Zhang YH, Yan J, Huang RM, Yan X Tags: Acta Pharmacol Sin Source Type: research

Inhibition of G9a by a small molecule inhibitor, UNC0642, induces apoptosis of human bladder cancer cells
Inhibition of G9a by a small molecule inhibitor, UNC0642, induces apoptosis of human bladder cancer cells, Published online: 14 February 2019; doi:10.1038/s41401-018-0205-5Inhibition of G9a by a small molecule inhibitor, UNC0642, induces apoptosis of human bladder cancer cells (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 14, 2019 Category: Drugs & Pharmacology Authors: Yue-peng Cao Jing-ya Sun Mei-qian Li Yu Dong Yuan-heng Zhang Jun Yan Rui-min Huang Xiang Yan Source Type: research

Low-intensity walking as mild medication for pressure control in prehypertensive and hypertensive subjects: how far shall we wander?
Abstract Successful prevention and treatment of hypertension depend on the appropriate combination of antihypertensive drug therapy and nondrug lifestyle modification. While most hypertension guidelines recommend moderate- to high-intensity exercise, we decided to explore a mild yet effective type of exercise to add to hypertension management, especially in populations with complications or frailty. After comparing the short-term cardiovascular effects of low-speed walking versus high-speed walking for 3 kilometers (km) (3 km/h versus 6 km/h) in young, healthy volunteers, we delivered low-speed walki...
Source: Acta Pharmacologica Sinica - February 13, 2019 Category: Drugs & Pharmacology Authors: Lu Q, Wang SM, Liu YX, Chen H, Zhang R, Zhang WH, Zou YY, Zhou JW, Guo XY, Zhang Y, Huang TL, Liu YH, Zhang SQ, Yamanishi K, Yamanishi H, Higashino H, Okamura H Tags: Acta Pharmacol Sin Source Type: research

Magnesium lithospermate B ameliorates microcirculation perfusion in rats by promoting vascular NO production via activating the PI3K/AKT pathway.
In this study we investigated the effects of magnesium lithospermate B (MLB), an active compound of the traditional Chinese medicine Slavia miltiorrhiza, on the microcirculation dysfunction in rats and the underlying molecular mechanisms. The effects of MLB on microcirculation were assessed in vivo by measuring the hindlimb blood perfusion in dextran-induced microcirculation dysfunction rats and mesentery blood flow in anesthetized rats. We demonstrated that administration of MLB restored the impaired rat hindlimb blood flow and promoted the mesenteric micoperfusion in vivo. We further revealed in these two animal models t...
Source: Acta Pharmacologica Sinica - February 13, 2019 Category: Drugs & Pharmacology Authors: Liu YL, Zhou XY, Xuan LJ Tags: Acta Pharmacol Sin Source Type: research

Magnesium lithospermate B ameliorates microcirculation perfusion in rats by promoting vascular NO production via activating the PI3K/AKT pathway
Magnesium lithospermate B ameliorates microcirculation perfusion in rats by promoting vascular NO production via activating the PI3K/AKT pathway, Published online: 13 February 2019; doi:10.1038/s41401-018-0203-7Magnesium lithospermate B ameliorates microcirculation perfusion in rats by promoting vascular NO production via activating the PI3K/AKT pathway (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 13, 2019 Category: Drugs & Pharmacology Authors: Ying-luo Liu Xiao-yu Zhou Li-jiang Xuan Source Type: research

Low-intensity walking as mild medication for pressure control in prehypertensive and hypertensive subjects: how far shall we wander?
Low-intensity walking as mild medication for pressure control in prehypertensive and hypertensive subjects: how far shall we wander?, Published online: 13 February 2019; doi:10.1038/s41401-018-0202-8Low-intensity walking as mild medication for pressure control in prehypertensive and hypertensive subjects: how far shall we wander? (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 13, 2019 Category: Drugs & Pharmacology Authors: Qin Lu Sheng-ming Wang Yi-xiao Liu Hong Chen Rui Zhang Wen-hui Zhang Yuan-yuan Zou Jia-wei Zhou Xin-yi Guo Ying Zhang Teng-Li Huang Yu-hang Liu Si-qi Zhang Kyosuke Yamanishi Hiromichi Yamanishi Hideaki Higashino Haruki Okamura Source Type: research

NLRP3 inflammasome pathway is involved in olfactory bulb pathological alteration induced by MPTP.
Abstract Olfactory bulb, as one of sensory organs opening to the outside, is susceptible to toxic environment and easy to deteriorate. Recent studies in Parkinson's disease (PD) patients and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated monkeys have shown that abnormal α-synuclein is accumulated in the olfactory glomeruli, suggesting that the lesions of PD are not only confined to the substantia nigra (SN) but also located in the olfactory bulb. Thus, olfactory bulb might be the region of onset in PD pathogenesis and a targeted region for diagnosis and treatment of PD. However, the relationship...
Source: Acta Pharmacologica Sinica - February 6, 2019 Category: Drugs & Pharmacology Authors: Chen Y, Zhang QS, Shao QH, Wang S, Yuan YH, Chen NH, Wang HB Tags: Acta Pharmacol Sin Source Type: research

Simvastatin improves olanzapine-induced dyslipidemia in rats through inhibiting hepatic mTOR signaling pathway.
In this study, we explored whether mTOR signaling was involved in olanzapine (OLZ)-induced dyslipidemia as well as the lipid-lowering effects of cotreatment of simvastatin (Sim) in rats. Model rats received OLZ (1.0 mg/kg, t.i.d.) for 7 weeks; from the third week a group of model rats were cotreatment of Sim (3.0 mg/kg, t.i.d.) for 5 weeks. We found that OLZ treatment significantly increased the plasma triglyceride (TG) and total cholesterol (TC) levels, and promoted lipid accumulation in the liver, whereas cotreatment of Sim reversed OLZ-induced dyslipidemia. Hepatic mTORC1 and p-mTORC1 expression was accele...
Source: Acta Pharmacologica Sinica - February 6, 2019 Category: Drugs & Pharmacology Authors: Liu XM, Zhao XM, Deng C, Zeng YP, Hu CH Tags: Acta Pharmacol Sin Source Type: research

NLRP3 inflammasome pathway is involved in olfactory bulb pathological alteration induced by MPTP
NLRP3 inflammasome pathway is involved in olfactory bulb pathological alteration induced by MPTP, Published online: 06 February 2019; doi:10.1038/s41401-018-0209-1NLRP3 inflammasome pathway is involved in olfactory bulb pathological alteration induced by MPTP (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 6, 2019 Category: Drugs & Pharmacology Authors: Ying Chen Qiu-shuang Zhang Qian-hang Shao Shuo Wang Yu-he Yuan Nai-hong Chen Hong-bo Wang Source Type: research

Simvastatin improves olanzapine-induced dyslipidemia in rats through inhibiting hepatic mTOR signaling pathway
Simvastatin improves olanzapine-induced dyslipidemia in rats through inhibiting hepatic mTOR signaling pathway, Published online: 06 February 2019; doi:10.1038/s41401-019-0212-1Simvastatin improves olanzapine-induced dyslipidemia in rats through inhibiting hepatic mTOR signaling pathway (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 6, 2019 Category: Drugs & Pharmacology Authors: Xue-mei Liu Xiao-min Zhao Chao Deng Yan-ping Zeng Chang-hua Hu Source Type: research

Histone methyltransferase NSD2 mediates the survival and invasion of triple-negative breast cancer cells via stimulating ADAM9-EGFR-AKT signaling.
Abstract Triple-negative breast cancer (TNBC) is a heterogeneous disease with a poor prognosis due to the lack of an effective targeted therapy. Histone lysine methyltransferases (KMTs) have emerged as attractive drug targets for cancer therapy. However, the function of the majority of KMTs in TNBC has remained largely unknown. In the current study, we found that KMT nuclear receptor binding SET domain protein 2 (NSD2) is overexpressed in TNBC tumors and that its overexpression is associated with poor survival of TNBC patients. NSD2 regulates TNBC cell survival and invasion and is required for tumorigenesis and tu...
Source: Acta Pharmacologica Sinica - January 22, 2019 Category: Drugs & Pharmacology Authors: Wang JJ, Zou JX, Wang H, Duan ZJ, Wang HB, Chen P, Liu PQ, Xu JZ, Chen HW Tags: Acta Pharmacol Sin Source Type: research

Cannabis, cannabinoid receptors, and endocannabinoid system: yesterday, today, and tomorrow.
Abstract PMID: 30670816 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 22, 2019 Category: Drugs & Pharmacology Authors: Wu J Tags: Acta Pharmacol Sin Source Type: research

Cannabis, cannabinoid receptors, and endocannabinoid system: yesterday, today, and tomorrow
Cannabis, cannabinoid receptors, and endocannabinoid system: yesterday, today, and tomorrow, Published online: 22 January 2019; doi:10.1038/s41401-019-0210-3Cannabis, cannabinoid receptors, and endocannabinoid system: yesterday, today, and tomorrow (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 22, 2019 Category: Drugs & Pharmacology Authors: Jie Wu Source Type: research

Histone methyltransferase NSD2 mediates the survival and invasion of triple-negative breast cancer cells via stimulating ADAM9-EGFR-AKT signaling
Histone methyltransferase NSD2 mediates the survival and invasion of triple-negative breast cancer cells via stimulating ADAM9-EGFR-AKT signaling, Published online: 22 January 2019; doi:10.1038/s41401-018-0199-zHistone methyltransferase NSD2 mediates the survival and invasion of triple-negative breast cancer cells via stimulating ADAM9-EGFR-AKT signaling (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 22, 2019 Category: Drugs & Pharmacology Authors: Jun-Jian Wang June X. Zou Hong Wang Zhi-Jian Duan Hai-Bin Wang Peng Chen Pei-Qing Liu Jian-Zhen Xu Hong-Wu Chen Source Type: research

Costunolide alleviates HKSA-induced acute lung injury via inhibition of macrophage activation.
Abstract Staphylococcus aureus (S. aureus) infection leads to a severe inflammatory response and causes acute lung injury (ALI), eventually threatening human life. Therefore, it is of importance to find an agent to inhibit inflammation and reduce ALI. Here, we found that costunolide, a sesquiterpene lactone, displays anti-inflammatory effects and ameliorates heat-killed S. aureus (HKSA)-induced pneumonia. Costunolide treatment attenuated HKSA-induced murine ALI in which pulmonary neutrophil infiltration was inhibited, lung edema was decreased, and the production of pro-inflammatory cytokines was significantly redu...
Source: Acta Pharmacologica Sinica - January 15, 2019 Category: Drugs & Pharmacology Authors: Chen YT, Du Y, Zhao B, Gan LX, Yu KK, Sun L, Wang J, Qian F Tags: Acta Pharmacol Sin Source Type: research

Costunolide alleviates HKSA-induced acute lung injury via inhibition of macrophage activation
Costunolide alleviates HKSA-induced acute lung injury via inhibition of macrophage activation, Published online: 15 January 2019; doi:10.1038/s41401-018-0192-6Costunolide alleviates HKSA-induced acute lung injury via inhibition of macrophage activation (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 15, 2019 Category: Drugs & Pharmacology Authors: Yun-tian Chen Yao Du Bo Zhao Li-xing Gan Kai-kai Yu Lei Sun Jian Wang Feng Qian Source Type: research